Ki Summary

Reaction Details

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Target

Apelin receptor

Ligand

BDBM456589

Substrate/Competitor

n/a

Meas. Tech.

GTPγS Binding

EC50

0.420±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

BDBM456589

n/a

Name

BDBM456589

Synonyms:

US10736883, Example 26.0

Type

Small organic molecule

Emp. Form.

C22H24N6O5S

Mol. Mass.

484.528

SMILES

COc1cccc(OC)c1-n1c(NS(=O)(=O)CCc2ncc(C)cn2)nnc1-c1ccc(C)o1 |(-6.05,-.03,;-4.57,-.43,;-3.48,.66,;-3.88,2.15,;-2.79,3.24,;-1.3,2.84,;-.9,1.35,;.59,.95,;1.68,2.04,;-1.99,.26,;-1.48,-1.73,;-.15,-2.5,;1.19,-1.73,;2.52,-2.5,;1.75,-3.83,;3.85,-3.27,;3.29,-1.17,;4.83,-1.17,;5.6,.17,;7.14,.17,;7.91,1.5,;7.14,2.83,;7.91,4.17,;5.6,2.83,;4.83,1.5,;-.47,-4.01,;-2,-4.17,;-2.63,-2.76,;-4.11,-2.36,;-4.81,-.99,;-6.33,-1.23,;-6.58,-2.75,;-7.91,-3.52,;-5.2,-3.45,)|

Structure