Assay Detail
Binding
CHEMBL3887328
Review assay metadata, readout intent, target linkage, and publication context from the same page.
DELFIA Assay: The kinase activity is measured by DELFIA assay (dissociation-enhanced lanthanide fluorescence immunoassay, Perkin Elmer). The cytoplasmic kinase domain of human IGF-1R (amino acids 964-1370) is expressed as a fusion protein with a glutathione-S-transferase tag (IGF-1R-GST) in High Five.TM. Cells (Invitrogen). Enzyme activity is measured in the presence of substances and a control substance. Poly-glutamate-tyrosine peptide (pEY, Sigma Aldrich) and biotinylated pEY (bio-pEY) are used as reaction substrates.10 uL of substance in 25% DMSO are mixed with 30 uL of IGF-1R-GST solution (67 mM HEPES pH 7.4, 15 ug/mL pEY, 1.7 ug/mL bio-pEY, 13.3 mM MgCl2, 3.3 mM dithiothreitol, 0.0033% Brij 35, 2 ng IGF-1R-GST) in 96-well plates. The reactions are started with 10 uL of a 750 uM ATP solution. After 40 min at RT the reactions are stopped with 50 .mu.L of stop solution (250 mM EDTA, 20 mM HEPES pH 7.4). 90 uL from each reaction are transferred.
174
Total Activities
171
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Target
Insulin-like growth factor 1 receptor (CHEMBL1957) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
5,8-dihydro-6H-pyrazolo[3,4-h]quinazolines as IGF-1R/IR inhibitors
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 174 | 9.43 | 10.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3950012 | — | — | 1 | 10.30 |
| CHEMBL3905758 | — | — | 1 | 10.30 |
| CHEMBL3928243 | — | — | 1 | 10.10 |
| CHEMBL3977170 | — | — | 1 | 10.10 |
| CHEMBL3979064 | — | — | 1 | 10.10 |
| CHEMBL3955626 | — | — | 1 | 10.10 |
| CHEMBL3896205 | — | — | 1 | 10.05 |
| CHEMBL3969930 | — | — | 1 | 10.05 |
| CHEMBL3979509 | — | — | 1 | 10.05 |
| CHEMBL3892425 | — | — | 1 | 10.00 |
| CHEMBL3985408 | — | — | 1 | 10.00 |
| CHEMBL3916799 | — | — | 1 | 10.00 |
| CHEMBL3893323 | — | — | 1 | 10.00 |
| CHEMBL3952080 | — | — | 2 | 10.00 |
| CHEMBL3986353 | — | — | 1 | 9.96 |
| CHEMBL3961098 | — | — | 1 | 9.96 |
| CHEMBL3921486 | — | — | 1 | 9.92 |
| CHEMBL3911964 | — | — | 1 | 9.89 |
| CHEMBL3965426 | — | — | 1 | 9.89 |
| CHEMBL3907737 | — | — | 1 | 9.89 |
| CHEMBL3939707 | — | — | 1 | 9.89 |
| CHEMBL3942607 | — | — | 1 | 9.89 |
| CHEMBL3947924 | — | — | 1 | 9.89 |
| CHEMBL3972210 | — | — | 1 | 9.85 |
| CHEMBL3958897 | — | — | 1 | 9.85 |
| CHEMBL3951322 | — | — | 1 | 9.85 |
| CHEMBL3946122 | — | — | 1 | 9.85 |
| CHEMBL3920050 | — | — | 1 | 9.82 |
| CHEMBL3976534 | — | — | 1 | 9.82 |
| CHEMBL3952388 | — | — | 1 | 9.82 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3905758 | — | IC50 | = | 0.05 | nM | 10.30 |
| CHEMBL3950012 | — | IC50 | = | 0.05 | nM | 10.30 |
| CHEMBL3979064 | — | IC50 | = | 0.08 | nM | 10.10 |
| CHEMBL3928243 | — | IC50 | = | 0.08 | nM | 10.10 |
| CHEMBL3977170 | — | IC50 | = | 0.08 | nM | 10.10 |
| CHEMBL3955626 | — | IC50 | = | 0.08 | nM | 10.10 |
| CHEMBL3896205 | — | IC50 | = | 0.09 | nM | 10.05 |
| CHEMBL3979509 | — | IC50 | = | 0.09 | nM | 10.05 |
| CHEMBL3969930 | — | IC50 | = | 0.09 | nM | 10.05 |
| CHEMBL3985408 | — | IC50 | = | 0.1 | nM | 10.00 |
| CHEMBL3893323 | — | IC50 | = | 0.1 | nM | 10.00 |
| CHEMBL3916799 | — | IC50 | = | 0.1 | nM | 10.00 |
| CHEMBL3952080 | — | IC50 | = | 0.1 | nM | 10.00 |
| CHEMBL3892425 | — | IC50 | = | 0.1 | nM | 10.00 |
| CHEMBL3961098 | — | IC50 | = | 0.11 | nM | 9.96 |
| CHEMBL3986353 | — | IC50 | = | 0.11 | nM | 9.96 |
| CHEMBL3921486 | — | IC50 | = | 0.12 | nM | 9.92 |
| CHEMBL3907737 | — | IC50 | = | 0.13 | nM | 9.89 |
| CHEMBL3939707 | — | IC50 | = | 0.13 | nM | 9.89 |
| CHEMBL3942607 | — | IC50 | = | 0.13 | nM | 9.89 |
| CHEMBL3965426 | — | IC50 | = | 0.13 | nM | 9.89 |
| CHEMBL3947924 | — | IC50 | = | 0.13 | nM | 9.89 |
| CHEMBL3911964 | — | IC50 | = | 0.13 | nM | 9.89 |
| CHEMBL3951322 | — | IC50 | = | 0.14 | nM | 9.85 |
| CHEMBL3958897 | — | IC50 | = | 0.14 | nM | 9.85 |
| CHEMBL3972210 | — | IC50 | = | 0.14 | nM | 9.85 |
| CHEMBL3946122 | — | IC50 | = | 0.14 | nM | 9.85 |
| CHEMBL3952388 | — | IC50 | = | 0.15 | nM | 9.82 |
| CHEMBL3920050 | — | IC50 | = | 0.15 | nM | 9.82 |
| CHEMBL3976534 | — | IC50 | = | 0.15 | nM | 9.82 |
| CHEMBL3928015 | — | IC50 | = | 0.16 | nM | 9.80 |
| CHEMBL3977626 | — | IC50 | = | 0.16 | nM | 9.80 |
| CHEMBL3891732 | — | IC50 | = | 0.16 | nM | 9.80 |
| CHEMBL3940776 | — | IC50 | = | 0.16 | nM | 9.80 |
| CHEMBL3950693 | — | IC50 | = | 0.16 | nM | 9.80 |
| CHEMBL3906800 | — | IC50 | = | 0.16 | nM | 9.80 |
| CHEMBL3985256 | — | IC50 | = | 0.16 | nM | 9.80 |
| CHEMBL3969767 | — | IC50 | = | 0.16 | nM | 9.80 |
| CHEMBL3967200 | — | IC50 | = | 0.16 | nM | 9.80 |
| CHEMBL3930224 | — | IC50 | = | 0.17 | nM | 9.77 |
| CHEMBL3959576 | — | IC50 | = | 0.17 | nM | 9.77 |
| CHEMBL3962155 | — | IC50 | = | 0.17 | nM | 9.77 |
| CHEMBL3985755 | — | IC50 | = | 0.17 | nM | 9.77 |
| CHEMBL3982422 | — | IC50 | = | 0.17 | nM | 9.77 |
| CHEMBL3956581 | — | IC50 | = | 0.18 | nM | 9.74 |
| CHEMBL3904495 | — | IC50 | = | 0.18 | nM | 9.74 |
| CHEMBL3983444 | — | IC50 | = | 0.19 | nM | 9.72 |
| CHEMBL3911240 | — | IC50 | = | 0.19 | nM | 9.72 |
| CHEMBL3952080 | — | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL3912872 | — | IC50 | = | 0.2 | nM | 9.70 |