Skip to main content
Free research Free research Free compound review with research home and workspace preview
Quick search ChEMBL 36
Compound Detail

CHEMBL5202233

Enter ChEMBL ID:
Free Research Context This compound will appear in recent viewed items on the research home for this browser.
Research home View demo workspace
COc1cccc(OC)c1-n1c(-c2csc(C)n2)nc(=O)c(C(=O)N2CCC(c3ccc(F)cc3F)C2)c1O

Basic Information

ChEMBL ID CHEMBL5202233
Phase Preclinical
Structure Type MOL
InChI Key QUKHSBMSXSWOPH-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

554.6
MW (Da)
4.30
ALogP
9
HBA
1
HBD
106.8
PSA (Ų)
0.38
QED
1
Ro5 Violations
6
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C27H24F2N4O5S
MW 554.58
Aromatic Rings 4
Heavy Atoms 39
NP-Likeness -1.19

Activity Summary

EC50 1 meas. best 10.52

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Apelin receptor
CHEMBL1628481
EC50 10.52 10.52 0.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Apelin receptor EC50 = 0.03 nM 10.52 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