Skip to main content
Free research Free research Free compound review with research home and workspace preview
Quick search ChEMBL 36
Compound Detail

CHEMBL4472335

Enter ChEMBL ID:
Free Research Context This compound will appear in recent viewed items on the research home for this browser.
Research home View demo workspace
C[C@]1(c2ccc(Cl)cc2Cl)OC[C@@H](COc2ccc(N3CCN(c4ccc(NC(=O)c5cccnc5)cc4)CC3)cc2)O1

Basic Information

ChEMBL ID CHEMBL4472335
Phase Preclinical
Structure Type MOL
InChI Key AOCSOWXEGDBAIH-CPBHLAHYSA-N
1
Targets
1
Activities
1
Assay Types
2
PK Parameters
8
Publications
0
Known Names

Molecular Properties

619.5
MW (Da)
6.63
ALogP
7
HBA
1
HBD
76.2
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 C33H32Cl2N4O4
MW 619.55
Aromatic Rings 4
Heavy Atoms 43
NP-Likeness -0.88

Activity Summary

IC50 1 meas. best 6.72

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Protein smoothened
CHEMBL6080
IC50 6.72 6.72 190.0 1

Pharmacokinetic Data

Parameter Value Units Species
CL 78300.0 mL.min-1.g-1 Homo sapiens
T1/2 0.1483 hr Homo sapiens

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Protein smoothened IC50 = 190.0 nM 6.72 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 No relevant target 2
30896941 10.1021/acs.jmedchem.8b01283 ADMET 2
30896941 10.1021/acs.jmedchem.8b01283 Protein smoothened 1
30896941 10.1021/acs.jmedchem.8b01283 Medulloblastoma cell 1
30896941 10.1021/acs.jmedchem.8b01283 Cytochrome P450 3A4 1
30896941 10.1021/acs.jmedchem.8b01283 Broad substrate specificity ATP-binding cassette transporter ABCG2 1
30896941 10.1021/acs.jmedchem.8b01283 ATP-dependent translocase ABCB1 1
30896941 10.1021/acs.jmedchem.8b01283 Voltage-gated inwardly rectifying potassium channel KCNH2 1

Data from ChEMBL 36 via Core Engine