 | 2-(Diphenylmethyl)-N-((2-methoxyphenyl)methyl)-1-azabicyclo(2.2.2)octan-3-amine | IC50 | 2.0 [1] |
| 2-(Diphenylmethyl)-N-((2-methoxyphenyl)methyl)-1-azabicyclo(2.2.2)octan-3-amine | Ki | 0.3 [1], 0.4 [2], 1.1 [3], 3.1 [4] |
 | 3-(2-Methoxybenzylamino)-2-phenylpiperidine | IC50 | 0.2 [1], 0.6 [2] |
| 3-(2-Methoxybenzylamino)-2-phenylpiperidine | Ki | 0.17 [1] |
 | 3,5-Bis(trifluoromethyl)benzyl N-acetyltryptophan | IC50 | 1.6 [1] |
| 3,5-Bis(trifluoromethyl)benzyl N-acetyltryptophan | Ki | 0.73 [1] |
 | Aprepitant | IC50 | 0.09 [1] |
| Aprepitant | Ki | 0.08 [1], 0.8 [2], 3.0 [3] |
 | Substance P | IC50 | 0.26 [1] |
| Substance P | Ki | 1.6 [1] |
 | (2S,3S)-2-Benzhydryl-3-[[3,5-bis(trifluoromethyl)phenyl]methoxy]-1-azabicyclo[2.2.2]octane | IC50 | 0.2 [1], 1.3 [2] |
 | 4-(3,5-Bis-trifluoromethyl-benzyloxymethyl)-4-phenyl-piperidine | IC50 | 1.0 [1] |
 | Bhsar-SP | IC50 | 0.11 [1], 0.24 [2], 0.32 [3], 2.1 [4] |
 | Talnetant | Ki | 10000.0 [1], 12589.25 [2], 100000.0 [3] |
 | (2-Benzhydryl-1-aza-bicyclo[2.2.2]oct-3-yl)-benzyl-amine | IC50 | 0.09 [1], 16.0 [2], 28.84 [3], 110.0 [4], 150.0 [5] |
 | (6R,7S,8S)-6-[(1R)-1-[3,5-Bis(trifluoromethyl)phenyl]ethoxy]-7-(4-fluorophenyl)-1,2,5,6,7,8-hexahydropyrrolizin-3-one | IC50 | 0.06 [1], 2.2 [2] |
 | (2S,3S)-2-Benzhydryl-3-[(3,5-dimethylphenyl)methoxy]-1-azabicyclo[2.2.2]octane | IC50 | 1.0 [1], 2.0 [2], 196.0 [3], 295.12 [4] |
 | (4S,7S,10S,13S,16S,19S,22S,25S,28S,31S,34S,37R)-37-[[(2S)-2-[(2-Aminoacetyl)amino]propanoyl]amino]-34-(4-aminobutyl)-31-(2-amino-2-oxoethyl)-13,25,28-tribenzyl-19-[(4-fluorophenyl)methyl]-10,16-bis[(1R)-1-hydroxyethyl]-7-(hydroxymethyl)-22-(1H-indol-3-ylmethyl)-6,9,12,15,18,21,24,27,30,33,36-undecaoxo-1,2-dithia-5,8,11,14,17,20,23,26,29,32,35-undecazacyclooctatriacontane-4-carboxylic acid | IC50 | 44.0 [1], 1400.0 [2], 2700.0 [3], 3600.0 [4], 8200.0 [5] |
 | [(2R,4S)-2-Benzyl-4-(quinolin-4-ylmethylamino)piperidin-1-yl]-(3,5-dimethylphenyl)methanone | IC50 | 12.0 [1], 13.0 [2], 55.0 [3] |
 | Vofopitant | IC50 | 0.08 [1] |
| Vofopitant | Ki | 0.03 [1], 0.05 [2] |
 | CP-122721 | IC50 | 0.14 [1], 0.19 [2], 0.4 [3] |
 | Vestipitant | IC50 | 0.25 [1] |
| Vestipitant | Ki | 0.22 [1], 0.25 [2] |
 | 3-[[(2S,3S)-2-[[3,5-Bis(trifluoromethyl)phenyl]methoxy]-3-phenylmorpholin-4-yl]methyl]-1,4-dihydro-1,2,4-triazol-5-one | IC50 | 0.09 [1] |
 | (2S,3S)-N-[[2-Methoxy-5-(tetrazol-1-yl)phenyl]methyl]-2-phenylpiperidin-3-amine | IC50 | 0.04 [1], 0.06 [2] |
| (2S,3S)-N-[[2-Methoxy-5-(tetrazol-1-yl)phenyl]methyl]-2-phenylpiperidin-3-amine | Ki | 0.04 [1], 0.05 [2] |
 | Unii-QK6iajla0M | IC50 | 0.55 [1], 1.0 [2], 1.05 [3], 5.9 [4] |
 | Serlopitant | IC50 | 0.06 [1], 9.5 [2] |
 | (3,5-Dimethylphenyl)methyl (2S)-2-acetamido-3-(1H-indol-3-yl)propanoate | IC50 | 52.48 [1], 67.0 [2] |
 | 1-[(4Z)-5-[[3,5-Bis(trifluoromethyl)phenyl]methoxy]-3-(3,4-dichlorophenyl)-4-methoxyiminopentyl]-4-phenylpiperidin-4-ol | Ki | 25.0 [1] |
 | N-[[3,5-Bis(trifluoromethyl)phenyl]methyl]-N,7-dimethyl-5-(4-methylphenyl)-8-oxo-1,7-naphthyridine-6-carboxamide | IC50 | 0.24 [1], 0.34 [2], 1.4 [3], 7.0 [4] |
 | (2R)-2-[[(2S)-2-Amino-3-(4-hydroxy-2,6-dimethylphenyl)propanoyl]amino]-N-[(4S)-2-[2-[[3,5-bis(trifluoromethyl)phenyl]methyl-methylamino]-2-oxoethyl]-3-oxo-4,5-dihydro-1H-2-benzazepin-4-yl]-5-(diaminomethylideneamino)pentanamide | Ki | 0.5 [1], 7.8 [2] |
 | (S)-1-(1H-Indol-3-yl)-2-(acetylamino)-5-[3,5-bis(trifluoromethyl)phenyl]-3-pentanone | IC50 | 2.2 [1], 3.09 [2], 3.1 [3], 10.0 [4] |
 | N-[(2S)-5-[3,5-Bis(trifluoromethyl)phenyl]-1-(1H-indol-3-yl)-3-oxopentan-2-yl]-4-morpholin-4-ylbutanamide | IC50 | 0.17 [1], 0.24 [2], 1.4 [3] |
 | 3-((E)-3-Carboxy-3-phenyl-allyl)-4,6-dichloro-1H-indole-2-carboxylic acid | IC50 | 3.0 [1], 3.11 [2], 10000.0 [3] |
| 3-((E)-3-Carboxy-3-phenyl-allyl)-4,6-dichloro-1H-indole-2-carboxylic acid | Ki | 0.3 [1] |
 | (6R,7S,8R)-1-Amino-6-[(1R)-1-[3,5-bis(trifluoromethyl)phenyl]ethoxy]-7-(4-fluorophenyl)-1,2,5,6,7,8-hexahydropyrrolizin-3-one | IC50 | 0.09 [1], 0.11 [2], 0.6 [3], 1.8 [4] |
 | (6R,7S,8S)-2-Amino-6-[(1R)-1-[3,5-bis(trifluoromethyl)phenyl]ethoxy]-7-(4-fluorophenyl)-1,2,5,6,7,8-hexahydropyrrolizin-3-one | IC50 | 0.06 [1], 0.38 [2] |
 | 2-[(2S,3S)-3-[[3,5-Bis(trifluoromethyl)phenyl]methoxy]-2-phenylpiperidin-1-yl]acetamide | IC50 | 1.0 [1], 1.29 [2], 1.3 [3] |
 | (4S,7S,10S,13S,16S,19S,22R,25S,28S,31S,34S,37R)-37-[[(2S)-2-[(2-Aminoacetyl)amino]propanoyl]amino]-34-(4-aminobutyl)-31-(2-amino-2-oxoethyl)-13,25,28-tribenzyl-19-[(4-fluorophenyl)methyl]-10,16-bis[(1R)-1-hydroxyethyl]-7-(hydroxymethyl)-22-(1H-indol-3-ylmethyl)-6,9,12,15,18,21,24,27,30,33,36-undecaoxo-1,2-dithia-5,8,11,14,17,20,23,26,29,32,35-undecazacyclooctatriacontane-4-carboxylic acid | IC50 | 220.0 [1], 240.0 [2], 950.0 [3], 6100.0 [4] |
 | (4S,7S,10S,13S,16S,19S,22R,25S,28S,31S,34S,37R)-37-Amino-34-(4-aminobutyl)-31-(2-amino-2-oxoethyl)-13,25,28-tribenzyl-19-[(4-fluorophenyl)methyl]-10,16-bis[(1R)-1-hydroxyethyl]-7-(hydroxymethyl)-22-(1H-indol-3-ylmethyl)-6,9,12,15,18,21,24,27,30,33,36-undecaoxo-1,2-dithia-5,8,11,14,17,20,23,26,29,32,35-undecazacyclooctatriacontane-4-carboxylic acid | IC50 | 250.0 [1], 260.0 [2], 900.0 [3], 9600.0 [4] |
 | Neurokinin B | IC50 | 97.5 [1], 98.0 [2] |
| Neurokinin B | Ki | 501.19 [1] |
 | Senktide | IC50 | 10000.0 [1] |
| Senktide | Ki | 10000.0 [1] |
 | (2S)-1-[(2S)-2-[[(2S)-2-[[2-[[(2R)-2-[[(2S)-2-Amino-3-(4-hydroxyphenyl)propanoyl]amino]propanoyl]amino]acetyl]amino]-3-phenylpropanoyl]amino]-4-methylsulfanylbutanoyl]-N-[(2S)-1-[[(2S)-1-[[3,5-bis(trifluoromethyl)phenyl]methylamino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]pyrrolidine-2-carboxamide | IC50 | 0.01 [1] |
| (2S)-1-[(2S)-2-[[(2S)-2-[[2-[[(2R)-2-[[(2S)-2-Amino-3-(4-hydroxyphenyl)propanoyl]amino]propanoyl]amino]acetyl]amino]-3-phenylpropanoyl]amino]-4-methylsulfanylbutanoyl]-N-[(2S)-1-[[(2S)-1-[[3,5-bis(trifluoromethyl)phenyl]methylamino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]pyrrolidine-2-carboxamide | Ki | 0.01 [1] |
 | 1H-Indole, 2-(4-bromophenyl)-3-[3-[4-(2-methoxyphenyl)-1-piperazinyl]-3-oxopropyl]-5-methyl- | IC50 | 1.0 [1] |
 | 5-{3,4,5-Tris-benzyloxy-6-[2-(1H-indol-3-yl)-ethoxy]-tetrahydro-pyran-2-ylmethoxy}-pentylamine | IC50 | 120.0 [1], 120000.0 [2] |
| 5-{3,4,5-Tris-benzyloxy-6-[2-(1H-indol-3-yl)-ethoxy]-tetrahydro-pyran-2-ylmethoxy}-pentylamine | Ki | 150.0 [1] |
 | 3-[[(2S,3S)-3-[[3,5-Bis(trifluoromethyl)phenyl]methoxy]-2-phenylpiperidin-1-yl]methyl]-1,4-dihydro-1,2,4-triazol-5-one | IC50 | 0.05 [1], 0.1 [2] |
 | 4-Benzyloxymethyl-4-phenyl-piperidine | IC50 | 1096.48 [1], 1100.0 [2], 1113.0 [3] |
 | 2-Dimethylamino-3-(1H-indol-3-yl)-propionic acid 3,5-dimethyl-benzyl ester | IC50 | 549.54 [1], 553.0 [2] |
 | 4-(3,5-Dimethyl-benzyloxymethyl)-4-phenyl-piperidine | IC50 | 8.91 [1], 9.0 [2], 9.1 [3] |
 | (3,5-Dimethylphenyl)methyl (2S)-2-benzamido-3-(1H-indol-3-yl)propanoate | IC50 | 21.88 [1], 22.0 [2] |
 | 1-[(4E)-5-[[3,5-Bis(trifluoromethyl)phenyl]methoxy]-3-(3,4-dichlorophenyl)-4-methoxyiminopentyl]-4-phenylpiperidin-4-ol | Ki | 25.0 [1] |
 | 4-Phenyl-4-(3-trifluoromethyl-benzyloxymethyl)-piperidine | IC50 | 57.0 [1], 57.54 [2] |
 | (2-Benzhydryl-1-aza-bicyclo[2.2.2]oct-3-yl)-(2-methoxy-benzyl)-amine | IC50 | 0.33 [1], 41.0 [2], 81000.0 [3] |
 | [3,5-Bis(trifluoromethyl)phenyl]methyl (2S)-2-[[(2S)-2-[[(2S)-1-[(2S)-2-[[(2S)-2-[[2-[[(2R)-2-[[(2S)-2-amino-3-(4-hydroxyphenyl)propanoyl]amino]propanoyl]amino]acetyl]amino]-3-phenylpropanoyl]amino]-4-methylsulfanylbutanoyl]pyrrolidine-2-carbonyl]amino]-4-methylpentanoyl]amino]-3-(1H-indol-3-yl)propanoate | IC50 | 0.13 [1], 0.95 [2] |
| [3,5-Bis(trifluoromethyl)phenyl]methyl (2S)-2-[[(2S)-2-[[(2S)-1-[(2S)-2-[[(2S)-2-[[2-[[(2R)-2-[[(2S)-2-amino-3-(4-hydroxyphenyl)propanoyl]amino]propanoyl]amino]acetyl]amino]-3-phenylpropanoyl]amino]-4-methylsulfanylbutanoyl]pyrrolidine-2-carbonyl]amino]-4-methylpentanoyl]amino]-3-(1H-indol-3-yl)propanoate | Ki | 0.08 [1] |
 | 2-({[3,5-Bis(trifluoromethyl)phenyl]methoxy}methyl)-2-phenylpiperidine | IC50 | 1.0 [1] |
| 2-({[3,5-Bis(trifluoromethyl)phenyl]methoxy}methyl)-2-phenylpiperidine | Ki | 1.0 [1] |
 | (S,3S)-3-[5-(1,1-Dimethyl-2,2,2-trifluoroethyl)-2-methoxybenzylamino]-2-phenylpiperidine | IC50 | 0.2 [1], 0.3 [2] |
 | 1-Benzofuran-2-ylmethyl N-[(2S)-2-[(dimethylamino)methyl]-3-(1H-indol-3-yl)-1-oxo-1-[[(1S)-1-phenylethyl]amino]propan-2-yl]carbamate | IC50 | 0.46 [1], 0.5 [2], 5.5 [3] |
 | N-[[3,5-Bis(trifluoromethyl)phenyl]methyl]-4-[4-(4-fluorophenyl)piperidin-1-yl]-1-phenylcyclohexane-1-carboxamide | IC50 | 0.34 [1], 150.0 [2] |
 | (2R,3R)-2-Benzhydryl-3-(3,5-bis-trifluoromethyl-benzyloxy)-1-aza-bicyclo[2.2.2]octane | IC50 | 300.0 [1], 570.0 [2], 575.44 [3] |
 | (2R,3S)-2-Benzhydryl-3-[[3,5-bis(trifluoromethyl)phenyl]methoxy]-1-azabicyclo[2.2.2]octane | IC50 | 0.2 [1], 0.7 [2], 0.71 [3] |
 | 2-Methyl-4-phenyl-quinoline-3-carboxylic acid 3,5-bis-trifluoromethyl-benzylamide | IC50 | 0.07 [1], 257.0 [2], 3900.0 [3] |
 | (2R)-2-[[(2S)-2-Amino-3-(4-hydroxy-2,6-dimethylphenyl)propanoyl]amino]-N-[(4S)-2-[3-[benzyl(methyl)amino]-3-oxopropyl]-3-oxo-4,5-dihydro-1H-2-benzazepin-4-yl]-5-(diaminomethylideneamino)pentanamide | Ki | 6.44 [1], 13.0 [2] |
 | 2-[[(2S)-3-[[3,5-Bis(trifluoromethyl)phenyl]methoxy]-1,1-diphenylpropan-2-yl]amino]acetamide | IC50 | 0.52 [1], 0.53 [2] |
| 2-[[(2S)-3-[[3,5-Bis(trifluoromethyl)phenyl]methoxy]-1,1-diphenylpropan-2-yl]amino]acetamide | Ki | 0.9 [1] |
 | (2S,3S,3Ar,6aS)-N-(2-methoxybenzyl)-2-phenyl-octahydrocyclopenta[b]pyrrol-3-amine | IC50 | 2.4 [1], 3.4 [2] |
| (2S,3S,3Ar,6aS)-N-(2-methoxybenzyl)-2-phenyl-octahydrocyclopenta[b]pyrrol-3-amine | Ki | 2.4 [1] |
 | N-[(2S)-5-[3,5-Bis(trifluoromethyl)phenyl]-1-(1H-indol-3-yl)-3-oxopentan-2-yl]-2-pyridin-4-ylacetamide | IC50 | 0.4 [1], 0.5 [2], 10.0 [3] |
 | 2-Benzylidene-3-(3,5-dimethyl-benzyloxy)-1-aza-bicyclo[2.2.2]octane | IC50 | 2933.0 [1], 7500.0 [2], 8200.0 [3] |
 | (2E)-2-Benzylidene-3-[(3,5-dimethylphenyl)methoxy]-1-azabicyclo[2.2.2]octane | IC50 | 120.0 [1], 129.0 [2], 615.0 [3] |
 | (S)-1-(1H-Indol-3-yl)-2-[(morpholinoacetyl)amino]-5-[3,5-bis(trifluoromethyl)phenyl]-3-pentanone | IC50 | 2.0 [1], 3.5 [2], 4.0 [3] |
 | 1-(3,5-Dimethyl-benzyloxymethyl)-2,2-diphenyl-ethylamine | IC50 | 9.3 [1] |
 | 1-(3,5-Bis-trifluoromethyl-benzyloxymethyl)-2,2-diphenyl-ethylamine | IC50 | 10.7 [1] |
 | 2-[1-(3,5-Bis-trifluoromethyl-benzyloxymethyl)-2,2-diphenyl-ethylamino]-acetamide | IC50 | 0.53 [1], 0.85 [2] |
 | 2-[3,5-Bis(trifluoromethyl)phenyl]-N-[4-(4-fluoro-2-methylphenyl)-6-[(2R,3S)-3-hydroxy-2-(hydroxymethyl)pyrrolidin-1-yl]pyridin-3-yl]-N,2-dimethylpropanamide | Ki | 0.7 [1], 1.1 [2] |
 | (2S)-1-[(4Ar)-1-oxo-4,4-diphenyl-2,3,4a,5,7,7a-hexahydrothiopyrano[2,3-c]pyrrol-6-yl]-2-(2-methoxyphenyl)propan-1-one | IC50 | 22.91 [1], 23.0 [2], 49.0 [3] |
 | (2S,3S)-2-Benzhydryl-3-[[3-(trifluoromethyl)phenyl]methoxy]-1-azabicyclo[2.2.2]octane | IC50 | 53.0 [1], 2100.0 [2] |
 | N-[(2S)-5-[3,5-Bis(trifluoromethyl)phenyl]-1-(1H-indol-3-yl)-3-oxopentan-2-yl]-1-azabicyclo[2.2.2]octane-4-carboxamide | IC50 | 0.9 [1], 1.0 [2], 8.0 [3] |
 | [(2S,4R)-2-Benzyl-4-(quinolin-4-ylmethylamino)piperidin-1-yl]-(3,5-dimethylphenyl)methanone | IC50 | 130.0 [1], 690.0 [2] |
 | Saredutant | IC50 | 593.0 [1], 800.0 [2] |
 | 7,7-Diphenyl-2-(1-imino-2-(2-methoxyphenyl)ethyl)perhydroisoindol-4-one | IC50 | 30.0 [1], 49.0 [2] |
 | (R)-(2-Methoxy-benzyl)-((S)-2-phenyl-piperidin-3-yl)-amine | IC50 | 0.5 [1] |
| (R)-(2-Methoxy-benzyl)-((S)-2-phenyl-piperidin-3-yl)-amine | Ki | 0.17 [1] |
 | Casopitant | Ki | 0.13 [1], 0.33 [2] |
 | Netupitant | IC50 | 0.95 [1] |
| Netupitant | Ki | 0.95 [1] |
 | Lanepitant | IC50 | 0.15 [1], 0.23 [2] |
 | SB 218795 | Ki | 100000.0 [1] |
 | Unii-qrt7W0TL6X | IC50 | 0.45 [1] |
 | Dapitant | IC50 | 13.0 [1], 13000.0 [2] |
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