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Target
Melanin-concentrating hormone receptor 1
Ligand
BDBM50174899
Substrate
n/a
Meas. Tech.
ChEMBL_326797 (CHEMBL860146)
IC50
20±n/a nM
Citation
Vasudevan, A; Souers, AJ; Freeman, JC; Verzal, MK; Gao, J; Mulhern, MM; Wodka, D; Lynch, JK; Engstrom, KM; Wagaw, SH; Brodjian, S; Dayton, B; Falls, DH; Bush, E; Brune, M; Shapiro, RD; Marsh, KC; Hernandez, LE; Collins, CA; Kym, PR Aminopiperidine indazoles as orally efficacious melanin concentrating hormone receptor-1 antagonists. Bioorg Med Chem Lett 15:5293-7 (2005) [PubMed] Article
More Info.:
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:
BDBM50174899
Synonyms:
(3-(1-(benzo[d][1,3]dioxol-5-ylmethyl)piperidin-4-ylamino)-5-chloro-1H-indazol-1-yl)(thiazol-4-yl)methanone | CHEMBL198835
Type:
Small organic molecule
Emp. Form.:
C24H22ClN5O3S
Mol. Mass.:
495.981
SMILES:
Clc1ccc2n(nc(NC3CCN(Cc4ccc5OCOc5c4)CC3)c2c1)C(=O)c1cscn1