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Compound Detail

CHEMBL4633558

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CCP(=O)(OC)c1ccc2oc(-c3ccc(F)cc3F)nc2c1

Basic Information

ChEMBL ID CHEMBL4633558
Phase Preclinical
Structure Type MOL
InChI Key NETWRZHGRNIPEM-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
8
PK Parameters
3
Publications
0
Known Names

Molecular Properties

337.3
MW (Da)
4.34
ALogP
4
HBA
0
HBD
52.3
PSA (Ų)
0.66
QED
0
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C16H14F2NO3P
MW 337.26
Aromatic Rings 3
Heavy Atoms 23
NP-Likeness -1.26

Activity Summary

EC50 1 meas. best 6.11

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Utrophin
CHEMBL4523230
EC50 6.11 6.11 777.0 1

Pharmacokinetic Data

Parameter Value Units Species
CL 14.4 mL.min-1.g-1 Mus musculus
CL 1.59 mL.min-1.g-1 Homo sapiens
CL 1.1 mL.min-1.g-1 Canis lupus familiaris
CL 3.31 mL.min-1.g-1 Rattus norvegicus
T1/2 1.6 hr Mus musculus
T1/2 14.48 hr Homo sapiens
T1/2 21.17 hr Canis lupus familiaris
T1/2 6.983 hr Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Utrophin EC50 = 777.0 nM 6.11 Modulation of human utrophinA expressed in mouse H2K cells assessed as upregulat... 32551645

Literature References

PubMed DOI Target Context # Activities
32551645 10.1021/acs.jmedchem.0c00807 ADMET 10
32551645 10.1021/acs.jmedchem.0c00807 Utrophin 1
32551645 10.1021/acs.jmedchem.0c00807 No relevant target 1

Data from ChEMBL 36 via Core Engine