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Assay Detail

CHEMBL5710155

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

Binding
Binding affinity to BCL-W (unknown origin) assessed as dissociation constant incubated for 1 hrs by TR-FRET assay
6
Total Activities
6
Compounds Tested
1
Activity Types
2
Assay Parameters

Assay Information

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

Target

Bcl-2-like protein 2 (CHEMBL4677)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Exploiting selective BCL-2 family inhibitors to dissect cell survival dependencies and define improved strategies for cancer therapy.
Leverson JD, Phillips DC, Mitten MJ, Boghaert ER, Diaz D, Tahir SK, Belmont LD, Nimmer P, Xiao Y, Ma XM, Lowes KN, Kovar P, Chen J, Jin S, Smith M, Xue J, Zhang H, Oleksijew A, Magoc TJ, Vaidya KS, Albert DH, Tarrant JM, La N, Wang L, Tao ZF, Wendt MD, Sampath D, Rosenberg SH, Tse C, Huang DC, Fairbrother WJ, Elmore SW, Souers AJ.
Sci Transl Med (2015) 7
PubMed 25787766 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 6 7.59 8.70

Assay Parameters

Parameter Type Value Units Text
EFO_ID EFO_ID - MONDO:0004992
EFO_TERM EFO_TERM - cancer

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5712050 1 8.70
CHEMBL3793424 1 8.40
CHEMBL3342332 A-1155463 1 8.10
CHEMBL443684 NAVITOCLAX 3.0 1 7.68
CHEMBL3137309 VENETOCLAX 4.0 1 6.61
CHEMBL4228713 A-1211212 1 6.07

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5712050 Ki = 2.0 nM 8.70
CHEMBL3793424 Ki = 4.0 nM 8.40
CHEMBL3342332 A-1155463 Ki = 8.0 nM 8.10
CHEMBL443684 NAVITOCLAX Ki = 21.0 nM 7.68
CHEMBL3137309 VENETOCLAX Ki = 245.0 nM 6.61
CHEMBL4228713 A-1211212 Ki = 852.0 nM 6.07