Reaction Details Report a problem with these data
Target
Apelin receptor
Ligand
BDBM507152
Substrate
n/a
Meas. Tech.
[35S]GTPgammaS Binding
EC50
1.10±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:
BDBM507152
Synonyms:
US11046680, Example 23.0
Type:
Small organic molecule
Emp. Form.:
C22H24FN7O5S
Mol. Mass.:
517.533
SMILES:
COc1cccc(OC)c1-n1c(NS(=O)(=O)[C@H](C)[C@H](O)c2ccc(F)cn2)nnc1-c1ccn(C)n1 |r,wU:18.19,wD:16.17,(2.3,-16.19,;.96,-16.96,;-.37,-16.19,;-.37,-14.65,;-1.7,-13.88,;-3.04,-14.65,;-3.04,-16.19,;-4.37,-16.96,;-5.71,-16.19,;-1.7,-16.96,;-1.7,-18.5,;-.46,-19.4,;1.03,-19,;2.12,-20.09,;1.03,-21.18,;3.21,-21.18,;3.21,-19,;2.81,-17.52,;4.69,-19.4,;5.09,-20.89,;5.78,-18.31,;5.39,-16.83,;6.47,-15.74,;7.96,-16.14,;9.05,-15.05,;8.36,-17.62,;7.27,-18.71,;-.93,-20.87,;-2.47,-20.87,;-2.95,-19.4,;-4.41,-18.93,;-4.89,-17.46,;-6.43,-17.46,;-6.91,-18.93,;-8.37,-19.4,;-5.66,-19.83,)|