Co-Target(s) Information

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Target General Information
Co-Targets of This Target
References
Target General Information  Top
Target ID T97729 Target Info
Target Name HUMAN two pore channel subtype 2 (TPC2)
Synonyms
Voltage-dependent calcium channel protein TPC2; TPC2
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Gene Name TPCN2
UniProt ID
TPC2_HUMAN
Co-Targets of This Target  Top
Co-Target Name Opioid receptor sigma 1 (OPRS1) Successful Target
UniProt ID SGMR1_HUMAN
Gene Name SIGMAR1
Synonyms
hSigmaR1; Sigma1R; Sigma1-receptor; Sigma non-opioid intracellular receptor 1; Sigma 1-type opioid receptor; SRBP; SR31747-binding protein; SR31747 binding protein 1; SR-BP; SIG-1R; Opioid receptor, sigma 1, isoform 1; OPRS1 protein; Aging-associated gene 8 protein; AAG8
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Representative Drug(s) Amiodarone Drug Info Ki = 1 nM [1]
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 Click to Show More [3]
2 Amiodarone Drug Info IC50 = 30 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 Voltage-gated L-type calcium channel (L-CaC) Successful Target
UniProt ID CAC1C_HUMAN; CAC1D_HUMAN; CAC1F_HUMAN; CAC1S_HUMAN
Gene Name NO-GeName
Synonyms
L-type voltage-dependent Ca(2+) channel; L-type Ca2+ channel; L-type Ca(2+) channel
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Representative Drug(s) Verapamil Drug Info IC50 = 200 nM Click to Show More [6]
2 Amiodarone Drug Info IC50 = 270 nM [4]
Co-Target Name Thyroid hormone receptor beta (THRB) Successful Target
UniProt ID THB_HUMAN
Gene Name THRB
Synonyms
c-erbA-beta; c-erbA-2; THR1; Nuclear receptor subfamily 1 group A member 2; NR1A2; ERBA2
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Representative Drug(s) Amiodarone Drug Info IC50 = 600 nM [7]
Co-Target Name Thyroid hormone receptor alpha (THRA) Successful Target
UniProt ID THA_HUMAN
Gene Name THRA
Synonyms
V-erbA-related protein 7; THRA2; THRA1; Nuclear receptor subfamily 1 group A member 1; NR1A1; ERBA1; EAR7; EAR-7; C-erbA-alpha; C-erbA-1
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Representative Drug(s) Amiodarone Drug Info IC50 = 650 nM [7]
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 [8]
Co-Target Name Cholestenol delta-isomerase (EBP) Clinical trial Target
UniProt ID EBP_HUMAN
Gene Name EBP
Synonyms
Emopamilbinding protein; EBP; Delta(8)Delta(7) sterol isomerase; D8D7 sterol isomerase; 3betahydroxysteroidDelta(8),Delta(7)isomerase
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Representative Drug(s) Amiodarone Drug Info Ki = 25 nM [1]
References  Top
REF 1 Discovery of high-affinity ligands of sigma1 receptor, ERG2, and emopamil binding protein by pharmacophore modeling and virtual screening. J Med Chem. 2005 Jul 28;48(15):4754-64.
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 Simulation of multiple ion channel block provides improved early prediction of compounds' clinical torsadogenic risk. Cardiovasc Res. 2011 Jul 1;91(1):53-61.
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 MICE models: superior to the HERG model in predicting Torsade de Pointes. Sci Rep. 2013;3:2100.
REF 7 Synthesis and preliminary characterization of a novel antiarrhythmic compound (KB130015) with an improved toxicity profile compared with amiodarone. J Med Chem. 2002 Jan 31;45(3):623-30.
REF 8 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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