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Compound Detail

CHEMBL1682904

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CC(C)[C@](O)(c1ccc2c3c(ccc2c1)C(=O)N(C)C3)c1c[nH]cn1

Basic Information

ChEMBL ID CHEMBL1682904
Phase Preclinical
Structure Type MOL
InChI Key UCYQUZAJMGMKEU-FQEVSTJZSA-N
2
Targets
2
Activities
1
Assay Types
5
PK Parameters
9
Publications
0
Known Names

Molecular Properties

335.4
MW (Da)
3.04
ALogP
3
HBA
2
HBD
69.2
PSA (Ų)
0.77
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 C20H21N3O2
MW 335.41
Aromatic Rings 3
Heavy Atoms 25
NP-Likeness 0.12

Activity Summary

IC50 2 meas. best 7.72

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Steroid 17-alpha-hydroxylase/17,20 lyase
CHEMBL3522
IC50 7.72 7.72 19.0 1
Cytochrome P450 2C8
CHEMBL3721
IC50 4.55 4.55 28000.0 1

Pharmacokinetic Data

Parameter Value Units Species
AUC 573.0 ng.hr.mL-1 Rattus norvegicus
AUC 7315.0 ng.hr.mL-1 Rattus norvegicus
Cmax 8774.34 nM Rattus norvegicus
F 127.7 % Rattus norvegicus
Tmax 0.42 hr Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Steroid 17-alpha-hydroxylase/17,20 lyase IC50 = 19.0 nM 7.72 Inhibition of 17,20 lyase activity in human 21316976
Cytochrome P450 2C8 IC50 = 28000.0 nM 4.55 Inhibition of human CYP2C8 21316976

Literature References

PubMed DOI Target Context # Activities
21316976 10.1016/j.bmc.2011.01.017 Rattus norvegicus 5
21316976 10.1016/j.bmc.2011.01.017 Cynomolgus monkey 4
21316976 10.1016/j.bmc.2011.01.017 Unchecked 3
21316976 10.1016/j.bmc.2011.01.017 Steroid 17-alpha-hydroxylase/17,20 lyase 2
21316976 10.1016/j.bmc.2011.01.017 Cytochrome P450 2C8 1
21316976 10.1016/j.bmc.2011.01.017 Cytochrome P450 2C9 1
21316976 10.1016/j.bmc.2011.01.017 Cytochrome P450c11B3 1
21316976 10.1016/j.bmc.2011.01.017 Cytochrome P450 3A4 1
21316976 10.1016/j.bmc.2011.01.017 Cytochrome P450 2D6 1

Data from ChEMBL 36 via Core Engine