Ki Summary BindingDB logo
myBDB logout
Reaction Details
Report a problem with these data
TargetMelanin-concentrating hormone receptor 1
LigandBDBM50170187
Substrate/Competitorn/a
Meas. Tech.ChEMBL_306788 (CHEMBL832373)
IC50 5800±n/a nM
Citation Kanuma, KOmodera, KNishiguchi, MFunakoshi, TChaki, SSemple, GTran, TAKramer, BHsu, DCasper, MThomsen, BSekiguchi, Y Lead optimization of 4-(dimethylamino)quinazolines, potent and selective antagonists for the melanin-concentrating hormone receptor 1. Bioorg Med Chem Lett15:3853-6 (2005) [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
Blast this sequence in BindingDB or PDB
  Blast E-value cutoff:
BDBM50170187
n/a
NameBDBM50170187
Synonyms:CHEMBL181727 | trans-4-Bromo-N-{4-[(4-dimethylamino-quinazolin-2-ylamino)-methyl]-cyclohexylmethyl}-N-methyl-2-trifluoromethoxy-benzenesulfonamide
TypeSmall organic molecule
Emp. Form.C26H31BrF3N5O3S
Mol. Mass.630.52
SMILESCN(C)c1nc(NCC2CCC(CN(C)S(=O)(=O)c3ccc(Br)cc3OC(F)(F)F)CC2)nc2ccccc12 |(-6.25,5.67,;-7.59,4.9,;-8.94,5.67,;-7.59,3.36,;-6.25,2.59,;-6.25,1.04,;-4.9,.25,;-3.57,1.03,;-2.24,.26,;-2.24,-1.27,;-.93,-2.04,;.42,-1.29,;1.75,-2.06,;3.08,-1.29,;3.07,.26,;4.42,-2.06,;4.4,-3.6,;4.4,-.51,;5.75,-1.27,;5.73,.26,;7.06,1.04,;8.4,.28,;9.73,1.07,;8.41,-1.26,;7.09,-2.04,;7.09,-3.58,;8.42,-4.35,;9.65,-5.05,;8.69,-5.93,;9.94,-3.77,;.42,.25,;-.91,1.03,;-7.59,.27,;-8.92,1.04,;-10.25,.27,;-11.59,1.04,;-11.59,2.57,;-10.25,3.36,;-8.92,2.59,)|
Structure
Search PDB for entries with ligand similarity:Similarity to this molecule at least: