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Name | Cannabinoid receptor 1 |
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Species | Rattus norvegicus (Rat) |
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 | MKSILDGLADTTFRTITTDLLYVGSNDIQYEDIKGDMASKLGYFPQKFPLTSFRGSPFQEKMTAGDNSPLVPAGDTTNITEFYNKSLSSFKENEENIQCGENFMDMECFMILNPSQQLAIAVLSLTLGTFTVLENLLVLCVILHSRSLRCRPSYHFIGSLAVADLLGSVIFVYSFVDFHVFHRKDSPNVFLFKLGGVTASFTASVGSLFLTAIDRYISIHRPLAYKRIVTRPKAVVAFCLMWTIAIVIAVLPLLGWNCKKLQSVCSDIFPLIDETYLMFWIGVTSVLLLFIVYAYMYILWKAHSHAVRMIQRGTQKSIIIHTSEDGKVQVTRPDQARMDIRLAKTLVLILVVLIICWGPLLAIMVYDVFGKMNKLIKTVFAFCSMLCLLNSTVNPIIYALRSKDLRHAFRSMFPSCEGTAQPLDNSMGDSDCLHKHANNTASMHRAAESCIKSTVKIAKVTMSVSTDTSAEAL |
UniProt | P20272 |
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 | CHEMBL3571 |
IUPHAR | 56 |
DrugBank | N/A |
Name | AM251 |
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Molecular formula | C22H21Cl2IN4O |
IUPAC name | 1-(2,4-dichlorophenyl)-5-(4-iodophenyl)-4-methyl-N-piperidin-1-ylpyrazole-3-carboxamide |
Molecular weight | 555.241 |
Hydrogen bond acceptor | 3 |
Hydrogen bond donor | 1 |
XlogP | 6.5 |
Synonyms | HY-15443 KBioGR_000245 MolPort-003-983-507 1H-Pyrazole-3-carboxamide,1-(2,4-dichlorophenyl)-5-(4-iodophenyl)-4-methyl-N-1-piperidinyl- NCGC00025011-03 [ Show all ] |
Inchi Key | BUZAJRPLUGXRAB-UHFFFAOYSA-N |
Inchi ID | InChI=1S/C22H21Cl2IN4O/c1-14-20(22(30)27-28-11-3-2-4-12-28)26-29(19-10-7-16(23)13-18(19)24)21(14)15-5-8-17(25)9-6-15/h5-10,13H,2-4,11-12H2,1H3,(H,27,30) |
PubChem CID | 2125 |
ChEMBL | CHEMBL285932 |
IUPHAR | 3317 |
BindingDB | 21279 |
DrugBank | N/A |
Structure | |
Lipinski's druglikeness | This ligand is heavier than 500 daltons. This ligand has a partition coefficient log P greater than 5. |
Parameter | Value | Reference | Database source |
---|---|---|---|
Activity | 35.0 % | PMID25752982 | ChEMBL |
Inhibition | 38.0 % | PMID26344596 | ChEMBL |
Ki | 0.6 nM | PMID12570386 | BindingDB,ChEMBL |
Ki | 6.0 nM | PMID11906286 | BindingDB,ChEMBL |
Ki | 7.49 nM | PMID10052983 | BindingDB,ChEMBL |
Ki | 7.94 nM | PMID10052983 | IUPHAR |
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