Target Validation Information
TTD ID T78709
Target Name 5-HT 1A receptor (HTR1A)
Type of Target
Successful
Drug Potency against Target Buspirone Drug Info IC50 = 24 nM [62]
Adatanserin Drug Info Ki = 1 nM [53]
Bifeprunox Drug Info Ki = 64.6 nM [59]
BTS-79018 Drug Info Ki = 3.6 nM [54]
Flibanserin Drug Info Ki = 1 nM
OPC-14523 Drug Info IC50 = 2.3 nM [56]
PD-158771 Drug Info Ki = 2.6 nM [55]
Sarizotan Drug Info Ki = 0.1 nM [58]
SLV-313 Drug Info Ki = 0.79 nM [60]
SSR-181507 Drug Info Ki = 0.242 nM [57]
Vilazodone Drug Info IC50 = 0.2 nM [61]
1192U90 Drug Info Ki = 3.8 nM [63]
(3-Chloro-phenyl)-piperazin-1-yl-methanone Drug Info Ki = 17100 nM [38]
(R)-(-)-10-methyl-11-hydroxyaporphine Drug Info Ki = 216 nM [19]
(R)-11-Amino-2-methoxyaporphine Drug Info Ki = 640 nM [24]
(R)-2,11-Diaminoaporphine Drug Info Ki = 2300 nM [24]
1,2,3,4-Tetrahydro-naphthalen-2-ylamine Drug Info Ki = 380 nM [39]
1,6-bis(4-(3-chlorophenyl)piperazin-1-yl)hexane Drug Info Ki = 16 nM [31]
1,6-bis(4-(3-methoxyphenyl)piperazin-1-yl)hexane Drug Info Ki = 8 nM [31]
1,6-bis(4-(pyridin-2-yl)piperazin-1-yl)hexane Drug Info Ki = 16 nM [31]
1,6-bis(4-m-tolylpiperazin-1-yl)hexane Drug Info Ki = 48 nM [31]
1,6-bis(4-phenylpiperazin-1-yl)hexane Drug Info Ki = 3 nM [31]
1-((S)-2-aminopropyl)-1H-indazol-6-ol Drug Info Ki = 141 nM [12]
1-(2,5-Dimethoxy-4-methyl-phenyl)-piperazine Drug Info Ki = 680 nM [38]
1-(2,5-Dimethoxy-phenyl)-piperazine Drug Info Ki = 1035 nM [38]
1-(2,5-dimethoxyphenyl)propan-2-amine Drug Info Ki = 1020 nM [40]
1-(2-((3-fluorophenoxy)methyl)phenyl)piperazine Drug Info Ki = 116 nM [28]
1-(2-(2-chlorophenoxy)pyridin-3-yl)piperazine Drug Info Ki = 4.5 nM [29]
1-(2-(2-fluorobenzyloxy)phenyl)piperazine Drug Info Ki = 31 nM [28]
1-(2-(3-fluorophenoxy)phenyl)piperazine Drug Info Ki = 9 nM [28]
1-(2-(4-fluorophenoxy)phenyl)piperazine Drug Info Ki = 8 nM [28]
1-(2-(benzyloxy)phenyl)piperazine Drug Info Ki = 28 nM [28]
1-(2-(phenoxymethyl)phenyl)piperazine Drug Info Ki = 189 nM [28]
1-(2-Butoxy-phenyl)-piperazine Drug Info Ki = 19.3 nM [36]
1-(2-Chloro-phenyl)-piperazine Drug Info Ki = 226 nM [13]
1-(2-Ethoxy-phenyl)-piperazine Drug Info Ki = 42.6 nM [36]
1-(2-Fluoro-phenyl)-piperazine Drug Info Ki = 57.9 nM [36]
1-(2-Isopropoxy-phenyl)-piperazine Drug Info Ki = 19 nM [36]
1-(2-Methoxy-phenyl)-4-propyl-piperazine Drug Info Ki = 249 nM [44]
1-(2-Methoxy-phenyl)-piperazine Drug Info Ki = 281 nM [13]
1-(2-methoxyphenyl)-4-pentylpiperazine Drug Info Ki = 5.16 nM [33]
1-(2-phenoxyphenyl)piperazine Drug Info Ki = 128 nM [28]
1-(3-Fluoro-phenyl)-piperazine Drug Info Ki = 86.5 nM [36]
1-(3-Nitro-phenyl)-piperazine Drug Info Ki = 250 nM [36]
1-(4-Bromo-2,5-dimethoxy-phenyl)-piperazine Drug Info Ki = 820 nM [38]
1-(7-Methoxy-naphthalen-2-yl)-piperazine Drug Info Ki = 2.8 nM [50]
1-(benzyloxy)-2-(2-phenylethyl)benzene Drug Info Ki = 5000 nM [17]
1-(benzyloxy)-2-[2-(3-methoxyphenyl)ethyl]benzene Drug Info Ki = 5000 nM [17]
1-Benzyl-4-chroman-2-ylmethyl-piperazine Drug Info Ki = 20.7 nM [7]
1-Butyl-4-(2-methoxy-phenyl)-piperazine Drug Info Ki = 57 nM [44]
1-Ethyl-4-(2-methoxy-phenyl)-piperazine Drug Info Ki = 203 nM [44]
1-Methyl-1,3-dihydro-indol-2-one Drug Info Ki = 29 nM [2]
1-Naphthalen-2-yl-piperazine Drug Info Ki = 265 nM [39]
1-naphthylpiperazine Drug Info Ki = 5 nM [39]
1-Propyl-3-(3-trifluoromethyl-phenyl)-pyrrolidine Drug Info Ki = 351 nM
1-[(3-methoxybenzyl)oxy]-2-(2-phenylethyl)benzene Drug Info Ki = 5000 nM [17]
2-(2'-methyl-biphenyl-3-yl)-ethylamine Drug Info Ki = 1470 nM [18]
2-(2-Amino-propyl)-5-bromo-4-methoxy-phenol Drug Info Ki = 1710 nM [40]
2-(2-chlorophenoxy)-3-(piperidin-4-yl)pyridine Drug Info Ki = 16 nM [29]
2-(2-fluorophenoxy)-3-(piperidin-4-yl)pyridine Drug Info Ki = 13 nM [29]
2-(2-Methoxy-phenyl)-1-methyl-ethylamine Drug Info Ki = 3500 nM [40]
2-(2-methoxyphenoxy)-3-(piperidin-4-yl)pyridine Drug Info Ki = 92 nM [29]
2-(3-Bromophenylthio)-N,N-dimethylethanamine Drug Info Ki = 676 nM [30]
2-(3-Methoxy-phenyl)-1-methyl-ethylamine Drug Info Ki = 2660 nM [40]
2-(4-Benzyl-piperidin-1-ylmethyl)-chroman-4-one Drug Info Ki = 297 nM [7]
2-(4-Bromo-2-methoxy-phenyl)-1-methyl-ethylamine Drug Info Ki = 2900 nM [40]
2-(4-Bromo-phenyl)-1-methyl-ethylamine Drug Info Ki = 2830 nM [40]
2-(4-Methyl-piperazin-1-yl)-4-phenyl-pyrimidine Drug Info Ki = 613 nM
2-(5-Methoxy-1H-indol-3-yl)-1-methyl-ethylamine Drug Info IC50 = 86.4 nM [4]
2-(Biphenyl-3-ylthio)-N,N-dimethylethanamine Drug Info Ki = 516 nM [30]
2-Dipropylamino-1,2,3,4-tetrahydro-anthracen-9-ol Drug Info Ki = 2520 nM
2-phenoxy-3-(piperidin-4-yl)pyridine Drug Info Ki = 101 nM [29]
2-Piperazin-1-yl-benzonitrile Drug Info Ki = 26.1 nM [36]
2-Piperazin-1-yl-phenol Drug Info Ki = 150 nM [38]
2-{[2-(2-phenylethyl)phenoxy]methyl}pyridine Drug Info Ki = 5000 nM [17]
3-(1,2,3,6-Tetrahydro-pyridin-4-yl)-1H-indole Drug Info IC50 = 140 nM [34]
3-(1-Propyl-pyrrolidin-3-yl)-phenol Drug Info Ki = 201 nM
3-(2-Amino-propyl)-1H-indol-5-ol Drug Info IC50 = 19.6 nM [4]
3-(2-Benzylamino-ethoxy)-phenol Drug Info Ki = 1782 nM [52]
3-(3-Methanesulfonyl-phenyl)-1-propyl-pyrrolidine Drug Info Ki = 807 nM
3-(4-Benzyl-piperidin-1-ylmethyl)-chroman-4-one Drug Info Ki = 260 nM [7]
3-(4-Benzyl-piperidin-1-ylmethyl)-chromen-4-one Drug Info Ki = 120 nM [7]
3-(piperidin-4-yl)-2-(o-tolyloxy)pyridine Drug Info Ki = 60 nM [29]
3-Amino-1-(2-amino-5-methoxy-phenyl)-propan-1-one Drug Info Ki = 345 nM [38]
3-Butyl-2,3,4,5-tetrahydro-1H-benzo[d]azepin-6-ol Drug Info IC50 = 420 nM [5]
3-Ethyl-2,3,4,5-tetrahydro-1H-benzo[d]azepin-6-ol Drug Info IC50 = 630 nM [5]
3-Naphthalen-1-yl-1-propyl-pyrrolidine Drug Info Ki = 73 nM
3-Naphthalen-1-yl-pyrrolidine Drug Info Ki = 95 nM
3-Phenyl-1-propyl-pyrrolidine Drug Info Ki = 453 nM
3-{[2-(2-phenylethyl)phenoxy]methyl}pyridine Drug Info Ki = 5000 nM [17]
4-(1H-indol-4-yloxy)-1-(isopropylamino)butan-2-ol Drug Info Ki = 1772 nM [21]
4-(2-(2-fluoro-5-methylphenoxy)phenyl)piperidine Drug Info Ki = 57 nM [28]
4-(2-(2-fluorobenzyloxy)phenyl)piperidine Drug Info Ki = 47 nM [28]
4-(2-(3-chlorophenoxy)phenyl)piperidine Drug Info Ki = 5 nM [28]
4-(2-(3-fluorophenoxy)phenyl)piperidine Drug Info Ki = 11 nM [28]
4-(2-(4-fluorobenzyloxy)phenyl)piperidine Drug Info Ki = 77 nM [28]
4-(2-(4-fluorophenoxy)phenyl)piperidine Drug Info Ki = 117 nM [28]
4-(2-(benzyloxy)-3-fluorophenyl)piperidine Drug Info Ki = 606 nM [28]
4-(2-(benzyloxy)-6-fluorophenyl)piperidine Drug Info Ki = 364 nM [28]
4-(2-(benzyloxy)phenyl)piperidine Drug Info Ki = 121 nM [28]
4-(2-fluoro-6-(2-fluorophenoxy)phenyl)piperidine Drug Info Ki = 4.6 nM [29]
4-(2-fluoro-6-(3-fluorophenoxy)phenyl)piperidine Drug Info Ki = 21 nM [28]
4-(2-fluoro-6-(4-fluorophenoxy)phenyl)piperidine Drug Info Ki = 156 nM [28]
4-(2-fluoro-6-phenoxyphenyl)piperidine Drug Info Ki = 128 nM [28]
4-(2-phenoxyphenyl)piperidine Drug Info Ki = 63 nM [28]
4-(3-fluoro-2-phenoxyphenyl)piperidine Drug Info Ki = 20 nM [28]
4-(4-butylpiperidin-1-yl)-1-o-tolylbutan-1-one Drug Info Ki = 280 nM [32]
4-Benzyl-1-chroman-2-ylmethyl-piperidine Drug Info Ki = 11.5 nM [7]
4-Benzyl-1-chroman-3-ylmethyl-piperidine Drug Info Ki = 226 nM [7]
5,6-dichloro-3,4-dihydroquinazolin-2-amine Drug Info Ki = 1080 nM [22]
5-chloro-3,4-dihydroquinazolin-2-amine Drug Info Ki = 1701 nM [22]
5-chloro-4-ethyl-3,4-dihydroquinazolin-2-amine Drug Info Ki = 1081 nM [22]
5-chloro-4-methyl-3,4-dihydroquinazolin-2-amine Drug Info Ki = 192 nM [22]
8-Methoxy-1,2,3,4-tetrahydro-naphthalen-2-ylamine Drug Info Ki = 158 nM
8-Methoxy-2-(4-methyl-piperazin-1-yl)-quinoline Drug Info Ki = 1900 nM [39]
8-Methoxy-2-piperazin-1-yl-quinoline Drug Info Ki = 415 nM [39]
8-methoxy-4-methyl-3,4-dihydroquinazolin-2-amine Drug Info Ki = 32 nM [22]
8-Methoxy-quinolin-2-ylamine Drug Info Ki = 10400 nM [39]
9-Methoxy-1,2,3,4-tetrahydro-anthracen-2-ylamine Drug Info Ki = 2520 nM
A-80426 Drug Info Ki = 2 nM [11]
AGROCLAVINE Drug Info IC50 = 140 nM [35]
AR-129330 Drug Info IC50 = 16.9 nM [26]
BMY-7378 Drug Info Ki = 8.2 nM [47]
BP-897 Drug Info Ki = 4.9 nM [3]
Brolamfetamine Drug Info Ki = 3340 nM [40]
CGS-12066B Drug Info IC50 = 19 nM [34]
CHLOROPHENYLPIPERAZINE Drug Info Ki = 25 nM [36]
CP-293019 Drug Info IC50 = 180 nM [51]
ESCHOLTZINE Drug Info Ki = 6000 nM [14]
Etisulergine Drug Info IC50 = 26 nM [41]
GR-127935 Drug Info IC50 = 425 nM [1]
LY-334370 Drug Info Ki = 22 nM [6]
LYSERGIC ACID DIETHYLAMIDE Drug Info Ki = 5.1 nM [42]
MAZAPERTINE Drug Info Ki = 1.7 nM [43]
MCL-516 Drug Info Ki = 151 nM [24]
N-(3-(1H-indol-4-yloxy)propyl)cyclohexanamine Drug Info Ki = 78.4 nM [21]
N-(3-(1H-indol-4-yloxy)propyl)cyclopentanamine Drug Info Ki = 233 nM [21]
N-Benzyl-4-(2-diphenyl)-1-piperazinehexanamide Drug Info Ki = 161 nM [25]
N-methyllaurotetanine Drug Info Ki = 85 nM [14]
N-[4-(4-Phenyl-piperazin-1-yl)-butyl]-benzamide Drug Info Ki = 11 nM [37]
PB-28 Drug Info Ki = 28.6 nM [46]
PG-01037 Drug Info Ki = 85.4 nM [20]
PHENYLPIPERAZINE Drug Info Ki = 135 nM [39]
QUIPAZINE Drug Info Ki = 1584 nM [27]
RWJ-25730 Drug Info Ki = 3.3 nM [43]
SB-271046 Drug Info Ki = 340 nM [23]
SB-656104 Drug Info Ki = 562 nM [9]
SEROTONIN Drug Info Ki = 1.6 nM [27]
SNAP-8719 Drug Info Ki = 300 nM [10]
Sumanirole Drug Info Ki = 73 nM [48]
Sunepitron Drug Info Ki = 92 nM [15]
TERTATOLOL Drug Info Ki = 18.2 nM
TFMPP Drug Info Ki = 20 nM [38]
TIOSPIRONE Drug Info IC50 = 2.85 nM [16]
UH-232 Drug Info Ki = 168 nM
UH-301 Drug Info Ki = 52 nM [49]
WAY-466 Drug Info Ki = 234 nM [8]
WB-4101 Drug Info Ki = 2.68 nM [45]
[3H]spiperone Drug Info Ki = 602 nM [45]
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