Compound Detail
CHEMBL4112930
PAMIPARIB 🧪 Phase III
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🧪 Phase III
Basic Information
| ChEMBL ID | CHEMBL4112930 |
| Name | PAMIPARIB |
| Phase | Phase III |
| Structure Type | MOL |
| InChI Key | DENYZIUJOTUUNY-MRXNPFEDSA-N |
17
Targets
38
Activities
2
Assay Types
30
PK Parameters
20
Publications
2
Known Names
13
Indications
2
Mechanisms
Molecular Properties
298.3
MW (Da)
2.08
ALogP
3
HBA
2
HBD
60.5
PSA (Ų)
0.78
QED
0
Ro5 Violations
0
Rot. Bonds
Drug Information
| Molecule Type | Small molecule |
| Chirality | Single Enantiomer |
Mechanism of Action
| Mechanism | Action Type | Target | Direct | Efficacy |
|---|---|---|---|---|
| Poly [ADP-ribose] polymerase-1 inhibitor | INHIBITOR | Poly [ADP-ribose] polymerase 1 | ✓ | ✓ |
| Poly [ADP-ribose] polymerase 2 inhibitor | INHIBITOR | Poly [ADP-ribose] polymerase 2 | ✓ | ✓ |
Indications
Neoplasms Neoplasms Biliary Tract Neoplasms Breast Neoplasms Ovarian Neoplasms Prostatic Neoplasms Prostatic Neoplasms, Castration-Resistant Small Cell Lung Carcinoma Stomach Neoplasms Carcinoma, Non-Small-Cell Lung Carcinoma, Squamous Cell Central Nervous System Neoplasms Glioblastoma
ATC Classification
L01XK06
pamiparib
Level 1: ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS
Level 2: ANTINEOPLASTIC AGENTS
Activity Summary
IC50 33 meas. best 9.96
EC50 5 meas. best 9.7
Target Activity Profile
| Target | Type | Best pChEMBL | Mean pChEMBL | Best (nM) | # Data |
|---|---|---|---|---|---|
| Poly [ADP-ribose] polymerase 2 CHEMBL5366 | IC50 | 9.96 | 9.374 | 0.1 | 5 |
| Poly [ADP-ribose] polymerase 1 CHEMBL3105 | EC50 | 9.7 | 8.795 | 0.2 | 2 |
| Poly [ADP-ribose] polymerase 1 CHEMBL3105 | IC50 | 9.08 | 8.8583 | 0.8 | 6 |
| MDA-MB-436 CHEMBL4296465 | EC50 | 7.97 | 7.97 | 10.6 | 1 |
| HCC1395 CHEMBL1075454 | EC50 | 7.37 | 7.37 | 42.5 | 1 |
| Unchecked CHEMBL612545 | EC50 | 7.27 | 7.27 | 53.8 | 1 |
| Protein mono-ADP-ribosyltransferase PARP3 CHEMBL5083 | IC50 | 7.17 | 6.95 | 68.0 | 2 |
| Poly [ADP-ribose] polymerase tankyrase-2 CHEMBL6154 | IC50 | 6.85 | 6.485 | 140.0 | 2 |
| Poly [ADP-ribose] polymerase tankyrase-1 CHEMBL6164 | IC50 | 6.64 | 6.64 | 230.0 | 1 |
| Unchecked CHEMBL612545 | IC50 | 6.3 | 6.3 | 500.0 | 1 |
| Protein mono-ADP-ribosyltransferase PARP12 CHEMBL2429709 | IC50 | 5.62 | 5.62 | 2400.0 | 1 |
| Protein mono-ADP-ribosyltransferase PARP11 CHEMBL2380189 | IC50 | 5.57 | 5.57 | 2700.0 | 1 |
| Protein mono-ADP-ribosyltransferase PARP8 CHEMBL3091262 | IC50 | 5.08 | 5.08 | 8400.0 | 1 |
| Protein mono-ADP-ribosyltransferase PARP10 CHEMBL2429708 | IC50 | 4.96 | 4.96 | 11000.0 | 1 |
| Protein mono-ADP-ribosyltransferase TIPARP CHEMBL2380188 | IC50 | 4.96 | 4.96 | 11000.0 | 1 |
| Solute carrier organic anion transporter family member 1B3 CHEMBL1743121 | IC50 | 4.71 | 4.71 | 19400.0 | 1 |
| Solute carrier organic anion transporter family member 1B1 CHEMBL1697668 | IC50 | 4.71 | 4.71 | 19400.0 | 1 |
| Organic anion transporter 3 CHEMBL1641348 | IC50 | 4.62 | 4.62 | 23900.0 | 1 |
| Solute carrier family 22 member 6 CHEMBL1641347 | IC50 | 4.32 | 4.32 | 47800.0 | 1 |
Pharmacokinetic Data
| Parameter | Value | Units | Species |
|---|---|---|---|
| AUC | 1600.0 | ng.hr.mL-1 | Canis lupus familiaris |
| AUC | 1085.0 | ng.hr.mL-1 | Canis lupus familiaris |
| AUC | 3469.0 | ng.hr.mL-1 | Rattus norvegicus |
| AUC | 1482.0 | ng.hr.mL-1 | Rattus norvegicus |
| AUC | 5521.0 | ng.hr.mL-1 | Mus musculus |
| AUC | 1757.0 | ng.hr.mL-1 | Mus musculus |
| CL | 15.2 | mL.min-1.kg-1 | Canis lupus familiaris |
| CL | 22.7 | mL.min-1.kg-1 | Rattus norvegicus |
| CL | 29.9 | mL.min-1.kg-1 | Mus musculus |
| CL | 7.2 | mL.min-1.g-1 | Rattus norvegicus |
| CL | 9.5 | mL.min-1.g-1 | Canis lupus familiaris |
| CL | 7.9 | mL.min-1.g-1 | Homo sapiens |
| CL | 12.9 | mL.min-1.kg-1 | Mus musculus |
| Cmax | 1682.76 | nM | Canis lupus familiaris |
| Cmax | 2886.16 | nM | Rattus norvegicus |
| Cmax | 9094.26 | nM | Mus musculus |
| F | 72.6 | % | Canis lupus familiaris |
| F | 98.7 | % | Mus musculus |
| F | 93.7 | % | Rattus norvegicus |
| Fu | 0.21 | - | Canis lupus familiaris |
| Fu | 0.151 | - | Rattus norvegicus |
| Fu | 0.15 | - | Mus musculus |
| Fu | 0.043 | - | Homo sapiens |
| T1/2 | 3.62 | hr | Canis lupus familiaris |
| T1/2 | 2.07 | hr | Canis lupus familiaris |
| T1/2 | 5.5 | hr | Rattus norvegicus |
| T1/2 | 5.3 | hr | Rattus norvegicus |
| T1/2 | 3.16 | hr | Mus musculus |
| T1/2 | 3.95 | hr | Mus musculus |
| Tmax | 0.417 | hr | Canis lupus familiaris |
Activity Data Samples
Top measurements by pChEMBL value
Literature References
Data from ChEMBL 36 via Core Engine