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Compound Detail

CHEMBL2331704

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COC(C)(C)c1cncc(-c2ccc3c(c2)CCc2nnc(C)n2-3)c1

Basic Information

ChEMBL ID CHEMBL2331704
Phase Preclinical
Structure Type MOL
InChI Key MDISRFPYOOBZRK-UHFFFAOYSA-N
4
Targets
6
Activities
1
Assay Types
4
PK Parameters
10
Publications
0
Known Names

Molecular Properties

334.4
MW (Da)
3.62
ALogP
5
HBA
0
HBD
52.8
PSA (Ų)
0.73
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 C20H22N4O
MW 334.42
Aromatic Rings 3
Heavy Atoms 25
NP-Likeness -0.74

Activity Summary

IC50 6 meas. best 8.52

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Unchecked
CHEMBL612545
IC50 8.52 8.52 3.0 1
Cytochrome P450 11B2, mitochondrial
CHEMBL2722
IC50 8.3 8.01 5.0 2
Cytochrome P450 11B1, mitochondrial
CHEMBL1908
IC50 6.97 6.815 108.0 2
Aromatase
CHEMBL1978
IC50 4.95 4.95 11160.0 1

Pharmacokinetic Data

Parameter Value Units Species
CL 107.0 mL.min-1.kg-1 Rattus norvegicus
CL 177.0 mL.min-1.kg-1 Rattus norvegicus
F 10.0 % Rattus norvegicus
T1/2 0.3 hr Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
26288685 10.1021/acsmedchemlett.5b00048 Rattus norvegicus 4
26288685 10.1021/acsmedchemlett.5b00048 Cytochrome P450 11B2, mitochondrial 2
24900679 10.1021/ml4000589 Cytochrome P450 11B1, mitochondrial 1
24900679 10.1021/ml4000589 Cytochrome P450 11B2, mitochondrial 1
26288685 10.1021/acsmedchemlett.5b00048 Cytochrome P450 11B1, mitochondrial 1
26288685 10.1021/acsmedchemlett.5b00048 Liver microsome 1
26288685 10.1021/acsmedchemlett.5b00048 Steroid 17-alpha-hydroxylase/17,20 lyase 1
26288685 10.1021/acsmedchemlett.5b00048 Aromatase 1
26288685 10.1021/acsmedchemlett.5b00048 Cytochrome P450 3A4 1
26288685 10.1021/acsmedchemlett.5b00048 Unchecked 1

Data from ChEMBL 36 via Core Engine