Cloned (Comment) | Organism |
---|---|
expression in Sf9 cell | Homo sapiens |
Crystallization (Comment) | Organism |
---|---|
in complex with inhibitor 4-[4-([[3-tert-butyl-1-(quinolin-6-yl)-1H-pyrazol-5-yl]carbamoyl]amino)-3-fluorophenoxy]-N-methylpyridine-2-carboxamide | Homo sapiens |
Inhibitors | Comment | Organism | Structure |
---|---|---|---|
4-[4-([[3-tert-butyl-1-(quinolin-6-yl)-1H-pyrazol-5-yl]carbamoyl]amino)-3-fluorophenoxy]-N-methylpyridine-2-carboxamide | inhibitor binds to residues Arg386/Glu282 that isoform ABL1 uses to switch between inactive and active conformations. It potently inhibits both unphosphorylated and phosphorylated ABL1 by inducing a type II inactive conformation, and retains efficacy against the majority of clinically relevant chronic myeloid leukemia resistance mutants, including T315I. The compound inhibits isoform BCR-ABL1T315I-expressing cell lines, prolongs survival in mouse models of T315I-mutant chronic myeloid leukemia and B-lymphoblastic leukemia, and inhibits primary patient leukemia cells expressing mutation T315I in vitro and in vivo | Homo sapiens |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Homo sapiens | P00519 | ABL1 | - |
Source Tissue | Comment | Organism | Textmining |
---|
Synonyms | Comment | Organism |
---|---|---|
ABL1 tyrosine kinase | - |
Homo sapiens |
IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
---|---|---|---|---|---|
0.0000008 | - |
wild-type, pH not specified in the publication, temperature not specified in the publication | Homo sapiens | 4-[4-([[3-tert-butyl-1-(quinolin-6-yl)-1H-pyrazol-5-yl]carbamoyl]amino)-3-fluorophenoxy]-N-methylpyridine-2-carboxamide | |
0.000004 | - |
mutant T315I, pH not specified in the publication, temperature not specified in the publication | Homo sapiens | 4-[4-([[3-tert-butyl-1-(quinolin-6-yl)-1H-pyrazol-5-yl]carbamoyl]amino)-3-fluorophenoxy]-N-methylpyridine-2-carboxamide |