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Assay Detail

CHEMBL859052

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Binding
Binding affinity to Bcl2 by fluorescence polarization assay
30
Total Activities
30
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Discovery and structure-activity relationship of antagonists of B-cell lymphoma 2 family proteins with chemopotentiation activity in vitro and in vivo.
Wendt MD, Shen W, Kunzer A, McClellan WJ, Bruncko M, Oost TK, Ding H, Joseph MK, Zhang H, Nimmer PM, Ng SC, Shoemaker AR, Petros AM, Oleksijew A, Marsh K, Bauch J, Oltersdorf T, Belli BA, Martineau D, Fesik SW, Rosenberg SH, Elmore SW.
J Med Chem (2006) 49 : 1165 -1181
PubMed 16451081 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 30 6.43 7.26

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL198903 1 7.26
CHEMBL201947 1 7.23
CHEMBL192571 1 7.17
CHEMBL380709 1 7.16
CHEMBL370835 1 7.14
CHEMBL379013 1 7.12
CHEMBL380502 1 7.04
CHEMBL202798 1 6.94
CHEMBL383399 1 6.92
CHEMBL370837 1 6.78
CHEMBL383229 1 6.72
CHEMBL370836 1 6.64
CHEMBL382648 1 6.50
CHEMBL201670 1 6.44
CHEMBL382018 1 6.40
CHEMBL204822 1 6.40
CHEMBL371861 1 6.36
CHEMBL434952 1 6.14
CHEMBL378820 1 6.13
CHEMBL380433 1 5.91
CHEMBL379895 1 5.90
CHEMBL372834 1 5.70
CHEMBL202964 1 5.67
CHEMBL202540 1 5.54
CHEMBL378808 1 5.49
CHEMBL203620 1 5.45
CHEMBL201669 1 5.34
CHEMBL382361 1 -
CHEMBL202509 1 -
CHEMBL204915 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL198903 Ki = 55.0 nM 7.26
CHEMBL201947 Ki = 58.8 nM 7.23
CHEMBL192571 Ki = 67.0 nM 7.17
CHEMBL380709 Ki = 70.0 nM 7.16
CHEMBL370835 Ki = 73.0 nM 7.14
CHEMBL379013 Ki = 75.0 nM 7.12
CHEMBL380502 Ki = 92.1 nM 7.04
CHEMBL202798 Ki = 116.0 nM 6.94
CHEMBL383399 Ki = 121.0 nM 6.92
CHEMBL370837 Ki = 165.0 nM 6.78
CHEMBL383229 Ki = 192.0 nM 6.72
CHEMBL370836 Ki = 231.0 nM 6.64
CHEMBL382648 Ki = 317.0 nM 6.50
CHEMBL201670 Ki = 366.0 nM 6.44
CHEMBL382018 Ki = 400.0 nM 6.40
CHEMBL204822 Ki = 402.0 nM 6.40
CHEMBL371861 Ki = 433.0 nM 6.36
CHEMBL434952 Ki = 721.0 nM 6.14
CHEMBL378820 Ki = 732.0 nM 6.13
CHEMBL380433 Ki = 1230.0 nM 5.91
CHEMBL379895 Ki = 1260.0 nM 5.90
CHEMBL372834 Ki = 1980.0 nM 5.70
CHEMBL202964 Ki = 2160.0 nM 5.67
CHEMBL202540 Ki = 2880.0 nM 5.54
CHEMBL378808 Ki = 3260.0 nM 5.49
CHEMBL203620 Ki = 3540.0 nM 5.45
CHEMBL201669 Ki = 4570.0 nM 5.34
CHEMBL382361 Ki > 10000.0 nM -
CHEMBL202509 Ki > 10000.0 nM -
CHEMBL204915 Ki > 10000.0 nM -