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Compound Detail

CHEMBL218143

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O=C(CN1CCN(c2ccc(C(F)(F)F)cn2)CC1)NC1C2CC3CC(C2)CC1(O)C3

Basic Information

ChEMBL ID CHEMBL218143
Phase Preclinical
Structure Type MOL
InChI Key HDLZHQFBHVJHLK-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
2
PK Parameters
4
Publications
0
Known Names

Molecular Properties

438.5
MW (Da)
2.28
ALogP
5
HBA
2
HBD
68.7
PSA (Ų)
0.76
QED
0
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C22H29F3N4O2
MW 438.49
Aromatic Rings 1
Heavy Atoms 31
NP-Likeness -1.47

Activity Summary

Ki 2 meas. best 6.96

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
11-beta-hydroxysteroid dehydrogenase 1
CHEMBL3910
Ki 6.96 6.96 110.0 1
11-beta-hydroxysteroid dehydrogenase 1
CHEMBL4235
Ki 6.75 6.75 180.0 1

Pharmacokinetic Data

Parameter Value Units Species
CL 216.67 mL.min-1.kg-1 Homo sapiens
CL 5133.33 mL.min-1.kg-1 Mus musculus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
17201418 10.1021/jm0609364 11-beta-hydroxysteroid dehydrogenase 1 3
17201418 10.1021/jm0609364 11-beta-hydroxysteroid dehydrogenase type 2 2
17201418 10.1021/jm0609364 Liver microsomes 1
17201418 10.1021/jm0609364 ADMET 1

Data from ChEMBL 36 via Core Engine