Co-Target(s) Information

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Target General Information
Co-Targets of This Target
References
Target General Information  Top
Target ID T85435 Target Info
Target Name Insulin receptor (INSR)
Synonyms
IR; CD220 antigen; CD220
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Target Type Successful Target
Gene Name INSR
Biochemical Class Kinase
UniProt ID
INSR_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) Meglitinides Drug Info Ki = 1.21 nM [1]
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) Meglitinides Drug Info Ki = 3.7 nM [2]
Co-Target Name Insulin-like growth factor I receptor (IGF1R) Successful Target
UniProt ID IGF1R_HUMAN
Gene Name IGF1R
Synonyms
Type 1 insulin-like growth factor receptor; Insulin-like growth factor 1 receptor; IGF-IR; IGF-I receptor; IGF-1R; IGF-1 receptor; CD221 antigen; CD221
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Representative Drug(s) AEW-541 Drug Info IC50 = 20 nM [3]
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) AEW-541 Drug Info IC50 = 130 nM [3]
Co-Target Name Peroxisome proliferator-activated receptor gamma (PPAR-gamma) Successful Target
UniProt ID PPARG_HUMAN
Gene Name PPARG
Synonyms
PPAR-gamma; Nuclear receptor subfamily 1 group C member 3; NR1C3
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Representative Drug(s) Mitoglitazone Drug Info EC50 = 657 nM Click to Show More [4]
2 MSDC-0602 Drug Info EC50 = 961 nM [4]
Co-Target Name Platelet-derived growth factor receptor alpha (PDGFRA) Successful Target
UniProt ID PGFRA_HUMAN
Gene Name PDGFRA
Synonyms
RHEPDGFRA; Platelet-derived growth factor receptor 2; Platelet-derived growth factor alpha receptor; PDGFR2; PDGFR-alpha; PDGFR-2; PDGF-R-alpha; CD140a antigen; CD140a; CD140 antigen-like family member A; Alpha-type platelet-derived growth factor receptor; Alpha platelet-derived growth factor receptor
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Representative Drug(s) AEW-541 Drug Info IC50 = 800 nM [3]
Co-Target Name Dopamine receptor (DR) Clinical trial Target
UniProt ID DRD1_HUMAN; DRD2_HUMAN; DRD3_HUMAN; DRD4_HUMAN; DRD5_HUMAN
Gene Name NO-GeName
Synonyms
Human dopamine receptor
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Representative Drug(s) Meglitinides Drug Info Ki = 5.1 nM [5]
References  Top
REF 1 Shuttle-cargo fusion molecules of transport peptides and the hD2/3 receptor antagonist fallypride: a feasible approach to preserve ligand-receptor binding?. J Med Chem. 2014 May 22;57(10):4368-81.
REF 2 Molecular modeling of the three-dimensional structure of dopamine 3 (D3) subtype receptor: discovery of novel and potent D3 ligands through a hybri... J Med Chem. 2003 Oct 9;46(21):4377-92.
REF 3 Optimisation of a 5-[3-phenyl-(2-cyclic-ether)-methyl-ether]-4-aminopyrrolopyrimidine series of IGF-1R inhibitors. Bioorg Med Chem Lett. 2016 Apr 15;26(8):2057-64.
REF 4 PPAR-sparing thiazolidinediones as insulin sensitizers. Design, synthesis and selection of compounds for clinical development. Bioorg Med Chem. 2018 Dec 1;26(22):5870-5884.
REF 5 N-fluoroalkylated and N-alkylated analogues of the dopaminergic D-2 receptor antagonist raclopride. J Med Chem. 1990 Sep;33(9):2430-7.

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