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Compound Detail

CHEMBL4173049

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N#Cc1cc(COC(=O)N2C[C@@H]3[C@@H](CNC(=O)c4ccc5[nH]nnc5c4)[C@@H]3C2)cc(C(=O)OC(F)(F)F)c1

Basic Information

ChEMBL ID CHEMBL4173049
Phase Preclinical
Structure Type MOL
InChI Key YXNYYDCPDWJEMT-NNZMDNLPSA-N
1
Targets
2
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

528.5
MW (Da)
2.75
ALogP
8
HBA
2
HBD
150.3
PSA (Ų)
0.46
QED
1
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C24H19F3N6O5
MW 528.45
Aromatic Rings 3
Heavy Atoms 38
NP-Likeness -1.24

Activity Summary

IC50 2 meas. best 8.82

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Autotaxin
CHEMBL3826870
IC50 8.82 8.285 1.5 2

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
29259743 10.1021/acsmedchemlett.7b00312 ADMET 4
29259743 10.1021/acsmedchemlett.7b00312 No relevant target 3
29259743 10.1021/acsmedchemlett.7b00312 Autotaxin 2
29259743 10.1021/acsmedchemlett.7b00312 Voltage-gated inwardly rectifying potassium channel KCNH2 1

Data from ChEMBL 36 via Core Engine