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

CHEMBL929948

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

Functional
Inhibition of LPS-induced TNFalpha biosynthesis in human PBMC
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type PBMC
Confidence 1 — Organism
Curated By Autocuration

Target

PBMC (CHEMBL613107)
Type CELL-LINE
Organism Homo sapiens

Publication

The discovery of (R)-2-(sec-butylamino)-N-(2-methyl-5-(methylcarbamoyl)phenyl) thiazole-5-carboxamide (BMS-640994)-A potent and efficacious p38alpha MAP kinase inhibitor.
Hynes J, Wu H, Pitt S, Shen DR, Zhang R, Schieven GL, Gillooly KM, Shuster DJ, Taylor TL, Yang X, McIntyre KW, McKinnon M, Zhang H, Marathe PH, Doweyko AM, Kish K, Kiefer SE, Sack JS, Newitt JA, Barrish JC, Dodd J, Leftheris K.
Bioorg Med Chem Lett (2008) 18 : 1762 -1767
PubMed 18313298 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 17 7.75 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL403200 1 9.00
CHEMBL255482 1 8.57
CHEMBL258202 1 8.54
CHEMBL258203 1 8.39
CHEMBL258223 1 8.19
CHEMBL255288 1 8.10
CHEMBL258201 1 8.06
CHEMBL255698 1 7.96
CHEMBL257994 1 7.64
CHEMBL257995 1 7.46
CHEMBL257996 1 7.38
CHEMBL403141 1 6.80
CHEMBL254365 1 6.62
CHEMBL258403 1 5.82
CHEMBL255254 1 -
CHEMBL258418 1 -
CHEMBL254169 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL403200 IC50 = 1.0 nM 9.00
CHEMBL255482 IC50 = 2.7 nM 8.57
CHEMBL258202 IC50 = 2.9 nM 8.54
CHEMBL258203 IC50 = 4.1 nM 8.39
CHEMBL258223 IC50 = 6.4 nM 8.19
CHEMBL255288 IC50 = 7.9 nM 8.10
CHEMBL258201 IC50 = 8.7 nM 8.06
CHEMBL255698 IC50 = 11.0 nM 7.96
CHEMBL257994 IC50 = 23.0 nM 7.64
CHEMBL257995 IC50 = 35.0 nM 7.46
CHEMBL257996 IC50 = 42.0 nM 7.38
CHEMBL403141 IC50 = 160.0 nM 6.80
CHEMBL254365 IC50 = 240.0 nM 6.62
CHEMBL258403 IC50 = 1500.0 nM 5.82
CHEMBL255254 IC50 > 2000.0 nM -
CHEMBL258418 IC50 > 250.0 nM -
CHEMBL254169 IC50 > 250.0 nM -