Target Validation Information
TTD ID T92609
Target Name Adrenergic receptor alpha-1A (ADRA1A)
Type of Target
Successful
Drug Potency against Target Dutasteride + tamsulosin Drug Info IC50 = 6 nM [31]
(+/-)-nantenine Drug Info Ki = 2 nM [14]
(-)-SNAP-5399 Drug Info Ki = 0.4 nM [7]
(2,6-Dichloro-phenyl)-(1H-imidazol-2-yl)-amine Drug Info Ki = 6000 nM [27]
(2-Bromo-phenyl)-(1H-imidazol-2-yl)-amine Drug Info Ki = 11000 nM [27]
1',2',3',6'-Tetrahydro-[2,4']bipyridinyl Drug Info Ki = 4000 nM [19]
1-(2-Chloro-phenyl)-piperazine Drug Info Ki = 710 nM [9]
1-(2-Methoxy-phenyl)-piperazine Drug Info Ki = 3508 nM [9]
1-(3-Fluoro-pyridin-2-yl)-4-methyl-piperazine Drug Info Ki = 490 nM [19]
1-(pyridin-2-yl)piperazine Drug Info Ki = 2400 nM [19]
2-(4-tert-Butyl-phenyl)-4,5-dihydro-1H-imidazole Drug Info Ki = 91 nM [6]
2-Pyridin-4-yl-1,2,3,4-tetrahydro-isoquinoline Drug Info Ki = 5800 nM [2]
4-((E)-1-Naphthalen-1-yl-propenyl)-1H-imidazole Drug Info Ki = 387 nM [26]
4-((Z)-1-Naphthalen-1-yl-propenyl)-1H-imidazole Drug Info Ki = 57 nM [26]
4-(1-Naphthalen-1-yl-ethyl)-1H-imidazole Drug Info Ki = 536 nM [24]
4-(1-Naphthalen-1-yl-propyl)-1H-imidazole Drug Info Ki = 574 nM [26]
4-(1-Naphthalen-1-yl-vinyl)-1H-imidazole Drug Info Ki = 1734 nM [26]
4-(2,3-Dihydro-1H-phenalen-1-yl)-1H-imidazole Drug Info Ki = 55 nM [26]
4-(3,4-Dihydro-1H-isoquinolin-2-yl)-quinoline Drug Info Ki = 3200 nM [2]
4-(3-Hydroxy-piperidin-3-yl)-benzene-1,2-diol Drug Info Ki = 15000 nM [4]
4-(4-butylpiperidin-1-yl)-1-o-tolylbutan-1-one Drug Info Ki = 18 nM [15]
4-(4-Isopropyl-morpholin-2-yl)-benzene-1,2-diol Drug Info Ki = 6700 nM [4]
4-(4-Methyl-indan-1-yl)-1H-imidazole Drug Info Ki = 73 nM [29]
4-Benzo[b]thiophen-4-yl-1H-imidazole Drug Info Ki = 343 nM [1]
4-Morpholin-2-yl-benzene-1,2-diol Drug Info Ki = 7400 nM [4]
5-Bromo-8-piperazin-1-yl-imidazo[1,2-a]pyrazine Drug Info Ki = 1490 nM [5]
8-Piperazin-1-yl-imidazo[1,2-a]pyrazine Drug Info Ki = 3100 nM [5]
A-119637 Drug Info Ki = 2.6 nM [7]
A-123189 Drug Info Ki = 4.2 nM [7]
A-131701 Drug Info Ki = 0.22 nM [7]
A-315456 Drug Info Ki = 490 nM [7]
AGN-192172 Drug Info Ki = 8900 nM
AGN-193080 Drug Info Ki = 470 nM
AR-129330 Drug Info IC50 = 300 nM [13]
BMY-7378 Drug Info Ki = 290 nM [8]
BP-897 Drug Info Ki = 33 nM [3]
CORYNANTHEINE Drug Info Ki = 29 nM [7]
FLUANISONE Drug Info Ki = 0.87 nM [18]
Imidazolidin-2-ylidene-o-tolyl-amine Drug Info Ki = 2500 nM
Imidazolidin-2-ylidene-quinoxalin-6-yl-amine Drug Info Ki = 11000 nM
ISOCLOZAPINE Drug Info IC50 = 64 nM [30]
L-765314 Drug Info Ki = 420 nM [7]
L-771688 Drug Info Ki = 0.36 nM [7]
LEVONORDEFRIN Drug Info Ki = 9221 nM [26]
MAZAPERTINE Drug Info Ki = 0.2 nM [23]
MEDETOMIDINE Drug Info Ki = 1102 nM [24]
N-(5-Bromo-quinoxalin-6-yl)-guanidine Drug Info Ki = 17000 nM
NAFTOPIDIL Drug Info Ki = 3.7 nM [7]
NIGULDIPINE Drug Info Ki = 1.8 nM [20]
OCTOCLOTHEPIN Drug Info Ki = 0.66 nM [16]
R-226161 Drug Info Ki = 125 nM [11]
REC-15-2739 Drug Info Ki = 1 nM [7]
Ro-11-04253 Drug Info Ki = 5 nM [7]
RS-100329 Drug Info Ki = 0.25 nM [7]
RS-100975 Drug Info Ki = 1.3 nM [7]
RS-513815 Drug Info Ki = 41 nM [7]
RWJ-25730 Drug Info Ki = 8.2 nM [23]
RWJ-38063 Drug Info Ki = 9.3 nM [7]
RWJ-68141 Drug Info Ki = 59 nM [7]
RWJ-68157 Drug Info Ki = 22 nM [7]
RWJ-69736 Drug Info Ki = 0.65 nM [7]
Siramesine Drug Info IC50 = 330 nM [22]
SK&F-104078 Drug Info Ki = 33 nM [20]
SK&F-104856 Drug Info Ki = 36 nM [20]
SK&F-105854 Drug Info Ki = 3300 nM [7]
SK&F-106686 Drug Info Ki = 58 nM [20]
SK&F-86466 Drug Info Ki = 449 nM [20]
SNAP-5036 Drug Info Ki = 4.4 nM [7]
SNAP-5089 Drug Info Ki = 1.3 nM [20]
SNAP-6201 Drug Info Ki = 0.2 nM [7]
SNAP-7915 Drug Info Ki = 0.17 nM [7]
SNAP-8719 Drug Info Ki = 1400 nM [8]
SNAP-94847 Drug Info Ki = 180 nM [12]
Sunepitron Drug Info Ki = 35 nM [10]
TIOSPIRONE Drug Info Ki = 1.5 nM [25]
UH-301 Drug Info Ki = 6080 nM [28]
WB-4101 Drug Info Ki = 0.35 nM [21]
[3H]RX821002 Drug Info Ki = 27 nM [17]
[3H]spiperone Drug Info Ki = 7.9 nM [7]
Action against Disease Model Alfuzosin Drug Info Alfuzosin significantly prolonged action potential duration (APD)(60) in rabbit Purkinje fibers (p < 0.05) and QT in isolated rabbit hearts (p < 0.05) at the clinically relevantconcentration of 300 nM. In man, the QT interval corrected with Fridericia's formula increased 7.7 ms, which exceeds the 5.0-ms threshold for a positive TCQS. Effects on hK(v)11.1, hK(v)4.3, and hK(v)7.1/hKCNE1 potassi uM currents and calci uM current were not involved. At 300 nM, approximately 30x C(max), alfuzosin significantly increased whole-cell peak sodi uM (hNa(v)1.5) current (p < 0.05), increased the probability of late hNa(v)1.5 single-channel openings, and significantly shortened the slow time constant for recovery from inactivation. [32]
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