Target
Short transient receptor potential channel 3
Ligand
BDBM50439228
Substrate
n/a
Meas. Tech.
ChEMBL_978642 (CHEMBL2422305)
IC50
1600±n/a nM
Citation
 Washburn, DGHolt, DADodson, JMcAtee, JJTerrell, LRBarton, LManns, SWaszkiewicz, APritchard, CGillie, DJMorrow, DMDavenport, EALozinskaya, IMGuss, JBasilla, JBNegron, LKKlein, MWillette, RNFries, REJensen, TCXu, XSchnackenberg, CGMarino, JP The discovery of potent blockers of the canonical transient receptor channels, TRPC3 and TRPC6, based on an anilino-thiazole pharmacophore. Bioorg Med Chem Lett 23:4979-84 (2013) [PubMed]  Article 
Target
Name:
Short transient receptor potential channel 3
Synonyms:
TRP-3 | TRP3 | TRPC3 | TRPC3_HUMAN | Transient receptor protein 3 | hTrp-3 | hTrp3
Type:
PROTEIN
Mol. Mass.:
96009.35
Organism:
Homo sapiens (Human)
Description:
ChEMBL_107641
Residue:
836
Sequence:
MREKGRRQAVRGPAFMFNDRGTSLTAEEERFLDAAEYGNIPVVRKMLEESKTLNVNCVDYMGQNALQLAVGNEHLEVTELLLKKENLARIGDALLLAISKGYVRIVEAILNHPGFAASKRLTLSPCEQELQDDDFYAYDEDGTRFSPDITPIILAAHCQKYEVVHMLLMKGARIERPHDYFCKCGDCMEKQRHDSFSHSRSRINAYKGLASPAYLSLSSEDPVLTALELSNELAKLANIEKEFKNDYRKLSMQCKDFVVGVLDLCRDSEEVEAILNGDLESAEPLEVHRHKASLSRVKLAIKYEVKKFVAHPNCQQQLLTIWYENLSGLREQTIAIKCLVVLVVALGLPFLAIGYWIAPCSRLGKILRSPFMKFVAHAASFIIFLGLLVFNASDRFEGITTLPNITVTDYPKQIFRVKTTQFTWTEMLIMVWVLGMMWSECKELWLEGPREYILQLWNVLDFGMLSIFIAAFTARFLAFLQATKAQQYVDSYVQESDLSEVTLPPEIQYFTYARDKWLPSDPQIISEGLYAIAVVLSFSRIAYILPANESFGPLQISLGRTVKDIFKFMVLFIMVFFAFMIGMFILYSYYLGAKVNAAFTTVEESFKTLFWSIFGLSEVTSVVLKYDHKFIENIGYVLYGIYNVTMVVVLLNMLIAMINSSYQEIEDDSDVEWKFARSKLWLSYFDDGKTLPPPFSLVPSPKSFVYFIMRIVNFPKCRRRRLQKDIEMGMGNSKSRLNLFTQSNSRVFESHSFNSILNQPTRYQQIMKRLIKRYVLKAQVDKENDEVNEGELKEIKQDISSLRYELLEDKSQATEELAILIHKLSEKLNPSMLRCE
  
Inhibitor
Name:
BDBM50439228
Synonyms:
CHEMBL2418822
Type:
Small organic molecule
Emp. Form.:
C16H17ClFN3OS
Mol. Mass.:
353.842
SMILES:
CC1CCN(CC1)C(=O)c1csc(Nc2ccc(Cl)cc2F)n1
Structure:
Search PDB for entries with ligand similarity: