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, JDMatthews, TPMcHardy, TProisy, NCheung, KMLainchbury, MBrown, NWalton, MIEve, PDBoxall, KJHayes, AHenley, ATValenti, MRDe Haven Brandon, AKBox, GJamin, YRobinson, SPWestwood, IMvan Montfort, RLLeonard, PMLamers, MBReader, JCAherne, GWRaynaud, FIEccles, SAGarrett, MDCollins, 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 
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|
Structure:
Search PDB for entries with ligand similarity: