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Assay Detail

CHEMBL3382383

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

Binding
Inhibition of BCL-2 (unknown origin) incubated for 1 hr by TR-FRET assay
13
Total Activities
13
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

Discovery of a Potent and Selective BCL-XL Inhibitor with in Vivo Activity.
Tao ZF, Hasvold L, Wang L, Wang X, Petros AM, Park CH, Boghaert ER, Catron ND, Chen J, Colman PM, Czabotar PE, Deshayes K, Fairbrother WJ, Flygare JA, Hymowitz SG, Jin S, Judge RA, Koehler MF, Kovar PJ, Lessene G, Mitten MJ, Ndubaku CO, Nimmer P, Purkey HE, Oleksijew A, Phillips DC, Sleebs BE, Smith BJ, Smith ML, Tahir SK, Watson KG, Xiao Y, Xue J, Zhang H, Zobel K, Rosenberg SH, Tse C, Leverson JD, Elmore SW, Souers AJ.
ACS Med Chem Lett (2014) 5 : 1088 -1093
PubMed 25313317 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 13 7.12 9.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3342193 1 9.85
CHEMBL3342197 1 7.22
CHEMBL3342332 A-1155463 1 7.10
CHEMBL3342333 1 7.06
CHEMBL3342191 A-1107969 1 7.05
CHEMBL3342334 1 7.05
CHEMBL3342189 1 7.00
CHEMBL3342196 1 6.85
CHEMBL3342194 1 6.82
CHEMBL3342192 1 6.77
CHEMBL3342190 1 6.66
CHEMBL3342195 1 6.62
CHEMBL3342198 1 6.55

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3342193 Ki = 0.14 nM 9.85
CHEMBL3342197 Ki = 60.0 nM 7.22
CHEMBL3342332 A-1155463 Ki = 80.0 nM 7.10
CHEMBL3342333 Ki = 88.0 nM 7.06
CHEMBL3342191 A-1107969 Ki = 90.0 nM 7.05
CHEMBL3342334 Ki = 90.0 nM 7.05
CHEMBL3342189 Ki = 100.0 nM 7.00
CHEMBL3342196 Ki = 140.0 nM 6.85
CHEMBL3342194 Ki = 150.0 nM 6.82
CHEMBL3342192 Ki = 170.0 nM 6.77
CHEMBL3342190 Ki = 220.0 nM 6.66
CHEMBL3342195 Ki = 240.0 nM 6.62
CHEMBL3342198 Ki = 280.0 nM 6.55