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TargetEndothelin receptor type B
LigandBDBM50395636
Substrate/Competitorn/a
Meas. Tech.ChEMBL_859880 (CHEMBL2166381)
IC50 457±n/a nM
Citation Bolli, MHBoss, CBinkert, CBuchmann, SBur, DHess, PIglarz, MMeyer, SRein, JRey, MTreiber, AClozel, MFischli, WWeller, T The discovery of N-[5-(4-bromophenyl)-6-[2-[(5-bromo-2-pyrimidinyl)oxy]ethoxy]-4-pyrimidinyl]-N'-propylsulfamide (Macitentan), an orally active, potent dual endothelin receptor antagonist. J Med Chem55:7849-61 (2012) [PubMed]  Article
More Info.:Get all data from this article,  Assay Method
 
Endothelin receptor type B
Name:Endothelin receptor type B
Synonyms:EDNRB | EDNRB_HUMAN | ENDOTHELIN B | ET-B | ETRB | Endothelin receptor ET-B | Endothelin receptor non-selective type | Endothelin receptor, ET-A/ET-B
Type:Enzyme Catalytic Domain
Mol. Mass.:49664.00
Organism:Homo sapiens (Human)
Description:ENDOTHELIN B EDNRB HUMAN::P24530
Residue:442
Sequence:
MQPPPSLCGRALVALVLACGLSRIWGEERGFPPDRATPLLQTAEIMTPPTKTLWPKGSNA
SLARSLAPAEVPKGDRTAGSPPRTISPPPCQGPIEIKETFKYINTVVSCLVFVLGIIGNS
TLLRIIYKNKCMRNGPNILIASLALGDLLHIVIDIPINVYKLLAEDWPFGAEMCKLVPFI
QKASVGITVLSLCALSIDRYRAVASWSRIKGIGVPKWTAVEIVLIWVVSVVLAVPEAIGF
DIITMDYKGSYLRICLLHPVQKTAFMQFYKTAKDWWLFSFYFCLPLAITAFFYTLMTCEM
LRKKSGMQIALNDHLKQRREVAKTVFCLVLVFALCWLPLHLSRILKLTLYNQNDPNRCEL
LSFLLVLDYIGINMASLNSCINPIALYLVSKRFKNCFKSCLCCWCQSFEEKQSLEEKQSC
LKFKANDHGYDNFRSSNKYSSS
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  Blast E-value cutoff:
BDBM50395636
n/a
NameBDBM50395636
Synonyms:CHEMBL2165329
TypeSmall organic molecule
Emp. Form.C24H23BrN6O6S
Mol. Mass.603.445
SMILESCOc1cccc(Oc2c(NS(=O)(=O)NCc3ccccc3)ncnc2OCCOc2ncc(Br)cn2)c1
Structure
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