Compound Detail
CHEMBL141
LAMIVUDINE 💊 Approved Drug
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💊 Approved Drug
Basic Information
| ChEMBL ID | CHEMBL141 |
| Name | LAMIVUDINE |
| Phase | Approved |
| Structure Type | MOL |
| InChI Key | JTEGQNOMFQHVDC-NKWVEPMBSA-N |
| Therapeutic | ✓ Yes |
| Active Moiety | CHEMBL1230 |
24
Targets
371
Activities
3
Assay Types
30
PK Parameters
20
Publications
27
Known Names
20
Indications
5
Mechanisms
Molecular Properties
229.3
MW (Da)
-0.59
ALogP
7
HBA
2
HBD
90.4
PSA (Ų)
0.70
QED
0
Ro5 Violations
2
Rot. Bonds
Drug Information
| Molecule Type | Small molecule |
| First Approval | 1995 |
| Availability | Prescription |
| Chirality | Single Enantiomer |
Mechanism of Action
| Mechanism | Action Type | Target | Direct | Efficacy |
|---|---|---|---|---|
| Human immunodeficiency virus type 1 reverse transcriptase inhibitor | INHIBITOR | Human immunodeficiency virus type 1 reverse transcriptase | ✓ | ✓ |
| DNA inhibitor | INHIBITOR | DNA | ✓ | ✓ |
| DNA inhibitor | INHIBITOR | DNA | ✓ | ✓ |
| DNA inhibitor | INHIBITOR | DNA | ✓ | ✓ |
| DNA polymerase/reverse transcriptase inhibitor | INHIBITOR | DNA polymerase/reverse transcriptase | ✓ | ✓ |
Indications
Autoimmune Diseases Hepatitis Hepatitis B Hepatitis B, Chronic Hepatitis B, Chronic HIV Infections HIV Infections Infections Inflammation Virus Diseases Acquired Immunodeficiency Syndrome AIDS-Associated Nephropathy Carcinoma, Hepatocellular Diarrhea Liver Cirrhosis Tuberculosis Colorectal Neoplasms Lymphoma Lymphoma, Non-Hodgkin Paraparesis, Tropical Spastic
ATC Classification
J05AF05
lamivudine
Level 1: ANTIINFECTIVES FOR SYSTEMIC USE
Level 2: ANTIVIRALS FOR SYSTEMIC USE
Drug Warnings
Black Box Warning
hepatotoxicity
Black Box Warning
metabolic toxicity
Black Box Warning
General Warning
Activity Summary
EC50 280 meas. best 8.74
IC50 89 meas. best 8.7
Kd 2 meas. best 5.82
Target Activity Profile
| Target | Type | Best pChEMBL | Mean pChEMBL | Best (nM) | # Data |
|---|---|---|---|---|---|
| Human immunodeficiency virus 1 CHEMBL378 | EC50 | 8.74 | 5.8641 | 1.8 | 166 |
| Human immunodeficiency virus CHEMBL613758 | EC50 | 8.74 | 6.668 | 1.8 | 5 |
| ADMET CHEMBL612558 | IC50 | 8.7 | 7.3533 | 2.0 | 3 |
| Hepatitis B virus CHEMBL613497 | EC50 | 8.42 | 6.6554 | 3.8 | 65 |
| HepG2 CHEMBL395 | EC50 | 8.1 | 7.064 | 8.0 | 5 |
| Hepatoma cell line CHEMBL614821 | EC50 | 8.0 | 8.0 | 10.0 | 1 |
| NON-PROTEIN TARGET CHEMBL3879801 | EC50 | 8.0 | 5.82 | 10.0 | 6 |
| ADMET CHEMBL612558 | EC50 | 8.0 | 7.46 | 10.0 | 4 |
| PBMC CHEMBL613107 | EC50 | 7.94 | 7.755 | 11.6 | 2 |
| Human immunodeficiency virus 1 CHEMBL378 | IC50 | 7.66 | 6.4914 | 21.8 | 21 |
| Hepatitis B virus CHEMBL613497 | IC50 | 7.6 | 6.073 | 25.0 | 23 |
| HBV genotype D CHEMBL612769 | EC50 | 7.52 | 6.9425 | 30.0 | 4 |
| Duck hepatitis B virus CHEMBL613761 | EC50 | 7.4 | 7.4 | 40.0 | 2 |
| Human immunodeficiency virus type 1 reverse transcriptase CHEMBL247 | EC50 | 7.38 | 7.38 | 42.0 | 1 |
| Hepatoblastoma cell line CHEMBL614820 | EC50 | 7.16 | 7.16 | 70.0 | 1 |
| Anas sp. CHEMBL612370 | IC50 | 7.0 | 7.0 | 100.0 | 1 |
| MT4 CHEMBL388 | IC50 | 7.0 | 6.614 | 100.0 | 5 |
| Human immunodeficiency virus 2 CHEMBL380 | EC50 | 6.75 | 5.3544 | 180.0 | 9 |
| Heat shock factor protein 1 CHEMBL5313 | EC50 | 6.54 | 6.54 | 287.0 | 1 |
| Core antigen CHEMBL1075091 | EC50 | 6.43 | 6.43 | 370.0 | 1 |
| MT4 CHEMBL388 | EC50 | 6.4 | 5.9533 | 400.0 | 3 |
| Human gammaherpesvirus 4 CHEMBL613124 | EC50 | 6.4 | 6.4 | 400.0 | 1 |
| Unchecked CHEMBL612545 | Kd | 5.82 | 5.82 | 1510.0 | 1 |
| Human alphaherpesvirus 1 CHEMBL377 | IC50 | 5.66 | 5.66 | 2200.0 | 1 |
| Unchecked CHEMBL612545 | EC50 | 4.95 | 4.72 | 11300.0 | 2 |
| Human immunodeficiency virus 2 CHEMBL380 | IC50 | 4.81 | 4.81 | 15500.0 | 2 |
| Albumin CHEMBL3253 | Kd | 4.36 | 4.36 | 44000.0 | 1 |
| CCRF-CEM CHEMBL382 | IC50 | 4.3 | 4.3 | 50000.0 | 2 |
| Voltage-gated L-type calcium channel CHEMBL2095229 | IC50 | 4.27 | 4.27 | 54200.0 | 1 |
| Human adenovirus 2 CHEMBL613715 | IC50 | 4.0 | 4.0 | 100000.0 | 1 |
Pharmacokinetic Data
| Parameter | Value | Units | Species |
|---|---|---|---|
| AUC | 10.42 | pmol | Homo sapiens |
| AUC | 70.01 | pmol | Homo sapiens |
| AUC | 65.19 | pmol | Homo sapiens |
| AUC | 15700.0 | ng.hr.mL-1 | Homo sapiens |
| AUC | 15500.0 | ng.hr.mL-1 | Homo sapiens |
| AUC | 0.03531 | ng.hr.mL-1 | Homo sapiens |
| AUC | 0.03691 | ng.hr.mL-1 | Homo sapiens |
| AUC | 7800.0 | ng.hr.mL-1 | Homo sapiens |
| AUC | 5420.0 | ng.hr.mL-1 | Homo sapiens |
| AUC | 3710.0 | ng.hr.mL-1 | Homo sapiens |
| AUC | 6540.0 | ng.hr.mL-1 | Homo sapiens |
| AUC | 4440.0 | ng.hr.mL-1 | Homo sapiens |
| AUC | 9800.0 | ng.hr.mL-1 | Homo sapiens |
| AUC | 8100.0 | ng.hr.mL-1 | Homo sapiens |
| AUC | 9100.0 | ng.hr.mL-1 | Homo sapiens |
| AUC | 9.8 | mg/L | Homo sapiens |
| AUC | 90523.31 | ng.hr.mL-1 | Macaca mulatta |
| AUC | 0.0298 | ng.hr.mL-1 | Macaca mulatta |
| CL | 4.8 | mL.min-1.kg-1 | Homo sapiens |
| CL | 1.4 | mL.min-1.kg-1 | Homo sapiens |
| CL | 4.8 | mL.min-1.kg-1 | Homo sapiens |
| CL | 72.0 | mL.min-1.kg-1 | Rattus norvegicus |
| CL | 4.8 | mL.min-1.kg-1 | Homo sapiens |
| CL | 13.0 | mL.min-1.kg-1 | Macaca |
| CL | 20.0 | mL.min-1.kg-1 | Homo sapiens |
| CL | 22.0 | mL.min-1.kg-1 | Canis lupus familiaris |
| CL | 46.5 | mL.min-1.kg-1 | Rattus norvegicus |
| Cmax | 0.00076 | nM | Homo sapiens |
| Cmax | 0.004424 | nM | Homo sapiens |
| Cmax | 0.00484 | nM | Homo sapiens |
Activity Data Samples
Top measurements by pChEMBL value
Literature References
Data from ChEMBL 36 via Core Engine