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TargetEndothelin receptor type B
LigandBDBM50395631
Substrate/Competitorn/a
Meas. Tech.ChEMBL_859880 (CHEMBL2166381)
IC50 461±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
Blast this sequence in BindingDB or PDB
  Blast E-value cutoff:
BDBM50395631
n/a
NameBDBM50395631
Synonyms:CHEMBL2165334
TypeSmall organic molecule
Emp. Form.C23H20Br2N6O4S
Mol. Mass.636.316
SMILESBrc1ccc(cc1)-c1c(NS(=O)(=O)NCc2ccccc2)ncnc1OCCOc1ncc(Br)cn1
Structure
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