Reaction Details Report a problem with these data
Target
Apelin receptor
Ligand
BDBM406533
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:
BDBM406533
Synonyms:
3-{5-[(5- chloropyridin-2- yl)methyl]-1,3,4- oxadiazol-2-yl}-5- (2,6- dimethoxyphenyl)- 6-(ethoxymethyl) pyridine-2,4-diol | US10336739, Example 127
Type:
Small organic molecule
Emp. Form.:
C24H23ClN4O6
Mol. Mass.:
498.916
SMILES:
CCOCc1nc(O)c(-c2nnc(Cc3ccc(Cl)cn3)o2)c(O)c1-c1c(OC)cccc1OC |(-8.68,-1.27,;-7.34,-2.04,;-6.01,-1.27,;-4.67,-2.04,;-3.34,-1.27,;-3.34,.27,;-2.01,1.04,;-2.01,2.58,;-.67,.27,;.66,1.04,;2.07,.41,;3.1,1.56,;2.33,2.89,;2.73,4.38,;4.21,4.78,;4.61,6.26,;6.1,6.66,;7.19,5.57,;8.68,5.97,;6.79,4.09,;5.3,3.69,;.82,2.57,;-.67,-1.27,;.66,-2.04,;-2.01,-2.04,;-2.01,-3.58,;-.67,-4.35,;.66,-3.58,;1.99,-4.35,;-.67,-5.89,;-2.01,-6.66,;-3.34,-5.89,;-3.34,-4.35,;-4.67,-3.58,;-6.01,-4.35,)|
Structure:
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