Reaction Details Report a problem with these data
Target
Apelin receptor
Ligand
BDBM406619
Substrate
n/a
Meas. Tech.
Intracellular cAMP Accumulation Assay
EC50
5.5±n/a nM
Citation
 Johnson, JA; Kim, S 4-hydroxy-3-(heteroaryl)pyridine-2-one APJ agonists US Patent  US10336739 Publication Date 7/2/2019 
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:
BDBM406619
Synonyms:
5-(2,6- dimethoxyphenyl)- 6-(ethoxymethyl)- 3-(5- {[1,2]oxazolo[4,5- b]pyridin-3- ylmethyl}-1,3,4- oxadiazol-2- yl)pyridine-2,4-diol | US10336739, Example 228
Type:
Small organic molecule
Emp. Form.:
C25H23N5O7
Mol. Mass.:
505.4794
SMILES:
CCOCc1nc(O)c(-c2nnc(Cc3noc4cccnc34)o2)c(O)c1-c1c(OC)cccc1OC |(-8.32,-1.02,;-6.99,-1.79,;-5.65,-1.02,;-4.32,-1.79,;-2.99,-1.02,;-2.99,.52,;-1.65,1.29,;-1.65,2.83,;-.32,.52,;1.01,1.29,;2.42,.67,;3.45,1.81,;2.68,3.15,;3.08,4.63,;4.57,5.03,;5.27,6.41,;6.79,6.16,;7.03,4.64,;8.32,3.8,;8.24,2.27,;6.87,1.57,;5.58,2.41,;5.66,3.94,;1.18,2.83,;-.32,-1.02,;1.01,-1.79,;-1.65,-1.79,;-1.65,-3.33,;-2.99,-4.1,;-4.32,-3.33,;-5.65,-4.1,;-2.99,-5.64,;-1.65,-6.41,;-.32,-5.64,;-.32,-4.1,;1.01,-3.33,;2.35,-4.1,)|
Structure:
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