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Assay Detail

CHEMBL867364

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

Functional
Inhibition of LPS-stimulated TNFalpha release in human whole blood
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Tissue Blood
Confidence 1 — Organism
Curated By Expert

Target

Homo sapiens (CHEMBL372)
Type ORGANISM
Organism Homo sapiens

Publication

p38 MAP kinase inhibitors. Part 3: SAR on 3,4-dihydropyrimido[4,5-d]pyrimidin-2-ones and 3,4-dihydropyrido[4,3-d]pyrimidin-2-ones.
Natarajan SR, Wisnoski DD, Thompson JE, O'Neill EA, O'Keefe SJ.
Bioorg Med Chem Lett (2006) 16 : 4400 -4404
PubMed 16750629 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 17 6.82 8.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL319556 1 8.00
CHEMBL377979 1 7.82
CHEMBL212803 1 7.77
CHEMBL212549 1 7.70
CHEMBL213190 1 7.50
CHEMBL209442 1 7.42
CHEMBL213142 1 7.38
CHEMBL211795 1 7.00
CHEMBL211426 1 6.60
CHEMBL213836 1 6.57
CHEMBL212091 1 6.44
CHEMBL213986 1 6.30
CHEMBL425785 1 6.07
CHEMBL215651 1 6.00
CHEMBL214138 1 6.00
CHEMBL425265 1 5.71
CHEMBL212821 1 5.70

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL319556 IC50 = 10.0 nM 8.00
CHEMBL377979 IC50 = 15.0 nM 7.82
CHEMBL212803 IC50 = 17.0 nM 7.77
CHEMBL212549 IC50 = 20.0 nM 7.70
CHEMBL213190 IC50 = 32.0 nM 7.50
CHEMBL209442 IC50 = 38.0 nM 7.42
CHEMBL213142 IC50 = 42.0 nM 7.38
CHEMBL211795 IC50 = 100.0 nM 7.00
CHEMBL211426 IC50 = 250.0 nM 6.60
CHEMBL213836 IC50 = 270.0 nM 6.57
CHEMBL212091 IC50 = 360.0 nM 6.44
CHEMBL213986 IC50 = 500.0 nM 6.30
CHEMBL425785 IC50 = 850.0 nM 6.07
CHEMBL215651 IC50 = 1000.0 nM 6.00
CHEMBL214138 IC50 = 1000.0 nM 6.00
CHEMBL425265 IC50 = 1940.0 nM 5.71
CHEMBL212821 IC50 = 2000.0 nM 5.70