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Compound Detail

CHEMBL5079641

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CC(C)C[C@@H]1NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](N)C/C=C\C[C@@H](C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N2CCC[C@H]2C(=O)N[C@@H](Cc2cc(C3CCCC3)c(OCc3ccccc3)c(C3CCCC3)c2)C(=O)O)NC(=O)[C@H](CO)NC1=O

Basic Information

ChEMBL ID CHEMBL5079641
Phase Preclinical
Structure Type MOL
InChI Key MFVUAFDQPMHIKF-AOMSCDDSSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
1
Publications
0
Known Names

Molecular Properties

1212.5
MW (Da)

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C62H93N13O12
MW 1212.50

Activity Summary

Ki 1 meas. best 5.57

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Apelin receptor
CHEMBL1628481
Ki 5.57 5.57 2670.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Apelin receptor Ki = 2670.0 nM 5.57 Displacement of [125I]-[Nle75,Tyr77][Pyr1]-Ape13 from YFP-tagged human APJ expre... 34982553

Literature References

PubMed DOI Target Context # Activities
34982553 10.1021/acs.jmedchem.1c01708 Apelin receptor 1

Data from ChEMBL 36 via Core Engine