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Assay Detail

CHEMBL871418

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Binding
Inhibition of c-ABL
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Tyrosine-protein kinase ABL1 (CHEMBL1862)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

3-Benzimidazol-2-yl-1H-indazoles as potent c-ABL inhibitors.
McBride CM, Renhowe PA, Gesner TG, Jansen JM, Lin J, Ma S, Zhou Y, Shafer CM.
Bioorg Med Chem Lett (2006) 16 : 3789 -3792
PubMed 16678414 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 17 7.14 8.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL210827 1 8.52
CHEMBL209753 1 8.15
CHEMBL376945 1 8.00
CHEMBL211508 1 7.70
CHEMBL211662 1 7.52
CHEMBL378024 1 7.52
CHEMBL379987 1 7.22
CHEMBL377346 1 7.22
CHEMBL211154 1 7.22
CHEMBL384213 1 6.89
CHEMBL377463 1 6.82
CHEMBL209704 1 6.70
CHEMBL209266 1 6.66
CHEMBL209305 1 6.64
CHEMBL1642 IMATINIB MESYLATE 4.0 1 6.37
CHEMBL378299 1 6.22
CHEMBL212673 1 6.05

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL210827 IC50 = 3.0 nM 8.52
CHEMBL209753 IC50 = 7.0 nM 8.15
CHEMBL376945 IC50 = 10.0 nM 8.00
CHEMBL211508 IC50 = 20.0 nM 7.70
CHEMBL211662 IC50 = 30.0 nM 7.52
CHEMBL378024 IC50 = 30.0 nM 7.52
CHEMBL379987 IC50 = 60.0 nM 7.22
CHEMBL377346 IC50 = 60.0 nM 7.22
CHEMBL211154 IC50 = 60.0 nM 7.22
CHEMBL384213 IC50 = 130.0 nM 6.89
CHEMBL377463 IC50 = 150.0 nM 6.82
CHEMBL209704 IC50 = 200.0 nM 6.70
CHEMBL209266 IC50 = 220.0 nM 6.66
CHEMBL209305 IC50 = 230.0 nM 6.64
CHEMBL1642 IMATINIB MESYLATE IC50 = 430.0 nM 6.37
CHEMBL378299 IC50 = 600.0 nM 6.22
CHEMBL212673 IC50 = 900.0 nM 6.05