Target
Apelin receptor
Ligand
BDBM480997
Substrate
n/a
Meas. Tech.
[35S]GTPγS Binding Assay
EC50
6.80±n/a nM
Citation
 Chen, NChen, YDebenedetto, MVDransfield, PJHarvey, JSHeath, JAHouze, JKhakoo, AYLai, SMa, ZNishimura, NPattaropong, VSwaminath, GYeh, WKreiman, C Triazole phenyl compounds as agonists of the APJ receptor US Patent  US10906890 Publication Date 2/2/2021 
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:
BDBM480997
Synonyms:
US10906890, Example 6.0
Type:
Small organic molecule
Emp. Form.:
C24H28N8O6S
Mol. Mass.:
556.594
SMILES:
CO[C@@H]([C@H](C)S(=O)(=O)Nc1nnc(-c2cccc(OC)c2)n1-c1c(OC)ncnc1OC)c1ncc(C)cn1 |r,wU:3.3,2.1,(4.32,-3.71,;5.41,-2.62,;5.01,-1.13,;3.52,-.73,;3.12,.76,;2.43,-1.82,;1.34,-2.91,;3.77,-2.59,;1.1,-1.05,;-.23,-1.82,;-.71,-3.28,;-2.25,-3.28,;-2.73,-1.82,;-4.21,-1.42,;-4.61,.07,;-6.1,.47,;-7.19,-.62,;-6.79,-2.11,;-7.88,-3.2,;-9.37,-2.8,;-5.3,-2.51,;-1.48,-.91,;-1.48,.63,;-2.81,1.4,;-4.15,.63,;-5.48,1.4,;-2.81,2.94,;-1.48,3.71,;-.15,2.94,;-.15,1.4,;1.19,.63,;2.52,1.4,;6.1,-.04,;7.59,-.44,;8.68,.65,;8.28,2.14,;9.37,3.23,;6.79,2.54,;5.7,1.45,)|
Structure:
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