Reaction Details Report a problem with these data
Target
Apelin receptor
Ligand
BDBM406501
Substrate
n/a
Meas. Tech.
Intracellular cAMP Accumulation Assay
EC50
55±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:
BDBM406501
Synonyms:
6-cyclopropyl-5- (2,6- dimethoxyphenyl) 3-{5-[(2-methyl- 1,3-thiazol-4- yl)methyl]-1,3,4- oxadiazol-2- yl}pyridine-2,4-diol | US10336739, Example 94
Type:
Small organic molecule
Emp. Form.:
C23H22N4O5S
Mol. Mass.:
466.51
SMILES:
COc1cccc(OC)c1-c1c(O)c(-c2nnc(Cc3csc(C)n3)o2)c(O)nc1C1CC1 |(1.12,-4.07,;-.22,-3.3,;-1.55,-4.07,;-1.55,-5.61,;-2.89,-6.38,;-4.22,-5.61,;-4.22,-4.07,;-5.55,-3.3,;-6.89,-4.07,;-2.89,-3.3,;-2.89,-1.76,;-1.55,-.99,;-.22,-1.76,;-1.55,.55,;-.22,1.32,;1.19,.69,;2.22,1.84,;1.45,3.17,;1.85,4.66,;3.33,5.06,;4.12,6.38,;5.62,6.05,;5.77,4.51,;7.09,3.73,;4.35,3.9,;-.06,2.85,;-2.89,1.32,;-2.89,2.86,;-4.22,.55,;-4.22,-.99,;-5.55,-1.76,;-6.32,-.43,;-7.09,-1.76,)|
Structure:
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