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Assay Detail

CHEMBL1914193

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

Functional
Antiinflammatory activity in po dosed Sprague-Dawley rat whole blood assessed as inhibition of LPS-induced TNFalpha production
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Rattus norvegicus
Tissue Blood
Confidence 1 — Organism
Curated By Autocuration

Target

Blood (CHEMBL613615)
Type TISSUE
Organism Rattus norvegicus

Publication

Azaxanthene based selective glucocorticoid receptor modulators: design, synthesis, and pharmacological evaluation of (S)-4-(5-(1-((1,3,4-thiadiazol-2-yl)amino)-2-methyl-1-oxopropan-2-yl)-5H-chromeno[2,3-b]pyridin-2-yl)-2-fluoro-N,N-dimethylbenzamide (BMS-776532) and its methylene homologue (BMS-791826).
Weinstein DS, Gong H, Doweyko AM, Cunningham M, Habte S, Wang JH, Holloway DA, Burke C, Gao L, Guarino V, Carman J, Somerville JE, Shuster D, Salter-Cid L, Dodd JH, Nadler SG, Barrish JC.
J Med Chem (2011) 54 : 7318 -7333
PubMed 21899328 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 2 6.70 6.72

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1911272 1 6.72
CHEMBL4296682 1 6.67

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1911272 EC50 = 189.0 nM 6.72
CHEMBL4296682 EC50 = 215.0 nM 6.67