Assay Detail
Binding
CHEMBL5732901
Review assay metadata, readout intent, target linkage, and publication context from the same page.
LANCE ULight TR-FRET Kinase Assay: CDK9 enzyme activities were measured using LANCE ULight TR-FRET kinase assay reagents (PerkinElmer, Waltham, Mass.). Compounds were directly added in 100% DMSO to white low volume assay plates (Perkin Elmer Proxiplate 6008289) using a Labcyte Echo acoustic dispenser. Assay reagents in serine/threonine kinase assay buffer containing 20 mM HEPES, 10 mM MgCl2, 100 mM Na3VO4, and 0.0075% Triton X-100. were added for final reaction mixture concentrations of 1000 μM ATP, 100 nM U-light MBP peptide (Perkin Elmer TRF0109M) and reaction initiated with 4 nM CDK9/Cyclin T1 (Carna Biosciences 04-110). The kinase reaction was carried out for 30 minutes before addition of stopping buffer to a final of 20 mM EDTA and 0.5 nM of LANCE Ultra Europium anti-phospho-MBP antibody (PerkinElmer TRF0201M) in LANCE detection buffer (PerkinElmer CR97-100). The reaction was equilibrated for 1 hour and the signal read in the Perkin Elmer Envision in TR-FRET mode (excitation at 320 nm and emission at 615/665 nm).
4089
Total Activities
1352
Compounds Tested
3
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 7 — Homologous single protein target |
| Curated By | Autocuration |
Publication
Pyrrolo [2,3-B] pyridine CDK9 kinase inhibitors
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 1363 | 7.03 | 8.40 |
| kon | 1363 | - | - |
| k_off | 1363 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL6065695 | — | — | 3 | 8.40 |
| CHEMBL3668457 | — | — | 3 | 8.40 |
| CHEMBL5986595 | — | — | 3 | 8.22 |
| CHEMBL5943573 | — | — | 3 | 8.15 |
| CHEMBL3668461 | — | — | 3 | 8.10 |
| CHEMBL3668473 | — | — | 3 | 8.10 |
| CHEMBL5902372 | — | — | 3 | 8.05 |
| CHEMBL5990315 | — | — | 3 | 8.05 |
| CHEMBL3663778 | — | — | 3 | 8.00 |
| CHEMBL3668361 | — | — | 6 | 8.00 |
| CHEMBL5782477 | — | — | 3 | 8.00 |
| CHEMBL3663759 | — | — | 3 | 7.96 |
| CHEMBL3668476 | — | — | 3 | 7.96 |
| CHEMBL3668418 | — | — | 3 | 7.92 |
| CHEMBL5769589 | — | — | 3 | 7.92 |
| CHEMBL3668375 | — | — | 3 | 7.92 |
| CHEMBL3663764 | — | — | 3 | 7.92 |
| CHEMBL3668378 | — | — | 3 | 7.89 |
| CHEMBL3663792 | — | — | 3 | 7.85 |
| CHEMBL3668370 | — | — | 3 | 7.85 |
| CHEMBL3668385 | — | — | 3 | 7.85 |
| CHEMBL3668401 | — | — | 3 | 7.85 |
| CHEMBL5834238 | — | — | 3 | 7.85 |
| CHEMBL5854326 | — | — | 3 | 7.85 |
| CHEMBL5984950 | — | — | 3 | 7.85 |
| CHEMBL3663746 | — | — | 3 | 7.82 |
| CHEMBL3663774 | — | — | 3 | 7.82 |
| CHEMBL3663796 | — | — | 3 | 7.82 |
| CHEMBL3663797 | — | — | 3 | 7.82 |
| CHEMBL3663802 | — | — | 3 | 7.82 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL6065695 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL3668457 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL5986595 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL5943573 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL3668461 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL3668473 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL5902372 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL5990315 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL3663778 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL5782477 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL3668361 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL3668476 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL3663759 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL3668418 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL3668375 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL3663764 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL5769589 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL3668378 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL3668385 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL5854326 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL3663792 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL5984950 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL5834238 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL3668370 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL3668401 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL3663746 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL3668427 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL5947200 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL5905192 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL3663802 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL3663774 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL3663796 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL3663797 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL5905080 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL5852792 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL3663743 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL6010037 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL3668350 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL3663777 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL5949412 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL3663769 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL5940848 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL6035846 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL3663799 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL3668421 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL5875544 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL6024010 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL6065926 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL3668480 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL3663775 | — | IC50 | = | 18.0 | nM | 7.75 |