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Compound Detail

CHEMBL386630

TESTOSTERONE
💊 Approved Drug
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💊 Approved Drug
C[C@]12CC[C@H]3[C@@H](CCC4=CC(=O)CC[C@@]43C)[C@@H]1CC[C@@H]2O

Basic Information

ChEMBL ID CHEMBL386630
Name TESTOSTERONE
Phase Approved
Structure Type MOL
InChI Key MUMGGOZAMZWBJJ-DYKIIFRCSA-N
Therapeutic ✓ Yes

Known Names

Androderm Androgel Androgel 1% Android-t Androlan Andropatch Axiron Fortesta Homosterone Intrinsa Livensa Natesto +18 more
18
Targets
52
Activities
4
Assay Types
30
PK Parameters
20
Publications
30
Known Names
20
Indications
1
Mechanisms

Molecular Properties

288.4
MW (Da)
3.88
ALogP
2
HBA
1
HBD
37.3
PSA (Ų)
0.73
QED
0
Ro5 Violations
0
Rot. Bonds

Drug Information

Molecule Type Small molecule
First Approval 1972
Availability Prescription
Chirality Single Enantiomer

Routes of Administration

Parenteral Topical

Flags

Black Box Warning Natural Product
USAN Stem -ster-; -terone

Extended Properties

Molecular Formula C19H28O2
MW 288.43
Aromatic Rings 0
Heavy Atoms 21
NP-Likeness 2.52

Mechanism of Action

Mechanism Action Type Target Direct Efficacy
Androgen Receptor agonist AGONIST Androgen receptor

Indications

Hypogonadism Hypogonadism Klinefelter Syndrome Neoplasms Neoplasms Orchitis Sexual Dysfunctions, Psychological Sexual Dysfunctions, Psychological Coronary Disease Disorders of Sex Development Erectile Dysfunction Hip Fractures Infertility Kidney Failure, Chronic Menopause Metabolic Syndrome Acquired Immunodeficiency Syndrome Anorexia Nervosa Carcinoma, Intraductal, Noninfiltrating Dwarfism

ATC Classification

G03BA03
testosterone
Level 1: GENITO URINARY SYSTEM AND SEX HORMONES
Level 2: SEX HORMONES AND MODULATORS OF THE GENITAL SYSTEM

Drug Warnings

Black Box Warning
General Warning
Country: United States

Activity Summary

IC50 29 meas. best 8.57
Ki 16 meas. best 8.85
EC50 5 meas. best 8.96
Kd 2 meas. best 9.4

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Androgen receptor
CHEMBL1871
Kd 9.4 9.4 0.4 1
Sex hormone-binding globulin
CHEMBL3305
Kd 9.2 9.2 0.6 1
Androgen receptor
CHEMBL1871
EC50 8.96 8.7267 1.1 3
Androgen receptor
CHEMBL3072
Ki 8.85 8.5133 1.4 6
Androgen receptor
CHEMBL3056
EC50 8.7 8.7 2.0 1
Androgen receptor
CHEMBL1871
IC50 8.57 8.3413 2.7 8
Androgen receptor
CHEMBL3072
IC50 8.49 7.6 3.2 4
Androgen receptor
CHEMBL3056
IC50 7.96 7.96 11.0 1
Sex hormone-binding globulin
CHEMBL3305
IC50 7.85 7.85 14.0 1
Androgen receptor
CHEMBL1871
Ki 7.54 7.54 29.0 1
Voltage-dependent L-type calcium channel subunit alpha-1C
CHEMBL1940
IC50 7.47 7.445 34.0 2
Cytochrome P450 3A4
CHEMBL340
IC50 7.43 6.9517 37.0 6
Corticosteroid-binding globulin
CHEMBL2421
Ki 6.72 6.72 190.6 1
Progesterone receptor
CHEMBL1909044
Ki 6.6 6.6 252.0 1
Aromatase
CHEMBL1978
Ki 6.22 6.22 600.0 1
Sigma non-opioid intracellular receptor 1
CHEMBL287
Ki 5.92 5.92 1200.0 1
Glucocorticoid receptor
CHEMBL2034
Ki 5.84 5.84 1457.0 1
Steroid 5-alpha-reductase
CHEMBL2096664
IC50 5.72 5.72 1900.0 1
Progesterone receptor
CHEMBL1909044
IC50 5.71 5.71 1935.0 1
Glucocorticoid receptor
CHEMBL2034
IC50 5.49 5.49 3206.0 1
Solute carrier organic anion transporter family member 1A1
CHEMBL1781859
Ki 5.27 5.27 5400.0 1
C-8 sterol isomerase ERG2
CHEMBL3224
Ki 5.11 5.11 7760.0 1
G-protein coupled bile acid receptor 1
CHEMBL5409
EC50 4.74 4.74 18300.0 1
Nuclear receptor subfamily 1 group I member 3
CHEMBL3069
IC50 4.52 4.52 30000.0 1
Lanosterol 14-alpha demethylase
CHEMBL3849
IC50 4.3 4.3 50000.0 1
Alpha-synuclein
CHEMBL6152
IC50 4.01 4.01 96800.0 1

Pharmacokinetic Data

Parameter Value Units Species
AUC 43.33 ng.hr.mL-1 Mus musculus
AUC 1.0 ng.hr.mL-1 Mus musculus
AUC 145.0 ng.hr.mL-1 Macaca fascicularis
Cavg 365.0 ng/dL Homo sapiens
Cavg 612.0 ng/dL Homo sapiens
CL 109.3 mL.min-1.g-1 Homo sapiens
CL 375.6 mL.min-1.g-1 Rattus norvegicus
CL 312.6 mL.min-1.g-1 Mus musculus
CL 150.0 uL.min-1.(10^6cells)-1 Homo sapiens
CL 692.1 mL.min-1.g-1 Mus musculus
CL 2725.1 mL.min-1.kg-1 Mus musculus
CL 87.1 mL.min-1.kg-1 Mus musculus
CL 1421.4 mL.min-1.g-1 Rattus norvegicus
CL 92.0 mL.min-1.g-1 Homo sapiens
CL 46.9 mL.min-1.kg-1 Homo sapiens
CL 96.0 mL.min-1.g-1 Homo sapiens
CL 82.2 mL.min-1.g-1 Homo sapiens
CL 74.0 mL.min-1.kg-1 Homo sapiens
CL 86.3 mL.min-1.kg-1 Homo sapiens
CL 95.9 mL.min-1.g-1 Homo sapiens
CL 70.1 mL.min-1.g-1 Homo sapiens
CL 0.0631 mL.min-1.kg-1 Homo sapiens
CL 106.0 mL.min-1.g-1 Homo sapiens
CL 95.4 mL.min-1.kg-1 Homo sapiens
CL 95.2 mL.min-1.g-1 Homo sapiens
CL 85.7 mL.min-1.kg-1 Homo sapiens
CL 0.0911 mL.min-1.kg-1 Homo sapiens
CL 3.776 mL.min-1.kg-1 Rattus norvegicus
CL 71.3 mL.min-1.g-1 Homo sapiens
CL 478.8 mL.min-1.g-1 Mus musculus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Androgen receptor Kd = 0.4 nM 9.4 Binding affinity to human Androgen receptor 35786895
Sex hormone-binding globulin Kd = 0.631 nM 9.2 Displacement of [3H]5alpha dihydrotestosterone from human sex hormone binding gl... 18330978
Androgen receptor EC50 = 1.1 nM 8.96 Androgenic activity at human androgen receptor expressed in African green monkey... 28696695
Androgen receptor Ki = 1.4 nM 8.85 Inhibitory constant against rat prostate cytosol androgen receptor using [3H]mib... 10966753
Androgen receptor Ki = 1.413 nM 8.85 Inhibition of [3H]mibolerone binding to cytosolic androgen receptor of rat ventr... 15715462
Androgen receptor EC50 = 1.9 nM 8.72 Modulation of Androgen receptor (unknown origin) 35063736
Androgen receptor EC50 = 1.995 nM 8.7 Agonist activity at androgen receptor in mouse NIH3T3 cells transiently transfec... 19856921
Androgen receptor IC50 = 2.7 nM 8.57 Binding affinity to androgen receptor 17448656
Androgen receptor IC50 = 2.7 nM 8.57 Binding affinity at AR 17890084
Androgen receptor IC50 = 2.7 nM 8.57 Inhibitory activity against AR 16309907
Androgen receptor EC50 = 3.162 nM 8.5 Agonist activity at androgen receptor in human MDA-KB2 cells transfected with MM... 19856921
Androgen receptor IC50 = 3.2 nM 8.49 In vitro antagonist activity against rat prostatic androgen receptor (AR) 3783591
Androgen receptor IC50 = 3.9 nM 8.41 Inhibition of human androgen receptor expressed in Escherichia coli 15456242
Androgen receptor Ki = 4.112 nM 8.39 DRUGMATRIX: Androgen (Testosterone) AR radioligand binding (ligand: [3H] Miboler... -
Androgen receptor IC50 = 4.17 nM 8.38 Antagonist activity against pSG5-tagged human androgen receptor expressed in COS... 25646649
Androgen receptor Ki = 4.3 nM 8.37 Displacement of [3H]Mibolerone from rat recombinant androgen receptor expressed ... 23403082
Androgen receptor IC50 = 4.27 nM 8.37 Displacement of [3H]R1881 from pSG5-tagged human androgen receptor expressed in ... 25646649
Androgen receptor IC50 = 4.571 nM 8.34 Displacement of [3H]R1881 from wild type human androgen receptor expressed in CO... 22746350
Androgen receptor Ki = 4.9 nM 8.31 Binding affinity against rat prostate cytosolic Androgen receptor using [3H]mibo... 11327585
Androgen receptor Ki = 4.9 nM 8.31 Inhibition of rat prostate cytosolic androgen receptor 15454212

Literature References

Data from ChEMBL 36 via Core Engine