Reaction Details
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Alpha-2A/Alpha-2B/Alpha-2C adrenergic receptor
Ligand
BDBM50284690
Substrate
n/a
Meas. Tech.
ChEMBL_32906 (CHEMBL872334)
IC50
>10000±n/a nM
Citation
Marfat, A; Chambers, R; Cheng, J; Cooper, K; Damon, D; Delehunt, J; Eggler, J; Masamune, H; Melvin, L; Watson, J The discovery of CP-96,021 and CP-96,486, balanced, combined, potent and orally active leukotriene D4 (LTD4)/platelet activating factor (PAF) receptor antagonists. Bioorg Med Chem Lett 5:1377-1382 (1995) Article More Info.:
Target
Name:
Alpha-2A/Alpha-2B/Alpha-2C adrenergic receptor
Synonyms:
Adrenergic receptor alpha-2 | Adrenergic Receptors (alpha 2)
Type:
n/a
Mol. Mass.:
n/a
Description:
ASSAY_ID of ChEMBL is 305672
Components:
This complex has 3 components.
Component 1
Name:
Alpha-2B adrenergic receptor
Synonyms:
ADA2B_HUMAN | ADRA2B | ADRA2L1 | ADRA2RL1 | Adrenergic alpha2B | Adrenergic receptor | Adrenergic receptor alpha | Adrenergic, alpha-2B-, receptor [Homo sapiens] | Alpha-2 adrenergic receptor subtype C2 | Alpha-2B adrenoceptor | Alpha-2B adrenoreceptor | Alpha-2BAR
Type:
Enzyme
Mol. Mass.:
49964.20
Organism:
Human
Description:
P18089
Residue:
450
Sequence:
MDHQDPYSVQATAAIAAAITFLILFTIFGNALVILAVLTSRSLRAPQNLFLVSLAAADILVATLIIPFSLANELLGYWYFRRTWCEVYLALDVLFCTSSIVHLCAISLDRYWAVSRALEYNSKRTPRRIKCIILTVWLIAAVISLPPLIYKGDQGPQPRGRPQCKLNQEAWYILASSIGSFFAPCLIMILVYLRIYLIAKRSNRRGPRAKGGPGQGESKQPRPDHGGALASAKLPALASVASAREVNGHSKSTGEKEEGETPEDTGTRALPPSWAALPNSGQGQKEGVCGASPEDEAEEEEEEEEEEEECEPQAVPVSPASACSPPLQQPQGSRVLATLRGQVLLGRGVGAIGGQWWRRRAQLTREKRFTFVLAVVIGVFVLCWFPFFFSYSLGAICPKHCKVPHGLFQFFFWIGYCNSSLNPVIYTIFNQDFRRAFRRILCRPWTQTAW
Component 2
Name:
Alpha-2A adrenergic receptor
Synonyms:
ADRA2R | Adrenergic receptor alpha | ADRA2A | Adrenergic alpha2A | Alpha-2 adrenergic receptor subtype C10 | alpha-2A adrenergic receptor [Homo sapiens] | ADRAR | ADA2A_HUMAN | Alpha-2AAR | Alpha-2A adrenoceptor | Alpha-2A adrenoreceptor
Type:
Enzyme
Mol. Mass.:
48979.91
Organism:
Human
Description:
P08913
Residue:
465
Sequence:
MFRQEQPLAEGSFAPMGSLQPDAGNASWNGTEAPGGGARATPYSLQVTLTLVCLAGLLMLLTVFGNVLVIIAVFTSRALKAPQNLFLVSLASADILVATLVIPFSLANEVMGYWYFGKAWCEIYLALDVLFCTSSIVHLCAISLDRYWSITQAIEYNLKRTPRRIKAIIITVWVISAVISFPPLISIEKKGGGGGPQPAEPRCEINDQKWYVISSCIGSFFAPCLIMILVYVRIYQIAKRRTRVPPSRRGPDAVAAPPGGTERRPNGLGPERSAGPGGAEAEPLPTQLNGAPGEPAPAGPRDTDALDLEESSSSDHAERPPGPRRPERGPRGKGKARASQVKPGDSLPRRGPGATGIGTPAAGPGEERVGAAKASRWRGRQNREKRFTFVLAVVIGVFVVCWFPFFFTYTLTAVGCSVPRTLFKFFFWFGYCNSSLNPVIYTIFNHDFRRAFKKILCRGDRKRIV
Component 3
Name:
Alpha-2C adrenergic receptor
Synonyms:
Adrenergic alpha2C | Adrenergic receptor alpha | Adrenergic, alpha-2C-, receptor | Alpha-2 adrenergic receptor subtype C4 | Alpha-2C adrenoceptor | Alpha-2C adrenoreceptor | adrenergic, alpha-2C-, receptor [Homo sapiens] | ADA2C_HUMAN | ADRA2C | ADRA2L2 | ADRA2RL2 | Adrenergic receptor
Type:
Enzyme
Mol. Mass.:
49552.32
Organism:
Human
Description:
P18825
Residue:
462
Sequence:
MASPALAAALAVAAAAGPNASGAGERGSGGVANASGASWGPPRGQYSAGAVAGLAAVVGFLIVFTVVGNVLVVIAVLTSRALRAPQNLFLVSLASADILVATLVMPFSLANELMAYWYFGQVWCGVYLALDVLFCTSSIVHLCAISLDRYWSVTQAVEYNLKRTPRRVKATIVAVWLISAVISFPPLVSLYRQPDGAAYPQCGLNDETWYILSSCIGSFFAPCLIMGLVYARIYRVAKLRTRTLSEKRAPVGPDGASPTTENGLGAAAGAGENGHCAPPPADVEPDESSAAAERRRRRGALRRGGRRRAGAEGGAGGADGQGAGPGAAESGALTASRSPGPGGRLSRASSRSVEFFLSRRRRARSSVCRRKVAQAREKRFTFVLAVVMGVFVLCWFPFFFSYSLYGICREACQVPGPLFKFFFWIGYCNSSLNPVIYTVFNQDFRRSFKHILFRRRRRGFRQ
Inhibitor
Name:
BDBM50284690
Synonyms:
CP-96021 | 1-(4-{3-[(E)-2-(5-Fluoro-benzothiazol-2-yl)-vinyl]-benzyloxy}-phenyl)-2-methyl-1H-imidazo[4,5-c]pyridine | CHEMBL31714
Type:
Small organic molecule
Emp. Form.:
C29 H21 F N4 O S
Mol. Mass.:
492.56664
SMILES:
Cc1nc2cnccc2n1-c1ccc(OCc2cccc(\C=C\c3nc4cc(F)ccc4s3)c2)cc1
