Reaction Details |
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Target | Cannabinoid receptor 2 |
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Ligand | BDBM29076 |
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Substrate/Competitor | BDBM21244 |
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Meas. Tech. | CB1 Radioligand Binding Assay (Ki) and GTP-gamma-[35S] Binding Assay (EC50) |
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Ki | >10000±n/a nM |
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Citation | Dow, RL; Carpino, PA; Hadcock, JR; Black, SC; Iredale, PA; DaSilva-Jardine, P; Schneider, SR; Paight, ES; Griffith, DA; Scott, DO; O'Connor, RE; Nduaka, CI Discovery of 2-(2-chlorophenyl)-3-(4-chlorophenyl)-7-(2,2-difluoropropyl)-6,7-dihydro-2H-pyrazolo[3,4-f][1,4]oxazepin-8(5H)-one (PF-514273), a novel, bicyclic lactam-based cannabinoid-1 receptor antagonist for the treatment of obesity. J Med Chem52:2652-5 (2009) [PubMed] Article |
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More Info.: | Get all data from this article, Solution Info, Assay Method |
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Cannabinoid receptor 2 |
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Name: | Cannabinoid receptor 2 |
Synonyms: | CANNABINOID CB2 | CB-2 | CB2 | CB2A | CB2B | CNR2 | CNR2_HUMAN | CX5 | Cannabinoid CB2 receptor | Cannabinoid receptor 2 (CB2) | Cannabinoid receptor 2 (CB2R) | hCB2 |
Type: | G Protein-Coupled Receptor (GPCR) |
Mol. Mass.: | 39690.94 |
Organism: | Homo sapiens (Human) |
Description: | P34972 |
Residue: | 360 |
Sequence: | MEECWVTEIANGSKDGLDSNPMKDYMILSGPQKTAVAVLCTLLGLLSALENVAVLYLILS
SHQLRRKPSYLFIGSLAGADFLASVVFACSFVNFHVFHGVDSKAVFLLKIGSVTMTFTAS
VGSLLLTAIDRYLCLRYPPSYKALLTRGRALVTLGIMWVLSALVSYLPLMGWTCCPRPCS
ELFPLIPNDYLLSWLLFIAFLFSGIIYTYGHVLWKAHQHVASLSGHQDRQVPGMARMRLD
VRLAKTLGLVLAVLLICWFPVLALMAHSLATTLSDQVKKAFAFCSMLCLINSMVNPVIYA
LRSGEIRSSAHHCLAHWKKCVRGLGSEAKEEAPRSSVTETEADGKITPWPDSRDLDLSDC
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BDBM29076 |
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BDBM21244 |
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Name | BDBM29076 |
Synonyms: | ether-based lactam, 19e |
Type | Small organic molecule |
Emp. Form. | C22H19Cl2F2N3O2 |
Mol. Mass. | 466.308 |
SMILES | CCC(F)(F)CN1CCOc2c(nn(c2-c2ccc(Cl)cc2)-c2ccccc2Cl)C1=O |
Structure |
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