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Compound Detail

CHEMBL365735

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c1cncc(-c2ccc3ccccc3c2)c1

Basic Information

ChEMBL ID CHEMBL365735
Phase Preclinical
Structure Type MOL
InChI Key JVWGLICJXUMGHN-UHFFFAOYSA-N
4
Targets
22
Activities
1
Assay Types
0
PK Parameters
19
Publications
0
Known Names

Molecular Properties

205.3
MW (Da)
3.90
ALogP
1
HBA
0
HBD
12.9
PSA (Ų)
0.59
QED
0
Ro5 Violations
1
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C15H11N
MW 205.26
Aromatic Rings 3
Heavy Atoms 16
NP-Likeness -0.76

Activity Summary

IC50 22 meas. best 7.55

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Cytochrome P450 11B2, mitochondrial
CHEMBL2722
IC50 7.55 7.1117 28.0 12
Cytochrome P450 11B1, mitochondrial
CHEMBL1908
IC50 5.62 5.4033 2395.0 6
Steroid 17-alpha-hydroxylase/17,20 lyase
CHEMBL3522
IC50 5.52 5.52 3000.0 1
Aromatase
CHEMBL1978
IC50 5.24 5.24 5700.0 3

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Cytochrome P450 11B2, mitochondrial IC50 = 28.4 nM 7.55 Inhibitory concentration against human cytochrome P450 11B2 expressing in V79 MZ... 16220979
Cytochrome P450 11B2, mitochondrial IC50 = 28.0 nM 7.55 Inhibition of human adrenal corticoid CYP11B2 expressed in chinese hamster V79 M... 18763754
Cytochrome P450 11B2, mitochondrial IC50 = 28.0 nM 7.55 Inhibition of human CYP11B2 23859149
Cytochrome P450 11B2, mitochondrial IC50 = 28.0 nM 7.55 Inhibition Assay: V79 MZh11B1 and V79 MZh 11B2 cells (8˙10^5 cells per well) wer... -
Cytochrome P450 11B2, mitochondrial IC50 = 28.4 nM 7.55 Inhibition Assay: V79 MZh11B1 and V79 MZh 11B2 cells (8˙10^5 cells per well) wer... -
Cytochrome P450 11B2, mitochondrial IC50 = 28.0 nM 7.55 Inhibition Assay: V79 MZh11B1 and V79 MZh 11B2 cells (8˙10^5 cells per well) wer... -
Cytochrome P450 11B2, mitochondrial IC50 = 28.4 nM 7.55 Inhibition Assay: V79 MZh11B1 and V79 MZh 11B2 cells (8˙10^5 cells per well) wer... -
Cytochrome P450 11B2, mitochondrial IC50 = 28.0 nM 7.55 Inhibitory concentration against human cytochrome P450 11B2 expressed in fission... 16220979
Cytochrome P450 11B2, mitochondrial IC50 = 163.9 nM 6.79 In Vitro Inhibition Assay: A suspension of fission yeast (S. pombe PE1) with a c... -
Cytochrome P450 11B2, mitochondrial IC50 = 163.9 nM 6.79 In Vitro Inhibition Assay: A suspension of fission yeast (S. pombe PE1) with a c... -
Cytochrome P450 11B2, mitochondrial IC50 = 2111.0 nM 5.68 In Vitro Inhibition Assay: A suspension of fission yeast (S. pombe PE1) with a c... -
Cytochrome P450 11B2, mitochondrial IC50 = 2111.0 nM 5.68 In Vitro Inhibition Assay: A suspension of fission yeast (S. pombe PE1) with a c... -
Cytochrome P450 11B1, mitochondrial IC50 = 2395.0 nM 5.62 Inhibition Assay: V79 MZh11B1 and V79 MZh 11B2 cells (8˙10^5 cells per well) wer... -
Cytochrome P450 11B1, mitochondrial IC50 = 2395.0 nM 5.62 Inhibition Assay: V79 MZh11B1 and V79 MZh 11B2 cells (8˙10^5 cells per well) wer... -
Steroid 17-alpha-hydroxylase/17,20 lyase IC50 = 3000.0 nM 5.52 Inhibition of human CYP17 23859149
Cytochrome P450 11B1, mitochondrial IC50 = 3449.0 nM 5.46 In Vitro Inhibition Assay: A suspension of fission yeast (S. pombe PE1) with a c... -
Cytochrome P450 11B1, mitochondrial IC50 = 5826.0 nM 5.24 Inhibitory concentration against human cytochrome P450 11B1 expressed in fission... 16220979
Aromatase IC50 = 5727.0 nM 5.24 Inhibitory concentration against human placental cytochrome P450 19A1 using [1-b... 16220979
Cytochrome P450 11B1, mitochondrial IC50 = 5826.0 nM 5.24 Inhibition of human adrenal corticoid CYP11B1 expressed in chinese hamster V79 M... 18763754
Aromatase IC50 = 5700.0 nM 5.24 Inhibition of human placental CYP19 19049427

Literature References

PubMed DOI Target Context # Activities
16220979 10.1021/jm0503704 Cytochrome P450 11B2, mitochondrial 3
18763754 10.1021/jm800683c Cytochrome P450 11B2, mitochondrial 2
19049427 10.1021/jm800888q Cytochrome P450 1A2 2
18763754 10.1021/jm800683c Unchecked 1
23859149 10.1021/jm400484p Unchecked 1
23859149 10.1021/jm400484p Aromatase 1
23859149 10.1021/jm400484p Steroid 17-alpha-hydroxylase/17,20 lyase 1
23859149 10.1021/jm400484p Cytochrome P450 11B2, mitochondrial 1
23859149 10.1021/jm400484p Cytochrome P450 11B1, mitochondrial 1
23859149 10.1021/jm400484p Cytochrome P450 3A4 1
19049427 10.1021/jm800888q Aromatase 1
19049427 10.1021/jm800888q Steroid 17-alpha-hydroxylase/17,20 lyase 1
18763754 10.1021/jm800683c Cytochrome P450 11B1, mitochondrial 1
16220979 10.1021/jm0503704 Caco-2 1
16220979 10.1021/jm0503704 No relevant target 1
16220979 10.1021/jm0503704 Unchecked 1
16220979 10.1021/jm0503704 Aromatase 1
16220979 10.1021/jm0503704 Steroid 17-alpha-hydroxylase/17,20 lyase 1
16220979 10.1021/jm0503704 Cytochrome P450 11B1, mitochondrial 1

Data from ChEMBL 36 via Core Engine