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Assay Detail

CHEMBL1837693

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
38
Total Activities
38
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

TGF-beta receptor type-1 (CHEMBL4439)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis and biological evaluation of 1-substituted-3-(6-methylpyridin-2-yl)-4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)pyrazoles as transforming growth factor-β type 1 receptor kinase inhibitors.
Jin CH, Krishnaiah M, Sreenu D, Subrahmanyam VB, Rao KS, Mohan AV, Park CY, Son JY, Sheen YY, Kim DK.
Bioorg Med Chem Lett (2011) 21 : 6049 -6053
PubMed 21911290 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 38 5.48 6.32

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL492634 1 6.32
CHEMBL1835709 1 6.30
CHEMBL1824446 1 6.23
CHEMBL1835710 1 6.22
CHEMBL1835622 1 5.84
CHEMBL1835624 1 5.77
CHEMBL1835521 1 5.70
CHEMBL1835630 1 5.61
CHEMBL1835112 1 5.55
CHEMBL1835625 1 5.54
CHEMBL1835528 1 5.53
CHEMBL1835534 1 5.52
CHEMBL1835712 1 5.50
CHEMBL1835535 1 5.49
CHEMBL1835536 1 5.43
CHEMBL1835520 1 5.43
CHEMBL1835629 1 5.42
CHEMBL1835623 1 5.42
CHEMBL1835621 1 5.42
CHEMBL1835529 1 5.38
CHEMBL1835525 1 5.37
CHEMBL1835533 1 5.30
CHEMBL1835628 1 5.30
CHEMBL1835532 1 5.28
CHEMBL1835531 1 5.28
CHEMBL1835627 1 5.27
CHEMBL1835527 1 5.26
CHEMBL1835519 1 5.26
CHEMBL1835518 1 5.25
CHEMBL1835626 1 5.24

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL492634 IC50 = 480.0 nM 6.32
CHEMBL1835709 IC50 = 496.0 nM 6.30
CHEMBL1824446 IC50 = 594.0 nM 6.23
CHEMBL1835710 IC50 = 598.0 nM 6.22
CHEMBL1835622 IC50 = 1450.0 nM 5.84
CHEMBL1835624 IC50 = 1690.0 nM 5.77
CHEMBL1835521 IC50 = 1980.0 nM 5.70
CHEMBL1835630 IC50 = 2460.0 nM 5.61
CHEMBL1835112 IC50 = 2800.0 nM 5.55
CHEMBL1835625 IC50 = 2850.0 nM 5.54
CHEMBL1835528 IC50 = 2960.0 nM 5.53
CHEMBL1835534 IC50 = 3000.0 nM 5.52
CHEMBL1835712 IC50 = 3200.0 nM 5.50
CHEMBL1835535 IC50 = 3220.0 nM 5.49
CHEMBL1835520 IC50 = 3680.0 nM 5.43
CHEMBL1835536 IC50 = 3680.0 nM 5.43
CHEMBL1835629 IC50 = 3840.0 nM 5.42
CHEMBL1835623 IC50 = 3810.0 nM 5.42
CHEMBL1835621 IC50 = 3830.0 nM 5.42
CHEMBL1835529 IC50 = 4120.0 nM 5.38
CHEMBL1835525 IC50 = 4280.0 nM 5.37
CHEMBL1835533 IC50 = 4950.0 nM 5.30
CHEMBL1835628 IC50 = 5040.0 nM 5.30
CHEMBL1835532 IC50 = 5230.0 nM 5.28
CHEMBL1835531 IC50 = 5220.0 nM 5.28
CHEMBL1835627 IC50 = 5390.0 nM 5.27
CHEMBL1835527 IC50 = 5530.0 nM 5.26
CHEMBL1835519 IC50 = 5440.0 nM 5.26
CHEMBL1835518 IC50 = 5680.0 nM 5.25
CHEMBL1835626 IC50 = 5810.0 nM 5.24
CHEMBL1835530 IC50 = 6360.0 nM 5.20
CHEMBL1835524 IC50 = 6430.0 nM 5.19
CHEMBL1835526 IC50 = 6670.0 nM 5.18
CHEMBL1835713 IC50 = 6580.0 nM 5.18
CHEMBL1835711 IC50 = 7260.0 nM 5.14
CHEMBL1835620 IC50 = 7560.0 nM 5.12
CHEMBL1835523 IC50 > 10000.0 nM -
CHEMBL1835522 IC50 > 10000.0 nM -