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Assay Detail

CHEMBL4056676

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

Binding
Inhibition of HCK (75 to 526 residues) (unknown origin) expressed in Sf9 insect cells after 120 mins
11
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Tyrosine-protein kinase HCK (CHEMBL3234)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Activity cliff for 7-substituted pyrrolo-pyrimidine inhibitors of HCK explained in terms of predicted basicity of the amine nitrogen.
Yuki H, Kikuzato K, Koda Y, Mikuni J, Tomabechi Y, Kukimoto-Niino M, Tanaka A, Shirai F, Shirouzu M, Koyama H, Honma T.
Bioorg Med Chem (2017) 25 : 4259 -4264
PubMed 28662963 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 11 6.97 9.37

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL45177 1 9.37
CHEMBL4093003 2 7.96
CHEMBL4085262 2 6.96
CHEMBL4065334 2 6.68
CHEMBL4103186 2 6.16
CHEMBL4073943 2 5.88

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL45177 IC50 = 0.4266 nM 9.37
CHEMBL4093003 IC50 = 10.96 nM 7.96
CHEMBL4093003 IC50 = 11.0 nM 7.96
CHEMBL4085262 IC50 = 111.0 nM 6.96
CHEMBL4085262 IC50 = 112.2 nM 6.95
CHEMBL4065334 IC50 = 208.93 nM 6.68
CHEMBL4065334 IC50 = 210.0 nM 6.68
CHEMBL4103186 IC50 = 691.83 nM 6.16
CHEMBL4103186 IC50 = 686.0 nM 6.16
CHEMBL4073943 IC50 = 1318.26 nM 5.88
CHEMBL4073943 IC50 = 1323.0 nM 5.88