Reaction Details Report a problem with these data
Target
Apelin receptor
Ligand
BDBM507260
Substrate
n/a
Meas. Tech.
[35S]GTPgammaS Binding
EC50
118±n/a nM
Citation
Chen, N; Chen, X; Chen, Y; Cheng, AC; Connors, RV; Deignan, J; Dransfield, PJ; Du, X; Fu, Z; Harvey, JS; Heath, JA; Heumann, LV; Horne, DB; Houze, J; Kaller, MR; Kayser, F; Khakoo, AY; Kopecky, DJ; Lai, S; Ma, Z; Medina, JC; Mihalic, JT; Nishimura, N; Olson, SH; Pattaropong, V; Swaminath, G; Wang, X; Wanska, M; Yang, K; Yeh, W Heteroaryl-substituted triazoles as APJ receptor agonists US Patent US11046680 Publication Date 6/29/2021
More Info.:
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:
BDBM507260
Synonyms:
US11046680, Example 139.0
Type:
Small organic molecule
Emp. Form.:
C21H20ClN5O5S
Mol. Mass.:
489.932
SMILES:
COc1cccc(OC)c1-n1c(NS(=O)(=O)CCc2ccc(Cl)cc2)nnc1-c1cocn1 |(-7.42,1.45,;-6.09,.68,;-4.76,1.45,;-4.76,2.99,;-3.42,3.76,;-2.09,2.99,;-2.09,1.45,;-.75,.68,;.58,1.45,;-3.42,.68,;-3.42,-1.22,;-2.18,-2.13,;-.71,-1.65,;.62,-2.42,;-.15,-3.76,;1.39,-3.76,;1.96,-1.65,;3.29,-2.42,;4.62,-1.65,;5.96,-2.42,;7.29,-1.65,;7.29,-.11,;8.62,.66,;5.96,.66,;4.62,-.11,;-2.65,-3.59,;-4.19,-3.59,;-4.67,-2.13,;-6.13,-1.65,;-7.38,-2.56,;-8.62,-1.65,;-8.15,-.19,;-6.61,-.19,)|