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Assay Detail

CHEMBL2091129

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
36
Total Activities
36
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 2-benzylamino-4(5)-(6-methylpyridin-2-yl)-5(4)-([1,2,4]triazolo[1,5-a]-pyridin-6-yl)thiazoles as transforming growth factor-β type 1 receptor kinase inhibitors.
Krishnaiah M, Jin CH, Sreenu D, Subrahmanyam VB, Rao KS, Son DH, Park HJ, Kim SW, Sheen YY, Kim DK.
Eur J Med Chem (2012) 57 : 74 -84
PubMed 23047226 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 36 5.39 6.32

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL492634 1 6.32
CHEMBL226838 1 6.23
CHEMBL2087967 1 5.48
CHEMBL2087966 1 5.45
CHEMBL2087983 1 5.45
CHEMBL2087971 1 5.42
CHEMBL2087984 1 5.42
CHEMBL2087968 1 5.27
CHEMBL2087965 1 5.26
CHEMBL2087979 1 5.23
CHEMBL2088219 1 5.21
CHEMBL2087982 1 5.14
CHEMBL2087970 1 5.13
CHEMBL2088218 1 5.10
CHEMBL2088221 1 5.05
CHEMBL2087972 1 5.04
CHEMBL2087978 1 -
CHEMBL2088224 1 -
CHEMBL2088223 1 -
CHEMBL2088222 1 -
CHEMBL2087969 1 -
CHEMBL2088220 1 -
CHEMBL2087973 1 -
CHEMBL2087974 1 -
CHEMBL2087975 1 -
CHEMBL2087976 1 -
CHEMBL2087977 1 -
CHEMBL2088217 1 -
CHEMBL2087980 1 -
CHEMBL2087981 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL492634 IC50 = 480.0 nM 6.32
CHEMBL226838 IC50 = 594.0 nM 6.23
CHEMBL2087967 IC50 = 3280.0 nM 5.48
CHEMBL2087966 IC50 = 3530.0 nM 5.45
CHEMBL2087983 IC50 = 3580.0 nM 5.45
CHEMBL2087971 IC50 = 3780.0 nM 5.42
CHEMBL2087984 IC50 = 3820.0 nM 5.42
CHEMBL2087968 IC50 = 5370.0 nM 5.27
CHEMBL2087965 IC50 = 5530.0 nM 5.26
CHEMBL2087979 IC50 = 5860.0 nM 5.23
CHEMBL2088219 IC50 = 6190.0 nM 5.21
CHEMBL2087982 IC50 = 7200.0 nM 5.14
CHEMBL2087970 IC50 = 7390.0 nM 5.13
CHEMBL2088218 IC50 = 7990.0 nM 5.10
CHEMBL2088221 IC50 = 8820.0 nM 5.05
CHEMBL2087972 IC50 = 9200.0 nM 5.04
CHEMBL2088216 IC50 > 10000.0 nM -
CHEMBL2088215 IC50 > 10000.0 nM -
CHEMBL2088214 IC50 > 10000.0 nM -
CHEMBL2088213 IC50 > 10000.0 nM -
CHEMBL2087986 IC50 > 10000.0 nM -
CHEMBL2087985 IC50 > 10000.0 nM -
CHEMBL2087981 IC50 > 10000.0 nM -
CHEMBL2087980 IC50 > 10000.0 nM -
CHEMBL2088217 IC50 > 10000.0 nM -
CHEMBL2087977 IC50 > 10000.0 nM -
CHEMBL2087976 IC50 > 10000.0 nM -
CHEMBL2087975 IC50 > 10000.0 nM -
CHEMBL2087974 IC50 > 10000.0 nM -
CHEMBL2087973 IC50 > 10000.0 nM -
CHEMBL2088220 IC50 > 10000.0 nM -
CHEMBL2087969 IC50 > 10000.0 nM -
CHEMBL2088222 IC50 > 10000.0 nM -
CHEMBL2088223 IC50 > 10000.0 nM -
CHEMBL2088224 IC50 > 10000.0 nM -
CHEMBL2087978 IC50 > 10000.0 nM -