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Target
Apelin receptor
Ligand
BDBM269522
Substrate
n/a
Meas. Tech.
[35S]GTPgammaS Binding Assay
pH
7.5±n/a
EC50
540±n/a nM
Comments
extracted
Citation
 Chen, N; Chen, X; Chen, Y; Fu, Z; Heath, JA; Horne, DB; Kaller, MR; Khakoo, AY; Kopecky, DJ; Ma, Z; Mihalic, JT; Swaminath, G; Wang, X; Yeh, W Methods of treating heart failure US Patent  US10058550 Publication Date 8/28/2018 
Target
Name:
Apelin receptor
Synonyms:
AGTRL1 | APJ | APJ_HUMAN | APLNR | Angiotensin receptor-like 1 | Apelin receptor | Apelin receptor (APJ) | G-protein coupled receptor APJ | G-protein coupled receptor HG11
Type:
Enzyme Catalytic Domain
Mol. Mass.:
42664.06
Organism:
Homo sapiens (Human)
Description:
P35414
Residue:
380
Sequence:
MEEGGDFDNYYGADNQSECEYTDWKSSGALIPAIYMLVFLLGTTGNGLVLWTVFRSSREKRRSADIFIASLAVADLTFVVTLPLWATYTYRDYDWPFGTFFCKLSSYLIFVNMYASVFCLTGLSFDRYLAIVRPVANARLRLRVSGAVATAVLWVLAALLAMPVMVLRTTGDLENTTKVQCYMDYSMVATVSSEWAWEVGLGVSSTTVGFVVPFTIMLTCYFFIAQTIAGHFRKERIEGLRKRRRLLSIIVVLVVTFALCWMPYHLVKTLYMLGSLLHWPCDFDLFLMNIFPYCTCISYVNSCLNPFLYAFFDPRFRQACTSMLCCGQSRCAGTSHSSSGEKSASYSSGHSQGPGPNMGKGGEQMHEKSIPYSQETLVVD
  
Inhibitor
Name:
BDBM269522
Synonyms:
(1R,2S)-N-(4-(3,5-bis(trifluoromethyl)phenyl)-5-(6-methoxy-2-pyridinyl)-4H-1,2,4-triazol-3-yl)-1-methoxy-1-(5-methyl-2-pyrimidinyl)-2-propanesulfonamide | US10058550, Example 39.0 | US10221162, Example 39.0 | US9845310, Example 39.0
Type:
Small organic molecule
Emp. Form.:
C25H23F6N7O4S
Mol. Mass.:
631.55
SMILES:
CO[C@@H]([C@H](C)S(=O)(=O)Nc1nnc(-c2cccc(OC)n2)n1-c1cc(cc(c1)C(F)(F)F)C(F)(F)F)c1ncc(C)cn1 |r|
Structure:
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