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Assay Detail

CHEMBL2186857

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

Functional
Antiproliferative activity against human KU812 cells expressing wild type Bcr-Abl after 72 hrs by CCK-8 assay
38
Total Activities
38
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type KU812
Confidence 1 — Organism
Curated By Autocuration

Publication

Design, synthesis, and biological evaluation of 3-(1H-1,2,3-triazol-1-yl)benzamide derivatives as Potent Pan Bcr-Abl inhibitors including the threonine(315)→isoleucine(315) mutant.
Li Y, Shen M, Zhang Z, Luo J, Pan X, Lu X, Long H, Wen D, Zhang F, Leng F, Li Y, Tu Z, Ren X, Ding K, Ding K.
J Med Chem (2012) 55 : 10033 -10046
PubMed 23088644 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 38 9.12 10.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2178277 1 10.10
CHEMBL1214141 1 10.10
CHEMBL2178278 1 10.00
CHEMBL2178276 1 10.00
CHEMBL2177645 1 9.96
CHEMBL2177642 1 9.85
CHEMBL2177646 1 9.82
CHEMBL2177632 1 9.80
CHEMBL2177634 1 9.80
CHEMBL2177647 1 9.72
CHEMBL2177633 1 9.70
CHEMBL2177635 1 9.70
CHEMBL2177636 1 9.66
CHEMBL2177649 1 9.62
CHEMBL2178268 1 9.42
CHEMBL2178279 1 9.41
CHEMBL2178271 1 9.40
CHEMBL2178274 1 9.40
CHEMBL2178270 1 9.37
CHEMBL2178267 1 9.34
CHEMBL2178273 1 9.34
CHEMBL2177650 1 9.33
CHEMBL2177648 1 9.17
CHEMBL2178272 1 9.14
CHEMBL2178275 1 8.87
CHEMBL2177637 1 8.84
CHEMBL2178269 1 8.83
CHEMBL2177631 1 8.82
CHEMBL2177638 1 8.80
CHEMBL2177639 1 8.72

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2178277 IC50 = 0.08 nM 10.10
CHEMBL1214141 IC50 = 0.08 nM 10.10
CHEMBL2178276 IC50 = 0.1 nM 10.00
CHEMBL2178278 IC50 = 0.1 nM 10.00
CHEMBL2177645 IC50 = 0.11 nM 9.96
CHEMBL2177642 IC50 = 0.14 nM 9.85
CHEMBL2177646 IC50 = 0.15 nM 9.82
CHEMBL2177632 IC50 = 0.16 nM 9.80
CHEMBL2177634 IC50 = 0.16 nM 9.80
CHEMBL2177647 IC50 = 0.19 nM 9.72
CHEMBL2177635 IC50 = 0.2 nM 9.70
CHEMBL2177633 IC50 = 0.2 nM 9.70
CHEMBL2177636 IC50 = 0.22 nM 9.66
CHEMBL2177649 IC50 = 0.24 nM 9.62
CHEMBL2178268 IC50 = 0.38 nM 9.42
CHEMBL2178279 IC50 = 0.39 nM 9.41
CHEMBL2178271 IC50 = 0.4 nM 9.40
CHEMBL2178274 IC50 = 0.4 nM 9.40
CHEMBL2178270 IC50 = 0.43 nM 9.37
CHEMBL2178267 IC50 = 0.46 nM 9.34
CHEMBL2178273 IC50 = 0.46 nM 9.34
CHEMBL2177650 IC50 = 0.47 nM 9.33
CHEMBL2177648 IC50 = 0.68 nM 9.17
CHEMBL2178272 IC50 = 0.73 nM 9.14
CHEMBL2178275 IC50 = 1.34 nM 8.87
CHEMBL2177637 IC50 = 1.44 nM 8.84
CHEMBL2178269 IC50 = 1.48 nM 8.83
CHEMBL2177631 IC50 = 1.51 nM 8.82
CHEMBL2177638 IC50 = 1.57 nM 8.80
CHEMBL2177639 IC50 = 1.89 nM 8.72
CHEMBL2178280 IC50 = 4.05 nM 8.39
CHEMBL2177630 IC50 = 11.1 nM 7.96
CHEMBL2177641 IC50 = 11.2 nM 7.95
CHEMBL2177644 IC50 = 12.2 nM 7.91
CHEMBL2178281 IC50 = 14.2 nM 7.85
CHEMBL2177629 IC50 = 14.6 nM 7.84
CHEMBL2177643 IC50 = 19.6 nM 7.71
CHEMBL2177640 IC50 = 158.0 nM 6.80