| Reaction Details |
|---|
 | Report a problem with these data |
| Target | Melanin-concentrating hormone receptor 1 |
|---|
| Ligand | BDBM50184921 |
|---|
| Substrate/Competitor | n/a |
|---|
| Meas. Tech. | ChEMBL_342542 (CHEMBL861585) |
|---|
| Ki | 2.8±n/a nM |
|---|
| Citation |  McBriar, MD; Guzik, H; Shapiro, S; Paruchova, J; Xu, R; Palani, A; Clader, JW; Cox, K; Greenlee, WJ; Hawes, BE; Kowalski, TJ; O'neill, K; Spar, BD; Weig, B; Weston, DJ; Farley, C; Cook, J Discovery of orally efficacious melanin-concentrating hormone receptor-1 antagonists as antiobesity agents. Synthesis, SAR, and biological evaluation of bicyclo[3.1.0]hexyl ureas. J Med Chem49:2294-310 (2006) [PubMed] Article |
|---|
| More Info.: | Get all data from this article, Assay Method |
|---|
| |
| Melanin-concentrating hormone receptor 1 |
|---|
| 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: | MSVGAMKKGVGRAVGLGGGSGCQATEEDPLPNCGACAPGQGGRRWRLPQPAWVEGSSARL
WEQATGTGWMDLEASLLPTGPNASNTSDGPDNLTSAGSPPRTGSISYINIIMPSVFGTIC
LLGIIGNSTVIFAVVKKSKLHWCNNVPDIFIINLSVVDLLFLLGMPFMIHQLMGNGVWHF
GETMCTLITAMDANSQFTSTYILTAMAIDRYLATVHPISSTKFRKPSVATLVICLLWALS
FISITPVWLYARLIPFPGGAVGCGIRLPNPDTDLYWFTLYQFFLAFALPFVVITAAYVRI
LQRMTSSVAPASQRSIRLRTKRVTRTAIAICLVFFVCWAPYYVLQLTQLSISRPTLTFVY
LYNAAISLGYANSCLNPFVYIVLCETFRKRLVLSVKPAAQGQLRAVSNAQTADEERTESK
GT
|
|
|
|---|
| BDBM50184921 |
|---|
| n/a |
|---|
| Name | BDBM50184921 |
|---|
| Synonyms: | CHEMBL204881 | N'-[4-fluoro-3-(trifluoromethyl)phenyl)-N-[trans-5-(4-methoxyphenyl)bicyclo[3.1.0]hex-2-yl]-N-[3-(4-methyl-1-piperazinyl)propyl]urea |
|---|
| Type | Small organic molecule |
|---|
| Emp. Form. | C29H36F4N4O2 |
|---|
| Mol. Mass. | 548.6154 |
|---|
| SMILES | COc1ccc(cc1)[C@@]12C[C@@H]1[C@@H](CC2)N(CCCN1CCN(C)CC1)C(=O)Nc1ccc(F)c(c1)C(F)(F)F |
|---|
| Structure | 
|
|---|
Search and Browse
