Ki Summary

Reaction Details

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Target

Apelin receptor

Ligand

BDBM456574

Substrate/Competitor

n/a

Meas. Tech.

GTPγS Binding

EC50

0.140±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

BDBM456574

n/a

Name

BDBM456574

Synonyms:

US10736883, Example 11.0

Type

Small organic molecule

Emp. Form.

C22H22ClN5O5S

Mol. Mass.

503.959

SMILES

COc1cccc(OC)c1-n1c(NS(=O)(=O)[C@@H](C)Cc2ccc(Cl)cn2)nnc1-c1ccco1 |r,wU:16.17,(1.57,-3.44,;.48,-4.53,;-1.01,-4.13,;-1.41,-2.64,;-2.9,-2.24,;-3.99,-3.33,;-3.59,-4.82,;-4.68,-5.91,;-6.16,-5.51,;-2.1,-5.22,;-1.7,-6.71,;-.24,-7.18,;1.1,-6.41,;2.43,-7.18,;3.76,-7.95,;1.66,-8.51,;3.2,-5.85,;2.43,-4.51,;4.74,-5.85,;5.51,-4.51,;7.05,-4.51,;7.82,-3.18,;7.05,-1.85,;7.82,-.51,;5.51,-1.85,;4.74,-3.18,;-.24,-8.72,;-1.7,-9.2,;-2.61,-7.95,;-4.09,-7.55,;-5,-6.31,;-6.46,-6.78,;-6.46,-8.32,;-5,-8.8,)|

Structure