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Assay Detail

CHEMBL922239

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Binding
Inhibition of human Chk1
10
Total Activities
10
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

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

Publication

Synthesis, checkpoint kinase 1 inhibitory properties and in vitro antiproliferative activities of new pyrrolocarbazoles.
Conchon E, Anizon F, Aboab B, Golsteyn RM, Léonce S, Pfeiffer B, Prudhomme M.
Bioorg Med Chem (2008) 16 : 4419 -4430
PubMed 18321713 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 10 6.70 7.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL388648 BIS-IMIDE A 1 7.70
CHEMBL265446 1 7.62
CHEMBL406938 1 7.29
CHEMBL240747 GRANULATIMIDE 1 7.09
CHEMBL413188 ISOGRANULATIMIDE 1 7.00
CHEMBL243930 1 6.57
CHEMBL244140 1 6.51
CHEMBL259432 1 5.72
CHEMBL265691 1 4.84
CHEMBL264661 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL388648 BIS-IMIDE A IC50 = 20.0 nM 7.70
CHEMBL265446 IC50 = 24.0 nM 7.62
CHEMBL406938 IC50 = 51.0 nM 7.29
CHEMBL240747 GRANULATIMIDE IC50 = 81.0 nM 7.09
CHEMBL413188 ISOGRANULATIMIDE IC50 = 100.0 nM 7.00
CHEMBL243930 IC50 = 269.0 nM 6.57
CHEMBL244140 IC50 = 311.0 nM 6.51
CHEMBL259432 IC50 = 1920.0 nM 5.72
CHEMBL265691 IC50 = 14500.0 nM 4.84
CHEMBL264661 IC50 - -