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Compound Detail

CHEMBL4636225

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CCn1cc(C(=O)N/N=C/c2ccc(F)cc2)c2cc(-c3nc(CN4CCN(CCO)CC4)cs3)ccc21

Basic Information

ChEMBL ID CHEMBL4636225
Phase Preclinical
Structure Type MOL
InChI Key FOQPAZWDSCOMKQ-OKCVXOCRSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
1
Publications
0
Known Names

Molecular Properties

534.7
MW (Da)
3.80
ALogP
8
HBA
2
HBD
86.0
PSA (Ų)
0.25
QED
1
Ro5 Violations
9
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C28H31FN6O2S
MW 534.66
Aromatic Rings 4
Heavy Atoms 38
NP-Likeness -2.21

Activity Summary

IC50 1 meas. best 6.87

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Autotaxin
CHEMBL3691
IC50 6.87 6.87 134.9 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Autotaxin IC50 = 134.9 nM 6.87 Inhibition of human ATX pre-incubated for 45 mins before fluorogenic substrate-3... 32479084

Literature References

PubMed DOI Target Context # Activities
32479084 10.1021/acs.jmedchem.0c00506 Autotaxin 1

Data from ChEMBL 36 via Core Engine