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Target
Melanin-concentrating hormone receptor 1
Ligand
BDBM50171590
Substrate
n/a
Meas. Tech.
ChEMBL_343377 (CHEMBL860697)
IC50
2±n/a nM
Citation
 Kym, PR; Souers, AJ; Campbell, TJ; Lynch, JK; Judd, AS; Iyengar, R; Vasudevan, A; Gao, J; Freeman, JC; Wodka, D; Mulhern, M; Zhao, G; Wagaw, SH; Napier, JJ; Brodjian, S; Dayton, BD; Reilly, RM; Segreti, JA; Fryer, RM; Preusser, LC; Reinhart, GA; Hernandez, L; Marsh, KC; Sham, HL; Collins, CA; Polakowski, JS Screening for cardiovascular safety: a structure-activity approach for guiding lead selection of melanin concentrating hormone receptor 1 antagonists. J Med Chem 49:2339-52 (2006) [PubMed]  Article 
Target
Name:
Melanin-concentrating hormone receptor 1
Synonyms:
G-protein coupled receptor 24 | GPR24 | MCH receptor 1 | MCH-1R | MCH-R1 | MCHR | MCHR-1 | MCHR1 | MCHR1_HUMAN | Melanin Concentrating Hormone 1 | Melanin-Concentrating Hormone Receptor 1 (MCH1R) | Melanin-concentrating hormone receptor | Melanin-concentrating hormone receptor 1 (MCH-1) | Melanin-concentrating hormone receptor 1 (MCH1) | Melanin-concentrating hormone receptor 1 (MCHR-1) | Melanin-concentrating hormone receptor 1 (MCHR1) | SLC-1 | SLC1 | Somatostatin receptor-like protein
Type:
G Protein-Coupled Receptor (GPCR)
Mol. Mass.:
45976.27
Organism:
Homo sapiens (Human)
Description:
Membranes from CHO-K1 cells stably expressing human MCH1R were used in assays.
Residue:
422
Sequence:
MSVGAMKKGVGRAVGLGGGSGCQATEEDPLPNCGACAPGQGGRRWRLPQPAWVEGSSARLWEQATGTGWMDLEASLLPTGPNASNTSDGPDNLTSAGSPPRTGSISYINIIMPSVFGTICLLGIIGNSTVIFAVVKKSKLHWCNNVPDIFIINLSVVDLLFLLGMPFMIHQLMGNGVWHFGETMCTLITAMDANSQFTSTYILTAMAIDRYLATVHPISSTKFRKPSVATLVICLLWALSFISITPVWLYARLIPFPGGAVGCGIRLPNPDTDLYWFTLYQFFLAFALPFVVITAAYVRILQRMTSSVAPASQRSIRLRTKRVTRTAIAICLVFFVCWAPYYVLQLTQLSISRPTLTFVYLYNAAISLGYANSCLNPFVYIVLCETFRKRLVLSVKPAAQGQLRAVSNAQTADEERTESKGT
  
Inhibitor
Name:
BDBM50171590
Synonyms:
CHEMBL194697 | N-(1-Benzo[1,3]dioxol-5-ylmethyl-piperidin-4-yl)-5-chloro-2-[(thiazol-2-ylmethyl)-amino]-benzamide | N-(1-benzo[1,3]dioxol-5-ylmethyl-piperidin-4-yl)-5-chloro-2-[(thiazol-2-ylmethyl)amino]benzamide
Type:
Small organic molecule
Emp. Form.:
C24H25ClN4O3S
Mol. Mass.:
484.998
SMILES:
Clc1ccc(NCc2nccs2)c(c1)C(=O)NC1CCN(Cc2ccc3OCOc3c2)CC1
Structure:
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