Chemogenomic set

Screened at 10 µM, closest targets as % of inhibition: SLC6A3 (-87.78%), HTR2B (48.2%); In-vitro potency (enzymatic assay): Ki(SLC6A3) >10000 nM

Screened at 10 µM, closest targets as % of inhibition: SLC6A3 (-151.28%), SIGMAR1 (83.25%), HTR2B (86.81%), GABA/PBR (64.56%), SLC6A2 (69.81%); In-vitro potency (enzymatic assay): Ki(SLC6A3) >10000 nM, Ki(SIGMAR1) = 416.9 nM, Ki(HTR2B) = 507.65 nM, Ki(GABA/PBR) = 1583.39 nM, Ki(SLC6A2) = 8271.8 nM

Screened at 10 µM, closest targets as % of inhibition: SLC6A3 (-151.28%), SIGMAR1 (83.25%), HTR2B (86.81%), GABA/PBR (64.56%), SLC6A2 (69.81%); In-vitro potency (enzymatic assay): Ki(SLC6A3) >10000 nM, Ki(SIGMAR1) = 416.9 nM, Ki(HTR2B) = 507.65 nM, Ki(GABA/PBR) = 1583.39 nM, Ki(SLC6A2) = 8271.8 nM

In-vitro potency of closest targets in the screen: IC50(TBK1) = 12.6 nM, IC50(STK17B) = 631 nM, IC50(IKBKE) = 631 nM, IC50(LRRK2) = 1259 nM, IC50(FLT4) = 1585 nM, IC50(CSNK2A1) = 2512 nM, full screening data are available as supporting information, https://pubmed.ncbi.nlm.nih.gov/31097999/;

Screened at 20 µM, closest targets: dTm(MAPK8) = 4.8 K, dTm(AAK1) = 4.6&), dTm(TTK) = 4K, dTm(STK6) = 4 K, dTm(BMP2K) = 3.8 K, dTm(STK17A) = 3.5 K, dTm(GAK) = 3 K, dTm(MAPK10) = 3 K, dTm(CDK16) = 0.9 K

Screened at 20 µM, closest targets: dTm(MAPK8) = 4.8 K, dTm(AAK1) = 4.6&), dTm(TTK) = 4K, dTm(STK6) = 4 K, dTm(BMP2K) = 3.8 K, dTm(STK17A) = 3.5 K, dTm(GAK) = 3 K, dTm(MAPK10) = 3 K, dTm(CDK16) = 0.9 K

Screened at 20 µM, closest targets: dTm(MAPK8) = 4.8 K, dTm(AAK1) = 4.6&), dTm(TTK) = 4K, dTm(STK6) = 4 K, dTm(BMP2K) = 3.8 K, dTm(STK17A) = 3.5 K, dTm(GAK) = 3 K, dTm(MAPK10) = 3 K, dTm(CDK16) = 0.9 K

Screened at 20 µM, closest targets: dTm(MAPK8) = 4.8 K, dTm(AAK1) = 4.6&), dTm(TTK) = 4K, dTm(STK6) = 4 K, dTm(BMP2K) = 3.8 K, dTm(STK17A) = 3.5 K, dTm(GAK) = 3 K, dTm(MAPK10) = 3 K, dTm(CDK16) = 0.9 K

Screened at 20 µM, closest targets: dTm(MAPK8) = 4.8 K, dTm(AAK1) = 4.6&), dTm(TTK) = 4K, dTm(STK6) = 4 K, dTm(BMP2K) = 3.8 K, dTm(STK17A) = 3.5 K, dTm(GAK) = 3 K, dTm(MAPK10) = 3 K, dTm(CDK16) = 0.9 K

Screened at 1 µM, closest targets as % of control: CDK16 (cyclin Y, 28.4%), NTRK1 (44.8%), NTRK2 (47.5%), CDK12 (cyclin K, 49.8%), CDK17 (p35NCK, 50.9%), CDK18 (cyclin Y, 54.3%); Screened against 100 kinases (DSF assay), closest targets: dTm(CDK16) = 9.2 K, dTm(MAPK15) = 5.8 K, dTm(PLK4) = 5.5 K, dTm(STK6) = 4.0 K, dTm(ULK3) = 3.3 K, dTm(CDK2) = 3.2 K, dTm(MAP2K6) = 3 K, dTm(GSK3B) = 2.9 K, dTm(MAPK10) = -1.6 K

Screened at 1 µM, closest targets as % of control: CDK16 (cyclin Y, 28.4%), NTRK1 (44.8%), NTRK2 (47.5%), CDK12 (cyclin K, 49.8%), CDK17 (p35NCK, 50.9%), CDK18 (cyclin Y, 54.3%); Screened against 100 kinases (DSF assay), closest targets: dTm(CDK16) = 9.2 K, dTm(MAPK15) = 5.8 K, dTm(PLK4) = 5.5 K, dTm(STK6) = 4.0 K, dTm(ULK3) = 3.3 K, dTm(CDK2) = 3.2 K, dTm(MAP2K6) = 3 K, dTm(GSK3B) = 2.9 K, dTm(MAPK10) = -1.6 K

Screened at 1 µM, closest targets as % of control: CDK16 (cyclin Y, 28.4%), NTRK1 (44.8%), NTRK2 (47.5%), CDK12 (cyclin K, 49.8%), CDK17 (p35NCK, 50.9%), CDK18 (cyclin Y, 54.3%); Screened against 100 kinases (DSF assay), closest targets: dTm(CDK16) = 9.2 K, dTm(MAPK15) = 5.8 K, dTm(PLK4) = 5.5 K, dTm(STK6) = 4.0 K, dTm(ULK3) = 3.3 K, dTm(CDK2) = 3.2 K, dTm(MAP2K6) = 3 K, dTm(GSK3B) = 2.9 K, dTm(MAPK10) = -1.6 K

Screened at 1 µM, closest targets as % of control: CDK16 (cyclin Y, 28.4%), NTRK1 (44.8%), NTRK2 (47.5%), CDK12 (cyclin K, 49.8%), CDK17 (p35NCK, 50.9%), CDK18 (cyclin Y, 54.3%); Screened against 100 kinases (DSF assay), closest targets: dTm(CDK16) = 9.2 K, dTm(MAPK15) = 5.8 K, dTm(PLK4) = 5.5 K, dTm(STK6) = 4.0 K, dTm(ULK3) = 3.3 K, dTm(CDK2) = 3.2 K, dTm(MAP2K6) = 3 K, dTm(GSK3B) = 2.9 K, dTm(MAPK10) = -1.6 K

Screened at 1 µM, closest targets as % of control: CDK16 (cyclin Y, 28.4%), NTRK1 (44.8%), NTRK2 (47.5%), CDK12 (cyclin K, 49.8%), CDK17 (p35NCK, 50.9%), CDK18 (cyclin Y, 54.3%); Screened against 100 kinases (DSF assay), closest targets: dTm(CDK16) = 9.2 K, dTm(MAPK15) = 5.8 K, dTm(PLK4) = 5.5 K, dTm(STK6) = 4.0 K, dTm(ULK3) = 3.3 K, dTm(CDK2) = 3.2 K, dTm(MAP2K6) = 3 K, dTm(GSK3B) = 2.9 K, dTm(MAPK10) = -1.6 K

Screened at 10 µM, against 45 GPCRs, closest targets as % of inhibition: SLC6A3 (72.51%), HTR1A (-28.41%), DRD3(71.05%), in-vitro potency of closest targets: Ki(SLC6A3) = 7216.06 nM, Ki(HTR1A) = 7661.26 nM, Ki(DRD3) = 8625.81 nM

Screened at 10 µM, against 45 GPCRs, closest targets as % of inhibition: SLC6A3 (72.51%), HTR1A (-28.41%), DRD3(71.05%), in-vitro potency of closest targets: Ki(SLC6A3) = 7216.06 nM, Ki(HTR1A) = 7661.26 nM, Ki(DRD3) = 8625.81 nM

Screened at 10 µM against target family members as % of inhibition: Tryptase (2%), Elastase (4%), Plasmin (4%), Chymotrypsin (-3%), TPA (%), Kallikrein (4%), Thrombin (-1%), Chymase (11%), Cathepsin G (13%), Proteinase 3 (7%), Factor VIIa (-5%), Urokinase (2%), Streptokinase (1%9, Trypsin (-10%9, Factor Xa (0%);
In-vitro potency (Radiometric assay using cell lysate and radiolabeled substrate and human FAAH): IC50(FAAH) = 4 µM, https://pubmed.ncbi.nlm.nih.gov/31818916/;
In-vitro potency (Radiometric assay using cell lysate and radiolabeled substrate and human ABHD6): IC50(ABHD6) > 10 µM, https://pubmed.ncbi.nlm.nih.gov/31818916/;
In-vitro potency (Radiometric assay using cell lysate and radiolabeled substrate and human ABHD12): IC50(ABHD12) >10 µM, https://pubmed.ncbi.nlm.nih.gov/31818916/;
In-cellular potency (Fluorescence assay using BODIPY FL containing PLA1-specific substrate, endothelial lipase): IC50 >30 µM, https://pubmed.ncbi.nlm.nih.gov/31818916/;
In-cellular potency (Fluorescence assay using BODIPY FL containing PLA1-specific substrate, hepatic lipase): IC50 >30 µM, https://pubmed.ncbi.nlm.nih.gov/31818916/;
In-cellular potency (Fluorescence assay using BODIPY FL containing PLA1-specific substrate, lipoprotein lipase): IC50 >30 µM, https://pubmed.ncbi.nlm.nih.gov/31818916/;
Screened at 10 µM, against 50 kinases, all targets <20% of inhibition, clean screen, data not available, https://pubmed.ncbi.nlm.nih.gov/31818916/;
Screened at 10 µM, against 50 enzymes (CEREP panel), closest targets as % of inhibition: KappaOpioid (66%), 5HT1B (56%), DA transporter (54%), Cl-channel (%), https://pubmed.ncbi.nlm.nih.gov/31818916/;

Screened at 10 µM, closest targets as % of inhibition: OPRK1 (90.74%), GABA/PBR (96.59%), CHARM4(51.56%), DRD4 (89.3%), DRD3 (89.96%), SLC6A3(79.87), ADRA1B(75.32%), full screening data available on DCP website;
In-vitro potency of closest targets in the PDSP screen (enzymatic assay): Ki(OPRK1) = 197.79 nM, Ki(GABA/PBR) = 306.41 nM, Ki(CHARM4) = 1307.68 nM, Ki(DRD4) = 3385.32 nM, Ki(DRD3) = 3603.3 nM, Ki(SLC6A3) = 6549.38 nM, Ki(ADRA1B) = 9783.63 nM, ttps://www.sgc-ffm.uni-frankfurt.de/#!specificprobeoverview/JNJ-9350;

Screened at 1 µM, in-vitro potency of closest targets: IC50(TNIK) = 1663 nM, IC50(AMPKA2) >10000 nM, IC50(DCAMKL2) >10000 nM, IC50(FMS) >10000 nM, IC50(NDR2) >10000 nM, IC50(TGFBR1) >10000 nM, IC50(SAPK2A) >10000 nM, IC50(SAPK2B) >10000 nM; Screened at 10 µM, against 45 GPCRs (PDSP screen), closest targets as % of inhibition: GABA/PBR (50.86%), SLC6A3 (43.78%), HTR1D (33.37%), in-vitro potency of closest targets: Ki(GABA/PBR) = 4525.85 nM

Screened at 1 µM, in-vitro potency of closest targets: IC50(TNIK) = 1663 nM, IC50(AMPKA2) >10000 nM, IC50(DCAMKL2) >10000 nM, IC50(FMS) >10000 nM, IC50(NDR2) >10000 nM, IC50(TGFBR1) >10000 nM, IC50(SAPK2A) >10000 nM, IC50(SAPK2B) >10000 nM; Screened at 10 µM, against 45 GPCRs (PDSP screen), closest targets as % of inhibition: GABA/PBR (50.86%), SLC6A3 (43.78%), HTR1D (33.37%), in-vitro potency of closest targets: Ki(GABA/PBR) = 4525.85 nM

Screened at 10 µM, closest targets as % of inhibition, HTR1D (100.58%), HTR1B (103.72%), GABA/PBR (114.1%), HTR2B (57.92%), OPRK1 (73.33%), TMEM97 (76.7%), ADRA2B (42.24%), ADRA2A (64.0%), full screening data available on DCP website;
In-vitro potency of closest targets in the PDSP screen (enzymatic assay): Ki(HTR1D) = 219.42 nM, Ki(HTR1B) = 477.93 nM, Ki(GABA/PBR) = 497.62 nM, Ki(HTR2B) = 897.02 nM, Ki(OPRK1) = 1168.96 nM, Ki(TMEM97) = 1924.86 nM, Ki(ADRA2B) = 3579.32 nM, Ki(ADRA2A) = 3826.48 nM, https://www.sgc-ffm.uni-frankfurt.de/#!specificprobeoverview/JNJ-9350; Screened at 10 µM against a panel of 13 receptors, (CEREP assay) targets as % of inhibition: 5HT1B (62.09%), 5-HT2A (69.87%), 5-HT2B (68.52%), A1 (98-93%), A2A (74.96%), A3 (75.06%), CCK1 (70.27%), KOP (74.06%), M4 (59.82%), ML1A (58.82%), NK2 (56.77%), PDE4D2 (63.05%), Sigma (62.77%), https://www.sgc-ffm.uni-frankfurt.de/#!specificprobeoverview/JNJ-9350;

Screened at 1 µM against NR1A1, NR1B1, NR1C3, NR1F3, NR1H3, NR1I1, NR1I2, NR1I3, NR2A1, NR2B1, NR4A1, NR5A2 and VP16 in a Gal4 hybrid reporter gene assay (HEK293T cells were cotransfected with pFR-Luc reporter, pRL-SV40 control reporter and pFA-CMV containing the Gal4-DBD fused with human NR-LBD of interest or pECE-SV40-Gal4-VP16): clean selectivty profile with no significant agonism/antagonism detected; Screened at 20 µM in a bromodomain and kinase panel against ABL1, AURKA, BRD4, BRPF1, CDK2, CSNK1D, FGFR3, GSK3B, MAPK1, TRIM24 in DSF assays: clean selectivity profile with no significant binding (?Tm < 2 K)

Screened at 1 µM against NR1A1, NR1B1, NR1C3, NR1F3, NR1H3, NR1I1, NR1I2, NR1I3, NR2A1, NR2B1, NR4A1, NR5A2 and VP16 in a Gal4 hybrid reporter gene assay (HEK293T cells were cotransfected with pFR-Luc reporter, pRL-SV40 control reporter and pFA-CMV containing the Gal4-DBD fused with human NR-LBD of interest or pECE-SV40-Gal4-VP16): clean selectivty profile with no significant agonism/antagonism detected; Screened at 20 µM in a bromodomain and kinase panel against ABL1, AURKA, BRD4, BRPF1, CDK2, CSNK1D, FGFR3, GSK3B, MAPK1, TRIM24 in DSF assays: clean selectivity profile with no significant binding (?Tm < 2 K)

Screened at 1 µM against NR1A1, NR1B1, NR1C3, NR1F3, NR1H3, NR1I1, NR1I2, NR1I3, NR2A1, NR2B1, NR4A1, NR5A2 and VP16 in a Gal4 hybrid reporter gene assay (HEK293T cells were cotransfected with pFR-Luc reporter, pRL-SV40 control reporter and pFA-CMV containing the Gal4-DBD fused with human NR-LBD of interest or pECE-SV40-Gal4-VP16): clean selectivty profile with no significant agonism/antagonism detected; Screened at 20 µM in a bromodomain and kinase panel against ABL1, AURKA, BRD4, BRPF1, CDK2, CSNK1D, FGFR3, GSK3B, MAPK1, TRIM24 in DSF assays: ?Tm(ABL1) = 2.06 K, all other bromodomains and kinases ?Tm < 2 K; IC50 = approx. 2000 nM reported in literature

Screened at 1 µM, closest targets as % inhibition: MAPK3 (99.9%), MAPK1 (99.7%), MAPK10 (98.8%), NIKE (98.3%), MAPK8(97.8%), DRAK1 (97.5%), DRAK2 (97.0%), MYLK4 (96.4%), MAP2K4(96.3%), MAPK9(95.9%), MAP2K3(95.8%), RIOK1 (94.1%), CSNK2A2 (92.6%), CLK2 (92.3%), AURKC (92.1%), other targets >90% of inhibition, full screening data available as supplemental information; In-vitro potency of closest targets (Enzymatic assay, ATP-competitive assay platform, Life technology): IC50(MAPK10) = 632 nM, IC50(MAPK8) = 1080 nM, IC50(DRAK1) = 114 nM, IC50(MAPK9) = 783 nM, IC50(MAP2K3) = 304 nM, IC50(AURKC) = 580 nM, IC50(CSNK2A2) >10000 nM, IC50(CLK2) = 104 nM, IC50(CLK1) = 508 nM, IC50(GSG2) = 398 nM, IC50(TTK) = 193 nM, IC50(MINK) = 942 nM, IC50(MAP4K4) = 503 nM, IC50(PRKD1) = 535 nM, https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4687050/; Screened at 1 µM againast 309 kinases (Invitrogen), closest targets as % of inhibition: CLK2 (65%), FLT4 (60%), GSG2 (51%), MAP4K4 (71%), MAPK1 (100%), MINK(66%), PRKD1 (50%), TTK (62%), https://pubmed.ncbi.nlm.nih.gov/23614898/;

Screened at 1 µM, closest targets as % inhibition: MAPK3 (99.9%), MAPK1 (99.7%), MAPK10 (98.8%), NIKE (98.3%), MAPK8(97.8%), DRAK1 (97.5%), DRAK2 (97.0%), MYLK4 (96.4%), MAP2K4(96.3%), MAPK9(95.9%), MAP2K3(95.8%), RIOK1 (94.1%), CSNK2A2 (92.6%), CLK2 (92.3%), AURKC (92.1%), other targets >90% of inhibition, full screening data available as supplemental information; In-vitro potency of closest targets (Enzymatic assay, ATP-competitive assay platform, Life technology): IC50(MAPK10) = 632 nM, IC50(MAPK8) = 1080 nM, IC50(DRAK1) = 114 nM, IC50(MAPK9) = 783 nM, IC50(MAP2K3) = 304 nM, IC50(AURKC) = 580 nM, IC50(CSNK2A2) >10000 nM, IC50(CLK2) = 104 nM, IC50(CLK1) = 508 nM, IC50(GSG2) = 398 nM, IC50(TTK) = 193 nM, IC50(MINK) = 942 nM, IC50(MAP4K4) = 503 nM, IC50(PRKD1) = 535 nM, https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4687050/; Screened at 1 µM againast 309 kinases (Invitrogen), closest targets as % of inhibition: CLK2 (65%), FLT4 (60%), GSG2 (51%), MAP4K4 (71%), MAPK1 (100%), MINK(66%), PRKD1 (50%), TTK (62%), https://pubmed.ncbi.nlm.nih.gov/23614898/;

Screened at 1 µM, closest targets as % of control: DYRK1B (18%), MAPK12 (34%); In-cellular potency (NanoBRET assay, HEK293T cells): IC50(DYRK1B) >10000 nM, IC50(CDK9, cyclin K) > 10000 nM, IC50(CDK16, cyclin Y) >10000 nM, IC50(CDK17, cyclin Y) >10000 nM, IC50(CDK18, cyclin Y) >10000 nM

Screened at 1 µM, closest targets as % of control: GSK3A (0.7%), CDKL5 (0.7%), CDK17 (1.3%), CDK7 (1.9%), CDK16 (5.5%), CDK13 (5.9%), CDK9 (8.3%), YSK4 (14%), CDK18 (17%), CDK4 (20%), GSK3B (51%); In-vitro potency (radiometric enzymatic assays, Eurofins): IC50(GSK3A) = 470 nM, IC50(CDKL5) = 11 nM, IC50(CDK17) = 89 nM, IC50(CDK7) = 300 nM, IC50(CDK16) = 62 nM, IC50(CDK13) >10000 nM, IC50(CDK9) = 20 nM, IC50(YSK4) >10000 nM, IC50(CDK18) = 100 nM, IC50(CDK4) = 1900 nM, IC50(GSK3B) = 2250 nM; In-cellular potency (NanoBRET assay, HEK293T cells): IC50(GSK3A) = 1500 nM, IC50(CDKL5) = 10 nM, IC50(CDK17) = 240 nM, IC50(CDK16) = 390 nM, IC50(CDK9) = 280 nM, IC50(CDK18) = 260 nM, IC50(GSK3B) = 2400 nM

Screened at 1 µM, closest targets as % of control: CDKL5 (0.2%), GSK3B (0.5%), DYRK2 (4.8%), CDK7 (5.6%), CDK16 (12%), GSK3A (14%), DYRK1A (19%), CDK17 (20%), HIPK1 (33%), HIPK2 (33%), RPS6KA4 (34%); In-vitro potency (enzymatic radiometric assays, Eurofins): IC50(DYRK2) = 770 nM, IC50(CDK7) >10000 nM, IC50(CDK16) = 590 nM, IC50(DYRK1A) = 1100 nM, IC50(CDK17) = 1000 nM, IC50(HIPK1) = 7900 nM, IC50(HIPK2) = 2300 nM, IC50(RPS6KA4) >10000 nM

Screened at 1 µM, closest targets as % of control: CDKL5 (0.2%), GSK3B (0.5%), DYRK2 (4.8%), CDK7 (5.6%), CDK16 (12%), GSK3A (14%), DYRK1A (19%), CDK17 (20%), HIPK1 (33%), HIPK2 (33%), RPS6KA4 (34%); In-vitro potency (enzymatic radiometric assays, Eurofins): IC50(DYRK2) = 770 nM, IC50(CDK7) >10000 nM, IC50(CDK16) = 590 nM, IC50(DYRK1A) = 1100 nM, IC50(CDK17) = 1000 nM, IC50(HIPK1) = 7900 nM, IC50(HIPK2) = 2300 nM, IC50(RPS6KA4) >10000 nM

Screened at 1 µM, closest targets as % of control: CDKL5 (0.2%), GSK3B (0.5%), DYRK2 (4.8%), CDK7 (5.6%), CDK16 (12%), GSK3A (14%), DYRK1A (19%), CDK17 (20%), HIPK1 (33%), HIPK2 (33%), RPS6KA4 (34%); In-vitro potency (enzymatic radiometric assays, Eurofins): IC50(DYRK2) = 770 nM, IC50(CDK7) >10000 nM, IC50(CDK16) = 590 nM, IC50(DYRK1A) = 1100 nM, IC50(CDK17) = 1000 nM, IC50(HIPK1) = 7900 nM, IC50(HIPK2) = 2300 nM, IC50(RPS6KA4) >10000 nM

Screened at 1 µM, closest targets as % of control: GSK3A (0%), GSK3B (0.2%), DYRK1A (0.4%), ICK(5.7%), DYRK2 (8.3%), DYRK1B (10%), MAPK8 (16%), CDK4 (20%), RPS6KA4 (29%), CLK1 (30%), CDKL5 (30%), CDK7 (31%), MAPK10 (31%), CLK4 (32%), CLK2 (34%), CDKL2 (77%), CDKL1(93%), CDKL3(100%); In-vitro potency of closest targets (enzymatic radiometric assays, Eurofins): IC50(DYRK1A) = 170 nM, IC50(ICK) = 520 nM, IC50(DYRK2) = 800 nM, IC50(DYRK1B) = 47 nM, IC50(MAPK8) >10000 nM, IC50(CDK4) = 3800 nM, IC50(RPS6KA4) >10000 nM, IC50(CLK1) = 620 nM, IC50(CDKL5) = 840 nM, IC50(CDK7) >10000 nM, IC50(MAPK10) = 2900 nM, IC50(CLK4) = 760 nM, IC50(CLK2) = 800 nM; In-cellular potency (NanoBRET assay, HEK293T cells): IC50(DYRK1B) = 2400 nM, IC50(CDKL5) = 1400 nM

Screened at 1 µM, closest targets as % of control: GSK3A (0%), GSK3B (0.2%), DYRK1A (0.4%), ICK(5.7%), DYRK2 (8.3%), DYRK1B (10%), MAPK8 (16%), CDK4 (20%), RPS6KA4 (29%), CLK1 (30%), CDKL5 (30%), CDK7 (31%), MAPK10 (31%), CLK4 (32%), CLK2 (34%), CDKL2 (77%), CDKL1(93%), CDKL3(100%); In-vitro potency of closest targets (enzymatic radiometric assays, Eurofins): IC50(DYRK1A) = 170 nM, IC50(ICK) = 520 nM, IC50(DYRK2) = 800 nM, IC50(DYRK1B) = 47 nM, IC50(MAPK8) >10000 nM, IC50(CDK4) = 3800 nM, IC50(RPS6KA4) >10000 nM, IC50(CLK1) = 620 nM, IC50(CDKL5) = 840 nM, IC50(CDK7) >10000 nM, IC50(MAPK10) = 2900 nM, IC50(CLK4) = 760 nM, IC50(CLK2) = 800 nM; In-cellular potency (NanoBRET assay, HEK293T cells): IC50(DYRK1B) = 2400 nM, IC50(CDKL5) = 1400 nM

Screened at 10 µM, closest targets as % on control: MAP3K7 (2%), CLK2 (4%), IRAK1 (4%), IRAK4 (7%), GCK (9%), MINK1 (9%), CSNK1G2 (13%), full screening data available as supporting information; In-vitro potency (enzymatic assay, MRC Dundee): IC50(MAP3K7) = 9.5 nM, IC50(IRAK4) = 120 nM, IC50(IRAK1) = 390 nM, IC50(GCK) = 430 nM, IC50(CLK2) = 430 nM, IC50(MINK1) = 1900 nM, https://pubmed.ncbi.nlm.nih.gov/28820959/; Kinase proteome profiling in RA-FLS cells, against 45 kinases, closest targets as % of activity: LCK (42.6%), full screening data available as supporting info, https://pubmed.ncbi.nlm.nih.gov/31847895/;

Screened against a panel of receptors, ion channels, and other enzymes (enzymatic assays), in-vitro potency of closest target: IC50(SLC6A4) = 0.31 µM, IC50(HTR1B) = 2.8 µM, IC50(CHRNA4) = 6.5 µM, other targets IC50 >10 µM, full screening data available as supplement information;

In-vitro potency (competition binding assay) of closest targets in the screen: Kd(MAPK3) = 160 nM, Kd(MAPK1) = 183 nM, Kd(TAO1) = 388 nM, Kd(PRKD2) = 6336 nM, full screening data available in paper https://www.science.org/doi/10.1126/science.aan4368, and Chembl;

Screened at 10 µM (panel of GPCRs, ion channels, transporters), closest targets as % of inhibition: PDE1A (7.7%), PDE2A (3.5%), PDE3A (-1.3%), PDE3B (0.8%), PDE4A (6.8%), PDE4B (10.6%), PDE4C (28.6%), PDE4D (19.1%), PDE5A (12.2%), PDE6 (16.7%), PDE7A (-1.6%), PDE7B (-2.1%), PDE8A (2.9%), PDE10A (1.6%), PDE11A (1.3%); In-vitro potency (Scintillation Proximity Assay): IC50(PDE1) = 0.753 nM, IC50(PDE2A) >10000 nM, IC50(PDE3B) >10000 nM, IC50(PDE4B) = 3960 nM, IC50(PDE5A) = 2980 nM, IC50(PDE6) = 1560 nM, IC50(PDE7B) >10000 nM, IC50(PDE8A) = 1490 nM, IC50(PDE10A) >10000 nM, IC50(PDE11A) = 6600 nM

Screened at 3 µM against NR1A1, NR2A1, NR2B1, NR2C1, NR2E1, NR4A1, NR5A1 and VP16 in a Gal4 hybrid reporter gene assay (HEK293T cells were cotransfected with pFR-Luc reporter, pRL-SV40 control reporter and pFA-CMV containing the Gal4-DBD fused with human NR-LBD of interest or pECE-SV40-Gal4-VP16): clean selectivty profile with no significant agonism/antagonism detected; Screened at 20 µM in a bromodomain and kinase panel against ABL1, AURKA, BRD4, BRPF1, CDK2, CSNK1D, FGFR3, GSK3B, MAPK1, TRIM24 in DSF assays: clean selectivity profile with no significant binding (?Tm < 2 K)

inactive at 3 µM for inactive at 1 µM for UL48, RXRA, HNF4A, NR2C1, NR2E1, NR4A1, NR5A1

Screened at 10 µM against NR1I1, NR1I3, NR2A1, NR2B1, NR2C1, NR2E1, NR4A1, NR5A1 and VP16 in a Gal4 hybrid reporter gene assay (HEK293T cells were cotransfected with pFR-Luc reporter, pRL-SV40 control reporter and pFA-CMV containing the Gal4-DBD fused with human NR-LBD of interest or pECE-SV40-Gal4-VP16): clean selectivty profile with no significant agonism/antagonism detected; Screened at 20 µM in a bromodomain and kinase panel against ABL1, AURKA, BRD4, BRPF1, CDK2, CSNK1D, FGFR3, GSK3B, MAPK1, TRIM24 in DSF assays: clean selectivity profile with no significant binding (?Tm < 2 K)

Screened at 1 µM against NR1I1, NR1I3, NR2A1, NR2B1, NR2C1, NR2E1, NR4A1, NR5A1 and VP16 in a Gal4 hybrid reporter gene assay (HEK293T cells were cotransfected with pFR-Luc reporter, pRL-SV40 control reporter and pFA-CMV containing the Gal4-DBD fused with human NR-LBD of interest or pECE-SV40-Gal4-VP16): clean selectivty profile with no significant agonism/antagonism detected; Screened at 20 µM in a bromodomain and kinase panel against ABL1, AURKA, BRD4, BRPF1, CDK2, CSNK1D, FGFR3, GSK3B, MAPK1, TRIM24 in DSF assays: clean selectivity profile with no significant binding (?Tm < 2 K)

Screened at 1 µM, closest targets as % of residual activity: EGFR (-5%), LYN(10%), BRSK1 (14%), full screening data are available at Chembl and in paper, also screened at 10 µM, https://pubmed.ncbi.nlm.nih.gov/23398362/;
In-vitro potency (radiometric assay, conc. ATP = 0.4 µM): IC50(ABL1) = 125 nM, https://pubmed.ncbi.nlm.nih.gov/10090785/;
In-vitro potency (radiometric assay, conc. ATP = 0.4 µM): IC50(SRC) >10000 nM, https://pubmed.ncbi.nlm.nih.gov/10090785/;
In-vitro potency (radiometric assay, conc. ATP = 0.4 µM): IC50(PRKCA) >10000 nM, https://pubmed.ncbi.nlm.nih.gov/10090785/;
In-vitro potency (ADP Hunter assay, conc. ATP = 100 µM): IC50(MNK1) = 530 nM, https://pubs.acs.org/doi/10.1021/jm1005513#_i23;

Screened at 1 µM, closest targets as % of inhibition: PI3KC2G (61%), CLK4 (57%), PIK3CD (47%), full screening data are available as supporting informationpubmed.ncbi.nlm.nih.gov/30346772/
In-cellular potency (cellular kinase assay): IC50(ATM) >30 µM, https://pubmed.ncbi.nlm.nih.gov/26517239/;
In-cellular potency (cellular kinase assay): IC50(DNAPK) >30 µM, https://pubmed.ncbi.nlm.nih.gov/26517239/;
In-cellular potency (cellular kinase assay): IC50(MTOR) >23 µM, https://pubmed.ncbi.nlm.nih.gov/26517239/;
In-cellular potency (cellular kinase assay): IC50(PIK3CA) >30 µM, https://pubmed.ncbi.nlm.nih.gov/26517239/;
In-vitro potency (enzymatic assay, Kinase Profiler Eurofins): IC50(ATR) = 0.134 µM, https://pubmed.ncbi.nlm.nih.gov/34911817/;
In-vitro potency (enzymatic assay, Kinase Profiler Eurofins): IC50(ATM) > 10 µM, https://pubmed.ncbi.nlm.nih.gov/34911817/;
In-vitro potency (enzymatic assay, Kinase Profiler Eurofins): IC50(DNAPK) = 7.4 µM, https://pubmed.ncbi.nlm.nih.gov/34911817/;
In-vitro potency (enzymatic assay, Kinase Profiler Eurofins): IC50(MTOR) = 3.8 µM, https://pubmed.ncbi.nlm.nih.gov/34911817/;
In-vitro potency (enzymatic assay, Kinase Profiler Eurofins): IC50(PIK3CA) >10 µM, https://pubmed.ncbi.nlm.nih.gov/34911817/;

Screened at 1 µM, closest targets as % of control: CSF1R (40%), NEK11 (41%), full screening data available as supporting information, https://pubmed.ncbi.nlm.nih.gov/25587754/;

Screened at 10 µM, closest targets as % of control: MST2 (3.4%), KIT(V5559D, 3.6%), PCTK1 (15%), RIOK2 (23%), STK16 (28%), YSK4 (49%), HIPK4 (49%), GSK3A (0.1%), GSK3B (11%), PRKX (42%), full screening data available as supporting information;

Screened at 10 µM, closest targets as % of control: MST2 (3.4%), KIT(V5559D, 3.6%), PCTK1 (15%), RIOK2 (23%), STK16 (28%), YSK4 (49%), HIPK4 (49%), GSK3A (0.1%), GSK3B (11%), PRKX (42%), full screening data available as supporting information;

Screened at 1 µM, closest targets as % of control: GSG2 (33%), PIK3CA (36%), PIK4CB (30%), LRRK2 (13%), MTOR (7.4%), full screening data are available as supporting information, https://pubs.acs.org/doi/10.1021/acs.jmedchem.7b01896;
In-cellular potency (Immunoblot assay, ATR dependent phosphorylation of CHEK1 at Ser345, using HT-29 cells): IC50(ATR) = 6.2 µM, https://pubs.acs.org/doi/10.1021/acs.jmedchem.7b01896;
In-cellular potency (ELISA, PIK3CA dependent phosphorylation of AKT1 at Thr308 using BT474 cells): IC50(PIK3CA) = 1.4 µM, https://pubs.acs.org/doi/10.1021/acs.jmedchem.7b01896;
In-cellular potency (Immunoblot assay, MTOR dependent phosphorylation of AKT1 at Ser473 using MDA-MB-468 cells): IC50(MTOR) = 0.61 µM, https://pubs.acs.org/doi/10.1021/acs.jmedchem.7b01896;
In-vitro potency (enzymatic assay): IC50(DNAPK) = 0.14 µM, https://pubs.acs.org/doi/10.1021/acs.jmedchem.7b01896;
In-vitro potency (enzymatic assay): IC50(MTOR) = 0.20 µM, https://pubs.acs.org/doi/10.1021/acs.jmedchem.7b01896;
In-vitro potency (enzymatic assay): IC50(PIK3CA) = 0.32 µM, https://pubs.acs.org/doi/10.1021/acs.jmedchem.7b01896;
In-vitro potency (enzymatic assay): IC50(PIK3CB) = 1.8 µM, https://pubs.acs.org/doi/10.1021/acs.jmedchem.7b01896;
In-vitro potency (enzymatic assay): IC50(PIK3CG) = 1.1 µM, https://pubs.acs.org/doi/10.1021/acs.jmedchem.7b01896;
In-vitro potency (enzymatic assay): IC50(PIK3CD) = 0.27 µM, https://pubs.acs.org/doi/10.1021/acs.jmedchem.7b01896;

Screened at 1 µM, closest targets with >50% of activity in the screen: CSF1R, NUAK1, SGK, screening data are not available in paper, https://pubmed.ncbi.nlm.nih.gov/29938225/;
Screened at 1 µM, against 125 kinases, Eurofins Panlabs screen, closest target with >50% of activity in the screen: FMS, screening data are not available in paper, https://pubmed.ncbi.nlm.nih.gov/29938225/;
In-vitro potency (enzymatic assay): IC50(ATR) >30 µM, https://pubmed.ncbi.nlm.nih.gov/29938225/;
In-vitro potency (enzymatic assay): IC50(PIK3CA) >12 µM, https://pubmed.ncbi.nlm.nih.gov/29938225/;
In-vitro potency (enzymatic assay): IC50(MTOR) >16.1 µM, https://pubmed.ncbi.nlm.nih.gov/29938225/;
In-vitro potency (enzymatic assay): IC50(DNAPK) >29.9 µM, https://pubmed.ncbi.nlm.nih.gov/29938225/;
In-vitro potency (enzymatic assay): IC50(HERG) = 6.55 µM, https://pubmed.ncbi.nlm.nih.gov/29938225/;

Screened at 1 µM, closest targets in the screen: BIKE, CRIK, MNK1, MNK2, % of inhibition not given in paper, https://pubmed.ncbi.nlm.nih.gov/35257579/;
Screened against panel of 249 kinases (literature), in-vitro potency of closest targets:
In-vitro potency (enzymatic assay): IC50(BIKE) = 1900 nM, https://pubmed.ncbi.nlm.nih.gov/35257579/;
In-vitro potency (enzymatic assay): IC50(GAK) = 800 nM, https://pubmed.ncbi.nlm.nih.gov/35257579/;
In-vitro potency (enzymatic assay): IC50(CRIK) = 410 nM, https://pubmed.ncbi.nlm.nih.gov/35257579/;
In-vitro potency (enzymatic assay): IC50(LATS2) = 660 nM, https://pubmed.ncbi.nlm.nih.gov/35257579/;
In-vitro potency (enzymatic assay): IC50(MKN1) = 160 nM, https://pubmed.ncbi.nlm.nih.gov/35257579/;
Screened at CEREB-like safety panel (literature) against 41 targets, in-vitro potency of closest target: IC50(NET) = 390 nM, all other targets >6 µM https://pubmed.ncbi.nlm.nih.gov/35257579/;

Screened at 3 µM, closest targets as % of activity remaining: MTOR (0%), FMS (43%), full screening data are available as supplemental information, https://pubmed.ncbi.nlm.nih.gov/26102506/;
In-vitro potency (HTR-FRET assay): IC50(PIK3CA) = 0.852 µM, https://pubmed.ncbi.nlm.nih.gov/26102506/;
In-vitro potency (enzymatic assay): IC50(ATM) >30 µM, https://pubmed.ncbi.nlm.nih.gov/26102506/;
In-vitro potency (enzymatic assay): IC50(ATR) >30 µM, https://pubmed.ncbi.nlm.nih.gov/26102506/;

Screened at 3 µM, closest targets as % of activity remaining: MTOR (0%), FMS (43%), full screening data are available as supplemental information, https://pubmed.ncbi.nlm.nih.gov/26102506/;
In-vitro potency (HTR-FRET assay): IC50(PIK3CA) = 0.852 µM, https://pubmed.ncbi.nlm.nih.gov/26102506/;
In-vitro potency (enzymatic assay): IC50(ATM) >30 µM, https://pubmed.ncbi.nlm.nih.gov/26102506/;
In-vitro potency (enzymatic assay): IC50(ATR) >30 µM, https://pubmed.ncbi.nlm.nih.gov/26102506/;

Screened at 1 µM, closest targets as % of control: FLT3 (ITD, D835V, 4%), FLT3 (ITD, F691L, 3.6%), RIOK1 (100%), RIOK2 (0%), RIOK3 (87%), full screening data are available as supporting information;

Screened at 1 µM, closest targets as % of control: MTOR (2.2%), DYRK1B (11%), VSP34 (17%), full screening data are available as supporting information, https://pubmed.ncbi.nlm.nih.gov/32502336/;
In-vitro potency (Competition binding assay, DiscoverX): Kd(DYRK1B) = 25000 nM, https://pubmed.ncbi.nlm.nih.gov/32502336/;
In-vitro potency (Competition binding assay, DiscoverX): Kd(GAK) = 580 nM, https://pubmed.ncbi.nlm.nih.gov/32502336/;
In-vitro potency (Competition binding assay, DiscoverX): Kd(GSK3B) >30000 nM, https://pubmed.ncbi.nlm.nih.gov/32502336/;
In-vitro potency (Competition binding assay, DiscoverX): Kd(RIOK2) = 660 nM, https://pubmed.ncbi.nlm.nih.gov/32502336/;
In-vitro potency (Competition binding assay, DiscoverX): Kd(VSP34) = 3200 nM, https://pubmed.ncbi.nlm.nih.gov/32502336/;
In-vitro potency (enzymatic assay): IC50(DNAPK) = 332 nM, https://pubmed.ncbi.nlm.nih.gov/32502336/;
In-vitro potency (TR-FRET assay): IC50(ATM) = 1420 nM, https://pubmed.ncbi.nlm.nih.gov/32502336/;
In-vitro potency (enzymatic assay): IC50(PIK3CB) = 3270 nM, https://pubmed.ncbi.nlm.nih.gov/32502336/;

Screened at 1 µM, closest targets as % of control: MTOR (2.2%), DYRK1B (11%), VSP34 (17%), full screening data are available as supporting information, https://pubmed.ncbi.nlm.nih.gov/32502336/;
In-vitro potency (Competition binding assay, DiscoverX): Kd(DYRK1B) = 25000 nM, https://pubmed.ncbi.nlm.nih.gov/32502336/;
In-vitro potency (Competition binding assay, DiscoverX): Kd(GAK) = 580 nM, https://pubmed.ncbi.nlm.nih.gov/32502336/;
In-vitro potency (Competition binding assay, DiscoverX): Kd(GSK3B) >30000 nM, https://pubmed.ncbi.nlm.nih.gov/32502336/;
In-vitro potency (Competition binding assay, DiscoverX): Kd(RIOK2) = 660 nM, https://pubmed.ncbi.nlm.nih.gov/32502336/;
In-vitro potency (Competition binding assay, DiscoverX): Kd(VSP34) = 3200 nM, https://pubmed.ncbi.nlm.nih.gov/32502336/;
In-vitro potency (enzymatic assay): IC50(DNAPK) = 332 nM, https://pubmed.ncbi.nlm.nih.gov/32502336/;
In-vitro potency (TR-FRET assay): IC50(ATM) = 1420 nM, https://pubmed.ncbi.nlm.nih.gov/32502336/;
In-vitro potency (enzymatic assay): IC50(PIK3CB) = 3270 nM, https://pubmed.ncbi.nlm.nih.gov/32502336/;

Screened at 1 µM, closest targets >95 % of control: MAP2K5, STK10, ZAK, GSK3B (100%) further targets not named;

Screened at 1 µM, closest targets as % of control: FLT3 (67%), DMPK (58%), AXL (57%), NTRK1 (56%), CSF1R (54%), EPHA7 (51%), further screening data not shown in paper, https://pubmed.ncbi.nlm.nih.gov/28814543/;

Screened at 1 µM, closest targets as % of control: FLT3 (67%), DMPK (58%), AXL (57%), NTRK1 (56%), CSF1R (54%), EPHA7 (51%), further screening data not shown in paper, https://pubmed.ncbi.nlm.nih.gov/28814543/;

Screened at 1 µM, S-Score(35) = 0.01, closest targets with >35% of inhibition: RPS6KA6, DYRK1A, https://pubmed.ncbi.nlm.nih.gov/30024858/;
In-vitro potency (competition-binding assay, DiscoverX): Kd(RPS6KA6) = 430 nM, https://pubmed.ncbi.nlm.nih.gov/30024858/;
In-vitro potency (competition-binding assay, DiscoverX): Kd(DYRK1A) = 220 nM, https://pubmed.ncbi.nlm.nih.gov/30024858/;
In-vitro potency (competition-binding assay, DiscoverX): Kd(MAP3K5) = 4.1 nM, https://pubmed.ncbi.nlm.nih.gov/30024858/;

Screened at 1 µM, closest targets as % of control: CLK4 (20%), ERN1 (33%), GAK (33%), KIT(V559D/V654A, 27%), CDK17 (2.7%), full screening data are available as supporting information, https://pubmed.ncbi.nlm.nih.gov/30779566/;
In-vitro potency (LanthaScreen Eu Kinase binding FRET assay): IC50(ERN2) = 7682 nM, https://pubmed.ncbi.nlm.nih.gov/30779566/;

Screened at 1 µM, closest targets as % of activity: FMS (46%), full screening data are available as supporting information, https://pubmed.ncbi.nlm.nih.gov/19808981/;
Screened at 1 µM, PI3-Kinase HTRF assay, closest targets: PIK3CB (9%), PIK3CG (3%), screening data are not available in paper, https://pubmed.ncbi.nlm.nih.gov/19808981/;
In-vitro potency (enzymatic assay): IC50(DNAPK) = 17 µM, https://pubmed.ncbi.nlm.nih.gov/19808981/;
In-vitro potency (enzymatic assay): IC50(ATR) >10 µM, https://pubmed.ncbi.nlm.nih.gov/19808981/;

Screened at 1 µM, closest targets as % of control: AAK1 (2.1%), PRP4 (28%). RIOK1 (3.9%), RIOK3 (6.6%), BIKE (3.5%), SGK085 (7.6%), SGK288 (13%), SRPK1 (19%), SRPK2 (28%), LBK1 (9.7%), DRAK1 (6.4%), DRAK2 (30%), PIP5K2C (9.5%), full screening data arae available as supporting information, https://pubmed.ncbi.nlm.nih.gov/27411717/;
Screened against 43 receptors, transporters, and enzymes (enzymatic assays), closest target: IC50(PDE4) = 8.3 µM, full screening data are available as supporting information, https://pubmed.ncbi.nlm.nih.gov/27411717/;
Screened against 8 receptors, transporters, and enzymes (enzymatic assays), closest target: IC50(α2A ) >1 µM, IC50(α2C) >1 µM, full screening data are available as supporting information, https://pubmed.ncbi.nlm.nih.gov/27411717/;

Screened at 1 µM, closest targets as % of control: AAK1 (2.1%), PRP4 (28%). RIOK1 (3.9%), RIOK3 (6.6%), BIKE (3.5%), SGK085 (7.6%), SGK288 (13%), SRPK1 (19%), SRPK2 (28%), LBK1 (9.7%), DRAK1 (6.4%), DRAK2 (30%), PIP5K2C (9.5%), full screening data arae available as supporting information, https://pubmed.ncbi.nlm.nih.gov/27411717/;
Screened against 43 receptors, transporters, and enzymes (enzymatic assays), closest target: IC50(PDE4) = 8.3 µM, full screening data are available as supporting information, https://pubmed.ncbi.nlm.nih.gov/27411717/;
Screened against 8 receptors, transporters, and enzymes (enzymatic assays), closest target: IC50(α2A ) >1 µM, IC50(α2C) >1 µM, full screening data are available as supporting information, https://pubmed.ncbi.nlm.nih.gov/27411717/;

Screened at 1.2 µM (85-fold ist cellular IC50), closest targets in the screen: EPHA1, EPHA2, EPHB2, EPHB3, EPHB4, FRK, SRC, WEE1;
In-cellular potency (NanoBRET assay, HEK293 cells): IC50(FRK) = 1.14 µM, https://pubmed.ncbi.nlm.nih.gov/35880755/;
In-cellular potency (NanoBRET assay, HEK293 cells): IC50(SRC) >8.3 µM, https://pubmed.ncbi.nlm.nih.gov/35880755/;
In-cellular potency (NanoBRET assay, HEK293 cells): IC50(WEE1) = 4.1 µM, https://pubmed.ncbi.nlm.nih.gov/35880755/;

Screened at 1.2 µM (85-fold ist cellular IC50), closest targets in the screen: EPHA1, EPHA2, EPHB2, EPHB3, EPHB4, FRK, SRC, WEE1;
In-cellular potency (NanoBRET assay, HEK293 cells): IC50(FRK) = 1.14 µM, https://pubmed.ncbi.nlm.nih.gov/35880755/;
In-cellular potency (NanoBRET assay, HEK293 cells): IC50(SRC) >8.3 µM, https://pubmed.ncbi.nlm.nih.gov/35880755/;
In-cellular potency (NanoBRET assay, HEK293 cells): IC50(WEE1) = 4.1 µM, https://pubmed.ncbi.nlm.nih.gov/35880755/;

Screened at 1.2 µM (85-fold ist cellular IC50), closest targets in the screen: EPHA1, EPHA2, EPHB2, EPHB3, EPHB4, FRK, SRC, WEE1;
In-cellular potency (NanoBRET assay, HEK293 cells): IC50(FRK) = 1.14 µM, https://pubmed.ncbi.nlm.nih.gov/35880755/;
In-cellular potency (NanoBRET assay, HEK293 cells): IC50(SRC) >8.3 µM, https://pubmed.ncbi.nlm.nih.gov/35880755/;
In-cellular potency (NanoBRET assay, HEK293 cells): IC50(WEE1) = 4.1 µM, https://pubmed.ncbi.nlm.nih.gov/35880755/;

Screened at 1.2 µM (85-fold ist cellular IC50), closest targets in the screen: EPHA1, EPHA2, EPHB2, EPHB3, EPHB4, FRK, SRC, WEE1;
In-cellular potency (NanoBRET assay, HEK293 cells): IC50(FRK) = 1.14 µM, https://pubmed.ncbi.nlm.nih.gov/35880755/;
In-cellular potency (NanoBRET assay, HEK293 cells): IC50(SRC) >8.3 µM, https://pubmed.ncbi.nlm.nih.gov/35880755/;
In-cellular potency (NanoBRET assay, HEK293 cells): IC50(WEE1) = 4.1 µM, https://pubmed.ncbi.nlm.nih.gov/35880755/;

Screened at 1.2 µM (85-fold ist cellular IC50), closest targets in the screen: EPHA1, EPHA2, EPHB2, EPHB3, EPHB4, FRK, SRC, WEE1;
In-cellular potency (NanoBRET assay, HEK293 cells): IC50(FRK) = 1.14 µM, https://pubmed.ncbi.nlm.nih.gov/35880755/;
In-cellular potency (NanoBRET assay, HEK293 cells): IC50(SRC) >8.3 µM, https://pubmed.ncbi.nlm.nih.gov/35880755/;
In-cellular potency (NanoBRET assay, HEK293 cells): IC50(WEE1) = 4.1 µM, https://pubmed.ncbi.nlm.nih.gov/35880755/;

Screened at 1.2 µM (85-fold ist cellular IC50), closest targets in the screen: EPHA1, EPHA2, EPHB2, EPHB3, EPHB4, FRK, SRC, WEE1;
In-cellular potency (NanoBRET assay, HEK293 cells): IC50(FRK) = 1.14 µM, https://pubmed.ncbi.nlm.nih.gov/35880755/;
In-cellular potency (NanoBRET assay, HEK293 cells): IC50(SRC) >8.3 µM, https://pubmed.ncbi.nlm.nih.gov/35880755/;
In-cellular potency (NanoBRET assay, HEK293 cells): IC50(WEE1) = 4.1 µM, https://pubmed.ncbi.nlm.nih.gov/35880755/;

Screened at 1.2 µM (85-fold ist cellular IC50), closest targets in the screen: EPHA1, EPHA2, EPHB2, EPHB3, EPHB4, FRK, SRC, WEE1;
In-cellular potency (NanoBRET assay, HEK293 cells): IC50(FRK) = 1.14 µM, https://pubmed.ncbi.nlm.nih.gov/35880755/;
In-cellular potency (NanoBRET assay, HEK293 cells): IC50(SRC) >8.3 µM, https://pubmed.ncbi.nlm.nih.gov/35880755/;
In-cellular potency (NanoBRET assay, HEK293 cells): IC50(WEE1) = 4.1 µM, https://pubmed.ncbi.nlm.nih.gov/35880755/;

Screened at 1 µM, the closest targets as % of inhibition: DAPK3 (98.8%), DAKP1 (96.1%), CDK9/cyclin T1 (94.7%), DMPK (94.1%), CDK8/cyclin C (91.0%), MAPK12 (85.1%), STK17A (84.4%), CLK4 (84.1%), DYRK1A (82.0%), GSK3B (80.5%), other kinases <80%, https://pubmed.ncbi.nlm.nih.gov/31131319/;
In-vitro potency of closest targets:
In-vitro potency (Adapta assay): IC50(DAPK3) = 160 nM, https://pubmed.ncbi.nlm.nih.gov/31131319/;
In-vitro potency (Adapta assay): IC50(DAPK1) = 49.8 nM, https://pubmed.ncbi.nlm.nih.gov/31131319/;
In-vitro potency (LanthaScreen Eu kinase binding assay): IC50(CDK9/cyclin T1) = 36.9 nM, https://pubmed.ncbi.nlm.nih.gov/31131319/;
In-vitro potency (LanthaScreen Eu kinase binding assay): IC50(DMPK) = 44.2 nM, https://pubmed.ncbi.nlm.nih.gov/31131319/;
In-vitro potency (LanthaScreen Eu kinase binding assay): IC50(CDK8/cyclin C) = 101 nM, https://pubmed.ncbi.nlm.nih.gov/31131319/;
In-vitro potency (Z′-LYTE biochemical assay, using 100 µM ATP): IC50(MAPK12) = 155 nM, https://pubmed.ncbi.nlm.nih.gov/31131319/;
In-vitro potency (LanthaScreen Eu kinase binding assay): IC50(STK17A) = 115 nM, https://pubmed.ncbi.nlm.nih.gov/31131319/;
In-vitro potency (LanthaScreen Eu kinase binding assay): IC50(CLK4) = 99 nM, https://pubmed.ncbi.nlm.nih.gov/31131319/;
In-vitro potency (Z′-LYTE biochemical assay, using 100 µM ATP): IC50(DYRK1A) = 148 nM, https://pubmed.ncbi.nlm.nih.gov/31131319/;
In-vitro potency (Z′-LYTE biochemical assay, using 100 µM ATP): IC50(GSK3B) = 338 nM, https://pubmed.ncbi.nlm.nih.gov/31131319/;
In-vitro potency (Z′-LYTE biochemical assay): IC50(CDK2) = 6300 nM, https://pubmed.ncbi.nlm.nih.gov/31131319/;
In-vitro potency (biochemical assay): Kd(CDC7) = 0.424 nM, https://pubmed.ncbi.nlm.nih.gov/31131319/;

Screened at 1 µM, using HUH7 cell lysate, closest target as % of inhibition: FER (82.7%), https://pubmed.ncbi.nlm.nih.gov/25075558/;

Screened at 1 µM, using HUH7 cell lysate, closest target as % of inhibition: FER (82.7%), https://pubmed.ncbi.nlm.nih.gov/25075558/;

Screened at 1 µM, using HUH7 cell lysate, closest target as % of inhibition: FER (82.7%), https://pubmed.ncbi.nlm.nih.gov/25075558/;

Screened at 1 µM, using HUH7 cell lysate, closest target as % of inhibition: FER (82.7%), https://pubmed.ncbi.nlm.nih.gov/25075558/;

Screened at 1 µM, closest targets as % of control: CSNK2A1 (25%), CSNK2A2 (7.3%), LRRK2 (45%), PIK3CD (32%), PIK3CG(37%), PIP5K1C (7.3%), MAP3K7 (0.85%), full screening data available as supporting information,https://pubmed.ncbi.nlm.nih.gov/33859795/;

Screened in competition binding assays, in-vitro potency of closest targets: Kd(CSF1R) = 18 nM, Kd(DDR1) = 270 nM, Kd(FLT1) = 9.6 nM, Kd(FLT4) = 330 nM, Kd(KIT) = 5.1 nM, Kd(PDGFRA) = 96 nM, Kd(PDGFRB) = 25 nM, Kd(VEGFR2) = 62 nM, full screening data are available as supporting information, https://www.nature.com/articles/nbt1358;
In-vitro potency (Radiometric assay, using 8 µM ATP): IC50(FLT1) = 77 nM, https://pubmed.ncbi.nlm.nih.gov/10786682/;
In-vitro potency (Radiometric assay, using 8 µM ATP): IC50(FLK) = 270 nM, https://pubmed.ncbi.nlm.nih.gov/10786682/;
In-vitro potency (Radiometric assay, using 8 µM ATP): IC50(FLT4) = 660 nM, https://pubmed.ncbi.nlm.nih.gov/10786682/;
In-vitro potency (Radiometric assay, using 8 µM ATP): IC50(KIT) = 730 nM, https://pubmed.ncbi.nlm.nih.gov/10786682/;
In-vitro potency (Radiometric assay, using 8 µM ATP): IC50(FMS) = 1400 nM, https://pubmed.ncbi.nlm.nih.gov/10786682/;
In-vitro potency (Radiometric assay, using 8 µM ATP): IC50(PDGFRB) = 580 nM, https://pubmed.ncbi.nlm.nih.gov/10786682/;

Screened in competition binding assays usisng K-562, COLO 205, SK-N-BE(2) and MV-4-11 cell lysates, in-vitro potency of closest targets: Kd(DYRK1A) = 40 nM, Kd(CSNK2A1) = 22 nM, Kd(PIM1) = 22 nM, Kd(TAO3) = 2292 nM, Kd(CIT) = 3659 nM, Kd(GSK3B) = 8793 nM, all other targets Kd >3000 nM, full screening data are available at Chembl;

Screened in competition binding assays usisng K-562, COLO 205, SK-N-BE(2) and MV-4-11 cell lysates, in-vitro potency of closest targets: Kd(DYRK1A) = 40 nM, Kd(CSNK2A1) = 22 nM, Kd(PIM1) = 22 nM, Kd(TAO3) = 2292 nM, Kd(CIT) = 3659 nM, Kd(GSK3B) = 8793 nM, all other targets Kd >3000 nM, full screening data are available at Chembl;

Screened at 5 µM, closest targets >75% inhibition: MAP2K1, MAPK14, TGFBR2, ACVR1, CAMK2A, details an targets are not listed in the paper;
In-vitro potency (enzymatic assay): IC50(MAP2K1) = 721.8 nM, https://pubmed.ncbi.nlm.nih.gov/31986961/;
In-vitro potency (enzymatic assay): IC50(MAPK14) = 283.9 nM, https://pubmed.ncbi.nlm.nih.gov/31986961/;
In-vitro potency (enzymatic assay): IC50(TGFBR2) = 809.3 nM, https://pubmed.ncbi.nlm.nih.gov/31986961/;
In-vitro potency (enzymatic assay): IC50(ACVR1) = 183.8 nM, https://pubmed.ncbi.nlm.nih.gov/31986961/;

Screened at 5 µM, closest targets >75% inhibition: MAP2K1, MAPK14, TGFBR2, ACVR1, CAMK2A, details an targets are not listed in the paper;
In-vitro potency (enzymatic assay): IC50(MAP2K1) = 721.8 nM, https://pubmed.ncbi.nlm.nih.gov/31986961/;
In-vitro potency (enzymatic assay): IC50(MAPK14) = 283.9 nM, https://pubmed.ncbi.nlm.nih.gov/31986961/;
In-vitro potency (enzymatic assay): IC50(TGFBR2) = 809.3 nM, https://pubmed.ncbi.nlm.nih.gov/31986961/;
In-vitro potency (enzymatic assay): IC50(ACVR1) = 183.8 nM, https://pubmed.ncbi.nlm.nih.gov/31986961/;

Screened at 5 µM, closest targets >75% inhibition: MAP2K1, MAPK14, TGFBR2, ACVR1, CAMK2A, details an targets are not listed in the paper;
In-vitro potency (enzymatic assay): IC50(MAP2K1) = 721.8 nM, https://pubmed.ncbi.nlm.nih.gov/31986961/;
In-vitro potency (enzymatic assay): IC50(MAPK14) = 283.9 nM, https://pubmed.ncbi.nlm.nih.gov/31986961/;
In-vitro potency (enzymatic assay): IC50(TGFBR2) = 809.3 nM, https://pubmed.ncbi.nlm.nih.gov/31986961/;
In-vitro potency (enzymatic assay): IC50(ACVR1) = 183.8 nM, https://pubmed.ncbi.nlm.nih.gov/31986961/;

Screened at 1 µM, closest targets as % of inhibition: MAPK7 (99.2%), SRPK1 (35%), full screening data are available as supporting information, https://pubmed.ncbi.nlm.nih.gov/27679845/;
Screened at 10 µM, Kinase panel (KiNative chemoproteomics profiling, Jurkat cells), >200 kinases, closest targets as % of inhibition: MAPK7 (96.1%), NLK1 (41.7%), CDK7 (40.1%), full screening data are available as supporting information, https://pubmed.ncbi.nlm.nih.gov/27679845/;

Screened at 1 µM, closest targets as % of control: AAK1 (13%), MNK2 (35%), ACK1 (39%), BIKE (50%), full screening data are available as supporting information;
In-vitro potency (enzymatic assay): IC50(AAK1) = 212 nM, https://pubmed.ncbi.nlm.nih.gov/38330278/;
In-vitro potency (enzymatic assay): IC50(BIKE) = 902 nM, https://pubmed.ncbi.nlm.nih.gov/38330278/;
In-vitro potency (enzymatic assay): IC50(MNK2) = 2180 nM, https://pubmed.ncbi.nlm.nih.gov/38330278/;
In-vitro potency (enzymatic assay): IC50(HIPK4) = 2275 nM, https://pubmed.ncbi.nlm.nih.gov/38330278/;
In-vitro potency (enzymatic assay): IC50(ACK1) >3000 nM, https://pubmed.ncbi.nlm.nih.gov/38330278/;
In-vitro potency (enzymatic assay): IC50(DRAK2) >3000 nM, https://pubmed.ncbi.nlm.nih.gov/38330278/;
In-vitro potency (NanoBRET assay, HEK293T cells): IC50(AAK1) = 6.2 µM, https://www.sgc-ffm.uni-frankfurt.de/#!detailedpotencydataview/C3TD879
In-vitro potency (NanoBRET assay, HEK293T cells): IC50(BMP2K) >10 µM, https://www.sgc-ffm.uni-frankfurt.de/#!detailedpotencydataview/C3TD879
In-vitro potency (NanoBRET assay, HEK293T cells): IC50(MKNK2) = 5.5 µM, https://www.sgc-ffm.uni-frankfurt.de/#!detailedpotencydataview/C3TD879
In-vitro potency (NanoBRET assay, HEK293T cells): IC50(HIPK4) >10 µM, https://www.sgc-ffm.uni-frankfurt.de/#!detailedpotencydataview/C3TD879
In-vitro potency (NanoBRET assay, HEK293T cells): IC50(STK17B) >10 µM, https://www.sgc-ffm.uni-frankfurt.de/#!detailedpotencydataview/C3TD879
In-vitro potency (NanoBRET assay, HEK293T cells): IC50(AURKA) >10 µM, https://www.sgc-ffm.uni-frankfurt.de/#!detailedpotencydataview/C3TD879
In-vitro potency (NanoBRET assay, HEK293T cells): IC50(AURKB) >10 µM, https://www.sgc-ffm.uni-frankfurt.de/#!detailedpotencydataview/C3TD879
In-vitro potency (NanoBRET assay, HEK293T cells): IC50(GAK) >10 µM, https://www.sgc-ffm.uni-frankfurt.de/#!detailedpotencydataview/C3TD879
In-vitro potency (NanoBRET assay, HEK293T cells): IC50(PRKACA) >10 µM, https://www.sgc-ffm.uni-frankfurt.de/#!detailedpotencydataview/C3TD879

Screened at 1 µM against NR1A1, NR1B1, NR1C1, NR1C2, NR1C3, NR1D1, NR1F3, NR1H3, NR1H4, NR1I1, NR1I3, NR2A1, NR2B1, NR2C1, NR2C2, NR2E1, NR2E3, NR4A1, NR5A1 and VP16 in a Gal4 hybrid reporter gene assay (HEK293T cells were cotransfected with pFR-Luc reporter, pRL-SV40 control reporter and pFA-CMV

Screened at 1 µM against NR1A1, NR1B1, NR1C1, NR1C2, NR1C3, NR1D1, NR1F3, NR1H3, NR1H4, NR1I1, NR1I3, NR2A1, NR2B1, NR2C1, NR2C2, NR2E1, NR2E3, NR4A1, NR5A1 and VP16 in a Gal4 hybrid reporter gene assay (HEK293T cells were cotransfected with pFR-Luc reporter, pRL-SV40 control reporter and pFA-CMV

Screened at 1 µM against NR1A1, NR1B1, NR1C1, NR1C2, NR1C3, NR1D1, NR1F3, NR1H3, NR1H4, NR1I1, NR1I3, NR2A1, NR2B1, NR2C1, NR2C2, NR2E1, NR2E3, NR4A1, NR5A1 and VP16 in a Gal4 hybrid reporter gene assay (HEK293T cells were cotransfected with pFR-Luc reporter, pRL-SV40 control reporter and pFA-CMV

Screened at 1 µM against NR1A1, NR1B1, NR1C1, NR1C2, NR1C3, NR1D1, NR1F3, NR1H3, NR1H4, NR1I1, NR1I3, NR2A1, NR2B1, NR2C1, NR2C2, NR2E1, NR2E3, NR4A1, NR5A1 and VP16 in a Gal4 hybrid reporter gene assay (HEK293T cells were cotransfected with pFR-Luc reporter, pRL-SV40 control reporter and pFA-CMV

Screened at 1 µM against NR1A1, NR1B1, NR1C1, NR1C2, NR1C3, NR1D1, NR1F3, NR1H3, NR1H4, NR1I1, NR1I3, NR2A1, NR2B1, NR2C1, NR2C2, NR2E1, NR2E3, NR4A1, NR5A1 and VP16 in a Gal4 hybrid reporter gene assay (HEK293T cells were cotransfected with pFR-Luc reporter, pRL-SV40 control reporter and pFA-CMV

Screened at 1 µM against NR1A1, NR1B1, NR1C1, NR1C2, NR1C3, NR1D1, NR1F3, NR1H3, NR1H4, NR1I1, NR1I3, NR2A1, NR2B1, NR2C1, NR2C2, NR2E1, NR2E3, NR4A1, NR5A1 and VP16 in a Gal4 hybrid reporter gene assay (HEK293T cells were cotransfected with pFR-Luc reporter, pRL-SV40 control reporter and pFA-CMV

Screened at 1 µM against NR1A1, NR1B1, NR1C1, NR1C2, NR1C3, NR1D1, NR1F3, NR1H3, NR1H4, NR1I1, NR1I3, NR2A1, NR2B1, NR2C1, NR2C2, NR2E1, NR2E3, NR4A1, NR5A1 and VP16 in a Gal4 hybrid reporter gene assay (HEK293T cells were cotransfected with pFR-Luc reporter, pRL-SV40 control reporter and pFA-CMV

Screened at 1 µM against NR1A1, NR1B1, NR1C1, NR1C2, NR1C3, NR1D1, NR1F3, NR1H3, NR1H4, NR1I1, NR1I3, NR2A1, NR2B1, NR2C1, NR2C2, NR2E1, NR2E3, NR4A1, NR5A1 and VP16 in a Gal4 hybrid reporter gene assay (HEK293T cells were cotransfected with pFR-Luc reporter, pRL-SV40 control reporter and pFA-CMV

Screened at 1 µM against NR1A1, NR1B1, NR1C1, NR1C2, NR1C3, NR1D1, NR1F3, NR1H3, NR1H4, NR1I1, NR1I3, NR2A1, NR2B1, NR2C1, NR2C2, NR2E1, NR2E3, NR4A1, NR5A1 and VP16 in a Gal4 hybrid reporter gene assay (HEK293T cells were cotransfected with pFR-Luc reporter, pRL-SV40 control reporter and pFA-CMV