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Assay Detail

CHEMBL1768524

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

Binding
Inhibition of human recombinant p38alpha expressed in Escherichia coli using ATF2 as a substrate by radioisotopic protein kinase assay
19
Total Activities
19
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

Synthesis and biological evaluation of 1-substituted-3(5)-(6-methylpyridin-2-yl)-4-(quinolin-6-yl)pyrazoles as transforming growth factor-β type 1 receptor kinase inhibitors.
Jin CH, Krishnaiah M, Sreenu D, Rao KS, Subrahmanyam VB, Park CY, Son JY, Sheen YY, Kim DK.
Bioorg Med Chem (2011) 19 : 2633 -2640
PubMed 21435890 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 19 6.25 6.32

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL492634 1 6.32
CHEMBL226838 1 6.23
CHEMBL1766456 1 6.20
CHEMBL1766441 1 -
CHEMBL1766442 1 -
CHEMBL1766443 1 -
CHEMBL1766444 1 -
CHEMBL1766445 1 -
CHEMBL1766446 1 -
CHEMBL1766447 1 -
CHEMBL1766448 1 -
CHEMBL1766440 1 -
CHEMBL1766450 1 -
CHEMBL1766451 1 -
CHEMBL1766452 1 -
CHEMBL1766453 1 -
CHEMBL1766454 1 -
CHEMBL1766455 1 -
CHEMBL1766449 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL492634 IC50 = 480.0 nM 6.32
CHEMBL226838 IC50 = 594.0 nM 6.23
CHEMBL1766456 IC50 = 630.0 nM 6.20
CHEMBL1766441 IC50 > 1000.0 nM -
CHEMBL1766442 IC50 > 1000.0 nM -
CHEMBL1766443 IC50 > 1000.0 nM -
CHEMBL1766444 IC50 > 1000.0 nM -
CHEMBL1766445 IC50 > 1000.0 nM -
CHEMBL1766446 IC50 > 1000.0 nM -
CHEMBL1766447 IC50 > 1000.0 nM -
CHEMBL1766448 IC50 > 1000.0 nM -
CHEMBL1766440 IC50 > 1000.0 nM -
CHEMBL1766450 IC50 > 1000.0 nM -
CHEMBL1766451 IC50 > 1000.0 nM -
CHEMBL1766452 IC50 > 1000.0 nM -
CHEMBL1766453 IC50 > 1000.0 nM -
CHEMBL1766454 IC50 > 1000.0 nM -
CHEMBL1766455 IC50 > 1000.0 nM -
CHEMBL1766449 IC50 > 1000.0 nM -