Target
Short transient receptor potential channel 3
Ligand
BDBM50439212
Substrate
n/a
Meas. Tech.
ChEMBL_978642 (CHEMBL2422305)
IC50
10000±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:
BDBM50439212
Synonyms:
CHEMBL2418816
Type:
Small organic molecule
Emp. Form.:
C21H20N4O3S
Mol. Mass.:
408.473
SMILES:
CC1N(CCc2ncccc12)C(=O)c1nc(Nc2ccc3OCOc3c2)sc1C
Structure:
Search PDB for entries with ligand similarity: