Reaction Details |
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Target | 5-hydroxytryptamine receptor 2A/2B/2C |
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Ligand | BDBM50009073 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_2212 (CHEMBL617037) |
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IC50 | >10000±n/a nM |
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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 Lett5:1377-1382 (1995) Article |
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More Info.: | Get all data from this article, Assay Method |
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5-hydroxytryptamine receptor 2A/2B/2C |
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Name: | 5-hydroxytryptamine receptor 2A/2B/2C |
Synonyms: | Serotonin 2 (5-HT2) receptor |
Type: | n/a |
Mol. Mass.: | n/a |
Description: | ASSAY_ID of ChEMBL is 306637 |
Components: | This complex has 3 components. |
Component 1 |
Name: | 5-hydroxytryptamine receptor 2B |
Synonyms: | 5-HT-2B | 5-HT2B | 5-hydroxytryptamine (serotonin) receptor 2B [Homo sapiens] | 5-hydroxytryptamine receptor 2B (5-HT2B) | 5-hydroxytryptamine receptor 2C (5HT2C) | 5HT2B_HUMAN | HTR2B | Serotonin (5-HT3) receptor | Serotonin 2b (5-HT2b) receptor | Serotonin Receptor 2B |
Type: | G Protein-Coupled Receptor (GPCR) |
Mol. Mass.: | 54312.47 |
Organism: | Homo sapiens (Human) |
Description: | Receptor binding assays were performed using human clone stably expressed in CHO cells. |
Residue: | 481 |
Sequence: | MALSYRVSELQSTIPEHILQSTFVHVISSNWSGLQTESIPEEMKQIVEEQGNKLHWAALL
ILMVIIPTIGGNTLVILAVSLEKKLQYATNYFLMSLAVADLLVGLFVMPIALLTIMFEAM
WPLPLVLCPAWLFLDVLFSTASIMHLCAISVDRYIAIKKPIQANQYNSRATAFIKITVVW
LISIGIAIPVPIKGIETDVDNPNNITCVLTKERFGDFMLFGSLAAFFTPLAIMIVTYFLT
IHALQKKAYLVKNKPPQRLTWLTVSTVFQRDETPCSSPEKVAMLDGSRKDKALPNSGDET
LMRRTSTIGKKSVQTISNEQRASKVLGIVFFLFLLMWCPFFITNITLVLCDSCNQTTLQM
LLEIFVWIGYVSSGVNPLVYTLFNKTFRDAFGRYITCNYRATKSVKTLRKRSSKIYFRNP
MAENSKFFKKHGIRNGINPAMYQSPMRLRSSTIQSSSIILLDTLLLTENEGDKTEEQVSY
V
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Component 2 |
Name: | 5-hydroxytryptamine receptor 2C |
Synonyms: | 5-HT-2C | 5-HT2C | 5-HT2C-INI | 5-HT2c VGI | 5-HTR2C | 5-hydroxytryptamine receptor 1C | 5-hydroxytryptamine receptor 2C (5-HT-2C) | 5-hydroxytryptamine receptor 2C (5HT-2C) | 5HT-1C | 5HT2C_HUMAN | HTR1C | HTR2C | Serotonin (5-HT3) receptor | Serotonin 2c (5-HT2c) receptor | Serotonin Receptor 2C |
Type: | G Protein-Coupled Receptor (GPCR) |
Mol. Mass.: | 51836.79 |
Organism: | Homo sapiens (Human) |
Description: | P28335 |
Residue: | 458 |
Sequence: | MVNLRNAVHSFLVHLIGLLVWQCDISVSPVAAIVTDIFNTSDGGRFKFPDGVQNWPALSI
VIIIIMTIGGNILVIMAVSMEKKLHNATNYFLMSLAIADMLVGLLVMPLSLLAILYDYVW
PLPRYLCPVWISLDVLFSTASIMHLCAISLDRYVAIRNPIEHSRFNSRTKAIMKIAIVWA
ISIGVSVPIPVIGLRDEEKVFVNNTTCVLNDPNFVLIGSFVAFFIPLTIMVITYCLTIYV
LRRQALMLLHGHTEEPPGLSLDFLKCCKRNTAEEENSANPNQDQNARRRKKKERRPRGTM
QAINNERKASKVLGIVFFVFLIMWCPFFITNILSVLCEKSCNQKLMEKLLNVFVWIGYVC
SGINPLVYTLFNKIYRRAFSNYLRCNYKVEKKPPVRQIPRVAATALSGRELNVNIYRHTN
EPVIEKASDNEPGIEMQVENLELPVNPSSVVSERISSV
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Component 3 |
Name: | 5-hydroxytryptamine receptor 2A |
Synonyms: | 5-HT-2 | 5-HT-2A | 5-HT2A | 5-hydroxytryptamine receptor 2A (5-HT-2A) | 5-hydroxytryptamine receptor 2A (5HT-2A) | 5-hydroxytryptamine receptor 2A (5HT2A) | 5HT2A_HUMAN | HTR2 | HTR2A | Serotonin receptor 2A |
Type: | undefined |
Mol. Mass.: | 52607.65 |
Organism: | Homo sapiens (Human) |
Description: | P28223 |
Residue: | 471 |
Sequence: | MDILCEENTSLSSTTNSLMQLNDDTRLYSNDFNSGEANTSDAFNWTVDSENRTNLSCEGC
LSPSCLSLLHLQEKNWSALLTAVVIILTIAGNILVIMAVSLEKKLQNATNYFLMSLAIAD
MLLGFLVMPVSMLTILYGYRWPLPSKLCAVWIYLDVLFSTASIMHLCAISLDRYVAIQNP
IHHSRFNSRTKAFLKIIAVWTISVGISMPIPVFGLQDDSKVFKEGSCLLADDNFVLIGSF
VSFFIPLTIMVITYFLTIKSLQKEATLCVSDLGTRAKLASFSFLPQSSLSSEKLFQRSIH
REPGSYTGRRTMQSISNEQKACKVLGIVFFLFVVMWCPFFITNIMAVICKESCNEDVIGA
LLNVFVWIGYLSSAVNPLVYTLFNKTYRSAFSRYIQCQYKENKKPLQLILVNTIPALAYK
SSQLQMGQKKNSKQDAKTTDNDCSMVALGKQHSEEASKDNSDGVNEKVSCV
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BDBM50009073 |
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n/a |
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Name | BDBM50009073 |
Synonyms: | 4-(5-cyclopentyloxycarbonylamino-1-methyl-1H-indol-3-ylmethyl)-3-methoxy-N-o-tolylsulfonylbenzamide | CHEMBL603 | ZAFIRLUKAST | cyclopentyl 3-(2-methoxy-4-((o-tolylsulfonyl)carbamoyl)benzyl)-1-methylindole-5-carbamate | cyclopentyl 3-[2-methoxy-4-(2-methylphenylsulfonylcarbamoyl)benzyl]-1-methyl-1H-indol-5-ylcarbamate |
Type | Small organic molecule |
Emp. Form. | C31H33N3O6S |
Mol. Mass. | 575.675 |
SMILES | COc1cc(ccc1Cc1cn(C)c2ccc(NC(=O)OC3CCCC3)cc12)C(=O)NS(=O)(=O)c1ccccc1C |
Structure |
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