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Name | Cannabinoid receptor 1 |
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Species | Mus musculus (Mouse) |
Gene | Cnr1 |
Synonym | SKR6R Neuronal cannabinoid receptor Central cannabinoid receptor CB1R CB1 receptor [ Show all ] |
Disease | N/A for non-human GPCRs |
Length | 473 |
Amino acid sequence | MKSILDGLADTTFRTITTDLLYVGSNDIQYEDIKGDMASKLGYFPQKFPLTSFRGSPFQEKMTAGDNSPLVPAGDTTNITEFYNKSLSSFKENEDNIQCGENFMDMECFMILNPSQQLAIAVLSLTLGTFTVLENLLVLCVILHSRSLRCRPSYHFIGSLAVADLLGSVIFVYSFVDFHVFHRKDSPNVFLFKLGGVTASFTASVGSLFLTAIDRYISIHRPLAYKRIVTRPKAVVAFCLMWTIAIVIAVLPLLGWNCKKLQSVCSDIFPLIDETYLMFWIGVTSVLLLFIVYAYMYILWKAHSHAVRMIQRGTQKSIIIHTSEDGKVQVTRPDQARMDIRLAKTLVLILVVLIICWGPLLAIMVYDVFGKMNKLIKTVFAFCSMLCLLNSTVNPIIYALRSKDLRHAFRSMFPSCEGTAQPLDNSMGDSDCLHKHANNTASMHRAAESCIKSTVKIAKVTMSVSTDTSAEAL |
UniProt | P47746 |
Protein Data Bank | N/A |
GPCR-HGmod model | N/A |
3D structure model | No available structures or models |
BioLiP | N/A |
Therapeutic Target Database | N/A |
ChEMBL | CHEMBL3037 |
IUPHAR | 56 |
DrugBank | N/A |
Name | Rimonabant |
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Molecular formula | C22H21Cl3N4O |
IUPAC name | 5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-N-piperidin-1-ylpyrazole-3-carboxamide |
Molecular weight | 463.787 |
Hydrogen bond acceptor | 3 |
Hydrogen bond donor | 1 |
XlogP | 6.5 |
Synonyms | AM84578 SMR003500713 BCP07803 SR141716 CHEBI:34967 [ Show all ] |
Inchi Key | JZCPYUJPEARBJL-UHFFFAOYSA-N |
Inchi ID | InChI=1S/C22H21Cl3N4O/c1-14-20(22(30)27-28-11-3-2-4-12-28)26-29(19-10-9-17(24)13-18(19)25)21(14)15-5-7-16(23)8-6-15/h5-10,13H,2-4,11-12H2,1H3,(H,27,30) |
PubChem CID | 104850 |
ChEMBL | CHEMBL111 |
IUPHAR | 743 |
BindingDB | 21278 |
DrugBank | DB06155 |
Structure | |
Lipinski's druglikeness | This ligand has a partition coefficient log P greater than 5. |
Parameter | Value | Reference | Database source |
---|---|---|---|
Activity | <90.0 % | PMID23357307 | ChEMBL |
Activity | 108.0 % | PMID27240274 | ChEMBL |
EC50 | 8990.0 nM | PMID17870539 | BindingDB,ChEMBL |
Intrinsic activity | 110.0 % | PMID27240274 | ChEMBL |
Kd | 190.55 nM | PMID17870539 | ChEMBL |
Ki | 1.5 nM | PMID23357307 | BindingDB,ChEMBL |
Ki | 1.8 nM | PMID16279795, PMID27240274 | BindingDB,ChEMBL |
Ki | 2.8 nM | PMID27240274 | BindingDB |
Ki | 2.82 nM | PMID27240274 | ChEMBL |
Occ | 87.0 % | PMID22959249 | ChEMBL |
pKb | 8.4 - | PMID17582659 | ChEMBL |
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