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Assay Detail

CHEMBL1805307

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

Binding
Inhibition of p38alpha assessed as phosphorylation FITC-labeled Hsp27 after 60 mins by fluorescence based cascade assay
14
Total Activities
12
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

Discovery of PH-797804, a highly selective and potent inhibitor of p38 MAP kinase.
Selness SR, Devraj RV, Devadas B, Walker JK, Boehm TL, Durley RC, Shieh H, Xing L, Rucker PV, Jerome KD, Benson AG, Marrufo LD, Madsen HM, Hitchcock J, Owen TJ, Christie L, Promo MA, Hickory BS, Alvira E, Naing W, Blevis-Bal R, Messing D, Yang J, Mao MK, Yalamanchili G, Vonder Embse R, Hirsch J, Saabye M, Bonar S, Webb E, Anderson G, Monahan JB.
Bioorg Med Chem Lett (2011) 21 : 4066 -4071
PubMed 21641211 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 14 7.88 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1802632 1 8.70
CHEMBL1088751 PH-797804 2.0 3 8.64
CHEMBL1802637 1 8.52
CHEMBL1802641 1 8.40
CHEMBL1802636 1 8.07
CHEMBL1802633 1 8.02
CHEMBL1797224 1 7.92
CHEMBL1802638 1 7.68
CHEMBL1802634 1 7.47
CHEMBL1802635 1 7.31
CHEMBL1802640 1 6.49
CHEMBL1802639 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1802632 IC50 = 2.0 nM 8.70
CHEMBL1088751 PH-797804 IC50 = 2.3 nM 8.64
CHEMBL1088751 PH-797804 IC50 = 2.5 nM 8.60
CHEMBL1802637 IC50 = 3.0 nM 8.52
CHEMBL1802641 IC50 = 4.0 nM 8.40
CHEMBL1802636 IC50 = 8.5 nM 8.07
CHEMBL1802633 IC50 = 9.5 nM 8.02
CHEMBL1797224 IC50 = 12.0 nM 7.92
CHEMBL1802638 IC50 = 21.0 nM 7.68
CHEMBL1802634 IC50 = 34.0 nM 7.47
CHEMBL1802635 IC50 = 48.5 nM 7.31
CHEMBL1088751 PH-797804 IC50 = 247.0 nM 6.61
CHEMBL1802640 IC50 = 325.0 nM 6.49
CHEMBL1802639 IC50 > 10000.0 nM -