| Reaction Details |
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 | Report a problem with these data |
| Target | Endothelin receptor type B |
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| Ligand | BDBM50058126 |
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| Substrate/Competitor | n/a |
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| Meas. Tech. | ChEMBL_64214 (CHEMBL675451) |
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| IC50 | 9.80±n/a nM |
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| Citation |  Wu, C; Decker, ER; Blok, N; Bui, H; You, TJ; Wang, J; Bourgoyne, AR; Knowles, V; Berens, KL; Holland, GW; Brock, TA; Dixon, RA Discovery, modeling, and human pharmacokinetics of N-(2-acetyl-4,6-dimethylphenyl)-3-(3,4-dimethylisoxazol-5-ylsulfamoyl)thiophene-2-carboxamide (TBC3711), a second generation, ETA selective, and orally bioavailable endothelin antagonist. J Med Chem47:1969-86 (2004) [PubMed] Article |
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| More Info.: | Get all data from this article, Assay Method |
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| Endothelin receptor type B |
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| Name: | Endothelin receptor type B |
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| Synonyms: | EDNRB | EDNRB_HUMAN | ENDOTHELIN B | ET-B | ETRB | Endothelin receptor ET-B | Endothelin receptor non-selective type | Endothelin receptor, ET-A/ET-B |
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| Type: | Enzyme Catalytic Domain |
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| Mol. Mass.: | 49664.00 |
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| Organism: | Homo sapiens (Human) |
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| Description: | ENDOTHELIN B EDNRB HUMAN::P24530 |
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| Residue: | 442 |
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| Sequence: | MQPPPSLCGRALVALVLACGLSRIWGEERGFPPDRATPLLQTAEIMTPPTKTLWPKGSNA
SLARSLAPAEVPKGDRTAGSPPRTISPPPCQGPIEIKETFKYINTVVSCLVFVLGIIGNS
TLLRIIYKNKCMRNGPNILIASLALGDLLHIVIDIPINVYKLLAEDWPFGAEMCKLVPFI
QKASVGITVLSLCALSIDRYRAVASWSRIKGIGVPKWTAVEIVLIWVVSVVLAVPEAIGF
DIITMDYKGSYLRICLLHPVQKTAFMQFYKTAKDWWLFSFYFCLPLAITAFFYTLMTCEM
LRKKSGMQIALNDHLKQRREVAKTVFCLVLVFALCWLPLHLSRILKLTLYNQNDPNRCEL
LSFLLVLDYIGINMASLNSCINPIALYLVSKRFKNCFKSCLCCWCQSFEEKQSLEEKQSC
LKFKANDHGYDNFRSSNKYSSS
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| BDBM50058126 |
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| n/a |
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| Name | BDBM50058126 |
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| Synonyms: | 2-[2-(6-Methyl-benzo[1,3]dioxol-5-yl)-acetyl]-thiophene-3-sulfonic acid (4-chloro-3-methyl-isoxazol-5-yl)-amide | 2-[2-(6-Methyl-benzo[1,3]dioxol-5-yl)-acetyl]-thiophene-3-sulfonic acid (4-chloro-3-methyl-isoxazol-5-yl)-amide (Sitaxsentan) | 2-{[3-(4-Chloro-3-methyl-isoxazol-5-ylsulfamoyl)-thiophene-2-carbonyl]-amino}-5-methyl-benzoic acid isopropyl ester | CHEMBL282724 | Sitaxentan |
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| Type | Small organic molecule |
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| Emp. Form. | C18H15ClN2O6S2 |
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| Mol. Mass. | 454.905 |
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| SMILES | Cc1noc(NS(=O)(=O)c2ccsc2C(=O)Cc2cc3OCOc3cc2C)c1Cl |
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| Structure | 
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