Reaction Details
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Potassium voltage-gated channel subfamily H member 2
Ligand
BDBM50566548
Substrate
n/a
Meas. Tech.
ChEMBL_2100973 (CHEMBL4809369)
IC50
>30000±n/a nM
Citation
Lapointe, G; Skepper, CK; Holder, LM; Armstrong, D; Bellamacina, C; Blais, J; Bussiere, D; Bian, J; Cepura, C; Chan, H; Dean, CR; De Pascale, G; Dhumale, B; Fisher, LM; Fulsunder, M; Kantariya, B; Kim, J; King, S; Kossy, L; Kulkarni, U; Lakshman, J; Leeds, JA; Ling, X; Lvov, A; Ma, S; Malekar, S; McKenney, D; Mergo, W; Metzger, L; Mhaske, K; Moser, HE; Mostafavi, M; Namballa, S; Noeske, J; Osborne, C; Patel, A; Patel, D; Patel, T; Piechon, P; Polyakov, V; Prajapati, K; Prosen, KR; Reck, F; Richie, DL; Sanderson, MR; Satasia, S; Savani, B; Selvarajah, J; Sethuraman, V; Shu, W; Tashiro, K; Thompson, KV; Vaarla, K; Vala, L; Veselkov, DA; Vo, J; Vora, B; Wagner, T; Wedel, L; Williams, SL; Yendluri, S; Yue, Q; Yifru, A; Zhang, Y; Rivkin, A Discovery and Optimization of DNA Gyrase and Topoisomerase IV Inhibitors with Potent Activity against Fluoroquinolone-Resistant Gram-Positive Bacteria. J Med Chem 64:6329-6357 (2021) [PubMed] Article More Info.:
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:
BDBM50566548
Synonyms:
CHEMBL4861063
Type:
Small organic molecule
Emp. Form.:
C23H26FN5O2S
Mol. Mass.:
455.548
SMILES:
Cc1c(N2CCC(C2)C2(N)CC2)c(F)cc2c(Cc3noc(=S)[nH]3)cc(=O)n(C3CC3)c12
Structure:
