Co-Target(s) Information

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Target General Information
Co-Targets of This Target
References
Target General Information  Top
Target ID T64795 Target Info
Target Name Voltage-gated calcium channel alpha Cav3.1 (CACNA1G)
Synonyms
Voltage-gated calcium channel alpha subunit Cav3.1; Voltage-dependent T-type calcium channel; NBR13; Cav3.1c; CACNA1G
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Target Type Successful Target
Gene Name CACNA1G
Biochemical Class Voltage-gated ion channel
UniProt ID
CAC1G_HUMAN
Co-Targets of This Target  Top
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) NGD 94-1 Drug Info Ki = 3.6 nM Click to Show More [1]
2 Penfluridol Drug Info Ki = 1000 nM [4]
Co-Target Name Multidrug resistance protein 1 (ABCB1) Clinical trial Target
UniProt ID MDR1_HUMAN
Gene Name ABCB1
Synonyms
PGY1; P-glycoprotein 1; MDR1; CD243 antigen; CD243; ATP-binding cassette sub-family B member 1
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Representative Drug(s) Verapamil Drug Info IC50 = 4.9 nM [2]
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) Verapamil Drug Info IC50 = 10 nM [3]
Co-Target Name Dopamine D5 receptor (D5R) Successful Target
UniProt ID DRD5_HUMAN
Gene Name DRD5
Synonyms
Dopamine receptor 5; DRD5; D1beta dopamine receptor; D(5)D(1B) dopamine receptor dopamine receptor; D(5) dopamine receptor
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Representative Drug(s) Penfluridol Drug Info Ki = 125 nM [4]
Co-Target Name Dopamine D3 receptor (D3R) Successful Target
UniProt ID DRD3_HUMAN
Gene Name DRD3
Synonyms
D(3) dopamine receptor
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Representative Drug(s) Penfluridol Drug Info Ki = 136 nM [4]
Co-Target Name Dopamine D1 receptor (D1R) Successful Target
UniProt ID DRD1_HUMAN
Gene Name DRD1
Synonyms
D(1A) dopamine receptor
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Representative Drug(s) Penfluridol Drug Info Ki = 147 nM [4]
Co-Target Name Voltage-gated calcium channel alpha Cav1.2 (CACNA1C) Successful Target
UniProt ID CAC1C_HUMAN
Gene Name CACNA1C
Synonyms
Voltage-gated calcium channel subunit alpha Cav1.2; Voltage-dependent L-type calcium channel subunit alpha-1C; Calcium channel, L type, alpha-1 polypeptide, isoform 1, cardiac muscle; CCHL1A1; CACNL1A1; CACN2; CACH2
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Representative Drug(s) Verapamil Drug Info IC50 = 150 nM [5]
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) Penfluridol Drug Info Ki = 159 nM [4]
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) NGD 94-1 Drug Info Ki = 180 nM Click to Show More [6]
2 Penfluridol Drug Info Ki = 356 nM [4]
Co-Target Name 5-HT 2B receptor (HTR2B) Successful Target
UniProt ID 5HT2B_HUMAN
Gene Name HTR2B
Synonyms
Serotonin receptor 2B; 5-hydroxytryptamine receptor 2B; 5-HT2B; 5-HT-2B; 5-HT 2B
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Representative Drug(s) Penfluridol Drug Info Ki = 184 nM [4]
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) Penfluridol Drug Info Ki = 361 nM [4]
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) Penfluridol Drug Info Ki = 401 nM [4]
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) Penfluridol Drug Info Ki = 445 nM [4]
Co-Target Name Adrenergic receptor beta-3 (ADRB3) Successful Target
UniProt ID ADRB3_HUMAN
Gene Name ADRB3
Synonyms
Beta3AR; Beta3-AR; Beta-3 adrenoreceptor; Beta-3 adrenoceptor; Beta-3 adrenergic receptor; B3AR; ADRB3R
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Representative Drug(s) Penfluridol Drug Info Ki = 515 nM [4]
Co-Target Name Norepinephrine transporter (NET) Successful Target
UniProt ID SC6A2_HUMAN
Gene Name SLC6A2
Synonyms
Solute carrier family 6 member 2; Sodium-dependent noradrenaline transporter; SLC6A2; NET1; NET; NAT1
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Representative Drug(s) Penfluridol Drug Info Ki = 588 nM [4]
Co-Target Name Adrenergic receptor alpha-1D (ADRA1D) Successful Target
UniProt ID ADA1D_HUMAN
Gene Name ADRA1D
Synonyms
Alpha-adrenergic receptor 1a; Alpha-1D adrenoreceptor; Alpha-1D adrenoceptor; Alpha-1D adrenergic receptor; Alpha adrenergic receptor 1a; Alpha 1D-adrenoreceptor; Alpha 1D-adrenoceptor; ADRA1A
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Representative Drug(s) Penfluridol Drug Info Ki = 602 nM [4]
Co-Target Name 5-HT 3A receptor (HTR3A) Successful Target
UniProt ID 5HT3A_HUMAN
Gene Name HTR3A
Synonyms
Serotonin-gated ion channel receptor; Serotonin receptor 3A; HTR3; 5HT3R; 5-hydroxytryptamine receptor 3A; 5-HT3RA; 5-HT3A; 5-HT3-A; 5-HT 3A
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Representative Drug(s) NGD 94-1 Drug Info Ki = 750 nM [6]
Co-Target Name Opioid receptor mu (MOP) Successful Target
UniProt ID OPRM_HUMAN
Gene Name OPRM1
Synonyms
hMOP; Mu-type opioid receptor; Mu opioid receptor; Mu opiate receptor; MOR1A; MOR1; MOR-1; M-OR-1
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Representative Drug(s) Penfluridol Drug Info Ki = 867 nM [4]
Co-Target Name 5-HT 2C receptor (HTR2C) Successful Target
UniProt ID 5HT2C_HUMAN
Gene Name HTR2C
Synonyms
Serotonin receptor 2C; HTR1C; 5HT-1C; 5-hydroxytryptamine receptor 2C; 5-hydroxytryptamine receptor 1C; 5-HTR2C; 5-HT2C receptor; 5-HT2C; 5-HT1C; 5-HT-2C; 5-HT-1C
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Representative Drug(s) Penfluridol Drug Info Ki = 881 nM [4]
Co-Target Name ATP-binding cassette transporter G2 (ABCG2) Successful Target
UniProt ID ABCG2_HUMAN
Gene Name ABCG2
Synonyms
Urate exporter; Placenta-specific ATP-binding cassette transporter; Mitoxantrone resistance-associated protein; MXR; CDw338; CD338; Breast cancer resistance protein; BCRP1; BCRP; ABCP
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Representative Drug(s) Verapamil Drug Info EC50 = 900 nM [7]
Co-Target Name Histamine H1 receptor (H1R) Successful Target
UniProt ID HRH1_HUMAN
Gene Name HRH1
Synonyms
HH1R; H1R
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Representative Drug(s) Penfluridol Drug Info Ki = 1000 nM [4]
Co-Target Name Histamine H2 receptor (H2R) Successful Target
UniProt ID HRH2_HUMAN
Gene Name HRH2
Synonyms
Histamine receptor 2; HH2R; Gastric receptor I
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Representative Drug(s) Penfluridol Drug Info Ki = 1000 nM [4]
Co-Target Name 5-HT 5A receptor (HTR5A) Successful Target
UniProt ID 5HT5A_HUMAN
Gene Name HTR5A
Synonyms
Serotonin receptor 5A; 5-hydroxytryptamine receptor 5A; 5-HT5A; 5-HT-5A; 5-HT-5; 5-HT 5A
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Representative Drug(s) Penfluridol Drug Info Ki = 1000 nM [4]
Co-Target Name Opioid receptor kappa (OPRK1) Successful Target
UniProt ID OPRK_HUMAN
Gene Name OPRK1
Synonyms
OPRK; Kappa-type opioid receptor; Kappa opioid receptor; KOR-1; KOR; K-OR-1
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Representative Drug(s) Penfluridol Drug Info Ki = 1000 nM [4]
Co-Target Name Serotonin transporter (SERT) Successful Target
UniProt ID SC6A4_HUMAN
Gene Name SLC6A4
Synonyms
Solute carrier family 6 member 4; HTT; 5HTT; 5HT transporter
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Representative Drug(s) Penfluridol Drug Info Ki = 1000 nM [4]
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) Penfluridol Drug Info Ki = 280 nM [4]
Co-Target Name 5-HT 6 receptor (HTR6) Clinical trial Target
UniProt ID 5HT6R_HUMAN
Gene Name HTR6
Synonyms
Serotonin receptor 6; 5-hydroxytryptamine receptor 6; 5-HT6 receptor; 5-HT6; 5-HT-6
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Representative Drug(s) Penfluridol Drug Info Ki = 1000 nM [4]
References  Top
REF 1 Current and novel approaches to the drug treatment of schizophrenia. J Med Chem. 2001 Feb 15;44(4):477-501.
REF 2 Synthesis and biological evaluation of novel H6 analogues as drug resistance reversal agents. Eur J Med Chem. 2019 Jan 1;161:364-377.
REF 3 Polypharmacology-foe or friend? J Med Chem. 2013 Nov 27;56(22):8955-71.
REF 4 Analogs of penfluridol as chemotherapeutic agents with reduced central nervous system activity. Bioorg Med Chem Lett. 2018 Dec 15;28(23:3652-7.
REF 5 Verapamil analogues with restricted molecular flexibility: synthesis and pharmacological evaluation of the four isomers of alpha-[1-[3-[N-[1- [2-(3,4-dimethoxyphenyl)ethyl]]-N-methylamino]cyclohexyl]]-alpha- isopropyl-3,4-dimethoxybenzene-acetonitrile. J Med Chem. 1993 Feb 19;36(4):439-45.
REF 6 Return of D 4 Dopamine Receptor Antagonists in Drug Discovery. J Med Chem. 2017 Sep 14;60(17):7233-7243.
REF 7 Design, synthesis and biological evaluation of stereo- and regioisomers of amino aryl esters as multidrug resistance (MDR) reversers. Eur J Med Chem. 2019 Nov 15;182:111655.

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