Activity-based CDK Profiler for compound profiling via radiometric HotSpotTM kinase assay.
Target Overview
CAT#
CDK
Enzyme
Human CDK
HGNC
CDK
Synonym
Cyclin-dependent kinase 1, p34 protein kinase, CDC2, Cell division control protein 2 homolog
Assay Properties
Reaction
Substrate + [γ-33P]-ATP = 33P-Substrate + ADP
Readout
Enzymatic activity
Reference Compound IC50s (nM)
Mutant | Staurosporine | Ro 31-8220 | GW 5074 | H-89 | Rottlerin | Abemaciclib | AT-7519 | OTS964 |
---|---|---|---|---|---|---|---|---|
CDK1/cyclin A | 9.3 | 88.7 | n.a. | 208,000 | n.a. | n.a. | n.a. | n.a. |
CDK1/cyclin B | 4.0 | 19 | >20,000 | >20,000 | n.a. | n.a. | n.a. | n.a. |
CDK1/cyclin E | 3.8 | 13.2 | 10,000 | 20,000 | >50,000 | n.a. | n.a. | n.a. |
CDK2/cyclin A | 1.3 | 3.7 | 5,700 | 12,000 | n.a. | n.a. | n.a. | n.a. |
CDK2/cyclin A1 | 1.2 | 4.6 | >50,000 | 11,000 | >50,000 | n.a. | n.a. | n.a. |
CDK2/cyclin E | 0.7 | 6.8 | 23,000 | 12,500 | n.a. | n.a. | n.a. | n.a. |
CDK2/cyclin E2 | 1.8 | 6.5 | 33,000 | 11,000 | >100,000 | n.a. | n.a. | n.a. |
CDK2/cyclin O | 0.98 | 3.1 | 16,700 | 8,000 | >50,000 | n.a. | n.a. | n.a. |
CDK3/Cyclin C | 0.5 | 52 | 550 | 2,700 | n.a. | >100,000 | n.a. | n.a. |
CDK3/cyclin E | 1.8 | 2.0 | 42,000 | 8,200 | >100,000 | n.a. | n.a. | n.a. |
CDK3/cyclin E2 | 1.5 | 1.1 | >100,000 | 11,000 | >100,000 | n.a. | n.a. | n.a. |
CDK4/cyclin D1 | 10 | 40 | 3,900 | >100,000 | 9,200 | n.a. | n.a. | n.a. |
CDK4/cyclin D2 | 11 | 5.8 | 5,800 | 15,000 | >100,000 | n.a. | n.a. | n.a. |
CDK4/cyclin D3 | 144 | 58 | 28,000 | n.a. | 265,000 | n.a. | n.a. | n.a. |
CDK5/p25 | 2.0 | 4.2 | 13,200 | 19,000 | n.a. | n.a. | n.a. | n.a. |
CDK5/p35 | 2.1 | 18 | >20,000 | 15,000 | n.a. | n.a. | n.a. | n.a. |
CDK6/cyclin D1 | 2.2 | 7.83 | 13,800 | >100,000 | 20,500 | n.a. | n.a. | n.a. |
CDK6/cyclin D2 | 47.4 | 21.2 | 6,500 | >100,000 | >100,000 | n.a. | n.a. | n.a. |
CDK6/cyclin D3 | 21 | 25 | 14,000 | 24,000 | >50,000 | n.a. | n.a. | n.a. |
CDK7/cyclin H | 115 | 160 | >100,000 | 11,300 | >100,000 | n.a. | n.a. | n.a. |
CDK8/cyclin C | 48 | 960 | 1,100 | 3,600 | >100,000 | n.a. | n.a. | n.a. |
CDK9/cyclin K | 7.2 | <1.0 | 5,600 | 6,300 | >100,000 | n.a. | n.a. | n.a. |
CDK9/cyclin T1 | 14 | 10 | 8,500 | 12,000 | n.a. | n.a. | n.a. | n.a. |
CDK9/cyclin T2 | 6.4 | <1.0 | 5,000 | 5,400 | 17,000 | n.a. | n.a. | n.a. |
CDK11B/Cyclin K | >100,000 | >100,000 | >100,000 | n.a. | n.a. | n.a. | 28 | 310 |
CDK12/cyclin K | 120 | 20 | 28,000 | 1,100 | >100,000 | n.a. | n.a. | n.a. |
CDK12 (R722C)/cyclin K | 70 | 16.3 | >100,000 | 1,500 | >100,000 | n.a. | n.a. | n.a. |
CDK13/cyclin K | 180 | 90 | >100,000 | 990 | >100,000 | n.a. | n.a. | n.a. |
CDK14/cyclin Y | 22 | 17 | 25,000 | 9,300 | >50,000 | n.a. | n.a. | n.a. |
CDK16/cyclin Y | 14 | 15.3 | 72,000 | 11,800 | 30,000 | n.a. | n.a. | n.a. |
CDK17/cyclin Y | 15 | 0.4 | 18,000 | 12,000 | >100,000 | n.a. | n.a. | n.a. |
CDK18/cyclin Y | 27 | 1.8 | 27,000 | 8,000 | 21,000 | n.a. | n.a. | n.a. |
CDK19/cyclin C | 0.3 | 94 | 1,000 | 4,800 | >100,000 | n.a. | n.a. | n.a. |
CDK15/Cyclin B1 | 1.9 | 2.4 | 8,400 | 15,000 | n.a. | 43 | n.a. | n.a. |
CDK15/Cyclin A2 | 0.8 | 5.8 | 14,000 | 3,900 | 2,200 | n.a. | n.a. | n.a. |
Screening Location
Malvern, PA, USA
Further Information
More information can be found on our website Kinase Assays.
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