Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL871263

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

Binding
Inhibition of CHK1
15
Total Activities
15
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

Serine/threonine-protein kinase Chk1 (CHEMBL4630)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

4-(Aminoalkylamino)-3-benzimidazole-quinolinones as potent CHK-1 inhibitors.
Ni ZJ, Barsanti P, Brammeier N, Diebes A, Poon DJ, Ng S, Pecchi S, Pfister K, Renhowe PA, Ramurthy S, Wagman AS, Bussiere DE, Le V, Zhou Y, Jansen JM, Ma S, Gesner TG.
Bioorg Med Chem Lett (2006) 16 : 3121 -3124
PubMed 16603354 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 15 7.99 9.49

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL377312 1 9.49
CHEMBL378967 1 9.46
CHEMBL209982 1 9.30
CHEMBL210639 1 8.98
CHEMBL382437 1 8.85
CHEMBL381952 1 8.48
CHEMBL210242 1 8.48
CHEMBL210035 1 8.14
CHEMBL377554 1 8.12
CHEMBL209256 1 7.66
CHEMBL377609 1 6.86
CHEMBL208937 1 6.32
CHEMBL383417 1 6.14
CHEMBL377345 1 5.53
CHEMBL209771 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL377312 IC50 = 0.32 nM 9.49
CHEMBL378967 IC50 = 0.35 nM 9.46
CHEMBL209982 IC50 = 0.5 nM 9.30
CHEMBL210639 IC50 = 1.04 nM 8.98
CHEMBL382437 IC50 = 1.4 nM 8.85
CHEMBL381952 IC50 = 3.3 nM 8.48
CHEMBL210242 IC50 = 3.3 nM 8.48
CHEMBL210035 IC50 = 7.2 nM 8.14
CHEMBL377554 IC50 = 7.6 nM 8.12
CHEMBL209256 IC50 = 21.7 nM 7.66
CHEMBL377609 IC50 = 138.0 nM 6.86
CHEMBL208937 IC50 = 482.0 nM 6.32
CHEMBL383417 IC50 = 731.0 nM 6.14
CHEMBL377345 IC50 = 2950.0 nM 5.53
CHEMBL209771 IC50 > 30000.0 nM -