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Assay Detail

CHEMBL990636

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

Functional
Antagonist activity at NK1 receptor
3
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Confidence 8 — Homologous single protein target
Curated By Intermediate

Target

Substance-P receptor (CHEMBL249)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Axial chirality and affinity at the GABA(A) receptor of pyrimido[1,2-a][1,4]benzodiazepines and related compounds.
Lee S, Kamide T, Tabata H, Takahashi H, Shiro M, Natsugari H.
Bioorg Med Chem (2008) 16 : 9519 -9523
PubMed 18829330 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 9.31 9.62

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL107172 7-METHYL-8-OXO-5-P-TOLYL-7,8-DIHYDRO-[1,7]NAPHTHYRIDINE-6-CARBOXYLIC ACID (3,5-BIS-TRIFLUOROMETHYL-BENZYL)-METHYL-AMIDE (STRUCTURAL MIX) 3 9.62

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL107172 7-METHYL-8-OXO-5-P-TOLYL-7,8-DIHYDRO-[1,7]NAPHTHYRIDINE-6-CARBOXYLIC ACID (3,5-BIS-TRIFLUOROMETHYL-BENZYL)-METHYL-AMIDE (STRUCTURAL MIX) IC50 = 0.24 nM 9.62
CHEMBL107172 7-METHYL-8-OXO-5-P-TOLYL-7,8-DIHYDRO-[1,7]NAPHTHYRIDINE-6-CARBOXYLIC ACID (3,5-BIS-TRIFLUOROMETHYL-BENZYL)-METHYL-AMIDE (STRUCTURAL MIX) IC50 = 0.34 nM 9.47
CHEMBL107172 7-METHYL-8-OXO-5-P-TOLYL-7,8-DIHYDRO-[1,7]NAPHTHYRIDINE-6-CARBOXYLIC ACID (3,5-BIS-TRIFLUOROMETHYL-BENZYL)-METHYL-AMIDE (STRUCTURAL MIX) IC50 = 1.4 nM 8.85