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Compound Detail

CHEMBL4075483

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CCc1nc2cnc(N3CCN(CC(=O)N4CC(O)C4)CC3)cn2c1N(C)c1nc(-c2ccc(F)cc2)c(C#N)s1

Basic Information

ChEMBL ID CHEMBL4075483
Phase Preclinical
Structure Type MOL
InChI Key QRRUOUGSMGFUEU-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

575.7
MW (Da)
2.52
ALogP
11
HBA
1
HBD
117.1
PSA (Ų)
0.35
QED
2
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C28H30FN9O2S
MW 575.67
Aromatic Rings 4
Heavy Atoms 41
NP-Likeness -1.74

Activity Summary

IC50 1 meas. best 6.99

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Autotaxin
CHEMBL3691
IC50 6.99 6.99 102.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Autotaxin IC50 = 102.0 nM 6.99 Inhibition of human ATX using LPC (16:0) as substrate after 30 mins by horseradi... 28414242

Literature References

PubMed DOI Target Context # Activities
28414242 10.1021/acs.jmedchem.7b00032 No relevant target 2
28414242 10.1021/acs.jmedchem.7b00032 Autotaxin 1
28414242 10.1021/acs.jmedchem.7b00032 Cytochrome P450 3A4 1

Data from ChEMBL 36 via Core Engine