Assay Detail
Binding
CHEMBL3706310
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 uM 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.
368
Total Activities
368
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Pyrrolo[2,3-B]pyridine CDK9 kinase inhibitors
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 368 | 7.27 | 8.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3673541 | — | — | 1 | 8.70 |
| CHEMBL3673542 | — | — | 1 | 8.70 |
| CHEMBL3673540 | — | — | 1 | 8.70 |
| CHEMBL3668457 | — | — | 1 | 8.40 |
| CHEMBL3673501 | — | — | 1 | 8.30 |
| CHEMBL3673503 | — | — | 1 | 8.30 |
| CHEMBL3673545 | — | — | 1 | 8.22 |
| CHEMBL3673532 | — | — | 1 | 8.15 |
| CHEMBL3668473 | — | — | 1 | 8.10 |
| CHEMBL3673539 | — | — | 1 | 8.10 |
| CHEMBL3668461 | — | — | 1 | 8.10 |
| CHEMBL3673494 | — | — | 1 | 8.05 |
| CHEMBL3673507 | — | — | 1 | 8.05 |
| CHEMBL3673530 | — | — | 1 | 8.05 |
| CHEMBL3673538 | — | — | 1 | 8.05 |
| CHEMBL3663778 | — | — | 1 | 8.00 |
| CHEMBL3673544 | — | — | 1 | 8.00 |
| CHEMBL3673512 | — | — | 1 | 8.00 |
| CHEMBL3673504 | — | — | 1 | 8.00 |
| CHEMBL3668361 | — | — | 1 | 8.00 |
| CHEMBL3663759 | — | — | 1 | 7.96 |
| CHEMBL3668476 | — | — | 1 | 7.96 |
| CHEMBL3673509 | — | — | 1 | 7.96 |
| CHEMBL3673523 | — | — | 1 | 7.96 |
| CHEMBL3673547 | — | — | 1 | 7.96 |
| CHEMBL3663764 | — | — | 1 | 7.92 |
| CHEMBL3668375 | — | — | 1 | 7.92 |
| CHEMBL3668418 | — | — | 1 | 7.92 |
| CHEMBL3673517 | — | — | 1 | 7.92 |
| CHEMBL3668378 | — | — | 1 | 7.89 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3673541 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3673542 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3673540 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3668457 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL3673501 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL3673503 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL3673545 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL3673532 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL3668461 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL3668473 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL3673539 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL3673507 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL3673538 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL3673530 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL3673494 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL3668361 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL3673504 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL3663778 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL3673544 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL3673512 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL3673509 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL3668476 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL3663759 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL3673547 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL3673523 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL3673517 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL3663764 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL3668418 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL3668375 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL3668378 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL3673520 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL3673531 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL3673518 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL3673524 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL3668385 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL3668370 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL3663792 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL3668401 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL3663796 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL3668427 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL3673493 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL3663746 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL3663774 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL3663797 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL3673515 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL3673500 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL3663802 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL3673521 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL3663743 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL3673533 | — | IC50 | = | 17.0 | nM | 7.77 |