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Compound Detail

CHEMBL4540110

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CC(=O)c1cccc(C(=O)Nc2ccc(N3CCN(c4ccc(OC[C@@H]5CO[C@@](C)(c6ccc(F)cc6F)C5)cc4)CC3)cc2)c1

Basic Information

ChEMBL ID CHEMBL4540110
Phase Preclinical
Structure Type MOL
InChI Key IARWAQVFAWUVLA-NGXVIIRPSA-N
1
Targets
1
Activities
1
Assay Types
2
PK Parameters
5
Publications
0
Known Names

Molecular Properties

625.7
MW (Da)
7.08
ALogP
6
HBA
1
HBD
71.1
PSA (Ų)
0.20
QED
2
Ro5 Violations
9
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C37H37F2N3O4
MW 625.72
Aromatic Rings 4
Heavy Atoms 46
NP-Likeness -0.78

Activity Summary

IC50 1 meas. best 7.62

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Unchecked
CHEMBL612545
IC50 7.62 7.62 24.0 1

Pharmacokinetic Data

Parameter Value Units Species
CL 20.0 mL.min-1.g-1 Homo sapiens
T1/2 1.917 hr Homo sapiens

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Unchecked IC50 = 24.0 nM 7.62 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