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Assay Detail

CHEMBL2328333

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Binding affinity to Bcl-2 (unknown origin) by surface plasmon resonance analysis
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Apoptosis regulator Bcl-2 (CHEMBL4860)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

The role of the acidity of N-heteroaryl sulfonamides as inhibitors of bcl-2 family protein-protein interactions.
Touré BB, Miller-Moslin K, Yusuff N, Perez L, Doré M, Joud C, Michael W, DiPietro L, van der Plas S, McEwan M, Lenoir F, Hoe M, Karki R, Springer C, Sullivan J, Levine K, Fiorilla C, Xie X, Kulathila R, Herlihy K, Porter D, Visser M.
ACS Med Chem Lett (2013) 4 : 186 -190
PubMed 24900652 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 10 8.16 9.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL376408 ABT 737 1.0 1 9.22
CHEMBL2326747 1 8.70
CHEMBL2326746 1 8.52
CHEMBL2326744 1 8.30
CHEMBL2326745 1 8.15
CHEMBL2322026 1 8.10
CHEMBL2322022 1 8.00
CHEMBL2322027 1 7.85
CHEMBL2322021 1 7.77
CHEMBL2322020 1 6.98

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL376408 ABT 737 Kd = 0.6 nM 9.22
CHEMBL2326747 Kd = 2.0 nM 8.70
CHEMBL2326746 Kd = 3.0 nM 8.52
CHEMBL2326744 Kd = 5.0 nM 8.30
CHEMBL2326745 Kd = 7.0 nM 8.15
CHEMBL2322026 Kd = 8.0 nM 8.10
CHEMBL2322022 Kd = 10.0 nM 8.00
CHEMBL2322027 Kd = 14.0 nM 7.85
CHEMBL2322021 Kd = 17.0 nM 7.77
CHEMBL2322020 Kd = 104.0 nM 6.98