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Compound Detail

CHEMBL4460235

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C[C@]1(c2ccc(F)cc2F)C[C@H](COc2ccc(N3CCN(c4ccc(NC(=O)c5cccc(O)c5)cc4)CC3)cc2)CO1

Basic Information

ChEMBL ID CHEMBL4460235
Phase Preclinical
Structure Type MOL
InChI Key FITZQTHCSRXHJV-CGDLVVIGSA-N
1
Targets
1
Activities
1
Assay Types
2
PK Parameters
5
Publications
0
Known Names

Molecular Properties

599.7
MW (Da)
6.58
ALogP
6
HBA
2
HBD
74.3
PSA (Ų)
0.24
QED
2
Ro5 Violations
8
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C35H35F2N3O4
MW 599.68
Aromatic Rings 4
Heavy Atoms 44
NP-Likeness -0.65

Activity Summary

IC50 1 meas. best 6.72

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Unchecked
CHEMBL612545
IC50 6.72 6.72 190.0 1

Pharmacokinetic Data

Parameter Value Units Species
CL 2.23 mL.min-1.g-1 Homo sapiens
T1/2 3.0 hr Homo sapiens

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Unchecked IC50 = 190.0 nM 6.72 Inhibition of hedgehog signaling pathway in mouse ASZ cells assessed as decrease... 30529635

Literature References

PubMed DOI Target Context # Activities
30529635 10.1016/j.ejmech.2018.11.056 ADMET 2
30529635 10.1016/j.ejmech.2018.11.056 Unchecked 1
30529635 10.1016/j.ejmech.2018.11.056 Cytochrome P450 3A4 1
30529635 10.1016/j.ejmech.2018.11.056 No relevant target 1
30529635 10.1016/j.ejmech.2018.11.056 Voltage-gated inwardly rectifying potassium channel KCNH2 1

Data from ChEMBL 36 via Core Engine