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Ligand source activities (1 row/activity)
Ligands | Receptor | Activity | Chemical information | ||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Common name | GPCRdb ID | Reference ligand | Vendors | Species | Assay Type | Activity Type | Activity Relation | Activity Value | p-value (-log) | Fold selectivity | Tested GPCRs | Assay Description | Source | Mol weight | Rot Bonds | H don | H acc | LogP | Smiles | DOI | |
Ligands | Receptor | Activity | Chemical information | ||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Common name | GPCRdb ID | Reference ligand | Vendors | Species | Assay Type | Activity Type | Activity Relation | Activity Value | p-value (-log) | Fold selectivity | Tested GPCRs | Assay Description | Source | Mol weight | Rot Bonds | H don | H acc | LogP | Smiles | DOI | |
| 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) | 20628 | None | 0 | Human | Binding | IC50 | = | 7.10 | 8.15 | - | 1 | Tachykinin receptor 1 antagonistic activity as ability to inhibit [125I]BH-SP binding in human IM-9 cells (lymphoblast cells) | ChEMBL | 559.2 | 3 | 0 | 4 | 6.85 | Cc1ccc(-c2c3n(c(=O)c4ncccc24)CCCCN(Cc2cc(C(F)(F)F)cc(C(F)(F)F)c2)C3=O)cc1 | https://dx.doi.org/10.1021/jm990220r | |
| 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) | 20628 | None | 0 | Human | Binding | IC50 | = | 0.68 | 9.17 | - | 1 | Tachykinin receptor 1 antagonistic activity as ability to inhibit [125I]BH-SP binding in human IM-9 cells (lymphoblast cells) | ChEMBL | 559.2 | 3 | 0 | 4 | 6.85 | Cc1ccc(-c2c3n(c(=O)c4ncccc24)CCCCN(Cc2cc(C(F)(F)F)cc(C(F)(F)F)c2)C3=O)cc1 | https://dx.doi.org/10.1021/jm990220r | |
| 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) | 20628 | None | 0 | Human | Binding | IC50 | = | 0.38 | 9.42 | - | 1 | Tachykinin receptor 1 antagonistic activity as ability to inhibit [125I]BH-SP binding in human IM-9 cells (lymphoblast cells) | ChEMBL | 559.2 | 3 | 0 | 4 | 6.85 | Cc1ccc(-c2c3n(c(=O)c4ncccc24)CCCCN(Cc2cc(C(F)(F)F)cc(C(F)(F)F)c2)C3=O)cc1 | https://dx.doi.org/10.1021/jm990220r | |
| 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) | 18941 | None | 0 | Human | Binding | IC50 | = | 8.60 | 8.07 | - | 1 | Tachykinin receptor 1 antagonistic activity as ability to inhibit [125I]BH-SP binding in human IM-9 cells (lymphoblast cells) | ChEMBL | 573.2 | 3 | 0 | 4 | 7.09 | Cc1ccc(-c2c3n(c(=O)c4ncccc24)CC[C@H](C)CN(Cc2cc(C(F)(F)F)cc(C(F)(F)F)c2)C3=O)cc1 | https://dx.doi.org/10.1021/jm990220r | |
| 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) | 18941 | None | 0 | Human | Binding | IC50 | = | 340.00 | 6.47 | - | 1 | Tachykinin receptor 1 antagonistic activity as ability to inhibit [125I]BH-SP binding in human IM-9 cells (lymphoblast cells) | ChEMBL | 573.2 | 3 | 0 | 4 | 7.09 | Cc1ccc(-c2c3n(c(=O)c4ncccc24)CC[C@H](C)CN(Cc2cc(C(F)(F)F)cc(C(F)(F)F)c2)C3=O)cc1 | https://dx.doi.org/10.1021/jm990220r | |
| 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) | 5411 | None | 0 | Human | Binding | IC50 | = | 0.34 | 9.47 | - | 1 | Tachykinin receptor 1 antagonistic activity as ability to inhibit [125I]BH-SP binding in human IM-9 cells (lymphoblast cells) | ChEMBL | 533.2 | 4 | 0 | 4 | 6.22 | Cc1ccc(-c2c(C(=O)N(C)Cc3cc(C(F)(F)F)cc(C(F)(F)F)c3)n(C)c(=O)c3ncccc23)cc1 | https://dx.doi.org/10.1021/jm990220r | |
| 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) | 5411 | None | 0 | Human | Binding | IC50 | = | 0.24 | 9.62 | - | 1 | Tachykinin receptor 1 antagonistic activity as ability to inhibit [125I]BH-SP binding in human IM-9 cells (lymphoblast cells) | ChEMBL | 533.2 | 4 | 0 | 4 | 6.22 | Cc1ccc(-c2c(C(=O)N(C)Cc3cc(C(F)(F)F)cc(C(F)(F)F)c3)n(C)c(=O)c3ncccc23)cc1 | https://dx.doi.org/10.1021/jm990220r | |
| 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) | 5411 | None | 0 | Human | Binding | IC50 | = | 1.40 | 8.85 | - | 1 | Tachykinin receptor 1 antagonistic activity as ability to inhibit [125I]BH-SP binding in human IM-9 cells (lymphoblast cells) | ChEMBL | 533.2 | 4 | 0 | 4 | 6.22 | Cc1ccc(-c2c(C(=O)N(C)Cc3cc(C(F)(F)F)cc(C(F)(F)F)c3)n(C)c(=O)c3ncccc23)cc1 | https://dx.doi.org/10.1021/jm990220r | |
| 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) | 5411 | None | 0 | Human | Binding | IC50 | = | 0.34 | 9.47 | - | 1 | Inhibition of [125I]-BH-Substance P binding to tachykinin receptor 1 in human IM-9 cells | ChEMBL | 533.2 | 4 | 0 | 4 | 6.22 | Cc1ccc(-c2c(C(=O)N(C)Cc3cc(C(F)(F)F)cc(C(F)(F)F)c3)n(C)c(=O)c3ncccc23)cc1 | https://dx.doi.org/10.1021/jm00016a014 | |
| 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) | 5411 | None | 0 | Human | Binding | IC50 | = | 7.00 | 8.15 | - | 1 | Inhibition of [125I]-BH-Substance P binding to tachykinin receptor 1 in human IM-9 cells | ChEMBL | 533.2 | 4 | 0 | 4 | 6.22 | Cc1ccc(-c2c(C(=O)N(C)Cc3cc(C(F)(F)F)cc(C(F)(F)F)c3)n(C)c(=O)c3ncccc23)cc1 | https://dx.doi.org/10.1021/jm00016a014 | |
| 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) | 5411 | None | 0 | Human | Binding | IC50 | = | 0.34 | 9.47 | - | 1 | Binding affinity at Tachykinin receptor 1 by measuring its ability to inhibit [125I]BH-SP binding in human IM-9 cells (Lymphoblast cells). | ChEMBL | 533.2 | 4 | 0 | 4 | 6.22 | Cc1ccc(-c2c(C(=O)N(C)Cc3cc(C(F)(F)F)cc(C(F)(F)F)c3)n(C)c(=O)c3ncccc23)cc1 | https://dx.doi.org/10.1021/jm980042m | |
| 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) | 5411 | None | 0 | Human | Binding | IC50 | = | 1.40 | 8.85 | - | 1 | Binding affinity at Tachykinin receptor 1 by measuring its ability to inhibit [125I]BH-SP binding in human IM-9 cells (Lymphoblast cells). | ChEMBL | 533.2 | 4 | 0 | 4 | 6.22 | Cc1ccc(-c2c(C(=O)N(C)Cc3cc(C(F)(F)F)cc(C(F)(F)F)c3)n(C)c(=O)c3ncccc23)cc1 | https://dx.doi.org/10.1021/jm980042m | |
| 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) | 5411 | None | 0 | Human | Binding | IC50 | = | 4.20 | 8.38 | - | 1 | Binding affinity at Tachykinin receptor 1 by measuring its ability to inhibit [125I]BH-SP binding in human IM-9 cells (Lymphoblast cells). | ChEMBL | 533.2 | 4 | 0 | 4 | 6.22 | Cc1ccc(-c2c(C(=O)N(C)Cc3cc(C(F)(F)F)cc(C(F)(F)F)c3)n(C)c(=O)c3ncccc23)cc1 | https://dx.doi.org/10.1021/jm980042m | |
| 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) | 5411 | None | 0 | Human | Binding | IC50 | = | 0.24 | 9.62 | - | 1 | Binding affinity at Tachykinin receptor 1 by measuring its ability to inhibit [125I]BH-SP binding in human IM-9 cells (Lymphoblast cells). | ChEMBL | 533.2 | 4 | 0 | 4 | 6.22 | Cc1ccc(-c2c(C(=O)N(C)Cc3cc(C(F)(F)F)cc(C(F)(F)F)c3)n(C)c(=O)c3ncccc23)cc1 | https://dx.doi.org/10.1021/jm980042m | |
| 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) | 5411 | None | 0 | Human | Binding | IC50 | = | 4.20 | 8.38 | - | 1 | Tachykinin receptor 1 antagonistic activity as ability to inhibit [125I]BH-SP binding in human IM-9 cells (lymphoblast cells) | ChEMBL | 533.2 | 4 | 0 | 4 | 6.22 | Cc1ccc(-c2c(C(=O)N(C)Cc3cc(C(F)(F)F)cc(C(F)(F)F)c3)n(C)c(=O)c3ncccc23)cc1 | https://dx.doi.org/10.1021/jm990220r | |
| 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) | 26095 | None | 0 | Human | Binding | IC50 | = | 620.00 | 6.21 | - | 1 | Binding affinity at Tachykinin receptor 1 by measuring its ability to inhibit [125I]BH-SP binding in human IM-9 cells (Lymphoblast cells). | ChEMBL | 547.2 | 4 | 0 | 4 | 6.78 | Cc1ccc(-c2c(C(=O)N(C)[C@H](C)c3cc(C(F)(F)F)cc(C(F)(F)F)c3)n(C)c(=O)c3ncccc23)cc1 | https://dx.doi.org/10.1021/jm980042m | |
| 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) | 26095 | None | 0 | Human | Binding | IC50 | = | 19.00 | 7.72 | - | 1 | Binding affinity at Tachykinin receptor 1 by measuring its ability to inhibit [125I]BH-SP binding in human IM-9 cells (Lymphoblast cells). | ChEMBL | 547.2 | 4 | 0 | 4 | 6.78 | Cc1ccc(-c2c(C(=O)N(C)[C@H](C)c3cc(C(F)(F)F)cc(C(F)(F)F)c3)n(C)c(=O)c3ncccc23)cc1 | https://dx.doi.org/10.1021/jm980042m | |
| 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) | 116649 | None | 0 | Human | Binding | IC50 | = | 0.80 | 9.10 | - | 1 | Binding affinity at Tachykinin receptor 1 by measuring its ability to inhibit [125I]BH-SP binding in human IM-9 cells (Lymphoblast cells). | ChEMBL | 547.2 | 4 | 0 | 4 | 6.78 | Cc1ccc(-c2c(C(=O)N(C)[C@@H](C)c3cc(C(F)(F)F)cc(C(F)(F)F)c3)n(C)c(=O)c3ncccc23)cc1 | https://dx.doi.org/10.1021/jm980042m | |
| 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) | 116649 | None | 0 | Human | Binding | IC50 | = | 44.00 | 7.36 | - | 1 | Binding affinity at Tachykinin receptor 1 by measuring its ability to inhibit [125I]BH-SP binding in human IM-9 cells (Lymphoblast cells). | ChEMBL | 547.2 | 4 | 0 | 4 | 6.78 | Cc1ccc(-c2c(C(=O)N(C)[C@@H](C)c3cc(C(F)(F)F)cc(C(F)(F)F)c3)n(C)c(=O)c3ncccc23)cc1 | https://dx.doi.org/10.1021/jm980042m | |
| A-85380 | 218616 | 3H-Leu,4,5 Substance P | 0 | Human | Binding | pKi | = | 10000.00 | 5.00 | -1 | 13 | - | PDSP KiDatabase | 164.1 | 3 | 1 | 3 | 0.82 | c1cncc(OCC2CCN2)c1 | - | |
Showing 1 to 20 of 3,660 entries
Ligands | Receptor | Activity | Chemical information | ||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Common name | GPCRdb ID | Reference ligand | Vendors | Species | Assay Type | Activity Type | Activity Relation | Activity Value | p-value (-log) | Fold selectivity | Tested GPCRs | Assay Description | Source | Mol weight | Rot Bonds | H don | H acc | LogP | Smiles | DOI | |
Ligands | Receptor | Activity | Chemical information | ||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Common name | GPCRdb ID | Reference ligand | Vendors | Species | Assay Type | Activity Type | Activity Relation | Activity Value | p-value (-log) | Fold selectivity | Tested GPCRs | Assay Description | Source | Mol weight | Rot Bonds | H don | H acc | LogP | Smiles | DOI | |
| 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) | 5411 | None | 0 | Human | Functional | IC50 | = | 0.24 | 9.62 | - | 1 | Antagonist activity at NK1 receptor | ChEMBL | 533.2 | 4 | 0 | 4 | 6.22 | Cc1ccc(-c2c(C(=O)N(C)Cc3cc(C(F)(F)F)cc(C(F)(F)F)c3)n(C)c(=O)c3ncccc23)cc1 | https://dx.doi.org/10.1016/j.bmc.2008.09.037 | |
| 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) | 5411 | None | 0 | Human | Functional | IC50 | = | 1.40 | 8.85 | - | 1 | Antagonist activity at NK1 receptor | ChEMBL | 533.2 | 4 | 0 | 4 | 6.22 | Cc1ccc(-c2c(C(=O)N(C)Cc3cc(C(F)(F)F)cc(C(F)(F)F)c3)n(C)c(=O)c3ncccc23)cc1 | https://dx.doi.org/10.1016/j.bmc.2008.09.037 | |
| 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) | 5411 | None | 0 | Human | Functional | IC50 | = | 0.34 | 9.47 | - | 1 | Antagonist activity at NK1 receptor | ChEMBL | 533.2 | 4 | 0 | 4 | 6.22 | Cc1ccc(-c2c(C(=O)N(C)Cc3cc(C(F)(F)F)cc(C(F)(F)F)c3)n(C)c(=O)c3ncccc23)cc1 | https://dx.doi.org/10.1016/j.bmc.2008.09.037 | |
| [Pro9]SP | 3194 | None | 0 | Rat | Functional | pIC50 | = | - | 8.60 | - | 1 | Unclassified | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/9243521 | |
| [Sar9,Met(O2)11]SP | 3486 | None | 0 | Human | Functional | pIC50 | = | - | 9.80 | - | 1 | Unclassified | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/8702757 | |
| aprepitant | 448 | None | 58 | Human | Functional | IC50 | = | 1.41 | 8.85 | 3 | 8 | Antagonist activity at NK1R (unknown origin) in presence of endogenous SP ligand preincubated for 10 mins followed by 30 min incubation with antagonist and SP by HTRF-FRET assay | ChEMBL | 534.1 | 6 | 2 | 5 | 4.95 | C[C@@H](O[C@H]1OCCN(Cc2nc(=O)[nH][nH]2)[C@H]1c1ccc(F)cc1)c1cc(C(F)(F)F)cc(C(F)(F)F)c1 | https://dx.doi.org/10.1021/acs.jmedchem.1c00793 | |
| aprepitant | 448 | None | 58 | Mongolian jird | Functional | pIC50 | = | 10.05 | 8.00 | -3 | 8 | None | Drug Central | 534.1 | 6 | 2 | 5 | 4.95 | C[C@@H](O[C@H]1OCCN(Cc2nc(=O)[nH][nH]2)[C@H]1c1ccc(F)cc1)c1cc(C(F)(F)F)cc(C(F)(F)F)c1 | - | |
| cefapirin | 220190 | None | 0 | Human | Functional | pIC50 | = | 4.89 | 8.31 | -1 | 14 | None | Drug Central | 423.1 | 7 | 2 | 8 | 0.47 | CC(=O)OCC1=C(C(=O)O)N2C(=O)[C@@H](NC(=O)CSc3ccncc3)[C@H]2SC1 | - | |
| CHEMBL100178 | 4200 | None | 0 | Rat | Functional | IC50 | = | 160.00 | 6.80 | - | 1 | Antagonism of NK1 receptor in rat liver microsomes. | ChEMBL | 267.2 | 4 | 1 | 2 | 3.70 | c1ccc(CO[C@H]2CCCN[C@H]2c2ccccc2)cc1 | https://dx.doi.org/10.1016/S0960-894X(97)10118-4 | |
| CHEMBL100636 | 4283 | None | 0 | Rat | Functional | IC50 | = | 0.09 | 10.05 | - | 1 | Antagonism of NK1 receptor in rat liver microsomes. | ChEMBL | 446.1 | 6 | 2 | 5 | 5.30 | C[C@@H](O[C@H]1CCCN(Cc2n[nH]c(O)n2)[C@H]1c1ccccc1)c1cc(Cl)cc(Cl)c1 | https://dx.doi.org/10.1016/S0960-894X(97)10118-4 | |
| CHEMBL101148 | 4366 | None | 0 | Rat | Functional | IC50 | = | 0.16 | 9.80 | - | 1 | Antagonism of NK1 receptor in rat liver microsomes. | ChEMBL | 498.2 | 6 | 1 | 4 | 6.33 | C[C@@H](O[C@H]1CCCN(Cc2nc[nH]n2)[C@H]1c1ccccc1)c1cc(C(F)(F)F)cc(C(F)(F)F)c1 | https://dx.doi.org/10.1016/S0960-894X(97)10118-4 | |
| CHEMBL102032 | 4495 | None | 0 | Rat | Functional | IC50 | = | 0.15 | 9.82 | - | 1 | Antagonism of NK1 receptor in rat liver microsomes. | ChEMBL | 417.2 | 4 | 1 | 2 | 6.29 | C[C@@H](O[C@H]1CCCN[C@H]1c1ccccc1)c1cc(C(F)(F)F)cc(C(F)(F)F)c1 | https://dx.doi.org/10.1016/S0960-894X(97)10118-4 | |
| CHEMBL102157 | 4508 | None | 0 | Rat | Functional | IC50 | = | 0.91 | 9.04 | - | 1 | Antagonism of NK1 receptor in rat liver microsomes. | ChEMBL | 349.1 | 4 | 1 | 2 | 5.56 | C[C@@H](O[C@H]1CCCN[C@H]1c1ccccc1)c1cc(Cl)cc(Cl)c1 | https://dx.doi.org/10.1016/S0960-894X(97)10118-4 | |
| CHEMBL103657 | 4736 | None | 0 | Rat | Functional | IC50 | = | 86.00 | 7.07 | - | 1 | Antagonism of NK1 receptor in rat liver microsomes. | ChEMBL | 281.2 | 4 | 1 | 2 | 4.26 | C[C@@H](O[C@H]1CCCN[C@H]1c1ccccc1)c1ccccc1 | https://dx.doi.org/10.1016/S0960-894X(97)10118-4 | |
| CHEMBL107502 | 5468 | None | 0 | Guinea pig | Functional | IC50 | = | 7500.00 | 5.12 | 1 | 2 | Tested for Tachykinin receptor 1 agonistic activity by measuring its ability to inhibit contractions evoked by [Sar9,Met(O2)11]-SP (4 nM) in guinea pig ileum | ChEMBL | 591.3 | 9 | 3 | 4 | 5.18 | CC(=O)Nc1ccccc1NC(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N(C)Cc1ccccc1 | https://dx.doi.org/10.1021/jm970499g | |
| CHEMBL107763 | 5631 | None | 0 | Guinea pig | Functional | IC50 | = | 5.00 | 8.30 | - | 2 | Tachykinin receptor 1 agonistic activity as inhibition of contractions evoked by 4 nM [Sar9,Met(O2)11]-SP in guinea pig ileum | ChEMBL | 534.3 | 8 | 2 | 3 | 5.22 | CN(Cc1ccccc1)C(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@@H]1CCCN1C(=O)Nc1ccccc1 | https://dx.doi.org/10.1021/jm970499g | |
| CHEMBL108040 | 6036 | None | 0 | Guinea pig | Functional | IC50 | = | 17.30 | 7.76 | - | 2 | Tachykinin receptor 1 agonistic activity as inhibition of contractions evoked by 4 nM [Sar9,Met(O2)11]-SP in guinea pig ileum | ChEMBL | 552.3 | 8 | 2 | 3 | 5.36 | CN(Cc1ccccc1)C(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@@H]1CCCN1C(=O)Nc1ccc(F)cc1 | https://dx.doi.org/10.1021/jm970499g | |
| CHEMBL110219 | 9175 | None | 0 | Guinea pig | Functional | Kd | = | 316.23 | 6.50 | - | 4 | Inhibition of the SP-induced NK1-mediated enhancement of the EFS-induced sympathetic neurogenic contractions of gpvd, used as a measure of antagonist activity. | ChEMBL | 592.2 | 7 | 1 | 4 | 5.89 | Cc1cc(C)cc(C(=O)N2CCN(C(=O)CNC3CCN(Cc4ccccc4)CC3)C(c3ccc(Cl)c(Cl)c3)C2)c1 | https://dx.doi.org/10.1016/s0960-894x(02)00645-5 | |
| CHEMBL110301 | 9185 | None | 0 | Guinea pig | Functional | IC50 | = | 4.20 | 8.38 | - | 2 | Tachykinin receptor 1 agonistic activity as inhibition of contractions evoked by 4 nM [Sar9,Met(O2)11]-SP in guinea pig ileum | ChEMBL | 535.3 | 8 | 2 | 4 | 4.62 | CN(Cc1ccccc1)C(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@@H]1CCCN1C(=O)Nc1cccnc1 | https://dx.doi.org/10.1021/jm970499g | |
| CHEMBL110770 | 9258 | None | 0 | Guinea pig | Functional | IC50 | = | 1.90 | 8.72 | - | 2 | Tachykinin receptor 1 agonistic activity as inhibition of contractions evoked by 4 nM [Sar9,Met(O2)11]-SP in guinea pig ileum | ChEMBL | 577.3 | 9 | 3 | 4 | 4.32 | CN(Cc1ccccc1)C(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@@H]1CCCN1C(=O)Nc1ccccc1C(N)=O | https://dx.doi.org/10.1021/jm970499g | |
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