Reaction Details Report a problem with these data
Target
Melanin-concentrating hormone receptor 1
Ligand
BDBM50492361
Substrate
n/a
Meas. Tech.
ChEMBL_971498 (CHEMBL2406560)
EC50
20±n/a nM
Citation
Qian, Y; Conde-Knape, K; Erickson, SD; Falcioni, F; Gillespie, P; Hakimi, I; Mennona, F; Ren, Y; Salari, H; So, SS; Tilley, JW Potent MCH-1 receptor antagonists from cis-1,4-diaminocyclohexane-derived indane analogs. Bioorg Med Chem Lett 23:4216-20 (2013) [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:
BDBM50492361
Synonyms:
CHEMBL2403864
Type:
Small organic molecule
Emp. Form.:
C28H34N4O
Mol. Mass.:
442.5958
SMILES:
Cc1ccc2n([C@@H]3CC[C@@H](CC3)NC[C@H]3Cc4ccc(cc4C3)C#N)c(nc2c1)C(C)(C)O |r,wU:6.5,9.12,14.14,(36.65,-12.27,;38.17,-12,;39.16,-13.18,;40.68,-12.9,;41.21,-11.45,;42.62,-10.88,;43.96,-11.65,;43.9,-13.21,;45.22,-14.03,;46.57,-13.31,;46.63,-11.75,;45.31,-10.93,;47.9,-14.1,;49.24,-13.34,;49.26,-11.8,;48.01,-10.88,;48.5,-9.42,;47.75,-8.1,;48.53,-6.78,;50.07,-6.79,;50.82,-8.13,;50.04,-9.44,;50.5,-10.91,;50.84,-5.46,;51.62,-4.14,;42.52,-9.32,;41.02,-8.96,;40.21,-10.27,;38.68,-10.55,;43.69,-8.32,;42.91,-6.99,;44.46,-6.98,;45.14,-8.85,)|