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Target
Potassium voltage-gated channel subfamily KQT member 1
Ligand
BDBM328993
Substrate
n/a
Meas. Tech.
ChEMBL_2051993 (CHEMBL4706994)
IC50
>10000±n/a nM
Citation
Osborne, JD; Matthews, TP; McHardy, T; Proisy, N; Cheung, KM; Lainchbury, M; Brown, N; Walton, MI; Eve, PD; Boxall, KJ; Hayes, A; Henley, AT; Valenti, MR; De Haven Brandon, AK; Box, G; Jamin, Y; Robinson, SP; Westwood, IM; van Montfort, RL; Leonard, PM; Lamers, MB; Reader, JC; Aherne, GW; Raynaud, FI; Eccles, SA; Garrett, MD; Collins, I Multiparameter Lead Optimization to Give an Oral Checkpoint Kinase 1 (CHK1) Inhibitor Clinical Candidate: (R)-5-((4-((Morpholin-2-ylmethyl)amino)-5-(trifluoromethyl)pyridin-2-yl)amino)pyrazine-2-carbonitrile (CCT245737). J Med Chem 59:5221-37 (2016) [PubMed] Article
More Info.:
Target
Name:
Potassium voltage-gated channel subfamily KQT member 1
Synonyms:
KCNA8 | KCNA9 | KCNQ (Kv7) potassium channel | KCNQ1 | KCNQ1_HUMAN | KVLQT1 | Voltage-gated potassium channel subunit Kv7.1 | Voltage-gated potassium channel subunit Kv7.1/Misshapen-like kinase 1
Type:
PROTEIN
Mol. Mass.:
74739.00
Organism:
Homo sapiens (Human)
Description:
ChEMBL_1454245
Residue:
676
Sequence:
MAAASSPPRAERKRWGWGRLPGARRGSAGLAKKCPFSLELAEGGPAGGALYAPIAPGAPGPAPPASPAAPAAPPVASDLGPRPPVSLDPRVSIYSTRRPVLARTHVQGRVYNFLERPTGWKCFVYHFAVFLIVLVCLIFSVLSTIEQYAALATGTLFWMEIVLVVFFGTEYVVRLWSAGCRSKYVGLWGRLRFARKPISIIDLIVVVASMVVLCVGSKGQVFATSAIRGIRFLQILRMLHVDRQGGTWRLLGSVVFIHRQELITTLYIGFLGLIFSSYFVYLAEKDAVNESGRVEFGSYADALWWGVVTVTTIGYGDKVPQTWVGKTIASCFSVFAISFFALPAGILGSGFALKVQQKQRQKHFNRQIPAAASLIQTAWRCYAAENPDSSTWKIYIRKAPRSHTLLSPSPKPKKSVVVKKKKFKLDKDNGVTPGEKMLTVPHITCDPPEERRLDHFSVDGYDSSVRKSPTLLEVSMPHFMRTNSFAEDLDLEGETLLTPITHISQLREHHRATIKVIRRMQYFVAKKKFQQARKPYDVRDVIEQYSQGHLNLMVRIKELQRRLDQSIGKPSLFISVSEKSKDRGSNTIGARLNRVEDKVTQLDQRLALITDMLHQLLSLHGGSTPGSGGPPREGGAHITQPCGSGGSVDPELFLPSNTLPTYEQLTVPRRGPDEGS
Inhibitor
Name:
BDBM328993
Synonyms:
5-[[4-[[(2R)-morpholin-2-yl]methylamino]-5-(trifluoromethyl)-2-pyridyl]amino]pyrazine-2-carbonitrile | US11787792, Compound 1 | US9663503, Compound 1
Type:
Small organic molecule
Emp. Form.:
C16H16F3N7O
Mol. Mass.:
379.3397
SMILES:
FC(F)(F)c1cnc(Nc2cnc(cn2)C#N)cc1NC[C@H]1CNCCO1 |r|