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GLASS

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GPCR

Name	Melanin-concentrating hormone receptor 1
Species	Homo sapiens (Human)
Gene	MCHR1
Synonym	SLC-1 Somatostatin receptor-like protein MCHR-1 MCHR MCH1R MCH1 receptor MCH-R1 MCH-1R MCH receptor 1 GPR24 G-protein coupled receptor 24 G protein-coupled receptor 24 [ Show all ]
Disease	Obesity Obesity; Anxiety; Depression
Length	422
Amino acid sequence	MSVGAMKKGVGRAVGLGGGSGCQATEEDPLPNCGACAPGQGGRRWRLPQPAWVEGSSARLWEQATGTGWMDLEASLLPTGPNASNTSDGPDNLTSAGSPPRTGSISYINIIMPSVFGTICLLGIIGNSTVIFAVVKKSKLHWCNNVPDIFIINLSVVDLLFLLGMPFMIHQLMGNGVWHFGETMCTLITAMDANSQFTSTYILTAMAIDRYLATVHPISSTKFRKPSVATLVICLLWALSFISITPVWLYARLIPFPGGAVGCGIRLPNPDTDLYWFTLYQFFLAFALPFVVITAAYVRILQRMTSSVAPASQRSIRLRTKRVTRTAIAICLVFFVCWAPYYVLQLTQLSISRPTLTFVYLYNAAISLGYANSCLNPFVYIVLCETFRKRLVLSVKPAAQGQLRAVSNAQTADEERTESKGT
UniProt	Q99705
Protein Data Bank	N/A
GPCR-HGmod model	Q99705
3D structure model	This predicted structure model is from GPCR-EXP Q99705.
BioLiP	N/A
Therapeutic Target Database	T09572
ChEMBL	CHEMBL344
IUPHAR	280
DrugBank	BE0003478

Ligand

Name	CHEMBL179501
Molecular formula	C28H30N4O2
IUPAC name	2-(4-phenylmethoxyphenyl)-N-[1-(2-pyrrolidin-1-ylethyl)indazol-6-yl]acetamide
Molecular weight	454.574
Hydrogen bond acceptor	4
Hydrogen bond donor	1
XlogP	4.3
Synonyms	SCHEMBL6069656 2-(4-Benzyloxy-phenyl)-N-[1-(2-pyrrolidin-1-yl-ethyl)-1H-indazol-6-yl]-acetamide 2-(4-benzyloxyphenyl)-N-[1-(2-pyrrolidin-1-yl-ethyl)-1h-indazol-6-yl]acetamide BDBM50162116 2-(4-(benzyloxy)phenyl)-N-(1-(2-(pyrrolidin-1-yl)ethyl)-1H-indazol-6-yl)acetamide OMZPZOSWJGZBRV-UHFFFAOYSA-N 2-[4-(benzyloxy)phenyl]-N-[1-(2-pyrrolidin-1-ylethyl)-1H-indazol-6-yl]acetamide [ Show all ]
Inchi Key	OMZPZOSWJGZBRV-UHFFFAOYSA-N
Inchi ID	InChI=1S/C28H30N4O2/c33-28(18-22-8-12-26(13-9-22)34-21-23-6-2-1-3-7-23)30-25-11-10-24-20-29-32(27(24)19-25)17-16-31-14-4-5-15-31/h1-3,6-13,19-20H,4-5,14-18,21H2,(H,30,33)
PubChem CID	11775399
ChEMBL	CHEMBL179501
IUPHAR	N/A
BindingDB	50162116
DrugBank	N/A
Structure SDF download
Lipinski's druglikeness	This ligand satisfies Lipinski's rule of five.

Experimental Data

Parameter	Value	Reference	Database source
IC50	1.4 nM	PMID16570930, PMID15743174, PMID21190859	BindingDB,ChEMBL
IC50	11.0 nM	PMID15743174	ChEMBL

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