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Target
Transient receptor potential cation channel subfamily M member 4
Ligand
BDBM50602162
Substrate
n/a
Meas. Tech.
ChEMBL_2239340 (CHEMBL5153236)
EC50
1349±n/a nM
Citation
 Sabat, M; Raveglia, LF; Aldegheri, L; Barilli, A; Bianchi, F; Brault, L; Brodbeck, D; Feriani, A; Lingard, I; Miura, J; Myers, R; Piccoli, L; Tassini, S; Tyhonas, J; Ton-Nu, T; Wang, H; Virginio, C The discovery of (1R, 3R)-1-(3-chloro-5-fluorophenyl)-3-(hydroxymethyl)-1,2,3,4-tetrahydroisoquinoline-6-carbonitrile, a potent and selective agonist of human transient receptor potential cation channel subfamily m member 5 (TRPM5) and evaluation of as a potential gastrointestinal prokinetic agent. Bioorg Med Chem 76:0 (2022) [PubMed] 
Target
Name:
Transient receptor potential cation channel subfamily M member 4
Synonyms:
Calcium-activated non-selective cation channel 1 | LTRPC4 | LTrpC-4 | Long transient receptor potential channel 4 | Melastatin-4 | TRPM4 | TRPM4_HUMAN | Transient receptor potential cation channel subfamily M member 4 | hTRPM4
Type:
PROTEIN
Mol. Mass.:
134320.63
Organism:
Homo sapiens
Description:
ChEMBL_103788
Residue:
1214
Sequence:
MVVPEKEQSWIPKIFKKKTCTTFIVDSTDPGGTLCQCGRPRTAHPAVAMEDAFGAAVVTVWDSDAHTTEKPTDAYGELDFTGAGRKHSNFLRLSDRTDPAAVYSLVTRTWGFRAPNLVVSVLGGSGGPVLQTWLQDLLRRGLVRAAQSTGAWIVTGGLHTGIGRHVGVAVRDHQMASTGGTKVVAMGVAPWGVVRNRDTLINPKGSFPARYRWRGDPEDGVQFPLDYNYSAFFLVDDGTHGCLGGENRFRLRLESYISQQKTGVGGTGIDIPVLLLLIDGDEKMLTRIENATQAQLPCLLVAGSGGAADCLAETLEDTLAPGSGGARQGEARDRIRRFFPKGDLEVLQAQVERIMTRKELLTVYSSEDGSEEFETIVLKALVKACGSSEASAYLDELRLAVAWNRVDIAQSELFRGDIQWRSFHLEASLMDALLNDRPEFVRLLISHGLSLGHFLTPMRLAQLYSAAPSNSLIRNLLDQASHSAGTKAPALKGGAAELRPPDVGHVLRMLLGKMCAPRYPSGGAWDPHPGQGFGESMYLLSDKATSPLSLDAGLGQAPWSDLLLWALLLNRAQMAMYFWEMGSNAVSSALGACLLLRVMARLEPDAEEAARRKDLAFKFEGMGVDLFGECYRSSEVRAARLLLRRCPLWGDATCLQLAMQADARAFFAQDGVQSLLTQKWWGDMASTTPIWALVLAFFCPPLIYTRLITFRKSEEEPTREELEFDMDSVINGEGPVGTADPAEKTPLGVPRQSGRPGCCGGRCGGRRCLRRWFHFWGAPVTIFMGNVVSYLLFLLLFSRVLLVDFQPAPPGSLELLLYFWAFTLLCEELRQGLSGGGGSLASGGPGPGHASLSQRLRLYLADSWNQCDLVALTCFLLGVGCRLTPGLYHLGRTVLCIDFMVFTVRLLHIFTVNKQLGPKIVIVSKMMKDVFFFLFFLGVWLVAYGVATEGLLRPRDSDFPSILRRVFYRPYLQIFGQIPQEDMDVALMEHSNCSSEPGFWAHPPGAQAGTCVSQYANWLVVLLLVIFLLVANILLVNLLIAMFSYTFGKVQGNSDLYWKAQRYRLIREFHSRPALAPPFIVISHLRLLLRQLCRRPRSPQPSSPALEHFRVYLSKEAERKLLTWESVHKENFLLARARDKRESDSERLKRTSQKVDLALKQLGHIREYEQRLKVLEREVQQCSRVLGWVAEALSRSALLPPGGPPPPDLPGSKD
  
Inhibitor
Name:
BDBM50602162
Synonyms:
CHEMBL5194924
Type:
Small organic molecule
Emp. Form.:
C16H14Cl2FNO
Mol. Mass.:
326.193
SMILES:
OC[C@@H]1Cc2ccc(Cl)cc2[C@@H](N1)c1cc(F)cc(Cl)c1 |r|
Structure:
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