Species | Target name | Source | Bibliographic reference |
---|---|---|---|
Homo sapiens | epidermal growth factor receptor | Starlite/ChEMBL | References |
Homo sapiens | erb-b2 receptor tyrosine kinase 2 | Starlite/ChEMBL | References |
Activity type | Activity value | Assay description | Source | Reference |
---|---|---|---|---|
Activity (ADMET) | Toxicity in BALB/c athymic mouse xenografted with human NCI-N87 cells assessed as weight loss at 200 mg/kg, po qd after 4 days | ChEMBL. | 24121234 | |
Activity (ADMET) | Toxicity in BALB/c athymic mouse xenografted with human SKOV3 cells assessed as hematuria at 200 mg/kg, po qd after 4 days | ChEMBL. | 24121234 | |
Activity (ADMET) | Toxicity in BALB/c athymic mouse xenografted with human NCI-N87 cells assessed as death at 200 mg/kg, po qd after 4 days | ChEMBL. | 24121234 | |
Activity (ADMET) | Toxicity in BALB/c athymic mouse xenografted with human SKOV3 cells assessed as lethargic condition at 200 mg/kg, po qd | ChEMBL. | 24121234 | |
Activity (ADMET) | Toxicity in BALB/c athymic mouse xenografted with human NCI-N87 cells assessed as lethargic condition at 200 mg/kg, po qd | ChEMBL. | 24121234 | |
Activity (ADMET) | Toxicity in BALB/c athymic mouse xenografted with human SKOV3 cells assessed as weight loss at 200 mg/kg, po qd after 4 days | ChEMBL. | 24121234 | |
Activity (ADMET) | Toxicity in BALB/c athymic mouse xenografted with human NCI-N87 cells assessed as diarrhea at 200 mg/kg, po qd | ChEMBL. | 24121234 | |
Activity (ADMET) | Toxicity in BALB/c athymic mouse xenografted with human NCI-N87 cells assessed as hematuria at 200 mg/kg, po qd after 4 days | ChEMBL. | 24121234 | |
Activity (ADMET) | Toxicity in BALB/c athymic mouse xenografted with human SKOV3 cells assessed as death at 200 mg/kg, po qd after 4 days | ChEMBL. | 24121234 | |
Activity (ADMET) | Toxicity in BALB/c athymic mouse xenografted with human NCI-N87 cells assessed as scruffy skin at 200 mg/kg, po qd | ChEMBL. | 24121234 | |
Activity (ADMET) | Toxicity in BALB/c athymic mouse xenografted with human SKOV3 cells assessed as scruffy skin at 200 mg/kg, po qd | ChEMBL. | 24121234 | |
Activity (ADMET) | Toxicity in BALB/c athymic mouse xenografted with human SKOV3 cells assessed as diarrhea at 200 mg/kg, po qd | ChEMBL. | 24121234 | |
IC50 (binding) | = 10.8 nM | Inhibition of EGFR (unknown origin) using poly-(Glu4-Tyr) as substrate after 1 hr by ELISA-based spectrophotometry | ChEMBL. | 24121234 |
IC50 (binding) | = 12.3 nM | Inhibition of HER-2 (unknown origin) using poly-(Glu4-Tyr) as substrate after 1 hr by ELISA-based spectrophotometry | ChEMBL. | 24121234 |
IC50 (functional) | = 29.2 nM | Cytotoxicity against human NCI-N87 cells after 72 hrs by SRB assay | ChEMBL. | 24121234 |
Species name | Source | Reference | Is orphan |
---|---|---|---|
Homo sapiens | ChEMBL23 | 24121234 |
Many chemical entities in TDR Targets come from high-throughput screenings with whole cells or tissue samples, and not all assayed compounds have been tested against a single a single target protein, probably because they get ruled out during screening process. Even if these compounds may have not been of interest in the original screening, they may come as interesting leads for other screening assays. Furthermore, we may be able to propose drug-target associations using chemical similarities and network patterns.
1 literature reference was collected for this gene.