General Information of the Protein
Protein ID
PT01195
Protein Name
D(1A) dopamine receptor
Secondarily
Protein Name
Dopamine D1 receptor
Gene Name
DRD1
Sequence
MRTLNTSAMDGTGLVVERDFSVRILTACFLSLLILSTLLGNTLVCAAVIRFRHLRSKVTNFFVISLAVSDLLVAVLVMPWKAVAEIAGFWPFGSFCNIWVAFDIMCSTASILNLCVISVDRYWAISSPFRYERKMTPKAAFILISVAWTLSVLISFIPVQLSWHKAKPTSPSDGNATSLAETIDNCDSSLSRTYAISSSVISFYIPVAIMIVTYTRIYRIAQKQIRRIAALERAAVHAKNCQTTTGNGKPVECSQPESSFKMSFKRETKVLKTLSVIMGVFVCCWLPFFILNCILPFCGSGETQPFCIDSNTFDVFVWFGWANSSLNPIIYAFNADFRKAFSTLLGCYRLCPATNNAIETVSINNNGAAMFSSHHEPRGSISKECNLVYLIPHAVGSSEDLKKEEAAGIARPLEKLSPALSVILDYDTDVSLEKIQPITQNGQHPT
    Show/Hide
Organism
Homo sapiens, Human
Protein Classification
Membrane receptor
>
Family A G protein-coupled receptor
>
Small molecule receptor (family A GPCR)
>
Monoamine receptor
>
Dopamine receptor
Function
Dopamine receptor whose activity is mediated by G proteins which activate adenylyl cyclase.
    Show/Hide
Uniprot ID
Primary ID:
P21728

Secondarily ID:
B2RA44
Q4QRJ0
    Show/Hide
HGNC ID
HGNC:3020
Subcellular Location
Cell membrane
Endoplasmic reticulum membrane
Cell projection
Cilium membrane
Cell projection
Dendrite
Cell projection
Dendritic spine
Map of Molecular Bioactivity Related to the Protein
Map of Molecular Bioactivity Related to the Protein

Protein
Cell Line
Compound

Bioactivity Value:

<= 0.1 μM
> 0.1 μM and <= 10 μM
> 10 μM
Imprecise Activity
Table of Molecular Bioactivities Related to the Protein
Cell Line ID: CL000053 , COS-7
Compound ID Compound Name Compound Formula
CP0036551
9-chloranyl-5-(4-hydroxyphenyl)-2,3,4,5-tetrahydro-1H-3-benzazepine-7,8-diol;methanesulfonic acid
   Show/Hide
C16H16ClNO3
 1
1
Kd = 28 nM
   TI
   LI
   LO
   TS
CP0087918
(R)-1-phenyl-2,3,4,5-tetrahydro-1H-benzo[d]azepine-7,8-diol
   Show/Hide
C16H17NO2
 1
1
Kd = 150 nM
   TI
   LI
   LO
   TS
CP0232734
(R)-3-Allyl-6-bromo-7,8-dihydroxy-1-phenyl-2,3,4,5-tetrahydro-1H-benzo[d]azepinium
   Show/Hide
C19H20BrNO2
 1
1
Kd = 384 nM
   TI
   LI
   LO
   TS
CP0042751
(6aR)-6-methyl-5,6,6a,7-tetrahydro-4H-dibenzo[de,g]quinoline-10,11-diol;hydrate;hydrochloride
   Show/Hide
C17H17NO2
 1
1
Kd = 680 nM
   TI
   LI
   LO
   TS
CP0118587
6-Propyl-5,6,6a,7-tetrahydro-4H-dibenzo[de,g]quinoline-10,11-diol; hydrochloride
   Show/Hide
C19H21NO2
 1
1
Kd = 1816 nM
   TI
   LI
   LO
   TS
CP0658310
SID124880138
   Show/Hide
C16H16ClNO3
 1
1
Kd = 1818 nM
   TI
   LI
   LO
   TS
CP0036921
3-HYDROXYTYRAMINE HYDROCHLORIDE
   Show/Hide
C8H11NO2
 1
1
Kd = 2500 nM
   TI
   LI
   LO
   TS
CP0699735
(6,7-Dihydroxy-1,2,3,4-tetrahydro-naphthalen-2-yl)-dimethyl-ammonium
   Show/Hide
C12H17NO2
 1
1
Kd = 4600 nM
   TI
   LI
   LO
   TS
CP0001238
14C-5-hydroxy tryptamine creatinine disulfate
   Show/Hide
C10H12N2O
 1
1
Kd = 9690 nM
   TI
   LI
   LO
   TS
CP0039930
(-)-arterenol
   Show/Hide
C8H11NO3
 1
1
Kd = 50000 nM
   TI
   LI
   LO
   TS
CP0042352
2,3-bis(oxidanyl)butanedioic acid;4-[(1R)-2-(methylamino)-1-oxidanyl-ethyl]benzene-1,2-diol
   Show/Hide
C9H13NO3
 1
1
Kd = 55000 nM
   TI
   LI
   LO
   TS
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0064183
4-[3-methyl-4-(6-methylimidazo[1,2-a]pyrazin-5-yl)phenoxy]furo[3,2-c]pyridine
   Show/Hide
C21H16N4O2
 1
1 EC50 = 17 nM
CP0240209
4-[3-methyl-4-(2-methylimidazo[4,5-c]pyridin-1-yl)phenoxy]furo[3,2-c]pyridine
   Show/Hide
C21H16N4O2
 1
1 EC50 = 153 nM
CP0113847
(+/-)-SKF-38393
   Show/Hide
C16H17NO2
 1
1 EC50 = 247.5 nM
CP0177109
4-[4-(2-methylpyrazol-3-yl)phenoxy]furo[3,2-c]pyridine
   Show/Hide
C17H13N3O2
 1
1 EC50 = 2519 nM
CP0680677
(R)-8-chloro-3-methyl-5-phenyl-2,3,4,5-tetrahydro-1H-benzo[d]azepin-7-ol maleate
   Show/Hide
C21H22ClNO5
 3
1 IC50 = 0.22 nM
2 IC50 = 0.27 nM
3 Ki = 0.11 nM
CP0046341
8-Chloro-3-methyl-5-phenyl-2,3,4,5-tetrahydro-1H-benzo[d]azepin-7-ol(SCH 23390)
   Show/Hide
C17H18ClNO
 10
1 IC50 = 0.66 nM
2 IC50 = 0.74 nM
3 IC50 = 0.82 nM
4 IC50 = 0.96 nM
5 Ki = 0.11 nM
6 Ki = 0.2 nM
7 Ki = 0.3 nM
8 Ki = 0.38 nM
9 Ki = 0.4266 nM
10 Ki = 1.4 nM
CP0385103
CAS_87075-17-0
   Show/Hide
C17H18ClNO
 1
1 IC50 = 740 nM
CP0272712
(13aS)-3,9,11-trimethoxy-6,8,13,13a-tetrahydro-5H-isoquinolino[2,1-b]isoquinolin-2-ol
   Show/Hide
C20H23NO4
 1
1 IC50 = 1400 nM
CP0272711
US9359372, DC037030
   Show/Hide
C20H23NO4
 1
1 IC50 = 1900 nM
CP0059819
11-methyl-11-aza-tricyclo[12.4.0.0.3,8]octadeca-1(18),3(8),4,6,14,16-hexaen-6-ol
   Show/Hide
C18H21NO
 3
1 Ki = 0.3548 nM
2 Ki = 0.39 nM
3 Ki = 0.4 nM
CP0338716
1-Chloro-2-hydroxy-7-methyl-5,6,7,8,9,14-hexahydrodibenzo[d,g]azecine
   Show/Hide
C18H20ClNO
 1
1 Ki = 0.46 nM
CP0298952
7-methyl-6,7,8,9,14,15-hexahydro-5H-indolo[3,2-f][3]benzazecin-11-ol
   Show/Hide
C20H22N2O
 1
1 Ki = 0.5623 nM
CP0165743
4-Chloro-3-hydroxy-7-methyl-5,6,7,8,9,14-hexahydrodibenzo[d,g]azecine
   Show/Hide
C18H20ClNO
 2
1 Ki = 0.8128 nM
2 Ki = 0.83 nM
CP0046343
(6aS,13bR)-11-Chloro-7-methyl-5,6a,7,8,9,13b-hexahydro-6H-7-aza-benzo[6,7]cyclohepta[1,2-a]naphthalen-12-ol
   Show/Hide
C19H20ClNO
 3
1 Ki = 0.9 nM
2 Ki = 1.2 nM
3 Ki = 1.9 nM
CP0118587
6-Propyl-5,6,6a,7-tetrahydro-4H-dibenzo[de,g]quinoline-10,11-diol; hydrochloride
   Show/Hide
C19H21NO2
 3
1 Ki = 1 nM
2 Ki = 490 nM
3 Ki = 1510 nM
CP0087918
(R)-1-phenyl-2,3,4,5-tetrahydro-1H-benzo[d]azepine-7,8-diol
   Show/Hide
C16H17NO2
 3
1 Ki = 1 nM
2 Ki = 73 nM
3 Ki = 320 nM
CP0082972
11-methyl-11,21-diazatetracyclo[12.7.0.0^{3,8}.0^{15,20}]henicosa-1(14),3(8),4,6,15,17,19-heptaene
   Show/Hide
C20H22N2
 3
1 Ki = 1.862 nM
2 Ki = 1.9 nM
3 Ki < 10 nM
CP0099064
3,11-Dihydroxy-7-methyl-5,6,7,8,9,14-hexahydrodibenzo[d,g]azecine
   Show/Hide
C18H21NO2
 1
1 Ki = 2 nM
CP0037230
8-methyl-5,6,7,8,9,10,15,16-octahydroindolo[3,2-g][4]benzazacycloundecine
   Show/Hide
C21H24N2
 1
1 Ki = 2.042 nM
CP0232734
(R)-3-Allyl-6-bromo-7,8-dihydroxy-1-phenyl-2,3,4,5-tetrahydro-1H-benzo[d]azepinium
   Show/Hide
C19H20BrNO2
 1
1 Ki = 3 nM
CP0059813
3-Chloro-2-hydroxy-7-methyl-5,6,7,8,9,14-hexahydrodibenzo[d,g]azecine
   Show/Hide
C18H20ClNO
 1
1 Ki = 3.1 nM
CP0059816
2,4-dichloro-3-hydroxy-7-methyl-5,6,7,8,9,14-hexahydrodibenzo[d,g]azecine
   Show/Hide
C18H19Cl2NO
 1
1 Ki = 3.2 nM
CP0175178
11-methyl-11-aza-tricyclo[12.4.0.03,8]octadeca-1(18),3(8),4,6,14,16-hexaene
   Show/Hide
C18H21N
 2
1 Ki = 3.467 nM
2 Ki = 4.5 nM
CP0074631
6-methyl-4,5,6,7,8,13-hexahydrothieno[2,3-f][3]benzazecine
   Show/Hide
C16H19NS
 1
1 Ki = 4 nM
CP0042751
(6aR)-6-methyl-5,6,6a,7-tetrahydro-4H-dibenzo[de,g]quinoline-10,11-diol;hydrate;hydrochloride
   Show/Hide
C17H17NO2
 2
1 Ki = 4.6 nM
2 Ki = 650 nM
CP0008601
4-[4-(4-Chloro-phenyl)-4-hydroxy-piperidin-1-yl]-1-(4-fluoro-phenyl)-butan-1-one;propionate(HCl)
   Show/Hide
C21H23ClFNO2
 6
1 Ki = 6.166 nM
2 Ki = 49 nM
3 Ki = 82 nM
4 Ki = 107 nM
5 Ki = 120 nM
6 Ki = 270 nM
CP0037328
(6aR,12bS)-10,11-Dihydroxy-5,6,6a,7,8,12b-hexahydro-benzo[a]phenanthridinium
   Show/Hide
C17H17NO2
 2
1 Ki = 6.2 nM
2 Ki = 1200 nM
CP0044469
(1S)-16-methoxy-5,7-dioxa-13-azapentacyclo[11.8.0.02,10.04,8.015,20]henicosa-2,4(8),9,15(20),16,18-hexaen-17-ol
   Show/Hide
C19H19NO4
 1
1 Ki = 6.5 nM
CP0025667
2-[4-(4-Methyl-benzyl)-piperazin-1-yl]-1-(2-methyl-2,3-dihydro-indol-1-yl)-ethanone
   Show/Hide
C18H19ClN4
 9
1 Ki = 7.5 nM
2 Ki = 21.38 nM
3 Ki = 31.62 nM
4 Ki = 44 nM
5 Ki = 53 nM
6 Ki = 180 nM
7 Ki = 290 nM
8 Ki = 540 nM
9 Ki = 1000 nM
CP0059820
1-methoxy-7-methyl-5,6,7,8,9,14-hexahydrodibenzo[d,g]azecine
   Show/Hide
C19H23NO
 1
1 Ki = 7.6 nM
CP0059821
1-Hydroxy-7-methyl-5,6,7,8,9,14-hexahydrodibenzo[d,g]azecine
   Show/Hide
C18H21NO
 1
1 Ki = 8.7 nM
CP0155138
2-Hydroxy-7-methyl-5,6,7,8,9,14-hexahydrodibenzo[d,g]azecine
   Show/Hide
C18H21NO
 1
1 Ki = 8.9 nM
CP0162167
2-Amino-3-hydroxy-7-methyl-5,6,7,8,9,14-hexahydrodibenzo[d,g]azecine
   Show/Hide
C18H22N2O
 1
1 Ki = 9.3 nM
CP0186639
3,11-Dimethoxy-7-methyl-5,6,7,8,9,14-hexahydrodibenzo[d,g]azecine
   Show/Hide
C20H25NO2
 1
1 Ki = 9.4 nM
CP0045063
2-methyl-4-(4-methylpiperazin-1-yl)-10H-thieno[2,3-b][1,5]benzodiazepine
   Show/Hide
C17H20N4S
 6
1 Ki = 10 nM
2 Ki = 47 nM
3 Ki = 52 nM
4 Ki = 100 nM
5 Ki = 119 nM
6 Ki = 250 nM
CP0258036
5-(2-chlorophenyl)-8-methoxy-3-methyl-1,2,4,5-tetrahydro-3-benzazepin-7-ol
   Show/Hide
C18H20ClNO2
 1
1 Ki = 14 nM
CP0040242
16-methoxy-11-methyl-11-aza-tricyclo[12.4.0.03,8]octadeca-1(18),3(8),4,6,14,16-hexaene
   Show/Hide
C19H23NO
 2
1 Ki = 22.91 nM
2 Ki = 28.5 nM
CP0141367
1,3-Dichloro-2-methoxy-7-methyl-5,6,7,8,9,14-hexahydrodibenzo[d,g]azecine
   Show/Hide
C19H21Cl2NO
 1
1 Ki = 25.3 nM
CP0263495
(5R)-9-chloro-5-phenyl-2,3,4,5-tetrahydro-1H-3-benzazepine-7,8-diol
   Show/Hide
C16H16ClNO2
 1
1 Ki = 30 nM
CP0036551
9-chloranyl-5-(4-hydroxyphenyl)-2,3,4,5-tetrahydro-1H-3-benzazepine-7,8-diol;methanesulfonic acid
   Show/Hide
C16H16ClNO3
 1
1 Ki = 40 nM
CP0181209
(-)-Tetrahydroberberine
   Show/Hide
C20H21NO4
 1
1 Ki = 48.6 nM
CP0059815
2-methoxy-7-methyl-5,6,7,8,9,14-hexahydrodibenzo[d,g]azecine
   Show/Hide
C19H23NO
 1
1 Ki = 82 nM
CP0061859
(+/-)-2,3-dihydroxy-6a,7,8,12b-tetrahydro-6H-chromeno[3,4-c]isoquinoline
   Show/Hide
C16H15NO3
 1
1 Ki = 98 nM
CP0169939
(-)-Corydalmine
   Show/Hide
C20H23NO4
 1
1 Ki = 107 nM
CP0127660
7-methyl-5,6,7,8,9,10,15,16-octahydroindolo[3,2-g][3]benzazacycloundecine
   Show/Hide
C21H24N2
 1
1 Ki = 158.49 nM
CP0036921
3-HYDROXYTYRAMINE HYDROCHLORIDE
   Show/Hide
C8H11NO2
 2
1 Ki = 192 nM
2 Ki = 18200 nM
CP0126302
(13aS)-2,9,10-trimethoxy-6,8,13,13a-tetrahydro-5H-isoquinolino[2,1-b]isoquinolin-3-ol
   Show/Hide
C20H23NO4
 1
1 Ki = 199 nM
CP0315086
3-chloro-6-(1-methyl-3,6-dihydro-2H-pyridin-4-yl)-11H-benzo[b][1,4]benzodiazepine
   Show/Hide
C19H18ClN3
 1
1 Ki = 380 nM
CP0078330
7-[4-[4-(2,3-dichlorophenyl)-1,4-diazepan-1-yl]butoxy]-3,4-dihydro-1H-quinolin-2-one
   Show/Hide
C24H29Cl2N3O2
 1
1 Ki = 825 nM
CP0042927
7-{4-[4-(2,3-dichlorophenyl)piperazin-1-yl]butoxy}-3,4-dihydroquinolin-2(1H)-one
   Show/Hide
C23H27Cl2N3O2
 2
1 Ki = 895 nM
2 Ki = 1000 nM
CP0045034
N-[4-[4-(2-methoxyphenyl)piperazin-1-yl]butyl]pyrazolo[1,5-a]pyridine-2-carboxamide
   Show/Hide
C23H29N5O2
 1
1 Ki = 1500 nM
CP0050995
(6aR)-6-propyl-5,6,6a,7-tetrahydro-4H-dibenzo[de,g]quinolin-11-ol
   Show/Hide
C19H21NO
 1
1 Ki = 4300 nM
CP0699735
(6,7-Dihydroxy-1,2,3,4-tetrahydro-naphthalen-2-yl)-dimethyl-ammonium
   Show/Hide
C12H17NO2
 1
1 Ki = 5400 nM
CP0038689
(4aS,5R,10bR)-5-phenyl-1,2,3,4,4a,5,6,10b-octahydrobenzo[h]isoquinoline-7,8-diol
   Show/Hide
C19H21NO2
 1
1 Ki = 18000 nM
Clinical Information about the Protein
Target 1 ( Dopamine D1 receptor (D1R) )
Target Type Successful Target
Disease 8 Target-related Diseases  8
1 Hypertension [ICD-11: BA00-BA04]
2 Spontaneous abortion [ICD-11: JA00.0]
3 Parkinson disease [ICD-11: 8A00.0]
4 Allergy [ICD-11: 4A80-4A85]
5 Cocaine addiction [ICD-11: 6C45.2]
6 Schizophrenia [ICD-11: 6A20]
7 Pain [ICD-11: MG30-MG3Z]
8 Type-2 diabetes [ICD-11: 5A11]
Approved Drug(s) 4 Approved Drugs  4
1 Fenoldopam Approved
Hypertension
2 Methylergonovine Approved
Spontaneous abortion
3 Pergolide Approved
Parkinson disease
4 Phenyltoloxamine Approved
Allergy
Clinical Trial Drug(s) 2 Clinical Trial Drugs  2
1 Ecopipam Phase 3
Cocaine addiction
2 Zicronapine Phase 3
Schizophrenia
Discontinued Drug(s) 5 Discontinued Drugs  5
1 CY-208243 Discontinued in Phase 2
Pain
2 A 77636 Terminated
Parkinson disease
3 A-68930 Terminated
Hypertension
4 SKF 38393 Terminated
Type-2 diabetes
5 SKF-81297 Terminated
Parkinson disease
Similar Protein(s) and Bioactivity Statistics
50% Identity
Protein ID Protein Name Protein Organism
PT04612 D(1B) dopamine receptor Rattus norvegicus, Rat
PT07597 D(1B) dopamine receptor Mus musculus, Mouse