Ki Summary

Reaction Details

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Target

Apelin receptor

Ligand

BDBM456590

Substrate/Competitor

n/a

Meas. Tech.

GTPγS Binding

EC50

0.460±n/a nM

Citation

Brown, M; Chen, N; Chen, X; Chen, Y; Cheng, AC; Connors, RV; Deignan, J; Dransfield, PJ; Du, X; Fu, Z; Harvey, JS; Heath, JA; Heumann, LV; Houze, J; Kayser, F; Khakoo, AY; Kopecky, D; Lai, S; Ma, Z; Medina, JC; Mihalic, JT; Olson, SH; Pattaropong, V; Swaminath, G; Wang, X; Wanska, M; Yeh, W Triazole furan compounds as agonists of the APJ receptor US Patent US10736883 Publication Date 8/11/2020

More Info.:

Get all data from this article, Assay Method

Apelin receptor

Name:

Apelin receptor

Synonyms:

Type:

Enzyme Catalytic Domain

Mol. Mass.:

42664.06

Organism:

Homo sapiens (Human)

Description:

P35414

Residue:

380

Sequence:

MEEGGDFDNYYGADNQSECEYTDWKSSGALIPAIYMLVFLLGTTGNGLVLWTVFRSSREK
RRSADIFIASLAVADLTFVVTLPLWATYTYRDYDWPFGTFFCKLSSYLIFVNMYASVFCL
TGLSFDRYLAIVRPVANARLRLRVSGAVATAVLWVLAALLAMPVMVLRTTGDLENTTKVQ
CYMDYSMVATVSSEWAWEVGLGVSSTTVGFVVPFTIMLTCYFFIAQTIAGHFRKERIEGL
RKRRRLLSIIVVLVVTFALCWMPYHLVKTLYMLGSLLHWPCDFDLFLMNIFPYCTCISYV
NSCLNPFLYAFFDPRFRQACTSMLCCGQSRCAGTSHSSSGEKSASYSSGHSQGPGPNMGK
GGEQMHEKSIPYSQETLVVD

BDBM456590

n/a

Name

BDBM456590

Synonyms:

US10736883, Example 27.0

Type

Small organic molecule

Emp. Form.

C24H23ClN6O6S

Mol. Mass.

558.994

SMILES

COc1cccc(OC)c1-n1c(NS(=O)(=O)CCc2ncc(Cl)cc2N2CCC2=O)nnc1-c1ccco1 |(-8.13,-.03,;-6.64,-.43,;-5.55,.66,;-5.95,2.15,;-4.86,3.24,;-3.38,2.84,;-2.98,1.35,;-1.49,.95,;-.4,2.04,;-4.07,.26,;-3.56,-1.73,;-2.23,-2.5,;-.89,-1.73,;.44,-2.5,;-.33,-3.83,;1.78,-3.27,;1.21,-1.17,;2.75,-1.17,;3.52,.17,;2.75,1.5,;3.52,2.83,;5.06,2.83,;5.83,4.17,;5.83,1.5,;5.06,.17,;5.83,-1.17,;5.43,-2.65,;6.92,-3.05,;7.32,-1.57,;8.65,-.8,;-2.55,-4.01,;-4.08,-4.17,;-4.7,-2.76,;-6.19,-2.36,;-6.89,-.99,;-8.41,-1.23,;-8.65,-2.75,;-7.28,-3.45,)|

Structure