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Assay Detail

CHEMBL4361671

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

Binding
Inhibition of human recombinant untagged p38alpha expressed in Escherichia coli using ATF2 as substrate incubated for 60 mins in presence of [33P]-ATP by radiometric assay
16
Total Activities
16
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

Mitogen-activated protein kinase 14 (CHEMBL260)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Design, synthesis, and antifibrosis evaluation of 4-(benzo-[c][1,2,5]thiadiazol-5-yl)-3(5)-(6-methyl- pyridin-2-yl)pyrazole and 3(5)-(6-methylpyridin- 2-yl)-4-(thieno-[3,2,-c]pyridin-2-yl)pyrazole derivatives.
Zhu WJ, Cui BW, Wang HM, Nan JX, Piao HR, Lian LH, Jin CH.
Eur J Med Chem (2019) 180 : 15 -27
PubMed 31299584 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 16 5.41 6.31

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2364611 GALUNISERTIB 2.0 1 6.31
CHEMBL3260567 VACTOSERTIB 2.0 1 5.66
CHEMBL4461256 1 5.42
CHEMBL4594036 1 5.24
CHEMBL4527908 1 5.15
CHEMBL4576703 1 5.09
CHEMBL4513885 1 5.02
CHEMBL4569982 1 -
CHEMBL4530888 1 -
CHEMBL4471215 1 -
CHEMBL4474331 1 -
CHEMBL4455044 1 -
CHEMBL4460586 1 -
CHEMBL4520187 1 -
CHEMBL4531718 1 -
CHEMBL4570292 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2364611 GALUNISERTIB IC50 = 490.0 nM 6.31
CHEMBL3260567 VACTOSERTIB IC50 = 2180.0 nM 5.66
CHEMBL4461256 IC50 = 3800.0 nM 5.42
CHEMBL4594036 IC50 = 5800.0 nM 5.24
CHEMBL4527908 IC50 = 7040.0 nM 5.15
CHEMBL4576703 IC50 = 8120.0 nM 5.09
CHEMBL4513885 IC50 = 9460.0 nM 5.02
CHEMBL4569982 IC50 > 10000.0 nM -
CHEMBL4530888 IC50 > 10000.0 nM -
CHEMBL4471215 IC50 > 10000.0 nM -
CHEMBL4474331 IC50 > 10000.0 nM -
CHEMBL4455044 IC50 > 10000.0 nM -
CHEMBL4460586 IC50 > 10000.0 nM -
CHEMBL4520187 IC50 > 10000.0 nM -
CHEMBL4531718 IC50 > 10000.0 nM -
CHEMBL4570292 IC50 > 10000.0 nM -