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Assay Detail

CHEMBL4344313

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Binding
Inhibition of N-terminal His6-tagged human Mcl1 expressed in Escherichia coli Rosetta2 DE3 by fluorescent labeled Flu-Bid peptide based fluorescence polarization assay
27
Total Activities
27
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

Publication

Discovery and Characterization of 2,5-Substituted Benzoic Acid Dual Inhibitors of the Anti-apoptotic Mcl-1 and Bfl-1 Proteins.
Kump KJ, Miao L, Mady ASA, Ansari NH, Shrestha UK, Yang Y, Pal M, Liao C, Perdih A, Abulwerdi FA, Chinnaswamy K, Meagher JL, Carlson JM, Khanna M, Stuckey JA, Nikolovska-Coleska Z.
J Med Chem (2020) 63 : 2489 -2510
PubMed 31971799 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 27 5.90 7.14

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4522193 1 7.14
CHEMBL4533559 1 7.13
CHEMBL4462138 1 7.06
CHEMBL4558313 1 7.05
CHEMBL4576854 1 7.03
CHEMBL4463305 1 6.70
CHEMBL4457901 1 6.66
CHEMBL4454113 1 6.54
CHEMBL4452560 1 6.48
CHEMBL4475729 1 6.24
CHEMBL4440719 1 6.11
CHEMBL4435041 1 6.09
CHEMBL4473975 1 6.08
CHEMBL4525910 1 6.02
CHEMBL4448621 1 5.82
CHEMBL4577267 1 5.77
CHEMBL4463594 1 5.70
CHEMBL4461974 1 5.58
CHEMBL4435893 1 5.57
CHEMBL4442233 1 5.47
CHEMBL4459843 1 5.33
CHEMBL4528399 1 5.21
CHEMBL4534654 1 4.88
CHEMBL4553113 1 4.72
CHEMBL4456253 1 4.48
CHEMBL285503 1 4.32
CHEMBL4461424 1 4.15

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4522193 Ki = 73.0 nM 7.14
CHEMBL4533559 Ki = 74.0 nM 7.13
CHEMBL4462138 Ki = 87.0 nM 7.06
CHEMBL4558313 Ki = 90.0 nM 7.05
CHEMBL4576854 Ki = 94.0 nM 7.03
CHEMBL4463305 Ki = 200.0 nM 6.70
CHEMBL4457901 Ki = 220.0 nM 6.66
CHEMBL4454113 Ki = 290.0 nM 6.54
CHEMBL4452560 Ki = 330.0 nM 6.48
CHEMBL4475729 Ki = 570.0 nM 6.24
CHEMBL4440719 Ki = 770.0 nM 6.11
CHEMBL4435041 Ki = 810.0 nM 6.09
CHEMBL4473975 Ki = 840.0 nM 6.08
CHEMBL4525910 Ki = 950.0 nM 6.02
CHEMBL4448621 Ki = 1500.0 nM 5.82
CHEMBL4577267 Ki = 1700.0 nM 5.77
CHEMBL4463594 Ki = 2000.0 nM 5.70
CHEMBL4461974 Ki = 2600.0 nM 5.58
CHEMBL4435893 Ki = 2700.0 nM 5.57
CHEMBL4442233 Ki = 3400.0 nM 5.47
CHEMBL4459843 Ki = 4700.0 nM 5.33
CHEMBL4528399 Ki = 6100.0 nM 5.21
CHEMBL4534654 Ki = 13100.0 nM 4.88
CHEMBL4553113 Ki = 19000.0 nM 4.72
CHEMBL4456253 Ki = 32800.0 nM 4.48
CHEMBL285503 Ki = 47800.0 nM 4.32
CHEMBL4461424 Ki = 70400.0 nM 4.15