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Assay Detail

CHEMBL807825

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

Functional
Inhibition of LPS-induced tumor necrosis factor-alpha (TNF-alpha) production in THP-1 cells
27
Total Activities
27
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type THP-1
Confidence 5 — Multiple protein complex / RNA
Curated By Autocuration

Target

MAP kinase p38 (CHEMBL2094115)
Type PROTEIN FAMILY
Organism Homo sapiens

Publication

Pyrazole urea-based inhibitors of p38 MAP kinase: from lead compound to clinical candidate.
Regan J, Breitfelder S, Cirillo P, Gilmore T, Graham AG, Hickey E, Klaus B, Madwed J, Moriak M, Moss N, Pargellis C, Pav S, Proto A, Swinamer A, Tong L, Torcellini C.
J Med Chem (2002) 45 : 2994 -3008
PubMed 12086485 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 27 6.16 7.75

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL103667 DORAMAPIMOD 2.0 1 7.75
CHEMBL10 SB-203580 1 7.22
CHEMBL314228 1 6.92
CHEMBL85461 1 6.89
CHEMBL315100 1 6.75
CHEMBL312873 1 6.60
CHEMBL100847 1 6.48
CHEMBL420047 1 6.43
CHEMBL84777 1 6.42
CHEMBL86318 1 6.39
CHEMBL314805 1 6.20
CHEMBL102547 1 6.16
CHEMBL314023 1 6.14
CHEMBL420231 1 6.11
CHEMBL314278 1 6.09
CHEMBL87224 1 6.02
CHEMBL86195 1 6.00
CHEMBL85860 1 6.00
CHEMBL84928 1 5.92
CHEMBL87580 1 5.89
CHEMBL312895 1 5.80
CHEMBL315059 1 5.72
CHEMBL85609 1 5.64
CHEMBL85942 1 5.48
CHEMBL87277 1 5.23
CHEMBL101035 1 5.21
CHEMBL407173 1 4.96

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL103667 DORAMAPIMOD EC50 = 18.0 nM 7.75
CHEMBL10 SB-203580 EC50 = 60.0 nM 7.22
CHEMBL314228 EC50 = 120.0 nM 6.92
CHEMBL85461 EC50 = 130.0 nM 6.89
CHEMBL315100 EC50 = 180.0 nM 6.75
CHEMBL312873 EC50 = 250.0 nM 6.60
CHEMBL100847 EC50 = 330.0 nM 6.48
CHEMBL420047 EC50 = 370.0 nM 6.43
CHEMBL84777 EC50 = 380.0 nM 6.42
CHEMBL86318 EC50 = 410.0 nM 6.39
CHEMBL314805 EC50 = 630.0 nM 6.20
CHEMBL102547 EC50 = 700.0 nM 6.16
CHEMBL314023 EC50 = 730.0 nM 6.14
CHEMBL420231 EC50 = 770.0 nM 6.11
CHEMBL314278 EC50 = 820.0 nM 6.09
CHEMBL87224 EC50 = 960.0 nM 6.02
CHEMBL86195 EC50 = 1000.0 nM 6.00
CHEMBL85860 EC50 = 1000.0 nM 6.00
CHEMBL84928 EC50 = 1200.0 nM 5.92
CHEMBL87580 EC50 = 1300.0 nM 5.89
CHEMBL312895 EC50 = 1600.0 nM 5.80
CHEMBL315059 EC50 = 1900.0 nM 5.72
CHEMBL85609 EC50 = 2300.0 nM 5.64
CHEMBL85942 EC50 = 3300.0 nM 5.48
CHEMBL87277 EC50 = 5900.0 nM 5.23
CHEMBL101035 EC50 = 6200.0 nM 5.21
CHEMBL407173 EC50 = 11000.0 nM 4.96