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Compound Detail

CHEMBL5184730

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COc1cccc(OC)c1-n1c(-c2ccc(F)cc2)nc(=O)c(C(=O)N2CC[C@H](c3ccccc3F)C2)c1O

Basic Information

ChEMBL ID CHEMBL5184730
Phase Preclinical
Structure Type MOL
InChI Key SMGFVYRLURYNSF-SFHVURJKSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

533.5
MW (Da)
4.53
ALogP
7
HBA
1
HBD
93.9
PSA (Ų)
0.39
QED
1
Ro5 Violations
6
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C29H25F2N3O5
MW 533.53
Aromatic Rings 4
Heavy Atoms 39
NP-Likeness -1.11

Activity Summary

EC50 1 meas. best 9.7

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Apelin receptor
CHEMBL1628481
EC50 9.7 9.7 0.2 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Apelin receptor EC50 = 0.2 nM 9.7 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 5
34855405 10.1021/acs.jmedchem.1c01504 Apelin receptor 1

Data from ChEMBL 36 via Core Engine