Assay Detail
Binding
CHEMBL750039
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Tachykinin receptor 1 antagonistic activity as ability to inhibit [125I]BH-SP binding in human IM-9 cells (lymphoblast cells)
16
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Cell Type | IM-9 |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Axially chiral 1,7-naphthyridine-6-carboxamide derivatives as orally active tachykinin NK(1) receptor antagonists: synthesis, antagonistic activity, and effects on bladder functions.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 16 | 8.67 | 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 |
| CHEMBL128369 | — | — | 1 | 9.55 |
| CHEMBL130834 | 7-(3,5-BIS-TRIFLUOROMETHYL-BENZYL)-5-P-TOLYL-8,9,10,11-TETRAHYDRO-7H-1,7,11A-TRIAZA-CYCLOOCTA[B]NAPHTHALENE-6,12-DIONE (ATROPISOMERIC MIX) | — | 3 | 9.42 |
| CHEMBL339486 | — | — | 2 | 9.35 |
| CHEMBL128384 | — | — | 1 | 9.07 |
| CHEMBL340732 | — | — | 1 | 8.74 |
| CHEMBL340931 | — | — | 1 | 8.64 |
| CHEMBL128586 | 7-(3,5-BIS-TRIFLUOROMETHYL-BENZYL)-9-METHYL-5-P-TOLYL-8,9,10,11-TETRAHYDRO-7H-1,7,11A-TRIAZA-CYCLOOCTA[B]NAPHTHALENE-6,12-DIONE (ATROPISOMERIC MIX) | — | 2 | 8.07 |
| CHEMBL129354 | — | — | 1 | 8.02 |
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 |
| CHEMBL128369 | — | IC50 | = | 0.28 | nM | 9.55 |
| 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 |
| CHEMBL130834 | 7-(3,5-BIS-TRIFLUOROMETHYL-BENZYL)-5-P-TOLYL-8,9,10,11-TETRAHYDRO-7H-1,7,11A-TRIAZA-CYCLOOCTA[B]NAPHTHALENE-6,12-DIONE (ATROPISOMERIC MIX) | IC50 | = | 0.38 | nM | 9.42 |
| CHEMBL339486 | — | IC50 | = | 0.45 | nM | 9.35 |
| CHEMBL130834 | 7-(3,5-BIS-TRIFLUOROMETHYL-BENZYL)-5-P-TOLYL-8,9,10,11-TETRAHYDRO-7H-1,7,11A-TRIAZA-CYCLOOCTA[B]NAPHTHALENE-6,12-DIONE (ATROPISOMERIC MIX) | IC50 | = | 0.68 | nM | 9.17 |
| CHEMBL128384 | — | IC50 | = | 0.85 | nM | 9.07 |
| 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 |
| CHEMBL340732 | — | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL340931 | — | IC50 | = | 2.3 | nM | 8.64 |
| 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 |
| CHEMBL130834 | 7-(3,5-BIS-TRIFLUOROMETHYL-BENZYL)-5-P-TOLYL-8,9,10,11-TETRAHYDRO-7H-1,7,11A-TRIAZA-CYCLOOCTA[B]NAPHTHALENE-6,12-DIONE (ATROPISOMERIC MIX) | IC50 | = | 7.1 | nM | 8.15 |
| CHEMBL128586 | 7-(3,5-BIS-TRIFLUOROMETHYL-BENZYL)-9-METHYL-5-P-TOLYL-8,9,10,11-TETRAHYDRO-7H-1,7,11A-TRIAZA-CYCLOOCTA[B]NAPHTHALENE-6,12-DIONE (ATROPISOMERIC MIX) | IC50 | = | 8.6 | nM | 8.07 |
| CHEMBL129354 | — | IC50 | = | 9.5 | nM | 8.02 |
| CHEMBL339486 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL128586 | 7-(3,5-BIS-TRIFLUOROMETHYL-BENZYL)-9-METHYL-5-P-TOLYL-8,9,10,11-TETRAHYDRO-7H-1,7,11A-TRIAZA-CYCLOOCTA[B]NAPHTHALENE-6,12-DIONE (ATROPISOMERIC MIX) | IC50 | = | 340.0 | nM | 6.47 |