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Assay Detail

CHEMBL4180100

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

Binding
Inhibition of recombinant human HCK SH3-SH2-KD (75 to 526 residues) after 20 mins by mobility shift assay
32
Total Activities
32
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

Identification of pyrrolo[2,3-d]pyrimidines as potent HCK and FLT3-ITD dual inhibitors.
Koda Y, Kikuzato K, Mikuni J, Tanaka A, Yuki H, Honma T, Tomabechi Y, Kukimoto-Niino M, Shirouzu M, Shirai F, Koyama H.
Bioorg Med Chem Lett (2017) 27 : 4994 -4998
PubMed 29037944 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 32 7.66 9.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL45177 1 9.40
CHEMBL4208645 1 8.74
CHEMBL4066401 1 8.43
CHEMBL4093003 1 8.36
CHEMBL4207885 1 8.27
CHEMBL4215201 1 8.20
CHEMBL4206460 1 8.16
CHEMBL4209781 1 8.13
CHEMBL4216163 1 8.12
CHEMBL4202763 1 7.92
CHEMBL4218162 1 7.89
CHEMBL4203665 1 7.82
CHEMBL4213227 1 7.82
CHEMBL4210294 1 7.75
CHEMBL4203527 1 7.64
CHEMBL4205400 1 7.62
CHEMBL4209498 1 7.57
CHEMBL4202997 1 7.55
CHEMBL4205815 1 7.44
CHEMBL4212500 1 7.44
CHEMBL4214689 1 7.41
CHEMBL4203767 1 7.40
CHEMBL4207351 1 7.28
CHEMBL4216680 1 7.19
CHEMBL4209614 1 7.14
CHEMBL4204499 1 7.13
CHEMBL4212241 1 7.10
CHEMBL4208669 1 6.98
CHEMBL4213372 1 6.92
CHEMBL4212432 1 6.86

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL45177 IC50 = 0.4 nM 9.40
CHEMBL4208645 IC50 = 1.8 nM 8.74
CHEMBL4066401 IC50 = 3.7 nM 8.43
CHEMBL4093003 IC50 = 4.4 nM 8.36
CHEMBL4207885 IC50 = 5.4 nM 8.27
CHEMBL4215201 IC50 = 6.3 nM 8.20
CHEMBL4206460 IC50 = 6.9 nM 8.16
CHEMBL4209781 IC50 = 7.4 nM 8.13
CHEMBL4216163 IC50 = 7.5 nM 8.12
CHEMBL4202763 IC50 = 12.0 nM 7.92
CHEMBL4218162 IC50 = 13.0 nM 7.89
CHEMBL4203665 IC50 = 15.0 nM 7.82
CHEMBL4213227 IC50 = 15.0 nM 7.82
CHEMBL4210294 IC50 = 18.0 nM 7.75
CHEMBL4203527 IC50 = 23.0 nM 7.64
CHEMBL4205400 IC50 = 24.0 nM 7.62
CHEMBL4209498 IC50 = 27.0 nM 7.57
CHEMBL4202997 IC50 = 28.0 nM 7.55
CHEMBL4205815 IC50 = 36.0 nM 7.44
CHEMBL4212500 IC50 = 36.0 nM 7.44
CHEMBL4214689 IC50 = 39.0 nM 7.41
CHEMBL4203767 IC50 = 40.0 nM 7.40
CHEMBL4207351 IC50 = 52.0 nM 7.28
CHEMBL4216680 IC50 = 65.0 nM 7.19
CHEMBL4209614 IC50 = 73.0 nM 7.14
CHEMBL4204499 IC50 = 74.0 nM 7.13
CHEMBL4212241 IC50 = 79.0 nM 7.10
CHEMBL4208669 IC50 = 105.0 nM 6.98
CHEMBL4213372 IC50 = 119.0 nM 6.92
CHEMBL4212432 IC50 = 137.0 nM 6.86
CHEMBL4211710 IC50 = 200.0 nM 6.70
CHEMBL4207785 IC50 = 226.0 nM 6.65