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Assay Detail

CHEMBL985386

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

Binding
Displacement of fluorescein labeled Bax peptide from Bcl2 by fluorescence polarization assay
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Intermediate

Target

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

Publication

Discovery of an orally bioavailable small molecule inhibitor of prosurvival B-cell lymphoma 2 proteins.
Park CM, Bruncko M, Adickes J, Bauch J, Ding H, Kunzer A, Marsh KC, Nimmer P, Shoemaker AR, Song X, Tahir SK, Tse C, Wang X, Wendt MD, Yang X, Zhang H, Fesik SW, Rosenberg SH, Elmore SW.
J Med Chem (2008) 51 : 6902 -6915
PubMed 18841882 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 19 8.62 8.62

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL452892 1 8.62
CHEMBL444481 1 -
CHEMBL508865 1 -
CHEMBL448740 1 -
CHEMBL473870 1 -
CHEMBL451683 1 -
CHEMBL466090 1 -
CHEMBL469778 1 -
CHEMBL501889 1 -
CHEMBL376408 ABT 737 1.0 1 -
CHEMBL510761 1 -
CHEMBL449676 1 -
CHEMBL508864 1 -
CHEMBL509460 1 -
CHEMBL508093 1 -
CHEMBL500815 1 -
CHEMBL510351 1 -
CHEMBL443684 NAVITOCLAX 3.0 1 -
CHEMBL508210 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL452892 Ki = 2.4 nM 8.62
CHEMBL444481 Ki < 1.0 nM -
CHEMBL508865 Ki < 1.0 nM -
CHEMBL448740 Ki < 1.0 nM -
CHEMBL473870 Ki < 1.0 nM -
CHEMBL451683 Ki < 1.0 nM -
CHEMBL466090 Ki < 1.0 nM -
CHEMBL469778 Ki < 1.0 nM -
CHEMBL501889 Ki < 1.0 nM -
CHEMBL376408 ABT 737 Ki < 1.0 nM -
CHEMBL510761 Ki < 1.0 nM -
CHEMBL449676 Ki < 1.0 nM -
CHEMBL508864 Ki < 1.0 nM -
CHEMBL509460 Ki < 1.0 nM -
CHEMBL508093 Ki < 1.0 nM -
CHEMBL500815 Ki < 1.0 nM -
CHEMBL510351 Ki < 1.0 nM -
CHEMBL443684 NAVITOCLAX Ki < 1.0 nM -
CHEMBL508210 Ki < 1.0 nM -