Compound name
A-1211212
Protein family
Apoptosis regulator
Target name
BCL2
Affinity biochemical (nM)
1.4
CG-Set
Other targets
Recommended Concentration
1 µM
Compound EUbOPEN ID
EUB0000263b
SMILES
CO[C@H]1CC[C@H](CNc2ccc(S(=O)(=O)NC(=O)c3ccc(N4CCN(CC5=C(c6ccc(Cl)cc6)CC(C)(C)CC5)CC4)cc3Oc3cnc4[nH]ccc4c3)cc2[N+](=O)[O-])CC1
InChIKey
CSBKUBOVPUXFLO-MAVVKCOWSA-N
NCBI gene ID
596
UniProt ID
P10415
Synonyms
BCL2
Mode of action
Inhibitor
Negative control
A-1210227
Affinity biochemical definition
IC50
Affinity biochemical assay type
TR-FRET assay
Affinity Biochemical Source Knowledge
https://doi.org/10.1126/scitranslmed.aaa4642
https://www.sgc-ffm.uni-frankfurt.de/#!specificprobeoverview/A-1211212
Affinity biochemical relation
=
Selectivity platform
CEREP panel (Eurofins)
Selectivity platform number of targets
71
Selectivity remarks
Screened at 10 µM (binding assays), closest targets as % inhibition: Ca2+ channel (L, dihydropyridine site); Screened against 468 kinases (KinomeScan DiscoverX) at 1 µM, closest targets as % of contr.: HIPK4 (4.4%), MAPK12 (47%); Screened against 45 GPCR targets (PDSP screen) at 10 µM, closest target: Ki(TMEM97) = 1491.08 nM; Screened in Eurofins-Cerep panel against 7 targets at 10 µM (enzymes and uptake assays): clean profile;
Selectivity Source Knowledge
https://www.sgc-ffm.uni-frankfurt.de/#!specificprobeoverview/A-1211212
Selectivity Number of Off-targets
0