Compound name
SCH772984
Protein family
Protein Kinase
Target name
MAPK3
Affinity biochemical (nM)
8.3
Affinity on-target cellular (nM)
4
CG-Set
Kinase set
Recommended Concentration
100 nM
Compound EUbOPEN ID
EUB0002309a
SMILES
O=C(Nc1ccc2[nH]nc(-c3ccncc3)c2c1)[C@@H]1CCN(CC(=O)N2CCN(c3ccc(-c4ncccn4)cc3)CC2)C1
InChIKey
HDAJDNHIBCDLQF-RUZDIDTESA-N
NCBI gene ID
5595
UniProt ID
P27361
Synonyms
ERK1, p44mapk, p44erk1
Mode of action
Inhibitor
Affinity biochemical definition
IC50
Affinity biochemical assay type
Enzymatic assay (ATP-competitive assay platform, Life technology)
Affinity Biochemical Source Knowledge
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4687050/
Affinity biochemical relation
=
Affinity on-target cellular definition
IC50
Affinity on-target cellular assay type
Immunoblot assay (phosphorylation of ERK using A375 cells)
Affinity on-target cellular source knowledge
https://pubmed.ncbi.nlm.nih.gov/25977981/
Affinity on-target cellular relation
=
Selectivity platform
Kinome Scan (DiscoverX)
Selectivity platform number of targets
456
Selectivity remarks
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/;
Selectivity Source Knowledge
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4687050/
Selectivity Number of Off-targets
13