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Assay Detail

CHEMBL2186852

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Functional
Antiproliferative activity against mouse BA/F3 cells expressing wild type Bcr-Abl after 72 hrs by CCK-8 assay
ChEMBL ↗
41
Total Activities
41
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Mus musculus
Cell Type BaF3
Confidence 1 — Organism
Curated By Autocuration

Target

NON-PROTEIN TARGET (CHEMBL3879801) ↗
Type NON-MOLECULAR

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 41 7.95 8.69

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2177646 — — 1 8.69
CHEMBL2177645 — — 1 8.61
CHEMBL2177647 — — 1 8.61
CHEMBL2178277 — — 1 8.60
CHEMBL2177634 — — 1 8.56
CHEMBL2178270 — — 1 8.56
CHEMBL2177636 — — 1 8.52
CHEMBL2177635 — — 1 8.52
CHEMBL2177648 — — 1 8.52
CHEMBL2177642 — — 1 8.50
CHEMBL1214141 — — 1 8.50
CHEMBL2178278 — — 1 8.48
CHEMBL2177633 — — 1 8.47
CHEMBL2177649 — — 1 8.46
CHEMBL2178271 — — 1 8.44
CHEMBL2178274 — — 1 8.43
CHEMBL2178276 — — 1 8.41
CHEMBL2178268 — — 1 8.40
CHEMBL2178275 — — 1 8.40
CHEMBL2178279 — — 1 8.39
CHEMBL2178267 — — 1 8.35
CHEMBL5416410 DASATINIB 4.0 1 8.35
CHEMBL2178273 — — 1 8.34
CHEMBL2177632 — — 1 8.34
CHEMBL2178272 — — 1 8.33
CHEMBL2177650 — — 1 8.27
CHEMBL2177631 — — 1 8.14
CHEMBL2178269 — — 1 7.62
CHEMBL2177629 — — 1 7.56
CHEMBL2177639 — — 1 7.55

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2177646 — IC50 = 2.03 nM 8.69
CHEMBL2177645 — IC50 = 2.44 nM 8.61
CHEMBL2177647 — IC50 = 2.47 nM 8.61
CHEMBL2178277 — IC50 = 2.49 nM 8.60
CHEMBL2177634 — IC50 = 2.74 nM 8.56
CHEMBL2178270 — IC50 = 2.76 nM 8.56
CHEMBL2177636 — IC50 = 3.01 nM 8.52
CHEMBL2177635 — IC50 = 3.04 nM 8.52
CHEMBL2177648 — IC50 = 3.01 nM 8.52
CHEMBL2177642 — IC50 = 3.16 nM 8.50
CHEMBL1214141 — IC50 = 3.15 nM 8.50
CHEMBL2178278 — IC50 = 3.28 nM 8.48
CHEMBL2177633 — IC50 = 3.35 nM 8.47
CHEMBL2177649 — IC50 = 3.43 nM 8.46
CHEMBL2178271 — IC50 = 3.66 nM 8.44
CHEMBL2178274 — IC50 = 3.68 nM 8.43
CHEMBL2178276 — IC50 = 3.9 nM 8.41
CHEMBL2178268 — IC50 = 4.02 nM 8.40
CHEMBL2178275 — IC50 = 3.98 nM 8.40
CHEMBL2178279 — IC50 = 4.04 nM 8.39
CHEMBL2178267 — IC50 = 4.46 nM 8.35
CHEMBL5416410 DASATINIB IC50 = 4.5 nM 8.35
CHEMBL2178273 — IC50 = 4.54 nM 8.34
CHEMBL2177632 — IC50 = 4.54 nM 8.34
CHEMBL2178272 — IC50 = 4.72 nM 8.33
CHEMBL2177650 — IC50 = 5.39 nM 8.27
CHEMBL2177631 — IC50 = 7.31 nM 8.14
CHEMBL2178269 — IC50 = 23.8 nM 7.62
CHEMBL2177629 — IC50 = 27.4 nM 7.56
CHEMBL2177639 — IC50 = 28.2 nM 7.55
CHEMBL2177638 — IC50 = 28.3 nM 7.55
CHEMBL2177637 — IC50 = 32.8 nM 7.48
CHEMBL2178280 — IC50 = 32.9 nM 7.48
CHEMBL2177630 — IC50 = 47.9 nM 7.32
CHEMBL2177644 — IC50 = 56.2 nM 7.25
CHEMBL255863 NILOTINIB IC50 = 65.2 nM 7.19
CHEMBL2177641 — IC50 = 316.0 nM 6.50
CHEMBL2178281 — IC50 = 420.0 nM 6.38
CHEMBL2177643 — IC50 = 435.0 nM 6.36
CHEMBL2177640 — IC50 = 1243.0 nM 5.91
CHEMBL941 IMATINIB IC50 = 1834.0 nM 5.74