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Compound Detail

CHEMBL4743411

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Cc1c(-c2ccccc2)nc2ccc(Br)cc2c1C(=O)NCC(CCC(=O)O)c1ccccc1Cl

Basic Information

ChEMBL ID CHEMBL4743411
Phase Preclinical
Structure Type MOL
InChI Key XDMSQVUSXYEOFO-UHFFFAOYSA-N
1
Targets
4
Activities
1
Assay Types
6
PK Parameters
5
Publications
0
Known Names

Molecular Properties

551.9
MW (Da)
7.00
ALogP
3
HBA
2
HBD
79.3
PSA (Ų)
0.25
QED
2
Ro5 Violations
8
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C28H24BrClN2O3
MW 551.87
Aromatic Rings 4
Heavy Atoms 35
NP-Likeness -0.72

Activity Summary

IC50 4 meas. best 8.18

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Prostaglandin F2-alpha receptor
CHEMBL1987
IC50 8.18 8.11 6.6 4

Pharmacokinetic Data

Parameter Value Units Species
CL 30.0 mL.min-1.kg-1 Rattus norvegicus
CL 50.0 mL.min-1.kg-1 Rattus norvegicus
F 59.0 % Rattus norvegicus
F 75.0 % Rattus norvegicus
F 59.0 % Rattus norvegicus
T1/2 5.5 hr Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
32969660 10.1021/acs.jmedchem.0c00834 Unchecked 12
32969660 10.1021/acs.jmedchem.0c00834 ADMET 6
32969660 10.1021/acs.jmedchem.0c00834 Cytochrome P450 3A4 2
32969660 10.1021/acs.jmedchem.0c00834 No relevant target 2
32969660 10.1021/acs.jmedchem.0c00834 Prostaglandin F2-alpha receptor 2

Data from ChEMBL 36 via Core Engine