Therapeutic Targets Database
BIDD Pharmainformatics Databases
 
   
 

 

Target Validation Information
TTD IDTTDS00103
Target Name5-hydroxytryptamine 2A receptor    
Type of TargetSuccessful target    
Drug Potency against TargetIloperidoneKI = 11 nM[1]
AsenapineKi = 0.07 nM[2]
OcaperidoneKi = 0.14 nM[3]
SR46349BKi = 1.26 nM[4]
SR46349BKi = 1.3 nM[5]
Abaperidone hydrochlorideKi = 1.9 nM[6]
FlibanserinKi = 125.9 nM[7]
Lurasidone hydrochlorideKi = 2.03 nM[8]
FlibanserinKi = 49 nM[9]
BlonanserinKi = 5460 nM[10]
AdatanserinKi = 73 nM[11]
PimavanserinKi = 8 nM[5]
LY367265Ki = 0.81 nM[12]
YM-992Ki = 21 nM[12]
1192U90Ki = 3.3 nM[13]
YM-992Ki = 86 nM[14]
(R)-1-(4-iodo-2,5-dimethoxyphenyl)propan-2-amineIC50 = 0.46 nM[15]
1-((S)-2-aminopropyl)-7-chloro-1H-indazol-6-olIC50 = 0.54 nM[16]
1-((S)-2-aminopropyl)-1H-indazol-6-olIC50 = 0.58 nM[16]
1-((S)-2-aminopropyl)-7-fluoro-1H-indazol-6-olIC50 = 0.73 nM[16]
1-((S)-2-aminopropyl)-7-methyl-1H-indazol-6-olIC50 = 0.74 nM[16]
1-(2-aminoethyl)-1H-indazol-6-olIC50 = 0.77 nM[16]
MDL-28161IC50 = 0.9 nM[17]
1-((S)-2-aminopropyl)-7-iodo-1H-indazol-6-olIC50 = 1.68 nM[16]
(S)-2-(6-methoxyindazol-1-yl)-1-methylethylamineIC50 = 1.91 nM[16]
ISOCLOZAPINEIC50 = 12 nM[18]
5-methoxy-alpha-methyltryptamineIC50 = 2 nM[16]
1-((R)-2-aminopropyl)-1H-indazol-6-olIC50 = 2.08 nM[16]
EtisulergineIC50 = 26 nM[19]
5-hydroxy-alpha-methyltryptamineIC50 = 3.5 nM[16]
RP-68303IC50 = 30 nM[20]
SB-243213IC50 = 32.4 nM[21]
WAY-208466IC50 = 351 nM[22]
5-MEO-DMTIC50 = 9.53 nM[16]
4-(4-butylpiperidin-1-yl)-1-o-tolylbutan-1-oneKi < 1000 nM[23]
VOLINANSERINKi = 0.36 nM[24]
PRUVANSERINKi = 0.48 nM[25]
3-(1-Phenethyl-piperidin-4-yl)-2-phenyl-1H-indoleKi = 0.5 nM[26]
NELOTANSERINKi = 0.51 nM[25]
TIOSPIRONEKi = 0.58 nM[27]
4-(10H-Anthracen-9-ylidene)-1-methyl-piperidineKi = 0.7 nM[28]
ALTANSERINKi = 0.72 nM[24]
(2S)-1-(1H-furo[2,3-g]indazol-1-yl)propan-2-amineKi = 0.78 nM[29]
EMD-281014Ki = 0.87 nM[30]
2,5-dimethoxy-4-bromophenethylamineKi = 0.88 nM[31]
SPIPERONEKi = 1 nM[32]
(S)-1-(5,6-difluoro-1H-indol-1-yl)propan-2-amineKi = 100 nM[33]
DOMKi = 100 nM[34]
1-(4-ethyl-2,5-dimethoxyphenyl)propan-2-amineKi = 100 nM[34]
[2-(6-Methoxy-indol-1-yl)-ethyl]-dimethyl-amineKi = 1040 nM[35]
11-Hexanoyloxy-N-n-propylnoraporphineKi = 109 nM[36]
11-Propionyloxy-N-n-propylnoraporphineKi = 109 nM[36]
N-(1-(1-phenylethyl)piperidin-4-yl)-2-naphthamideKi = 110 nM[37]
4-(4-Fluoro-benzyl)-piperidine; hydrochlorideKi = 1100 nM[17]
1,2,3,4-Tetrahydro-naphthalen-2-ylamineKi = 11100 nM[38]
VER-5384Ki = 112 nM[39]
(S)-(-)-(4,5,6-trimethoxyindan-1-yl)methanamineKi = 1120 nM[40]
3-Naphthalen-1-yl-1-propyl-pyrrolidineKi = 113 nM[41]
11-Hydroxy-N-propylnoraporphineKi = 114 nM[36]
8-Bromo-4,9-dihydro-3H-beta-carbolineKi = 115 nM[42]
N,N-dimethyl-4,4-diphenylbutan-1-amineKi = 1151 nM[43]
1-methoxy-9-aminomethyl-9,10-dihydroanthraceneKi = 1158 nM[44]
5-chloro-3,4-dihydroquinazolin-2-amineKi = 1164 nM[45]
2-Phenyl-3-piperidin-4-yl-1H-indoleKi = 12.1 nM[26]
MDL-11939Ki = 12.5 nM[17]
8-Methoxy-2-(4-methyl-piperazin-1-yl)-quinolineKi = 1200 nM[38]
3-(2-Dimethylamino-ethyl)-2-methyl-1H-indol-4-olKi = 122 nM[46]
4-methoxy-9-aminomethyl-9,10-dihydroanthraceneKi = 124 nM[44]
SEROTONINKi = 1258 nM[47]
BrolamfetamineKi = 13 nM[48]
YM-348Ki = 13 nM[49]
1-(3-(phenylthio)propyl)-4-m-tolylpiperazineKi = 13.6 nM[50]
2-methoxy-9-aminomethyl-9,10-dihydroanthraceneKi = 1367 nM[44]
5-METHOXYTRYPTAMINEKi = 14 nM[51]
6-Methoxy-2,3,4,9-tetrahydro-1H-beta-carbolineKi = 1400 nM[42]
A-80426Ki = 144 nM[52]
N-methyl-3,3-diphenylpropan-1-amineKi = 1498 nM[43]
(R,S)-1-(5-bromo-1H-indol-1-yl)propan-2-amineKi = 159 nM[33]
(R,S)-1-(5-fluoro-1H-indol-1-yl)propan-2-amineKi = 159 nM[33]
1-(3-Trifluoromethyl-phenyl)-piperazineKi = 160 nM[53]
2-(1H-indol-3-yl)-N,N-dimethylethanamineKi = 1636 nM[34]
N,N-Dimethyl-3,3-diphenylpropan-1-amineKi = 1636 nM[43]
MAZAPERTINEKi = 165 nM[54]
PHENETHYLAMINEKi = 16820 nM[28]
C-(9H-Xanthen-9-yl)-methylamineKi = 170 nM[28]
N-3'-ethylaplysinopsinKi = 1700 nM[55]
2-Piperazin-1-yl-phenolKi = 17200 nM[53]
SB-271046Ki = 1740 nM[56]
1-Naphthalen-1-yl-piperazineKi = 18 nM[38]
Racemic DOIKi = 19 nM[34]
BARETTINKi = 1930 nM[57]
2-Phenyl-3-(2-piperidin-1-yl-ethyl)-1H-indoleKi = 2.7 nM[26]
ZOTEPINEKi = 2.7 nM[58]
1,6-bis(4-m-tolylpiperazin-1-yl)hexaneKi = 20 nM[59]
C-(9,10-Dihydro-anthracen-9-yl)-methylamineKi = 20 nM[28]
(R,S)-1-(5-chloro-1H-indol-1-yl)propan-2-amineKi = 200 nM[33]
6-bromoaplysinopsinKi = 2000 nM[55]
2-(4-Methyl-piperazin-1-yl)-4-phenyl-pyrimidineKi = 2095 nM[60]
2-(piperazin-1-yl)-5,6,7,8-tetrahydroquinolineKi = 21 nM[61]
8-Bromo-2,3,4,9-tetrahydro-1H-beta-carbolineKi = 21 nM[42]
2-(2-Amino-propyl)-5-bromo-4-methoxy-phenolKi = 210 nM[62]
PHENYLPIPERAZINEKi = 2100 nM[38]
N-(1-(4-phenylbutyl)piperidin-4-yl)-2-naphthamideKi = 213 nM[37]
7-Methoxy-2,3,4,9-tetrahydro-1H-beta-carbolineKi = 2200 nM[42]
N-(1-(4-bromobenzyl)piperidin-4-yl)-2-naphthamideKi = 223 nM[63]
1-Butyl-4-(2-methoxy-phenyl)-piperazineKi = 2280 nM[64]
1-(4-Bromo-2,5-dimethoxy-phenyl)-piperazineKi = 2430 nM[53]
N-(1-(1-phenylethyl)piperidin-4-yl)-1-naphthamideKi = 248 nM[37]
1-Methyl-1,3-dihydro-indol-2-oneKi = 25 nM[65]
1-(4-Bromo-2,5-difluorophenyl)-2-aminopropaneKi = 2505 nM[34]
(R,S)-1-(6-fluoro-1H-indol-1-yl)propan-2-amineKi = 251 nM[33]
5-chloro-N-(pyridin-3-yl)indoline-1-carboxamideKi = 2512 nM[33]
8-Methoxy-4,9-dihydro-3H-beta-carbolineKi = 2550 nM[42]
4,4-Diphenylbutan-1-amineKi = 2589 nM[43]
N-(1-(4-nitrobenzyl)piperidin-4-yl)-2-naphthamideKi = 278 nM[63]
1,6-bis(4-(3-methoxyphenyl)piperazin-1-yl)hexaneKi = 28 nM[59]
3-(1-Benzyl-piperidin-4-yl)-2-phenyl-1H-indoleKi = 28 nM[26]
LYSERGIC ACID DIETHYLAMIDEKi = 3.5 nM[40]
TRYPTOLINEKi = 3000 nM[42]
1,6-bis(4-phenylpiperazin-1-yl)hexaneKi = 31 nM[59]
VER-2692Ki = 31 nM[66]
1-Butyl-3-(2-dimethylamino-ethyl)-1H-indol-4-olKi = 310 nM[46]
8-Methoxy-2-piperazin-1-yl-quinolineKi = 310 nM[38]
1-Ethyl-4-(2-methoxy-phenyl)-piperazineKi = 3120 nM[64]
1-(10-Bromoanthracen-9-yl)-2-aminopropaneKi = 313 nM[34]
9-(2-aminopropyl)-9,10-dihydroanthraceneKi = 32 nM[43]
8-Chloro-1,2,3,4-tetrahydro-pyrazino[1,2-a]indoleKi = 320 nM[35]
PSILOCINKi = 323 nM[34]
1-(2-Methoxy-phenyl)-4-propyl-piperazineKi = 3290 nM[64]
Racemic DOTFMKi = 33 nM[34]
6-Chloro-1,2,3,4-tetrahydro-pyrazino[1,2-a]indoleKi = 330 nM[35]
[2-(4-Fluoro-1H-indol-3-yl)-ethyl]-dimethyl-amineKi = 335 nM[46]
1-(2-Methoxy-phenyl)-piperazineKi = 3500 nM[53]
1-(2,6-dimethoxy-4-methylphenyl)propan-2-amineKi = 351 nM[34]
VER-3323Ki = 351 nM[39]
4-Benzyl-1-methyl-piperidine; hydrochlorideKi = 3870 nM[17]
Ro-60-0175;Ro-600175Ki = 39 nM[29]
CINANSERINKi = 4 nM[51]
3-Naphthalen-1-yl-pyrrolidineKi = 40 nM[41]
8-Methoxy-2,3,4,9-tetrahydro-1H-beta-carbolineKi = 400 nM[42]
C-(5H-Dibenzo[a,d]cyclohepten-5-yl)-methylamineKi = 4125 nM[28]
N-(1-phenethylpiperidin-4-yl)-2-naphthamideKi = 42 nM[37]
GR-127935Ki = 42.7 nM[67]
3-(2-Pyrrolidin-1-yl-ethyl)-1H-indol-4-olKi = 429 nM[46]
5,6-dichloro-3,4-dihydroquinazolin-2-amineKi = 434 nM[45]
N-(1-benzylpiperidine-4-yl)-2-naphthamideKi = 44 nM[63]
1,6-bis(4-(pyridin-2-yl)piperazin-1-yl)hexaneKi = 45 nM[59]
L-745870Ki = 453 nM[68]
7,8,9,10-tetrahydro-6H-furo-[3,2-g][3]benzazepineKi = 46 nM[49]
N-(1-(3-bromobenzyl)piperidin-4-yl)-1-naphthamideKi = 462 nM[63]
2-(4-Bromo-phenyl)-1-methyl-ethylamineKi = 4650 nM[62]
C-(5-bromo-4,7-dimethoxyindan-1-yl)methylamineKi = 47 nM[31]
1-(2,5-Dimethoxy-4-methyl-phenyl)-piperazineKi = 4710 nM[53]
CHLOROPHENYLPIPERAZINEKi = 48 nM[69]
9-(2-aminoethyl)-9,10-dihydroanthraceneKi = 480 nM[43]
N-(1-(4-phenylbutyl)piperidin-4-yl)-1-naphthamideKi = 487 nM[37]
2-(4-Bromo-2-methoxy-phenyl)-1-methyl-ethylamineKi = 4870 nM[62]
3-Dimethylaminomethyl-1-methyl-1H-indol-4-olKi = 498 nM[46]
TRYPTAMINEKi = 50 nM[51]
5-Methoxy-4,9-dihydro-3H-beta-carbolineKi = 500 nM[42]
FLUANISONEKi = 52 nM[70]
1-(2,5-dimethoxyphenyl)propan-2-amineKi = 5200 nM[34]
N-(1-(3-bromobenzyl)piperidin-4-yl)-2-naphthamideKi = 53 nM[63]
VER-5593Ki = 53 nM[39]
N-(1-phenethylpiperidin-4-yl)-1-naphthamideKi = 543 nM[37]
MESCALINEKi = 5500 nM[34]
11-Butyryloxy-N-n-propylnoraporphineKi = 56 nM[36]
1-Propyl-3-(3-trifluoromethyl-phenyl)-pyrrolidineKi = 569 nM[41]
2,2-Diphenyl-ethylamineKi = 5700 nM[28]
3-(3-Dimethylamino-propyl)-1H-indol-4-olKi = 588 nM[46]
2-(3,5-dimethoxy-4-phenethoxyphenyl)ethanamineKi = 59 nM[34]
APLYSINOPSINKi = 598 nM[33]
PG-01037Ki = 62.4 nM[71]
1,2,3,4-Tetrahydro-pyrazino[1,2-a]indoleKi = 635 nM[35]
C-(9H-Thioxanthen-9-yl)-methylamineKi = 65 nM[28]
(2-Indol-1-yl-ethyl)-dimethyl-amineKi = 650 nM[35]
(R)-(+)-(4,5,6-trimethoxyindan-1-yl)methanamineKi = 69 nM[40]
(E)-2-(4-fluorostyryl)-5-(phenylsulfonyl)pyridineKi = 7.4 nM[72]
3-methoxy-9-aminomethyl-9,10-dihydroanthraceneKi = 7.5 nM[44]
(E)-2-(4-fluorostyryl)-5-(phenylsulfinyl)pyridineKi = 7.7 nM[72]
3-(1-Methyl-piperidin-4-yl)-2-phenyl-1H-indoleKi = 7.8 nM[26]
1-Naphthalen-2-yl-piperazineKi = 70 nM[38]
9-(N-benzylaminomethyl)-9,10-dihydroanthraceneKi = 721 nM[73]
N,N-dimethyl-2,2-diphenylethanamineKi = 7356 nM[43]
5-Methoxy-2,3,4,9-tetrahydro-1H-beta-carbolineKi = 75 nM[42]
N-methyl-4,4-diphenylbutan-1-amineKi = 754 nM[43]
3-(2-Dimethylamino-ethyl)-1H-indol-6-olKi = 7600 nM[46]
2-(3-Methoxy-phenyl)-1-methyl-ethylamineKi = 7850 nM[62]
(R,S)-1-(5-methyl-1H-indol-1-yl)propan-2-amineKi = 794 nM[33]
QUIPAZINEKi = 794 nM[47]
6-chloro-N-(pyridin-3-yl)indoline-1-carboxamideKi = 794 nM[33]
7-Chloro-1,2,3,4-tetrahydro-pyrazino[1,2-a]indoleKi = 80 nM[35]
5-Bromo-2,3,4,9-tetrahydro-1H-beta-carbolineKi = 80 nM[42]
2-(2-Methoxy-phenyl)-1-methyl-ethylamineKi = 8130 nM[62]
(2S)-1-(6-fluoro-1H-indazol-1-yl)propan-2-amineKi = 82 nM[29]
(+/-)-nantenineKi = 832 nM[74]
1-(2,5-Dimethoxy-phenyl)-piperazineKi = 8430 nM[53]
3-Amino-1-(2-amino-5-methoxy-phenyl)-propan-1-oneKi = 8480 nM[53]
(2S)-1-(5-fluoro-1H-indazol-1-yl)propan-2-amineKi = 89 nM[29]
(1-Phenethyl-piperidin-4-yl)-phenyl-methanoneKi = 9.6 nM[58]
3-(2-Dimethylamino-ethyl)-1-methyl-1H-indol-4-olKi = 900 nM[46]
11-valeryloxynoraporphineKi = 92 nM[36]
2-(9,10-dihydroanthracen-9-yl)-N-methylethanamineKi = 92 nM[43]
3-Dimethylaminomethyl-1H-indol-4-olKi = 923 nM[46]
6,7-dichloro-2,3,4,5-tetrahydro-1H-3-benzazepineKi = 93 nM[49]
11-Heptanoyloxy-N-n-propylnoraporphineKi = 95 nM[36]
(R)-3-(4-propylmorpholin-2-yl)phenolKi = 970 nM[75]
1,6-bis(4-(3-chlorophenyl)piperazin-1-yl)hexaneKi = 98 nM[59]
3-(2-Dimethylamino-propyl)-1H-indol-4-olKi = 982 nM[46]
7,8,9,10-tetrahydro-6H-furo-[2,3-g][3]benzazepineKi = 99 nM[49]
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