Compound name
BI 605906
Protein family
Protein Kinase
Target name
IKBKB
Affinity biochemical (nM)
49
Affinity on-target cellular (nM)
900
CG-Set
Kinase set
Recommended Concentration
1 µM
Compound EUbOPEN ID
EUB0001492b
SMILES
CCC(F)(F)c1cc(N2CCC(S(C)(=O)=O)CC2)nc2sc(C(N)=O)c(N)c12
InChIKey
IYHHRZBKXXKDDY-UHFFFAOYSA-N
NCBI gene ID
3551
UniProt ID
O14920
Synonyms
IKK2, NFKBIKB, IKK-beta, IKKB
Mode of action
inhibitor
Negative control
BI-5026
Affinity biochemical definition
IC50
Affinity biochemical assay type
Enzymatic inhibition assay
Affinity Biochemical Source Knowledge
https://www.sgc-ffm.uni-frankfurt.de/chemProbes#!specificprobeoverview/BI%20605906
Affinity biochemical relation
=
Affinity on-target cellular definition
EC50
Affinity on-target cellular assay type
Cellular assay (inhibition of phospho-IKBKB in HeLa cells)
Affinity on-target cellular source knowledge
https://www.sgc-ffm.uni-frankfurt.de/chemProbes#!specificprobeoverview/BI%20605906
Affinity on-target cellular relation
=
Selectivity platform
Kinase panel (Boehringer Ingelheim)
Selectivity platform number of targets
397
Selectivity remarks
Screened at 10 µM, in-vitro potencies of closest targets (enzymatic assays): IC50(AAK1) = 188 nM, IC50(GAK) = 272 nM, IC50(IRAK3) = 921 nM; In-cellulo follow-up of closest targets (NanoBRET assay in HEK293T cells): IC50(AAK1) = 7 µM, IC50(GAK) = 6.5 µM, IC50(IRAK3) >20 µM (https://www.sgc-ffm.uni-frankfurt.de/chemProbes#!specificprobeoverview/BI%20605906); Screened at 10 µM in Panlabs panel, closest targets as % of contr.: PDE3A (31%), all other targets >50% (https://www.sgc-ffm.uni-frankfurt.de/chemProbes#!specificprobeoverview/BI%20605906); Screened at 10 µM against 45 GPCRs (PDSP screen), in-vitro potencies of closest targets: Ki(DRD3) = 428.07 nM, Ki(DRD2) = 341.44 nM, Ki(GABA/PBR) = 2622.51 nM (https://www.sgc-ffm.uni-frankfurt.de/chemProbes#!specificprobeoverview/BI%20605906);
Selectivity Source Knowledge
https://www.sgc-ffm.uni-frankfurt.de/chemProbes#!specificprobeoverview/BI%20605906