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Assay Detail

CHEMBL807960

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

Binding
Binding affinity at Tachykinin receptor 1 by measuring its ability to inhibit [125I]BH-SP binding in human IM-9 cells (Lymphoblast cells).
ChEMBL ↗
10
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type IM-9
Confidence 9 — Direct single protein target
Curated By Expert

Target

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

Publication

Axially chiral N-benzyl-N,7-dimethyl-5-phenyl-1, 7-naphthyridine-6-carboxamide derivatives as tachykinin NK1 receptor antagonists: determination of the absolute stereochemical requirements.
Ikeura Y, Ishichi Y, Tanaka T, Fujishima A, Murabayashi M, Kawada M, Ishimaru T, Kamo I, Doi T, Natsugari H.
J Med Chem (1998) 41 : 4232 -4239
PubMed 9784098 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 10 7.94 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) — 4 9.62
CHEMBL336589 7-METHYL-8-OXO-5-P-TOLYL-7,8-DIHYDRO-[1,7]NAPHTHYRIDINE-6-CARBOXYLIC ACID (S)-[(S)-1-(3,5-BIS-TRIFLUOROMETHYL-PHENYL)-ETHYL]-METHYL-AMIDE (ENANTIOMERIC MIX) — 2 9.10
CHEMBL135572 7-METHYL-8-OXO-5-P-TOLYL-7,8-DIHYDRO-[1,7]NAPHTHYRIDINE-6-CARBOXYLIC ACID (S)-[(R)-1-(3,5-BIS-TRIFLUOROMETHYL-PHENYL)-ETHYL]-METHYL-AMIDE (ENANTIOMERIC MIX) — 2 7.72
CHEMBL1169534 — — 1 6.89
CHEMBL134415 — — 1 5.77

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
CHEMBL336589 7-METHYL-8-OXO-5-P-TOLYL-7,8-DIHYDRO-[1,7]NAPHTHYRIDINE-6-CARBOXYLIC ACID (S)-[(S)-1-(3,5-BIS-TRIFLUOROMETHYL-PHENYL)-ETHYL]-METHYL-AMIDE (ENANTIOMERIC MIX) IC50 = 0.8 nM 9.10
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
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 = 4.2 nM 8.38
CHEMBL135572 7-METHYL-8-OXO-5-P-TOLYL-7,8-DIHYDRO-[1,7]NAPHTHYRIDINE-6-CARBOXYLIC ACID (S)-[(R)-1-(3,5-BIS-TRIFLUOROMETHYL-PHENYL)-ETHYL]-METHYL-AMIDE (ENANTIOMERIC MIX) IC50 = 19.0 nM 7.72
CHEMBL336589 7-METHYL-8-OXO-5-P-TOLYL-7,8-DIHYDRO-[1,7]NAPHTHYRIDINE-6-CARBOXYLIC ACID (S)-[(S)-1-(3,5-BIS-TRIFLUOROMETHYL-PHENYL)-ETHYL]-METHYL-AMIDE (ENANTIOMERIC MIX) IC50 = 44.0 nM 7.36
CHEMBL1169534 — IC50 = 130.0 nM 6.89
CHEMBL135572 7-METHYL-8-OXO-5-P-TOLYL-7,8-DIHYDRO-[1,7]NAPHTHYRIDINE-6-CARBOXYLIC ACID (S)-[(R)-1-(3,5-BIS-TRIFLUOROMETHYL-PHENYL)-ETHYL]-METHYL-AMIDE (ENANTIOMERIC MIX) IC50 = 620.0 nM 6.21
CHEMBL134415 — IC50 = 1700.0 nM 5.77