Co-Target(s) Information

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Target General Information
Co-Targets of This Target
References
Target General Information  Top
Target ID T02551 Target Info
Target Name Dopamine D3 receptor (D3R)
Synonyms
D(3) dopamine receptor
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Target Type Successful Target
Gene Name DRD3
Biochemical Class GPCR rhodopsin
UniProt ID
DRD3_HUMAN
Co-Targets of This Target  Top
Co-Target Name Dopamine D2 receptor (D2R) Successful Target
UniProt ID DRD2_HUMAN
Gene Name DRD2
Synonyms
Dopamine receptor 2; D(2) dopamine receptor
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Representative Drug(s) Cariprazine Drug Info EC50 = 0.4 nM Click to Show More [1]
2 Cariprazine Drug Info EC50 = 3 nM [1]
3 Ropinirole Drug Info Ki = 3.7 nM [4]
4 Pramipexole Drug Info Ki = 4.7 nM [5]
5 GSK598809 Drug Info Ki = 251.19 nM [7]
Co-Target Name Dopamine D4 receptor (D4R) Successful Target
UniProt ID DRD4_HUMAN
Gene Name DRD4
Synonyms
DRD4; D(2C)D(4) dopamine receptor dopamine receptor
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Representative Drug(s) Pramipexole Drug Info Ki = 0.49 nM Click to Show More [2]
2 Ropinirole Drug Info Ki = 7.8 nM [4]
3 Cariprazine Drug Info Ki = 110 nM [6]
Co-Target Name 5-HT 1A receptor (HTR1A) Successful Target
UniProt ID 5HT1A_HUMAN
Gene Name HTR1A
Synonyms
Serotonin receptor 1A; G-21; ADRBRL1; ADRB2RL1; 5-hydroxytryptamine receptor 1A; 5-HT1A receptor; 5-HT1A; 5-HT-1A
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Representative Drug(s) Cariprazine Drug Info Ki = 2.6 nM [3]
Co-Target Name 5-HT 2A receptor (HTR2A) Successful Target
UniProt ID 5HT2A_HUMAN
Gene Name HTR2A
Synonyms
Serotonin receptor 2A; HTR2; 5-hydroxytryptamine receptor 2A; 5-HT-2A; 5-HT-2
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Representative Drug(s) Cariprazine Drug Info Ki = 18.8 nM [3]
Co-Target Name Adrenergic receptor alpha-2C (ADRA2C) Successful Target
UniProt ID ADA2C_HUMAN
Gene Name ADRA2C
Synonyms
Subtype C4; Alpha-2CAR; Alpha-2C adrenoreceptor; Alpha-2C adrenoceptor; Alpha-2C adrenergic receptor; Alpha-2 adrenergic receptor subtype C4; ADRA2RL2; ADRA2L2
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Representative Drug(s) Pramipexole Drug Info Ki = 52.2 nM [5]
Co-Target Name Adrenergic receptor alpha-2B (ADRA2B) Successful Target
UniProt ID ADA2B_HUMAN
Gene Name ADRA2B
Synonyms
Subtype C2; Alpha-2BAR; Alpha-2B adrenoreceptor; Alpha-2B adrenoceptor; Alpha-2B adrenergic receptor; Alpha-2 adrenergic receptor subtype C2; ADRA2RL1; ADRA2L1
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Representative Drug(s) Pramipexole Drug Info Ki = 67.7 nM [5]
Co-Target Name Adrenergic receptor alpha-2A (ADRA2A) Successful Target
UniProt ID ADA2A_HUMAN
Gene Name ADRA2A
Synonyms
Alpha-2AAR; Alpha-2A adrenoreceptor; Alpha-2A adrenoceptor; Alpha-2A adrenergic receptor; Alpha-2 adrenergic receptor subtype C10; ADRAR; ADRA2R
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Representative Drug(s) Pramipexole Drug Info Ki = 75.7 nM [5]
Co-Target Name Voltage-gated potassium channel Kv11.1 (KCNH2) Successful Target
UniProt ID KCNH2_HUMAN
Gene Name KCNH2
Synonyms
hERG1; hERG-1; Voltage-gated potassium channel subunit Kv11.1; Potassium voltage-gated channel subfamily H member 2; HERG K+ channel; HERG; H-ERG; Ether-a-go-go-related protein 1; Ether-a-go-go-related gene potassium channel 1; Ether-a-go-go related protein 1; Ether-a-go-go related gene potassium channel 1; Eag related protein 1; Eag homolog; ERG-1; ERG
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Representative Drug(s) GSK598809 Drug Info IC50 = 460 nM [7]
Co-Target Name 5-HT 7 receptor (HTR7) Clinical trial Target
UniProt ID 5HT7R_HUMAN
Gene Name HTR7
Synonyms
Serotonin receptor 7; 5HT7; 5-hydroxytryptamine receptor 7; 5-HT7 receptor; 5-HT7; 5-HT-X; 5-HT-7
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Representative Drug(s) Cariprazine Drug Info Ki = 111 nM [3]
References  Top
REF 1 D 2 Dopamine Receptor G Protein-Biased Partial Agonists Based on Cariprazine. J Med Chem. 2019 May 9;62(9):4755-4771.
REF 2 Thiazoloindans and thiazolobenzopyrans: a novel class of orally active central dopamine (partial) agonists. J Med Chem. 2000 Sep 21;43(19):3549-57.
REF 3 Synthesis and biological evaluation of new multi-target 3-(1H-indol-3-yl)pyrrolidine-2,5-dione derivatives with potential antidepressant effect. Eur J Med Chem. 2019 Dec 1;183:111736.
REF 4 Investigation of novel ropinirole analogues: synthesis, pharmacological evaluation and computational analysis of dopamine D2 receptor functionalized congeners and homobivalent ligands. Medchemcomm. 2014;5:891-8.
REF 5 Discovery, Optimization, and Characterization of ML417: A Novel and Highly Selective D 3 Dopamine Receptor Agonist. J Med Chem. 2020 May 28;63(10):5526-5567.
REF 6 Functionally selective dopamine D?, D? receptor partial agonists. J Med Chem. 2014 Jun 12;57(11):4861-75.
REF 7 1,2,4-Triazolyl azabicyclo[3.1.0]hexanes: a new series of potent and selective dopamine D(3) receptor antagonists. J Med Chem. 2010 Jan 14;53(1):374-91.

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