Compound Detail
CHEMBL4068509
PRN-1371 Phase I
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Phase I
C=CC(=O)N1CCN(CCCn2c(=O)c(-c3c(Cl)c(OC)cc(OC)c3Cl)cc3cnc(NC)nc32)CC1
Basic Information
| ChEMBL ID | CHEMBL4068509 |
| Name | PRN-1371 |
| Phase | Phase I |
| Structure Type | MOL |
| InChI Key | PUIXMSRTTHLNKI-UHFFFAOYSA-N |
14
Targets
26
Activities
3
Assay Types
26
PK Parameters
20
Publications
3
Known Names
1
Indications
Molecular Properties
561.5
MW (Da)
3.54
ALogP
9
HBA
1
HBD
101.8
PSA (Ų)
0.40
QED
1
Ro5 Violations
9
Rot. Bonds
Drug Information
| Molecule Type | Small molecule |
| Chirality | Achiral |
Indications
Urinary Bladder Neoplasms
Activity Summary
IC50 21 meas. best 9.22
Ki 4 meas. best 8.89
Kd 1 meas.
Target Activity Profile
| Target | Type | Best pChEMBL | Mean pChEMBL | Best (nM) | # Data |
|---|---|---|---|---|---|
| Fibroblast growth factor receptor 1 CHEMBL3650 | IC50 | 9.22 | 9.0717 | 0.6 | 6 |
| Fibroblast growth factor receptor 2 CHEMBL4142 | Ki | 8.89 | 8.89 | 1.3 | 1 |
| Fibroblast growth factor receptor 2 CHEMBL4142 | IC50 | 8.89 | 8.74 | 1.3 | 2 |
| Fibroblast growth factor receptor 1 CHEMBL3650 | Ki | 8.8 | 8.8 | 1.6 | 1 |
| Fibroblast growth factor receptor 3 CHEMBL2742 | Ki | 8.66 | 8.66 | 2.2 | 1 |
| SNU-16 CHEMBL613529 | IC50 | 8.59 | 8.59 | 2.6 | 1 |
| Fibroblast growth factor receptor 3 CHEMBL2742 | IC50 | 8.39 | 8.39 | 4.1 | 1 |
| Macrophage colony-stimulating factor 1 receptor CHEMBL1844 | IC50 | 8.09 | 8.09 | 8.1 | 1 |
| Fibroblast growth factor receptor 4 CHEMBL3973 | IC50 | 7.71 | 7.71 | 19.3 | 1 |
| Fibroblast growth factor receptor 4 CHEMBL3973 | Ki | 7.14 | 7.14 | 73.0 | 1 |
| Cytoplasmic tyrosine-protein kinase BMX CHEMBL3834 | IC50 | 6.57 | 6.57 | 272.0 | 1 |
| Tyrosine-protein kinase Blk CHEMBL2250 | IC50 | 6.43 | 6.43 | 371.0 | 1 |
| Vascular endothelial growth factor receptor 3 CHEMBL1955 | IC50 | 6.39 | 6.39 | 410.0 | 1 |
| Tyrosine-protein kinase JAK3 CHEMBL2148 | IC50 | 6.25 | 6.25 | 556.0 | 1 |
| Tyrosine-protein kinase Lyn CHEMBL3905 | IC50 | 6.2 | 6.195 | 631.0 | 2 |
| Vascular endothelial growth factor receptor 2 CHEMBL279 | IC50 | 6.15 | 6.15 | 705.0 | 1 |
| Eukaryotic translation initiation factor 2-alpha kinase 3 CHEMBL6030 | IC50 | 6.1 | 6.1 | 792.0 | 1 |
| Serine/threonine-protein kinase TAO2 CHEMBL1075195 | IC50 | 5.93 | 5.93 | 1175.0 | 1 |
Pharmacokinetic Data
| Parameter | Value | Units | Species |
|---|---|---|---|
| AUC | 208.0 | ng.hr.mL-1 | Rattus norvegicus |
| AUC | 4348.0 | ng.hr.mL-1 | Rattus norvegicus |
| AUC | 284.0 | ng.hr.mL-1 | Canis lupus familiaris |
| AUC | 1344.0 | ng.hr.mL-1 | Canis lupus familiaris |
| AUC | 472.0 | ng.hr.mL-1 | Macaca fascicularis |
| AUC | 84.4 | ng.hr.mL-1 | Macaca fascicularis |
| CL | - | mL.min-1.g-1 | Homo sapiens |
| CL | 1.35 | mL.min-1.g-1 | Homo sapiens |
| CL | 160.0 | mL.min-1.kg-1 | Rattus norvegicus |
| CL | 117.0 | mL.min-1.kg-1 | Canis lupus familiaris |
| CL | 42.9 | mL.min-1.kg-1 | Macaca fascicularis |
| Cmax | 1061.5 | nM | Rattus norvegicus |
| Cmax | 3179.15 | nM | Rattus norvegicus |
| Cmax | 1935.99 | nM | Canis lupus familiaris |
| Cmax | 1964.49 | nM | Canis lupus familiaris |
| Cmax | 1779.26 | nM | Macaca fascicularis |
| Cmax | 170.62 | nM | Macaca fascicularis |
| F | 208.0 | % | Rattus norvegicus |
| F | 94.0 | % | Canis lupus familiaris |
| F | 2.3 | % | Macaca fascicularis |
| T1/2 | 0.764 | hr | Rattus norvegicus |
| T1/2 | 3.77 | hr | Rattus norvegicus |
| T1/2 | 0.33 | hr | Canis lupus familiaris |
| T1/2 | 0.58 | hr | Canis lupus familiaris |
| T1/2 | 0.349 | hr | Macaca fascicularis |
| T1/2 | 0.486 | hr | Macaca fascicularis |
Activity Data Samples
Top measurements by pChEMBL value
Literature References
Data from ChEMBL 36 via Core Engine