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Compound Detail

CHEMBL2043433

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CN1CC[C@@H](NC(=O)Nc2ccc3c(c2)OCCO3)C[C@@H]1c1nc2ccccc2[nH]1

Basic Information

ChEMBL ID CHEMBL2043433
Phase Preclinical
Structure Type MOL
InChI Key LYAJEDCSRBEEKH-CRAIPNDOSA-N
1
Targets
1
Activities
1
Assay Types
2
PK Parameters
2
Publications
0
Known Names

Molecular Properties

407.5
MW (Da)
3.29
ALogP
5
HBA
3
HBD
91.5
PSA (Ų)
0.62
QED
0
Ro5 Violations
3
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C22H25N5O3
MW 407.47
Aromatic Rings 3
Heavy Atoms 30
NP-Likeness -1.41

Activity Summary

IC50 1 meas. best 7.35

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Protein smoothened
CHEMBL6080
IC50 7.35 7.35 45.0 1

Pharmacokinetic Data

Parameter Value Units Species
CL 0.012 mL.min-1.kg-1 Homo sapiens
CL 0.0076 mL.min-1.kg-1 Homo sapiens

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Protein smoothened IC50 = 45.0 nM 7.35 Inhibition of Smo in mouse C3H10T1/2 cells using human recombinant SHH assessed ... 24900436

Literature References

PubMed DOI Target Context # Activities
24900436 10.1021/ml2002423 Protein smoothened 2
24900436 10.1021/ml2002423 Liver microsomes 2

Data from ChEMBL 36 via Core Engine