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Target
Potassium voltage-gated channel subfamily H member 2
Ligand
BDBM50091549
Substrate
n/a
Meas. Tech.
ChEMBL_1498163 (CHEMBL3583383)
Ki
2870±n/a nM
Citation
 Shah, SK; He, S; Guo, L; Truong, Q; Qi, H; Du, W; Lai, Z; Liu, J; Jian, T; Hong, Q; Dobbelaar, P; Ye, Z; Sherer, E; Feng, Z; Yu, Y; Wong, F; Samuel, K; Madiera, M; Karanam, BV; Reddy, VB; Mitelman, S; Tong, SX; Chicchi, GG; Tsao, KL; Trusca, D; Feng, Y; Wu, M; Shao, Q; Trujillo, ME; Eiermann, GJ; Li, C; Pachanski, M; Fernandez, G; Nelson, D; Bunting, P; Morissette, P; Volksdorf, S; Kerr, J; Zhang, BB; Howard, AD; Zhou, YP; Pasternak, A; Nargund, RP; Hagmann, WK Discovery of MK-1421, a Potent, Selective sstr3 Antagonist, as a Development Candidate for Type 2 Diabetes. ACS Med Chem Lett 6:513-7 (2015) [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:
BDBM50091549
Synonyms:
CHEMBL3582310
Type:
Small organic molecule
Emp. Form.:
C27H23FN4
Mol. Mass.:
422.4967
SMILES:
CC1(N[C@H](Cc2c1[nH]c1ccccc21)c1nc(c[nH]1)-c1ccc(F)cc1)c1ccccc1 |r|
Structure:
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