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Target
Potassium voltage-gated channel subfamily H member 2
Ligand
BDBM50585824
Substrate
n/a
Meas. Tech.
ChEMBL_2164004 (CHEMBL5048865)
IC50
>80000±n/a nM
Citation
 Shi, Y; Wang, Y; Meng, W; Brigance, RP; Ryono, DE; Bolton, S; Zhang, H; Chen, S; Smirk, R; Tao, S; Tino, JA; Williams, KN; Sulsky, R; Nielsen, L; Ellsworth, B; Wong, MKY; Sun, JH; Leith, LW; Sun, D; Wu, DR; Gupta, A; Rampulla, R; Mathur, A; Chen, BC; Wang, A; Fuentes-Catanio, HG; Kunselman, L; Cap, M; Zalaznick, J; Ma, X; Liu, H; Taylor, JR; Zebo, R; Jones, B; Kalinowski, S; Swartz, J; Staal, A; O'Malley, K; Kopcho, L; Muckelbauer, JK; Krystek, SR; Spronk, SA; Marcinkeviciene, J; Everlof, G; Chen, XQ; Xu, C; Li, YX; Langish, RA; Yang, Y; Wang, Q; Behnia, K; Fura, A; Janovitz, EB; Pannacciulli, N; Griffen, S; Zinker, BA; Krupinski, J; Kirby, M; Whaley, J; Zahler, R; Barrish, JC; Robl, JA; Cheng, PTW Discovery of a Partial Glucokinase Activator Clinical Candidate: Diethyl ((3-(3-((5-(Azetidine-1-carbonyl)pyrazin-2-yl)oxy)-5-isopropoxybenzamido)-1 J Med Chem 65:4291-4317 (2022) [PubMed]  Article 
Target
Name:
Potassium voltage-gated channel subfamily H member 2
Synonyms:
1,3-beta-glucan synthase component GLS2 | Cytochrome P450 3A4 | ERG | ERG1 | Eag-related protein 1 | Ether a-go-go related gene potassium channel (hERG) | Ether-a-go-go-related gene (HERG) | Ether-a-go-go-related gene potassium channel (hERG) | Ether-a-go-go-related gene potassium channel 1 | Ether-a-go-go-related gene potassium channel 1 (HERG) | Ether-a-go-go-related gene potassium channel 1 (hERG1) | Ether-a-go-go-related protein (hERG) | Ether-a-go-go-related protein 1 | Ether-a-go-go-related protein 1 (HERG) | H-ERG | HERG | KCNH2 | KCNH2_HUMAN | Potassium voltage-gated channel subfamily H member 2 (hERG) | Transcriptional regulator ERG | Voltage-gated potassium channel subunit Kv11.1 | eag homolog | hERG Potassium Channel 1 | putative potassium channel subunit
Type:
Multi-pass membrane protein
Mol. Mass.:
126672.65
Organism:
Homo sapiens (Human)
Description:
Q12809
Residue:
1159
Sequence:
MPVRRGHVAPQNTFLDTIIRKFEGQSRKFIIANARVENCAVIYCNDGFCELCGYSRAEVMQRPCTCDFLHGPRTQRRAAAQIAQALLGAEERKVEIAFYRKDGSCFLCLVDVVPVKNEDGAVIMFILNFEVVMEKDMVGSPAHDTNHRGPPTSWLAPGRAKTFRLKLPALLALTARESSVRSGGAGGAGAPGAVVVDVDLTPAAPSSESLALDEVTAMDNHVAGLGPAEERRALVGPGSPPRSAPGQLPSPRAHSLNPDASGSSCSLARTRSRESCASVRRASSADDIEAMRAGVLPPPPRHASTGAMHPLRSGLLNSTSDSDLVRYRTISKIPQITLNFVDLKGDPFLASPTSDREIIAPKIKERTHNVTEKVTQVLSLGADVLPEYKLQAPRIHRWTILHYSPFKAVWDWLILLLVIYTAVFTPYSAAFLLKETEEGPPATECGYACQPLAVVDLIVDIMFIVDILINFRTTYVNANEEVVSHPGRIAVHYFKGWFLIDMVAAIPFDLLIFGSGSEELIGLLKTARLLRLVRVARKLDRYSEYGAAVLFLLMCTFALIAHWLACIWYAIGNMEQPHMDSRIGWLHNLGDQIGKPYNSSGLGGPSIKDKYVTALYFTFSSLTSVGFGNVSPNTNSEKIFSICVMLIGSLMYASIFGNVSAIIQRLYSGTARYHTQMLRVREFIRFHQIPNPLRQRLEEYFQHAWSYTNGIDMNAVLKGFPECLQADICLHLNRSLLQHCKPFRGATKGCLRALAMKFKTTHAPPGDTLVHAGDLLTALYFISRGSIEILRGDVVVAILGKNDIFGEPLNLYARPGKSNGDVRALTYCDLHKIHRDDLLEVLDMYPEFSDHFWSSLEITFNLRDTNMIPGSPGSTELEGGFSRQRKRKLSFRRRTDKDTEQPGEVSALGPGRAGAGPSSRGRPGGPWGESPSSGPSSPESSEDEGPGRSSSPLRLVPFSSPRPPGEPPGGEPLMEDCEKSSDTCNPLSGAFSGVSNIFSFWGDSRGRQYQELPRCPAPTPSLLNIPLSSPGRRPRGDVESRLDALQRQLNRLETRLSADMATVLQLLQRQMTLVPPAYSAVTTPGPGPTSTSPLLPVSPLPTLTLDSLSQVSQFMACEELPPGAPELPQEGPTRRLSLPGQLGALTSQPLHRHGSDPGS
  
Inhibitor
Name:
BDBM50585824
Synonyms:
CHEMBL5084870
Type:
Small organic molecule
Emp. Form.:
C24H31N4O8PS
Mol. Mass.:
566.564
SMILES:
CCOP(=O)(Cn1ccc(NC(=O)c2cc(OC(C)C)cc(Oc3ccc(nc3)S(C)(=O)=O)c2)n1)OCC
Structure:
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