Ki Summary

Reaction Details

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Target

Apelin receptor

Ligand

BDBM456587

Substrate/Competitor

n/a

Meas. Tech.

GTPγS Binding

EC50

0.360±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

BDBM456587

n/a

Name

BDBM456587

Synonyms:

US10736883, Example 24.0

Type

Small organic molecule

Emp. Form.

C23H26N6O5S

Mol. Mass.

498.555

SMILES

COc1cccc(OC)c1-n1c(NS(=O)(=O)[C@@H](C)Cc2cnc(C)cn2)nnc1-c1ccc(C)o1 |r,wU:16.17,(-5.41,-5.53,;-3.93,-5.93,;-2.84,-4.84,;-3.24,-3.35,;-2.15,-2.27,;-.66,-2.66,;-.26,-4.15,;1.23,-4.55,;2.32,-3.46,;-1.35,-5.24,;-.84,-7.23,;.49,-8,;1.83,-7.23,;3.16,-8,;2.39,-9.34,;4.49,-8.77,;3.93,-6.67,;3.16,-5.34,;5.47,-6.67,;6.24,-5.34,;7.78,-5.34,;8.55,-4,;7.78,-2.67,;8.55,-1.34,;6.24,-2.67,;5.47,-4,;.17,-9.51,;-1.36,-9.67,;-1.99,-8.26,;-3.47,-7.87,;-4.17,-6.49,;-5.69,-6.73,;-5.94,-8.26,;-7.27,-9.03,;-4.56,-8.95,)|

Structure