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Compound Detail

CHEMBL4072606

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C=CC[C@H](NC(=O)[C@H](Cc1cnc[nH]1)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]1CCC(=O)N1)C(=O)NCC(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCC)C(=O)N[C@@H](CC=C)C(=O)N[C@@H](Cc1ccccc1)C(=O)O

Basic Information

ChEMBL ID CHEMBL4072606
Phase Preclinical
Structure Type MOL
InChI Key UDERDGVNNBKLQE-PEWBXTNBSA-N
1
Targets
3
Activities
2
Assay Types
0
PK Parameters
1
Publications
0
Known Names

Molecular Properties

1484.7
MW (Da)

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C69H105N21O16
MW 1484.73

Activity Summary

EC50 2 meas. best 9.1
Ki 1 meas. best 8.64

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Apelin receptor
CHEMBL1628481
EC50 9.1 8.17 0.8 2
Apelin receptor
CHEMBL1628481
Ki 8.64 8.64 2.3 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
29461833 10.1021/acs.jmedchem.7b01353 Apelin receptor 3

Data from ChEMBL 36 via Core Engine