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Compound Detail

CHEMBL4061039

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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@](C)(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](CCCNC(=N)N)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 CHEMBL4061039
Phase Preclinical
Structure Type MOL
InChI Key PAKPFUXSKFBVQH-FOOUNLHFSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

2201.5
MW (Da)

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C97H159BrN34O20
MW 2201.46

Activity Summary

Ki 1 meas. best 9.74

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Apelin receptor
CHEMBL2398
Ki 9.74 9.74 0.2 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Apelin receptor Ki = 0.18 nM 9.74 Displacement of [125I]-pyr-1-apelin-13 from rat C-terminal EGFP-tagged APJ recep... 28685579

Literature References

PubMed DOI Target Context # Activities
28685579 10.1021/acs.jmedchem.7b00723 Neprilysin 4
28685579 10.1021/acs.jmedchem.7b00723 Apelin receptor 1
28685579 10.1021/acs.jmedchem.7b00723 Mus musculus 1

Data from ChEMBL 36 via Core Engine