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Compound Detail

CHEMBL4450586

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CC(=O)c1cccc(C(=O)Nc2ccc(N3CCN(c4ccc(OC[C@@H]5CO[C@](C)(c6ccc(Cl)cc6Cl)O5)cc4)CC3)cc2)c1

Basic Information

ChEMBL ID CHEMBL4450586
Phase Preclinical
Structure Type MOL
InChI Key CZRAKZRYPDKNPT-KUFVUHJUSA-N
1
Targets
1
Activities
1
Assay Types
2
PK Parameters
7
Publications
0
Known Names

Molecular Properties

660.6
MW (Da)
7.44
ALogP
7
HBA
1
HBD
80.3
PSA (Ų)
0.19
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 C36H35Cl2N3O5
MW 660.60
Aromatic Rings 4
Heavy Atoms 46
NP-Likeness -0.75

Activity Summary

IC50 1 meas. best 7.05

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Protein smoothened
CHEMBL6080
IC50 7.05 7.05 89.0 1

Pharmacokinetic Data

Parameter Value Units Species
CL 61000.0 mL.min-1.g-1 Homo sapiens
T1/2 0.19 hr Homo sapiens

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Protein smoothened IC50 = 89.0 nM 7.05 Inhibition of smo-mediated hedgehog signaling pathway in mouse ASZ001 cells asse... 30896941

Literature References

PubMed DOI Target Context # Activities
30896941 10.1021/acs.jmedchem.8b01283 ADMET 2
30896941 10.1021/acs.jmedchem.8b01283 Protein smoothened 1
30896941 10.1021/acs.jmedchem.8b01283 Unchecked 1
30896941 10.1021/acs.jmedchem.8b01283 Medulloblastoma cell 1
30896941 10.1021/acs.jmedchem.8b01283 No relevant target 1
30896941 10.1021/acs.jmedchem.8b01283 Cytochrome P450 3A4 1
30896941 10.1021/acs.jmedchem.8b01283 Voltage-gated inwardly rectifying potassium channel KCNH2 1

Data from ChEMBL 36 via Core Engine