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Compound Detail

CHEMBL4764067

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CCCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](N)CCCCN)C(=O)NC(C)(C)C(=O)N[C@@H](Cc1ccc(Br)cc1)C(=O)O

Basic Information

ChEMBL ID CHEMBL4764067
Phase Preclinical
Structure Type MOL
InChI Key QTANYACIHNQWJA-HESOAQJPSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
1
Publications
0
Known Names

Molecular Properties

2102.3
MW (Da)

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C93H150BrN31O20
MW 2102.32

Activity Summary

IC50 1 meas. best 9.66

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Apelin receptor
CHEMBL2398
IC50 9.66 9.66 0.2 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Apelin receptor IC50 = 0.2188 nM 9.66 Displacement of [125I]-pyr-1-apelin-13 from EGFP-tagged wild-type rat apelin rec... 33001648

Literature References

PubMed DOI Target Context # Activities
33001648 10.1021/acs.jmedchem.0c01395 Apelin receptor 1

Data from ChEMBL 36 via Core Engine