Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL2027255

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

Binding
Inhibition of p38alpha kinase using KRELVEPLTPSGEAPNQALLR as substrate for 20 mins by lactate dehydrogenase-coupled spectrophotometric assay
28
Total Activities
28
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

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

Publication

The Discovery of VX-745: A Novel and Selective p38α Kinase Inhibitor.
Duffy JP, Harrington EM, Salituro FG, Cochran JE, Green J, Gao H, Bemis GW, Evindar G, Galullo VP, Ford PJ, Germann UA, Wilson KP, Bellon SF, Chen G, Taslimi P, Jones P, Huang C, Pazhanisamy S, Wang YM, Murcko MA, Su MS.
ACS Med Chem Lett (2011) 2 : 758 -763
PubMed 24900264 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 28 6.17 8.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL119385 NEFLAMAPIMOD 2.0 1 8.05
CHEMBL420134 1 7.44
CHEMBL326629 1 6.91
CHEMBL115491 1 6.75
CHEMBL326089 1 6.70
CHEMBL324091 1 6.66
CHEMBL113806 1 6.60
CHEMBL331361 1 6.58
CHEMBL114430 1 6.55
CHEMBL117211 1 6.44
CHEMBL114962 1 6.35
CHEMBL431865 1 6.30
CHEMBL2024530 1 6.12
CHEMBL114057 1 6.10
CHEMBL114121 1 5.85
CHEMBL324089 1 5.85
CHEMBL2024528 1 5.77
CHEMBL326944 1 5.72
CHEMBL2024529 1 5.46
CHEMBL2024352 1 5.39
CHEMBL2024349 1 5.36
CHEMBL2024347 1 5.30
CHEMBL2024351 1 4.96
CHEMBL2024350 1 4.92
CHEMBL2024348 1 -
CHEMBL2024353 1 -
CHEMBL2024526 1 -
CHEMBL2024527 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL119385 NEFLAMAPIMOD IC50 = 9.0 nM 8.05
CHEMBL420134 IC50 = 36.0 nM 7.44
CHEMBL326629 IC50 = 123.0 nM 6.91
CHEMBL115491 IC50 = 180.0 nM 6.75
CHEMBL326089 IC50 = 200.0 nM 6.70
CHEMBL324091 IC50 = 220.0 nM 6.66
CHEMBL113806 IC50 = 250.0 nM 6.60
CHEMBL331361 IC50 = 260.0 nM 6.58
CHEMBL114430 IC50 = 280.0 nM 6.55
CHEMBL117211 IC50 = 360.0 nM 6.44
CHEMBL114962 IC50 = 450.0 nM 6.35
CHEMBL431865 IC50 = 500.0 nM 6.30
CHEMBL2024530 IC50 = 750.0 nM 6.12
CHEMBL114057 IC50 = 800.0 nM 6.10
CHEMBL114121 IC50 = 1400.0 nM 5.85
CHEMBL324089 IC50 = 1400.0 nM 5.85
CHEMBL2024528 IC50 = 1700.0 nM 5.77
CHEMBL326944 IC50 = 1900.0 nM 5.72
CHEMBL2024529 IC50 = 3500.0 nM 5.46
CHEMBL2024352 IC50 = 4100.0 nM 5.39
CHEMBL2024349 IC50 = 4400.0 nM 5.36
CHEMBL2024347 IC50 = 5000.0 nM 5.30
CHEMBL2024351 IC50 = 11000.0 nM 4.96
CHEMBL2024350 IC50 = 12000.0 nM 4.92
CHEMBL2024348 IC50 > 20000.0 nM -
CHEMBL2024353 IC50 > 20000.0 nM -
CHEMBL2024526 IC50 > 20000.0 nM -
CHEMBL2024527 IC50 > 20000.0 nM -