Target
Apelin receptor
Ligand
BDBM406474
Substrate
n/a
Meas. Tech.
Intracellular cAMP Accumulation Assay
EC50
5.5±n/a nM
Citation
 Johnson, JAKim, 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:
BDBM406474
Synonyms:
6-butyl-3-[5- (cyclohexylmethyl)- 1,3,4-oxadiazol-2- yl]-5-(2,6- dimethoxyphenyl) pyridine-2,4-diol | US10336739, Example 67
Type:
Small organic molecule
Emp. Form.:
C26H33N3O5
Mol. Mass.:
467.5573
SMILES:
CCCCc1nc(O)c(-c2nnc(CC3CCCCC3)o2)c(O)c1-c1c(OC)cccc1OC |(-7.93,-1.27,;-6.6,-2.04,;-5.26,-1.27,;-3.93,-2.04,;-2.6,-1.27,;-2.6,.27,;-1.26,1.04,;-1.26,2.58,;.07,.27,;1.4,1.04,;2.81,.41,;3.84,1.56,;3.07,2.89,;3.47,4.38,;4.96,4.78,;6.05,3.69,;7.53,4.09,;7.93,5.57,;6.84,6.66,;5.36,6.26,;1.56,2.57,;.07,-1.27,;1.4,-2.04,;-1.26,-2.04,;-1.26,-3.58,;.07,-4.35,;1.4,-3.58,;2.74,-4.35,;.07,-5.89,;-1.26,-6.66,;-2.6,-5.89,;-2.6,-4.35,;-3.93,-3.58,;-5.26,-4.35,)|
Structure:
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