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Target
Apoptosis regulator Bcl-2
Ligand
BDBM356821
Substrate
n/a
Meas. Tech.
TR-FRET (Time-Resolved Fluorescence-Resonance-Energy-Transfer) assay
Ki
<0.010±n/a nM
Citation
 Catron, N; Lindley, D; Miller, JM; Schmitt, EA; Tong, P Solid dispersions containing an apoptosis-inducing agent US Patent  US10213433 Publication Date 2/26/2019 
Target
Name:
Apoptosis regulator Bcl-2
Synonyms:
Apoptosis regulator Bcl-2 Protein | B-cell lymphoma 2 protein (Bcl-2) | BCL-2 | BCL2 | BCL2_HUMAN | Bcl-2 Protein
Type:
Homodimer or heterodimer
Mol. Mass.:
26269.11
Organism:
Homo sapiens (Human)
Description:
P10415
Residue:
239
Sequence:
MAHAGRTGYDNREIVMKYIHYKLSQRGYEWDAGDVGAAPPGAAPAPGIFSSQPGHTPHPAASRDPVARTSPLQTPAAPGAAAGPALSPVPPVVHLTLRQAGDDFSRRYRRDFAEMSSQLHLTPFTARGRFATVVEELFRDGVNWGRIVAFFEFGGVMCVESVNREMSPLVDNIALWMTEYLNRHLHTWIQDNGGWDAFVELYGPSMRPLFDFSWLSLKTLLSLALVGACITLGAYLGHK
  
Inhibitor
Name:
BDBM356821
Synonyms:
4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-[(4-{[(1R,4R,5R,6S)-5,6-dihydroxybicyclo[2.2.1]hept-2-yl]methoxy}-3-nitrophenyl)sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide | US10213433, Compound 203 | US11369599, Compound 203 | US20240043404, Example 203
Type:
Small organic molecule
Emp. Form.:
C47H51ClN6O9S
Mol. Mass.:
911.461
SMILES:
CC1(C)CCC(CN2CCN(CC2)c2ccc(C(=O)NS(=O)(=O)c3ccc(OCC4C[C@@H]5C[C@H]4[C@H](O)[C@@H]5O)c(c3)[N+]([O-])=O)c(Oc3cnc4[nH]ccc4c3)c2)=C(C1)c1ccc(Cl)cc1 |c:61,TLB:37:36:32:29.30,28:29:32:34.36,THB:35:34:32:29.30|
Structure:
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