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Compound Detail

CHEMBL2180682

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CCN1Cc2c(c3ccc(OC)cc3c3cc(OC)c(OC)cc23)C(O)C1

Basic Information

ChEMBL ID CHEMBL2180682
Phase Preclinical
Structure Type MOL
InChI Key YDGQYKBAQLQULF-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
8
PK Parameters
12
Publications
0
Known Names

Molecular Properties

367.4
MW (Da)
3.89
ALogP
5
HBA
1
HBD
51.2
PSA (Ų)
0.71
QED
0
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C22H25NO4
MW 367.45
Aromatic Rings 3
Heavy Atoms 27
NP-Likeness 0.29

Activity Summary

EC50 2 meas. best 7.4

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Transmissible gastroenteritis virus
CHEMBL613311
EC50 7.4 7.4 40.0 1
RAW264.7
CHEMBL612557
EC50 7.16 7.16 70.0 1

Pharmacokinetic Data

Parameter Value Units Species
AUC 999.0 ng.hr.mL-1 Rattus norvegicus
AUC 646.0 ng.hr.mL-1 Rattus norvegicus
CL 51.8 mL.min-1.kg-1 Rattus norvegicus
Cmax 197.03 nM Rattus norvegicus
F 63.5 % Rattus norvegicus
T1/2 11.8 hr Rattus norvegicus
T1/2 0.8 hr Rattus norvegicus
Tmax 0.3 hr Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
23167614 10.1021/jm300705j Rattus norvegicus 11
23167614 10.1021/jm300705j RAW264.7 4
23167614 10.1021/jm300705j A549 4
23167614 10.1021/jm300705j Transmissible gastroenteritis virus 3
23167614 10.1021/jm300705j MCF7 3
23167614 10.1021/jm300705j NCI-H460 3
23167614 10.1021/jm300705j Mus musculus 3
23167614 10.1021/jm300705j No relevant target 2
23167614 10.1021/jm300705j Murine hepatitis virus 2
23167614 10.1021/jm300705j NON-PROTEIN TARGET 1
23167614 10.1021/jm300705j HepG2 1
23167614 10.1021/jm300705j NUGC-3 1

Data from ChEMBL 36 via Core Engine