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Assay Detail

CHEMBL1176863

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Functional
Antiproliferative activity against mouse BA/F3 cells expressing ABL T315I mutant after 3 days by MTS assay
ChEMBL ↗
43
Total Activities
43
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

BaF3 (CHEMBL614524) ↗
Type CELL-LINE
Organism Mus musculus

Publication

Discovery of 3-[2-(imidazo[1,2-b]pyridazin-3-yl)ethynyl]-4-methyl-N-{4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl}benzamide (AP24534), a potent, orally active pan-inhibitor of breakpoint cluster region-abelson (BCR-ABL) kinase including the T315I gatekeeper mutant.
Huang WS, Metcalf CA, Sundaramoorthi R, Wang Y, Zou D, Thomas RM, Zhu X, Cai L, Wen D, Liu S, Romero J, Qi J, Chen I, Banda G, Lentini SP, Das S, Xu Q, Keats J, Wang F, Wardwell S, Ning Y, Snodgrass JT, Broudy MI, Russian K, Zhou T, Commodore L, Narasimhan NI, Mohemmad QK, Iuliucci J, Rivera VM, Dalgarno DC, Sawyer TK, Clackson T, Shakespeare WC.
J Med Chem (2010) 53 : 4701 -4719
PubMed 20513156 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 43 6.99 8.14

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1172004 — — 1 8.14
CHEMBL1173424 — — 1 8.07
CHEMBL1171837 PONATINIB 4.0 1 8.06
CHEMBL1171836 — — 1 7.89
CHEMBL1171479 — — 1 7.85
CHEMBL1171432 — — 1 7.85
CHEMBL1171247 — — 1 7.77
CHEMBL1170077 — — 1 7.66
CHEMBL1171086 — — 1 7.58
CHEMBL1171658 — — 1 7.51
CHEMBL1173352 — — 1 7.47
CHEMBL1173498 — — 1 7.46
CHEMBL1173423 — — 1 7.41
CHEMBL1171657 — — 1 7.38
CHEMBL1171044 — — 1 7.38
CHEMBL1171043 — — 1 7.37
CHEMBL1172585 — — 1 7.36
CHEMBL1169882 — — 1 7.31
CHEMBL1171281 — — 1 7.30
CHEMBL1171473 — — 1 7.24
CHEMBL1172397 — — 1 7.14
CHEMBL1169881 — — 1 7.11
CHEMBL1171038 — — 1 6.87
CHEMBL1169705 — — 1 6.80
CHEMBL1171045 — — 1 6.78
CHEMBL1170078 — — 1 6.69
CHEMBL1172718 — — 1 6.68
CHEMBL1173201 — — 1 6.68
CHEMBL1171282 — — 1 6.63
CHEMBL1171085 — — 1 6.60

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1172004 — IC50 = 7.3 nM 8.14
CHEMBL1173424 — IC50 = 8.6 nM 8.07
CHEMBL1171837 PONATINIB IC50 = 8.8 nM 8.06
CHEMBL1171836 — IC50 = 13.0 nM 7.89
CHEMBL1171479 — IC50 = 14.0 nM 7.85
CHEMBL1171432 — IC50 = 14.0 nM 7.85
CHEMBL1171247 — IC50 = 17.0 nM 7.77
CHEMBL1170077 — IC50 = 22.0 nM 7.66
CHEMBL1171086 — IC50 = 26.0 nM 7.58
CHEMBL1171658 — IC50 = 31.0 nM 7.51
CHEMBL1173352 — IC50 = 34.0 nM 7.47
CHEMBL1173498 — IC50 = 35.0 nM 7.46
CHEMBL1173423 — IC50 = 39.0 nM 7.41
CHEMBL1171657 — IC50 = 42.0 nM 7.38
CHEMBL1171044 — IC50 = 42.0 nM 7.38
CHEMBL1171043 — IC50 = 43.0 nM 7.37
CHEMBL1172585 — IC50 = 44.0 nM 7.36
CHEMBL1169882 — IC50 = 49.0 nM 7.31
CHEMBL1171281 — IC50 = 50.0 nM 7.30
CHEMBL1171473 — IC50 = 58.0 nM 7.24
CHEMBL1172397 — IC50 = 72.0 nM 7.14
CHEMBL1169881 — IC50 = 77.0 nM 7.11
CHEMBL1171038 — IC50 = 135.0 nM 6.87
CHEMBL1169705 — IC50 = 157.0 nM 6.80
CHEMBL1171045 — IC50 = 166.0 nM 6.78
CHEMBL1170078 — IC50 = 203.0 nM 6.69
CHEMBL1172718 — IC50 = 210.0 nM 6.68
CHEMBL1173201 — IC50 = 211.0 nM 6.68
CHEMBL1171282 — IC50 = 232.0 nM 6.63
CHEMBL1171085 — IC50 = 251.0 nM 6.60
CHEMBL1172719 — IC50 = 256.0 nM 6.59
CHEMBL559826 — IC50 = 298.0 nM 6.53
CHEMBL1173200 — IC50 = 295.0 nM 6.53
CHEMBL1171679 — IC50 = 295.0 nM 6.53
CHEMBL539433 — IC50 = 422.0 nM 6.38
CHEMBL1172586 — IC50 = 471.0 nM 6.33
CHEMBL1171835 — IC50 = 500.0 nM 6.30
CHEMBL1171280 — IC50 = 513.0 nM 6.29
CHEMBL1169875 — IC50 = 548.0 nM 6.26
CHEMBL1171283 — IC50 = 727.0 nM 6.14
CHEMBL1172720 — IC50 = 1132.0 nM 5.95
CHEMBL556874 — IC50 = 2746.0 nM 5.56
CHEMBL1169876 — IC50 = 7122.0 nM 5.15