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Assay Detail

CHEMBL1679302

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

Binding
Inhibition of EGF-induced BMK1 autophosphorylation in human HeLa cells by SDS-PAGE analysis
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Mitogen-activated protein kinase 7 (CHEMBL5332)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of a benzo[e]pyrimido-[5,4-b][1,4]diazepin-6(11H)-one as a Potent and Selective Inhibitor of Big MAP Kinase 1.
Deng X, Yang Q, Kwiatkowski N, Sim T, McDermott U, Settleman JE, Lee JD, Gray NS.
ACS Med Chem Lett (2011) 2 : 195 -200
PubMed 21412406 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 19 6.41 6.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1673049 1 6.89
CHEMBL1673039 1 6.72
CHEMBL1673043 1 6.70
CHEMBL1673051 1 6.70
CHEMBL1673053 1 6.70
CHEMBL1673042 1 6.64
CHEMBL1673052 1 6.64
CHEMBL1673050 1 6.62
CHEMBL1673046 1 6.62
CHEMBL1673040 1 6.62
CHEMBL1673041 1 6.58
CHEMBL1673044 1 6.58
CHEMBL1673045 1 6.55
CHEMBL1673047 1 6.51
CHEMBL1673048 1 6.50
CHEMBL1673056 1 5.91
CHEMBL1673055 1 5.88
CHEMBL1673054 1 5.51
CHEMBL1673057 1 4.94

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1673049 IC50 = 130.0 nM 6.89
CHEMBL1673039 IC50 = 190.0 nM 6.72
CHEMBL1673043 IC50 = 200.0 nM 6.70
CHEMBL1673051 IC50 = 200.0 nM 6.70
CHEMBL1673053 IC50 = 200.0 nM 6.70
CHEMBL1673042 IC50 = 230.0 nM 6.64
CHEMBL1673052 IC50 = 230.0 nM 6.64
CHEMBL1673050 IC50 = 240.0 nM 6.62
CHEMBL1673046 IC50 = 240.0 nM 6.62
CHEMBL1673040 IC50 = 240.0 nM 6.62
CHEMBL1673041 IC50 = 260.0 nM 6.58
CHEMBL1673044 IC50 = 260.0 nM 6.58
CHEMBL1673045 IC50 = 280.0 nM 6.55
CHEMBL1673047 IC50 = 310.0 nM 6.51
CHEMBL1673048 IC50 = 320.0 nM 6.50
CHEMBL1673056 IC50 = 1240.0 nM 5.91
CHEMBL1673055 IC50 = 1320.0 nM 5.88
CHEMBL1673054 IC50 = 3100.0 nM 5.51
CHEMBL1673057 IC50 = 11380.0 nM 4.94