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Assay Detail

CHEMBL909602

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

Binding
Displacement of Bax-derived peptide from Bcl2 by fluorescence polarization assay
ChEMBL ↗
53
Total Activities
53
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Studies leading to potent, dual inhibitors of Bcl-2 and Bcl-xL.
Bruncko M, Oost TK, Belli BA, Ding H, Joseph MK, Kunzer A, Martineau D, McClellan WJ, Mitten M, Ng SC, Nimmer PM, Oltersdorf T, Park CM, Petros AM, Shoemaker AR, Song X, Wang X, Wendt MD, Zhang H, Fesik SW, Rosenberg SH, Elmore SW.
J Med Chem (2007) 50 : 641 -662
PubMed 17256834 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 53 8.11 9.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL374303 — — 1 9.15
CHEMBL221750 — — 1 9.00
CHEMBL375770 — — 1 8.85
CHEMBL426558 — — 1 8.82
CHEMBL268908 — — 1 8.80
CHEMBL375628 — — 1 8.74
CHEMBL376659 — — 1 8.70
CHEMBL376254 — — 1 8.70
CHEMBL374214 — — 1 8.68
CHEMBL373631 — — 1 8.60
CHEMBL375841 — — 1 8.57
CHEMBL375842 — — 1 8.51
CHEMBL385119 — — 1 8.49
CHEMBL385101 — — 1 8.47
CHEMBL221856 — — 1 8.46
CHEMBL387142 — — 1 8.35
CHEMBL437148 — — 1 8.34
CHEMBL439495 — — 1 8.21
CHEMBL386955 — — 1 8.19
CHEMBL374271 — — 1 8.18
CHEMBL373712 — — 1 8.09
CHEMBL222069 — — 1 8.03
CHEMBL376696 — — 1 8.02
CHEMBL373544 — — 1 7.89
CHEMBL221218 — — 1 7.80
CHEMBL218408 — — 1 7.77
CHEMBL374270 — — 1 7.70
CHEMBL373713 — — 1 7.45
CHEMBL376921 — — 1 7.40
CHEMBL221708 — — 1 7.34

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL374303 — Ki = 0.7 nM 9.15
CHEMBL221750 — Ki = 1.0 nM 9.00
CHEMBL375770 — Ki = 1.4 nM 8.85
CHEMBL426558 — Ki = 1.5 nM 8.82
CHEMBL268908 — Ki = 1.6 nM 8.80
CHEMBL375628 — Ki = 1.8 nM 8.74
CHEMBL376659 — Ki = 2.0 nM 8.70
CHEMBL376254 — Ki = 2.0 nM 8.70
CHEMBL374214 — Ki = 2.1 nM 8.68
CHEMBL373631 — Ki = 2.5 nM 8.60
CHEMBL375841 — Ki = 2.7 nM 8.57
CHEMBL375842 — Ki = 3.1 nM 8.51
CHEMBL385119 — Ki = 3.2 nM 8.49
CHEMBL385101 — Ki = 3.4 nM 8.47
CHEMBL221856 — Ki = 3.5 nM 8.46
CHEMBL387142 — Ki = 4.5 nM 8.35
CHEMBL437148 — Ki = 4.6 nM 8.34
CHEMBL439495 — Ki = 6.1 nM 8.21
CHEMBL386955 — Ki = 6.5 nM 8.19
CHEMBL374271 — Ki = 6.6 nM 8.18
CHEMBL373712 — Ki = 8.1 nM 8.09
CHEMBL222069 — Ki = 9.4 nM 8.03
CHEMBL376696 — Ki = 9.6 nM 8.02
CHEMBL373544 — Ki = 13.0 nM 7.89
CHEMBL221218 — Ki = 16.0 nM 7.80
CHEMBL218408 — Ki = 16.9 nM 7.77
CHEMBL374270 — Ki = 20.0 nM 7.70
CHEMBL373713 — Ki = 35.2 nM 7.45
CHEMBL376921 — Ki = 39.8 nM 7.40
CHEMBL221708 — Ki = 46.0 nM 7.34
CHEMBL373577 — Ki = 56.0 nM 7.25
CHEMBL385104 — Ki = 61.9 nM 7.21
CHEMBL374941 — Ki = 68.0 nM 7.17
CHEMBL192571 — Ki = 67.0 nM 7.17
CHEMBL387141 — Ki = 67.0 nM 7.17
CHEMBL437146 — Ki = 300.0 nM 6.52
CHEMBL221295 — Ki < 1.0 nM -
CHEMBL221294 — Ki < 1.0 nM -
CHEMBL374309 — Ki < 1.0 nM -
CHEMBL266944 — Ki < 1.0 nM -
CHEMBL374097 — Ki < 1.0 nM -
CHEMBL217960 — Ki < 1.0 nM -
CHEMBL376409 — Ki < 1.0 nM -
CHEMBL376408 ABT 737 Ki < 1.0 nM -
CHEMBL218524 — Ki < 1.0 nM -
CHEMBL384218 — Ki < 1.0 nM -
CHEMBL384217 — Ki < 1.0 nM -
CHEMBL221805 — Ki < 1.0 nM -
CHEMBL426535 — Ki < 1.0 nM -
CHEMBL376410 — Ki < 1.0 nM -