Ki Summary

Reaction Details

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Target

Apelin receptor

Ligand

BDBM456582

Substrate/Competitor

n/a

Meas. Tech.

GTPγS Binding

EC50

0.290±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

BDBM456582

n/a

Name

BDBM456582

Synonyms:

US10736883, Example 19.0

Type

Small organic molecule

Emp. Form.

C23H22N6O5S

Mol. Mass.

494.523

SMILES

COc1cccc(OC)c1-n1c(NS(=O)(=O)CCc2ccc(cn2)C#N)nnc1-c1ccc(C)o1 |(1.13,.76,;.04,-.32,;-1.45,.07,;-1.85,1.56,;-3.34,1.96,;-4.43,.87,;-4.03,-.62,;-5.12,-1.7,;-6.6,-1.31,;-2.54,-1.01,;-2.14,-2.5,;-.68,-2.98,;.66,-2.21,;1.99,-2.98,;3.32,-3.75,;1.22,-4.31,;2.76,-1.64,;4.3,-1.64,;5.07,-.31,;6.61,-.31,;7.38,1.02,;6.64,2.4,;5.07,2.36,;4.3,1.02,;7.41,3.74,;8.18,5.07,;-.68,-4.52,;-2.14,-4.99,;-3.05,-3.75,;-4.53,-3.35,;-5.59,-2.26,;-6.9,-2.58,;-6.9,-4.12,;-8.15,-5.02,;-5.44,-4.59,)|

Structure