Reaction Details |
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Target | Potassium voltage-gated channel subfamily H member 2 |
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Ligand | BDBM29991 |
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Substrate/Competitor | BDBM24064 |
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Meas. Tech. | hERG Radioligand Binding Assay |
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pH | 7.4±n/a |
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Temperature | 295.15±n/a K |
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IC50 | 8500±n/a nM |
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Citation | Kobayashi, K; Uchiyama, M; Takahashi, H; Kawamoto, H; Ito, S; Yoshizumi, T; Nakashima, H; Kato, T; Shimizu, A; Yamamoto, I; Asai, M; Miyazoe, H; Ohno, A; Hirayama, M; Ozaki, S; Tani, T; Ishii, Y; Tanaka, T; Mochidome, T; Tadano, K; Fukuroda, T; Ohta, H; Okamoto, O 2-Cyclohexylcarbonylbenzimidazoles as potent, orally available and brain-penetrable opioid receptor-like 1 (ORL1) antagonists. Bioorg Med Chem Lett19:3096-9 (2009) [PubMed] Article |
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More Info.: | Get all data from this article, Solution Info, Assay Method |
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Potassium voltage-gated channel subfamily H member 2 |
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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: | MPVRRGHVAPQNTFLDTIIRKFEGQSRKFIIANARVENCAVIYCNDGFCELCGYSRAEVM
QRPCTCDFLHGPRTQRRAAAQIAQALLGAEERKVEIAFYRKDGSCFLCLVDVVPVKNEDG
AVIMFILNFEVVMEKDMVGSPAHDTNHRGPPTSWLAPGRAKTFRLKLPALLALTARESSV
RSGGAGGAGAPGAVVVDVDLTPAAPSSESLALDEVTAMDNHVAGLGPAEERRALVGPGSP
PRSAPGQLPSPRAHSLNPDASGSSCSLARTRSRESCASVRRASSADDIEAMRAGVLPPPP
RHASTGAMHPLRSGLLNSTSDSDLVRYRTISKIPQITLNFVDLKGDPFLASPTSDREIIA
PKIKERTHNVTEKVTQVLSLGADVLPEYKLQAPRIHRWTILHYSPFKAVWDWLILLLVIY
TAVFTPYSAAFLLKETEEGPPATECGYACQPLAVVDLIVDIMFIVDILINFRTTYVNANE
EVVSHPGRIAVHYFKGWFLIDMVAAIPFDLLIFGSGSEELIGLLKTARLLRLVRVARKLD
RYSEYGAAVLFLLMCTFALIAHWLACIWYAIGNMEQPHMDSRIGWLHNLGDQIGKPYNSS
GLGGPSIKDKYVTALYFTFSSLTSVGFGNVSPNTNSEKIFSICVMLIGSLMYASIFGNVS
AIIQRLYSGTARYHTQMLRVREFIRFHQIPNPLRQRLEEYFQHAWSYTNGIDMNAVLKGF
PECLQADICLHLNRSLLQHCKPFRGATKGCLRALAMKFKTTHAPPGDTLVHAGDLLTALY
FISRGSIEILRGDVVVAILGKNDIFGEPLNLYARPGKSNGDVRALTYCDLHKIHRDDLLE
VLDMYPEFSDHFWSSLEITFNLRDTNMIPGSPGSTELEGGFSRQRKRKLSFRRRTDKDTE
QPGEVSALGPGRAGAGPSSRGRPGGPWGESPSSGPSSPESSEDEGPGRSSSPLRLVPFSS
PRPPGEPPGGEPLMEDCEKSSDTCNPLSGAFSGVSNIFSFWGDSRGRQYQELPRCPAPTP
SLLNIPLSSPGRRPRGDVESRLDALQRQLNRLETRLSADMATVLQLLQRQMTLVPPAYSA
VTTPGPGPTSTSPLLPVSPLPTLTLDSLSQVSQFMACEELPPGAPELPQEGPTRRLSLPG
QLGALTSQPLHRHGSDPGS
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BDBM29991 |
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BDBM24064 |
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Name | BDBM29991 |
Synonyms: | 2-Cyclohexylcarbonylbenzimidazole, 9 |
Type | Small organic molecule |
Emp. Form. | C21H27ClN4O2 |
Mol. Mass. | 402.918 |
SMILES | CCN1CCN(CC1)c1cc2[nH]c(nc2cc1Cl)C(=O)C1(C)CCC(=O)CC1 |
Structure |
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