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Compound Detail

CHEMBL3099695

OSILODROSTAT
💊 Approved Drug
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💊 Approved Drug
N#Cc1ccc([C@H]2CCc3cncn32)c(F)c1
ChEMBL ↗ Properties Compare Identifier

Basic Information

ChEMBL ID CHEMBL3099695
Name OSILODROSTAT
Phase Approved
Structure Type MOL
InChI Key USUZGMWDZDXMDG-CYBMUJFWSA-N
Therapeutic ✓ Yes

Known Names

Lci-699 LCI-699-NX Lci699 LCI699-NX Osilodrostat
9
Targets
34
Activities
1
Assay Types
3
PK Parameters
20
Publications
5
Known Names
8
Indications

Molecular Properties

227.2
MW (Da)
2.43
ALogP
3
HBA
0
HBD
41.6
PSA (Ų)
0.75
QED
0
Ro5 Violations
1
Rot. Bonds

Drug Information

Molecule Type Small molecule
First Approval 2020
Availability Prescription
Chirality Single Enantiomer

Routes of Administration

Oral

Flags

First in Class
USAN Stem -stat
USAN Year 2015

Extended Properties

Molecular Formula C13H10FN3
MW 227.24
Aromatic Rings 2
Heavy Atoms 17
NP-Likeness -1.10

Indications

Adrenal Gland Diseases Pituitary ACTH Hypersecretion Cushing Syndrome Essential Hypertension Hyperaldosteronism Hypertension Kidney Diseases Liver Diseases

ATC Classification

H02CA02
osilodrostat
Level 1: SYSTEMIC HORMONAL PREPARATIONS, EXCL. SEX HORMONES AND INSULINS
Level 2: CORTICOSTEROIDS FOR SYSTEMIC USE

Activity Summary

IC50 34 meas. best 9.7

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Cytochrome P450 11B2, mitochondrial
CHEMBL2722
 IC50 9.7 9.2646 0.2 13
Cytochrome P450 11B1, mitochondrial
CHEMBL1908
 IC50 8.6 8.436 2.5 10
Unchecked
CHEMBL612545
 IC50 7.7 7.52 19.9 3
Cytochrome P450 11B2, mitochondrial
CHEMBL3237
 IC50 6.96 6.96 111.0 1
Cytochrome P450 11B2, mitochondrial
CHEMBL3621020
 IC50 6.68 6.68 210.0 1
Cytochrome P450 11B1, mitochondrial
CHEMBL4970
 IC50 6.3 6.3 495.0 1
Aromatase
CHEMBL1978
 IC50 6.07 5.6967 856.0 3
Steroid 17-alpha-hydroxylase/17,20 lyase
CHEMBL3522
 IC50 5.4 5.4 3981.1 1
ADMET
CHEMBL612558
 IC50 5.32 5.32 4800.0 1

Pharmacokinetic Data

Parameter Value Units Species
F 42.0 % Rattus norvegicus
T1/2 4.0 hr Homo sapiens
Tmax 1.0 hr Homo sapiens

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Cytochrome P450 11B2, mitochondrial IC50 = 0.2 nM 9.7 Inhibition of human CYP11B2 expressed in hamster V79MZh cells using deoxycortico... 24899257
Cytochrome P450 11B2, mitochondrial IC50 = 0.2 nM 9.7 Inhibition of human aldosterone synthase expressed in V79 MZ cells 24422519
Cytochrome P450 11B2, mitochondrial IC50 = 0.2 nM 9.7 Inhibition of CYP11B2 in human V79MZ cells using [3H]-11-deoxycorticosterone as ... 25528333
Cytochrome P450 11B2, mitochondrial IC50 = 0.2 nM 9.7 Inhibition of human CYP11B2 expressed in V79 MZh cells using [14C]-deoxycorticos... 25711516
Cytochrome P450 11B2, mitochondrial IC50 = 0.2 nM 9.7 Inhibition of human CYP11B2 expressed in hamster V79MZ cells using [1,2-3H]-11-d... 28570067
Cytochrome P450 11B2, mitochondrial IC50 = 0.2 nM 9.7 Inhibition of CYP11B2 (unknown origin) 24899257
Cytochrome P450 11B2, mitochondrial IC50 = 0.5 nM 9.3 Inhibition of human CYP11B2 expressed in Chinese hamster V79 MZh cells using [14... 35975976
Cytochrome P450 11B2, mitochondrial IC50 = 0.7 nM 9.15 Inhibition of human recombinant CYP11B2 using 11-deoxycorticosterone as substrat... 24900631
Cytochrome P450 11B2, mitochondrial IC50 = 0.7 nM 9.15 Inhibition of human recombinant CYP11B2 using 11-deoxycorticosterone as substrat... 26540564
Cytochrome P450 11B2, mitochondrial IC50 = 0.7 nM 9.15 Inhibition of recombinant human CYP11B2 36155354
Cytochrome P450 11B2, mitochondrial IC50 = 1.2 nM 8.92 Inhibition of human CYP11B2 expressed in Chinese hamster V79 cell mitochondria a... 29878770
Cytochrome P450 11B1, mitochondrial IC50 = 2.5 nM 8.6 Inhibition of human recombinant CYP11B1 using 11-deoxycortisol as substrate by c... 24900631
Cytochrome P450 11B1, mitochondrial IC50 = 2.5 nM 8.6 Inhibition human recombinant CYP11B1 using 11-deoxycorticosterone as substrate a... 26540564
Cytochrome P450 11B1, mitochondrial IC50 = 2.5 nM 8.6 Inhibition of recombinant human CYP11B1 36155354
Cytochrome P450 11B1, mitochondrial IC50 = 2.9 nM 8.54 Inhibition of human CYP11B1 expressed in V79 MZh cells using [14C]-deoxycorticos... 25711516
Cytochrome P450 11B1, mitochondrial IC50 = 2.9 nM 8.54 Inhibition of CYP11B1 in human V79MZ cells using [3H]-11-deoxycorticosterone as ... 25528333
Cytochrome P450 11B1, mitochondrial IC50 = 2.9 nM 8.54 Inhibition of human CYP11B1 expressed in hamster V79MZh cells using deoxycortico... 24899257
Cytochrome P450 11B1, mitochondrial IC50 = 2.9 nM 8.54 Inhibition of human CYP11B1 expressed in V79 MZ cells 24422519
Cytochrome P450 11B2, mitochondrial IC50 = 3.0 nM 8.52 Inhibition of human CYP11B2 expressed in renal leiomyoblastoma cells 26403853
Cytochrome P450 11B1, mitochondrial IC50 = 3.0 nM 8.52 Inhibition of human CYP11B1 expressed in hamster V79MZ cells using [1,2-3H]-11-d... 28570067

Literature References

PubMed DOI Target Context # Activities
24422519 10.1021/jm401430e Homo sapiens 11
25874338 10.1016/j.ejmech.2015.04.013 Homo sapiens 6
26403853 10.1021/acs.jmedchem.5b00851 Mus musculus 6
24900631 10.1021/ml400324c Rattus norvegicus 4
24900631 10.1021/ml400324c Cytochrome P450 11B2, mitochondrial 3
26288685 10.1021/acsmedchemlett.5b00048 Homo sapiens 3
26403853 10.1021/acs.jmedchem.5b00851 Cynomolgus monkey 3
29254646 10.1016/j.bmcl.2017.12.015 Unchecked 3
24900631 10.1021/ml400324c Cytochrome P450 11B1, mitochondrial 2
31312408 10.1021/acsmedchemlett.9b00152 Cynomolgus monkey 2
- 10.6019/CHEMBL4495565 SARS-CoV-2 2
29878770 10.1021/acs.jmedchem.8b00328 ADMET 2
26403853 10.1021/acs.jmedchem.5b00851 Cytochrome P450 11B2, mitochondrial 2
37468498 10.1038/s41467-023-40064-9 Cannabinoid receptor 1 2
24899257 10.1021/jm500140c Cytochrome P450 11B2, mitochondrial 2
37468498 10.1038/s41467-023-40064-9 Gamma-aminobutyric acid receptor subunit alpha-1 2
24422519 10.1021/jm401430e Unchecked 1
36155354 10.1016/j.ejmech.2022.114742 Unchecked 1
24422519 10.1021/jm401430e Cytochrome P450 11B2, mitochondrial 1
24900631 10.1021/ml400324c ADMET 1

Data from ChEMBL 36 via Core Engine