Target Validation Information
Target ID T32060
Target Name 5-hydroxytryptamine 2A receptor
Target Type
Successful
Drug Potency against Target (R,S)-1-(5-methyl-1H-indol-1-yl)propan-2-amine Drug Info Ki = 794 nM
SR46349B Drug Info Ki = 1.26 nM [553190]
Blonanserin Drug Info Ki = 5460 nM [553210]
1,6-bis(4-phenylpiperazin-1-yl)hexane Drug Info Ki = 31 nM [530927]
2-Piperazin-1-yl-phenol Drug Info Ki = 17200 nM [533476]
1-(2,5-Dimethoxy-4-methyl-phenyl)-piperazine Drug Info Ki = 4710 nM [533476]
Flibanserin Drug Info Ki = 49 nM
4-methoxy-9-aminomethyl-9,10-dihydroanthracene Drug Info Ki = 124 nM [529672]
(E)-2-(4-fluorostyryl)-5-(phenylsulfinyl)pyridine Drug Info Ki = 7.7 nM [528690]
GR-127935 Drug Info Ki = 42.7 nM [527726]
3-(2-Pyrrolidin-1-yl-ethyl)-1H-indol-4-ol Drug Info Ki = 429 nM [527668]
BARETTIN Drug Info Ki = 1930 nM [528498]
N-methyl-4,4-diphenylbutan-1-amine Drug Info Ki = 754 nM [530331]
Brolamfetamine Drug Info Ki = 13 nM [529463]
QUIPAZINE Drug Info Ki = 794 nM [530451]
1-(2,5-Dimethoxy-phenyl)-piperazine Drug Info Ki = 8430 nM [533476]
1-Naphthalen-1-yl-piperazine Drug Info Ki = 18 nM [533482]
1-(4-Bromo-2,5-dimethoxy-phenyl)-piperazine Drug Info Ki = 2430 nM [533476]
2-(2-Amino-propyl)-5-bromo-4-methoxy-phenol Drug Info Ki = 210 nM [533498]
2-(3-Methoxy-phenyl)-1-methyl-ethylamine Drug Info Ki = 7850 nM [533498]
1,6-bis(4-(3-methoxyphenyl)piperazin-1-yl)hexane Drug Info Ki = 28 nM [530927]
5,6-dichloro-3,4-dihydroquinazolin-2-amine Drug Info Ki = 434 nM [529148]
5-MEO-DMT Drug Info IC50 = 9.53 nM [527952]
(R)-1-(4-iodo-2,5-dimethoxyphenyl)propan-2-amine Drug Info IC50 = 0.46 nM [528778]
11-Propionyloxy-N-n-propylnoraporphine Drug Info Ki = 109 nM [529686]
APLYSINOPSIN Drug Info Ki = 598 nM
1192U90 Drug Info Ki = 3.3 nM [553241]
2-methoxy-9-aminomethyl-9,10-dihydroanthracene Drug Info Ki = 1367 nM [529672]
11-valeryloxynoraporphine Drug Info Ki = 92 nM [529686]
11-Butyryloxy-N-n-propylnoraporphine Drug Info Ki = 56 nM [529686]
4-(4-butylpiperidin-1-yl)-1-o-tolylbutan-1-one Drug Info Ki < 1000 nM [531079]
VOLINANSERIN Drug Info Ki = 0.36 nM [530045]
ZOTEPINE Drug Info Ki = 2.7 nM [525963]
4-(4-Fluoro-benzyl)-piperidine hydrochloride Drug Info Ki = 1100 nM [526959]
6-chloro-N-(pyridin-3-yl)indoline-1-carboxamide Drug Info Ki = 794 nM
N,N-dimethyl-4,4-diphenylbutan-1-amine Drug Info Ki = 1151 nM [530331]
N,N-dimethyl-2,2-diphenylethanamine Drug Info Ki = 7356 nM [530331]
9-(2-aminoethyl)-9,10-dihydroanthracene Drug Info Ki = 480 nM [530331]
4,4-Diphenylbutan-1-amine Drug Info Ki = 2589 nM [530331]
Ocaperidone Drug Info Ki = 0.14 nM [552375]
(R)-(+)-(4,5,6-trimethoxyindan-1-yl)methanamine Drug Info Ki = 69 nM [528294]
(S)-(-)-(4,5,6-trimethoxyindan-1-yl)methanamine Drug Info Ki = 1120 nM [528294]
LYSERGIC ACID DIETHYLAMIDE Drug Info Ki = 3.5 nM [528294]
C-(5-bromo-4,7-dimethoxyindan-1-yl)methylamine Drug Info Ki = 47 nM [528433]
[2-(6-Methoxy-indol-1-yl)-ethyl]-dimethyl-amine Drug Info Ki = 1040 nM [526235]
9-(Aminomethyl)-9,10-dihydroanthracene Drug Info Ki = 20 nM [525993]
CHLOROPHENYLPIPERAZINE Drug Info Ki = 48 nM [530589]
RP-68303 Drug Info IC50 = 30 nM [534052]
YM-348 Drug Info Ki = 13 nM [529221]
VER-3323 Drug Info Ki = 351 nM [527037]
2-(5-Methoxy-1H-indol-3-yl)-1-methyl-ethylamine Drug Info IC50 = 2 nM [527952]
Ro-60-0175 Drug Info Ki = 39 nM [529168]
1-(2-aminoethyl)-1H-indazol-6-ol Drug Info IC50 = 0.77 nM [527952]
1-Butyl-3-(2-dimethylamino-ethyl)-1H-indol-4-ol Drug Info Ki = 310 nM [527668]
3-(2-Dimethylamino-propyl)-1H-indol-4-ol Drug Info Ki = 982 nM [527668]
3-(3-Dimethylamino-propyl)-1H-indol-4-ol Drug Info Ki = 588 nM [527668]
(2S)-1-(5-fluoro-1H-indazol-1-yl)propan-2-amine Drug Info Ki = 89 nM [529168]
7,8,9,10-tetrahydro-6H-furo-[2,3-g][3]benzazepine Drug Info Ki = 99 nM [529221]
PRUVANSERIN Drug Info Ki = 0.48 nM [531083]
2-(4-Bromo-2-methoxy-phenyl)-1-methyl-ethylamine Drug Info Ki = 4870 nM [533498]
3-(1-Methyl-piperidin-4-yl)-2-phenyl-1H-indole Drug Info Ki = 7.8 nM [525940]
2-Phenyl-3-(2-piperidin-1-yl-ethyl)-1H-indole Drug Info Ki = 2.7 nM [525940]
3-(1-Benzyl-piperidin-4-yl)-2-phenyl-1H-indole Drug Info Ki = 28 nM [525940]
2-(4-Methyl-piperazin-1-yl)-4-phenyl-pyrimidine Drug Info Ki = 2095 nM
TRYPTAMINE Drug Info Ki = 50 nM [533464]
9-(N-benzylaminomethyl)-9,10-dihydroanthracene Drug Info Ki = 721 nM [530613]
11-Heptanoyloxy-N-n-propylnoraporphine Drug Info Ki = 95 nM [529686]
11-Hexanoyloxy-N-n-propylnoraporphine Drug Info Ki = 109 nM [529686]
3-Dimethylaminomethyl-1-methyl-1H-indol-4-ol Drug Info Ki = 498 nM [527668]
Iloperidone Drug Info KI = 11 nM [553182]
VER-2692 Drug Info Ki = 31 nM [527833]
1-Naphthalen-2-yl-piperazine Drug Info Ki = 70 nM [533482]
SEROTONIN Drug Info Ki = 1258 nM [530451]
3-Dimethylaminomethyl-1H-indol-4-ol Drug Info Ki = 923 nM [527668]
(R)-3-(4-propylmorpholin-2-yl)phenol Drug Info Ki = 970 nM [529128]
2-(4-Bromo-phenyl)-1-methyl-ethylamine Drug Info Ki = 4650 nM [533498]
8-Methoxy-2-(4-methyl-piperazin-1-yl)-quinoline Drug Info Ki = 1200 nM [533482]
PHENYLPIPERAZINE Drug Info Ki = 2100 nM [533482]
3-(2-Amino-propyl)-1H-indol-5-ol Drug Info IC50 = 3.5 nM [527952]
1,2,3,4-Tetrahydro-naphthalen-2-ylamine Drug Info Ki = 11100 nM [533482]
Etisulergine Drug Info IC50 = 26 nM [533501]
3-Amino-1-(2-amino-5-methoxy-phenyl)-propan-1-one Drug Info Ki = 8480 nM [533476]
1-(2-Methoxy-phenyl)-piperazine Drug Info Ki = 3500 nM [533476]
2-(2-Methoxy-phenyl)-1-methyl-ethylamine Drug Info Ki = 8130 nM [533498]
(1-Phenethyl-piperidin-4-yl)-phenyl-methanone Drug Info Ki = 9.6 nM [525963]
3-Naphthalen-1-yl-1-propyl-pyrrolidine Drug Info Ki = 113 nM
NELOTANSERIN Drug Info Ki = 0.51 nM [531083]
SPIPERONE Drug Info Ki = 1 nM [534417]
ALTANSERIN Drug Info Ki = 0.72 nM [530045]
1,6-bis(4-(pyridin-2-yl)piperazin-1-yl)hexane Drug Info Ki = 45 nM [530927]
CINANSERIN Drug Info Ki = 4 nM [533464]
(R,S)-1-(6-fluoro-1H-indol-1-yl)propan-2-amine Drug Info Ki = 251 nM
FLUANISONE Drug Info Ki = 52 nM [533378]
3-Naphthalen-1-yl-pyrrolidine Drug Info Ki = 40 nM
1-Propyl-3-(3-trifluoromethyl-phenyl)-pyrrolidine Drug Info Ki = 569 nM
1-Ethyl-4-(2-methoxy-phenyl)-piperazine Drug Info Ki = 3120 nM [533873]
1-(3-(phenylthio)propyl)-4-m-tolylpiperazine Drug Info Ki = 13.6 nM [528625]
MDL-11939 Drug Info Ki = 12.5 nM [526959]
MDL-28161 Drug Info IC50 = 0.9 nM [526959]
C-(9H-Thioxanthen-9-yl)-methylamine Drug Info Ki = 65 nM [525993]
8-Methoxy-2,3,4,9-tetrahydro-1H-beta-carboline Drug Info Ki = 400 nM [526899]
5-Methoxy-2,3,4,9-tetrahydro-1H-beta-carboline Drug Info Ki = 75 nM [526899]
7-Methoxy-2,3,4,9-tetrahydro-1H-beta-carboline Drug Info Ki = 2200 nM [526899]
2,2-Diphenyl-ethylamine Drug Info Ki = 5700 nM [525993]
1,6-bis(4-m-tolylpiperazin-1-yl)hexane Drug Info Ki = 20 nM [530927]
N,N-Dimethyl-3,3-diphenylpropan-1-amine Drug Info Ki = 1636 nM [530331]
Pimavanserin Drug Info Ki = 8 nM [552847]
6-bromoaplysinopsin Drug Info Ki = 2000 nM [526321]
Adatanserin Drug Info Ki = 73 nM [534942]
TIOSPIRONE Drug Info Ki = 0.58 nM [534093]
ISOCLOZAPINE Drug Info IC50 = 12 nM [534532]
N-(1-benzylpiperidine-4-yl)-2-naphthamide Drug Info Ki = 44 nM [528638]
Racemic DOI Drug Info Ki = 19 nM [529336]
N-(1-(4-nitrobenzyl)piperidin-4-yl)-2-naphthamide Drug Info Ki = 278 nM [528638]
(R,S)-1-(5-bromo-1H-indol-1-yl)propan-2-amine Drug Info Ki = 159 nM
1-Butyl-4-(2-methoxy-phenyl)-piperazine Drug Info Ki = 2280 nM [533873]
N-(1-(3-bromobenzyl)piperidin-4-yl)-2-naphthamide Drug Info Ki = 53 nM [528638]
7-Chloro-1,2,3,4-tetrahydro-pyrazino[1,2-a]indole Drug Info Ki = 80 nM [526235]
8-Chloro-1,2,3,4-tetrahydro-pyrazino[1,2-a]indole Drug Info Ki = 320 nM [526235]
(2S)-1-(6-fluoro-1H-indazol-1-yl)propan-2-amine Drug Info Ki = 82 nM [529168]
(E)-2-(4-fluorostyryl)-5-(phenylsulfonyl)pyridine Drug Info Ki = 7.4 nM [528690]
PG-01037 Drug Info Ki = 62.4 nM [528974]
2,5-dimethoxy-4-bromophenethylamine Drug Info Ki = 0.88 nM [528433]
(R,S)-1-(5-chloro-1H-indol-1-yl)propan-2-amine Drug Info Ki = 200 nM
YM-992 Drug Info Ki = 21 nM [536286]
1-methoxy-9-aminomethyl-9,10-dihydroanthracene Drug Info Ki = 1158 nM [529672]
Lurasidone hydrochloride Drug Info Ki = 2.03 nM [552724]
WAY-208466 Drug Info IC50 = 351 nM [530209]
5-chloro-N-(pyridin-3-yl)indoline-1-carboxamide Drug Info Ki = 2512 nM
2-(piperazin-1-yl)-5,6,7,8-tetrahydroquinoline Drug Info Ki = 21 nM [530516]
5-METHOXYTRYPTAMINE Drug Info Ki = 14 nM [533464]
Racemic DOTFM Drug Info Ki = 33 nM [529336]
VER-5593 Drug Info Ki = 53 nM [527037]
1-(2,6-dimethoxy-4-methylphenyl)propan-2-amine Drug Info Ki = 351 nM [529336]
1-(4-Bromo-2,5-difluorophenyl)-2-aminopropane Drug Info Ki = 2505 nM [529336]
4-Benzyl-1-methyl-piperidine hydrochloride Drug Info Ki = 3870 nM [526959]
PRUVANSERIN Drug Info Ki = 0.87 nM [528150]
8-Methoxy-4,9-dihydro-3H-beta-carboline Drug Info Ki = 2550 nM [526899]
2-(1H-indol-3-yl)-N,N-dimethylethanamine Drug Info Ki = 1636 nM [529336]
N-3'-ethylaplysinopsin Drug Info Ki = 1700 nM [526321]
C-(9H-Xanthen-9-yl)-methylamine Drug Info Ki = 170 nM [525993]
1-(3-Trifluoromethyl-phenyl)-piperazine Drug Info Ki = 160 nM [533476]
8-Methoxy-2-piperazin-1-yl-quinoline Drug Info Ki = 310 nM [533482]
1-((S)-2-aminopropyl)-7-methyl-1H-indazol-6-ol Drug Info IC50 = 0.74 nM [527952]
MAZAPERTINE Drug Info Ki = 165 nM [533800]
4-(10H-Anthracen-9-ylidene)-1-methyl-piperidine Drug Info Ki = 0.7 nM [525993]
5-Methoxy-4,9-dihydro-3H-beta-carboline Drug Info Ki = 500 nM [526899]
9-(2-aminopropyl)-9,10-dihydroanthracene Drug Info Ki = 32 nM [530331]
(R)-(-)-11-hydroxy-N-n-propylnoraporphine Drug Info Ki = 114 nM [529686]
2-(9,10-dihydroanthracen-9-yl)-N-methylethanamine Drug Info Ki = 92 nM [530331]
N-methyl-3,3-diphenylpropan-1-amine Drug Info Ki = 1498 nM [530331]
1-(2-Methoxy-phenyl)-4-propyl-piperazine Drug Info Ki = 3290 nM [533873]
3-(2-Dimethylamino-ethyl)-1H-indol-6-ol Drug Info Ki = 7600 nM [527668]
[2-(4-Fluoro-1H-indol-3-yl)-ethyl]-dimethyl-amine Drug Info Ki = 335 nM [527668]
DOM Drug Info Ki = 100 nM [529336]
N-(1-(4-bromobenzyl)piperidin-4-yl)-2-naphthamide Drug Info Ki = 223 nM [528638]
2-(3,5-dimethoxy-4-phenethoxyphenyl)ethanamine Drug Info Ki = 59 nM [529336]
C-(5H-Dibenzo[a,d]cyclohepten-5-yl)-methylamine Drug Info Ki = 4125 nM [525993]
N-(1-phenethylpiperidin-4-yl)-2-naphthamide Drug Info Ki = 42 nM [528639]
TRYPTOLINE Drug Info Ki = 3000 nM [526899]
SB-271046 Drug Info Ki = 1740 nM [529191]
5-chloro-3,4-dihydroquinazolin-2-amine Drug Info Ki = 1164 nM [529148]
2-Phenyl-3-piperidin-4-yl-1H-indole Drug Info Ki = 12.1 nM [525940]
1-(10-Bromoanthracen-9-yl)-2-aminopropane Drug Info Ki = 313 nM [529336]
1-(2,5-dimethoxyphenyl)propan-2-amine Drug Info Ki = 5200 nM [529336]
1-((R)-2-aminopropyl)-1H-indazol-6-ol Drug Info IC50 = 2.08 nM [527952]
6-Methoxy-2,3,4,9-tetrahydro-1H-beta-carboline Drug Info Ki = 1400 nM [526899]
8-Bromo-4,9-dihydro-3H-beta-carboline Drug Info Ki = 115 nM [526899]
5-Bromo-2,3,4,9-tetrahydro-1H-beta-carboline Drug Info Ki = 80 nM [526899]
3-(1-Phenethyl-piperidin-4-yl)-2-phenyl-1H-indole Drug Info Ki = 0.5 nM [525940]
1-(4-ethyl-2,5-dimethoxyphenyl)propan-2-amine Drug Info Ki = 100 nM [529336]
8-Bromo-2,3,4,9-tetrahydro-1H-beta-carboline Drug Info Ki = 21 nM [526899]
3-methoxy-9-aminomethyl-9,10-dihydroanthracene Drug Info Ki = 7.5 nM [529672]
(2S)-1-(1H-furo[2,3-g]indazol-1-yl)propan-2-amine Drug Info Ki = 0.78 nM [529168]
PHENETHYLAMINE Drug Info Ki = 16820 nM [525993]
1,2,3,4-Tetrahydro-pyrazino[1,2-a]indole Drug Info Ki = 635 nM [526235]
7,8,9,10-tetrahydro-6H-furo-[3,2-g][3]benzazepine Drug Info Ki = 46 nM [529221]
1,6-bis(4-(3-chlorophenyl)piperazin-1-yl)hexane Drug Info Ki = 98 nM [530927]
N-(1-(1-phenylethyl)piperidin-4-yl)-1-naphthamide Drug Info Ki = 248 nM [528639]
PSILOCIN Drug Info Ki = 323 nM [529336]
MESCALINE Drug Info Ki = 5500 nM [529336]
N-(1-phenethylpiperidin-4-yl)-1-naphthamide Drug Info Ki = 543 nM [528639]
N-(1-(4-phenylbutyl)piperidin-4-yl)-2-naphthamide Drug Info Ki = 213 nM [528639]
N-(1-(3-bromobenzyl)piperidin-4-yl)-1-naphthamide Drug Info Ki = 462 nM [528638]
(2-Indol-1-yl-ethyl)-dimethyl-amine Drug Info Ki = 650 nM [526235]
N-(1-(4-phenylbutyl)piperidin-4-yl)-1-naphthamide Drug Info Ki = 487 nM [528639]
N-(1-(1-phenylethyl)piperidin-4-yl)-2-naphthamide Drug Info Ki = 110 nM [528639]
6-Chloro-1,2,3,4-tetrahydro-pyrazino[1,2-a]indole Drug Info Ki = 330 nM [526235]
VER-5384 Drug Info Ki = 112 nM [527037]
1-((S)-2-aminopropyl)-1H-indazol-6-ol Drug Info IC50 = 0.58 nM [527952]
A-80426 Drug Info Ki = 144 nM [527799]
(+/-)-nantenine Drug Info Ki = 832 nM [530558]
1-((S)-2-aminopropyl)-7-iodo-1H-indazol-6-ol Drug Info IC50 = 1.68 nM [527952]
(2S)-1-(6-methoxy-1H-indazol-1-yl)propan-2-amine Drug Info IC50 = 1.91 nM [527952]
3-(2-Dimethylamino-ethyl)-1-methyl-1H-indol-4-ol Drug Info Ki = 900 nM [527668]
1-((S)-2-aminopropyl)-7-fluoro-1H-indazol-6-ol Drug Info IC50 = 0.73 nM [527952]
3-(2-Dimethylamino-ethyl)-2-methyl-1H-indol-4-ol Drug Info Ki = 122 nM [527668]
1-((S)-2-aminopropyl)-7-chloro-1H-indazol-6-ol Drug Info IC50 = 0.54 nM [527952]
6,7-dichloro-2,3,4,5-tetrahydro-1H-3-benzazepine Drug Info Ki = 93 nM [529221]
(S)-1-(5,6-difluoro-1H-indol-1-yl)propan-2-amine Drug Info Ki = 100 nM
1-Methyl-1,3-dihydro-indol-2-one Drug Info Ki = 25 nM [526055]
(R,S)-1-(5-fluoro-1H-indol-1-yl)propan-2-amine Drug Info Ki = 159 nM
References
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Ref 528294J Med Chem. 2006 Jul 13;49(14):4269-74.C-(4,5,6-trimethoxyindan-1-yl)methanamine: a mescaline analogue designed using a homology model of the 5-HT2A receptor.
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