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Compound Detail

CHEMBL5197398

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CCc1cccc(CC)c1-n1c(-c2ccn(C)n2)nc(=O)c(C(=O)N2CC[C@H](c3ccccc3F)C2)c1O

Basic Information

ChEMBL ID CHEMBL5197398
Phase Preclinical
Structure Type MOL
InChI Key DGVLFASAPIUBMI-FQEVSTJZSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

515.6
MW (Da)
4.23
ALogP
7
HBA
1
HBD
93.2
PSA (Ų)
0.41
QED
1
Ro5 Violations
6
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C29H30FN5O3
MW 515.59
Aromatic Rings 4
Heavy Atoms 38
NP-Likeness -1.37

Activity Summary

EC50 1 meas. best 10.4

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Apelin receptor
CHEMBL1628481
EC50 10.4 10.4 0.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Apelin receptor EC50 = 0.04 nM 10.4 Agonist activity at human APJ expressed in HEK293 cells assessed as inhibition o... 34855405

Literature References

PubMed DOI Target Context # Activities
34855405 10.1021/acs.jmedchem.1c01504 ADMET 3
34855405 10.1021/acs.jmedchem.1c01504 Apelin receptor 1

Data from ChEMBL 36 via Core Engine