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Target
Potassium voltage-gated channel subfamily H member 2
Ligand
BDBM315582
Substrate
n/a
Meas. Tech.
Patch Clamp Assay
Ki
<10000±n/a nM
Citation
 Fuchss, T; Emde, U; Buchstaller, H; Mederski, W Arylquinazolines US Patent  US9732094 Publication Date 8/15/2017 
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:
BDBM315582
Synonyms:
(6-Chloro-5-methoxy- pyridazin-3-yl)-[4-fluoro- 3-(7-morpholin-4-yl- quinazolin-4-yl)phenyl- methanol1H NMR (500 MHz, DMSO-d6) ppm = 9.10 (s, 1H), 7.88 (d, J = 1.0, 1H), 7.63-7.58 (m, 2H), 7.55- 7.47 (m, 2H), 7.42-7.35 (m, 1H), 7.20 (d, J = 2.3, 1H), 6.46 (d, J = 4.3, 1H), 5.85-5.82 (m, 1H), 4.00 (s, 3H), 3.81-3.74 (m, 4H), 3.48-3.41 (m, 4H) | US10172859, Example 286 | US10172859, Example 9 | US11065253, Example 286 | US9732094, Example 286
Type:
Small organic molecule
Emp. Form.:
C24H21ClFN5O3
Mol. Mass.:
481.907
SMILES:
COc1nnc(Cl)cc1C(O)c1ccc(F)c(c1)-c1ncnc2cc(ccc12)N1CCOCC1
Structure:
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