CDK Profiler Service

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
CDK1/cyclin A 9.3 88.7 n.a. 208,000 n.a.
CDK1/cyclin B 4.0 19 >20,000 >20,000 n.a.
CDK1/cyclin E 3.8 13.2 10,000 20,000 >50,000
CDK2/cyclin A 1.3 3.7 5,700 12,000 n.a.
CDK2/cyclin A1 1.2 4.6 >50,000 11,000 >50,000
CDK2/cyclin E 0.7 6.8 23,000 12,500 n.a.
CDK2/cyclin E2 1.8 6.5 33,000 11,000 >100,000
CDK2/cyclin O 0.98 3.1 16,700 8,000 >50,000
CDK3/cyclin E 1.8 2.0 42,000 8,200 >100,000
CDK3/cyclin E2 1.5 1.1 >100,000 11,000 >100,000
CDK4/cyclin D1 10 40 3,900 >100,000 9,200
CDK4/cyclin D2 11 5.8 5,800 15,000 >100,000
CDK4/cyclin D3 144 58 28,000 n.a. 265,000
CDK5/p25 2.0 4.2 13,200 19,000 n.a.
CDK5/p35 2.1 18 >20,000 15,000 n.a.
CDK6/cyclin D1 2.2 7.83 13,800 >100,000 20,500
CDK6/cyclin D2 47.4 21.2 6,500 >100,000 >100,000
CDK6/cyclin D3 21 25 14,000 24,000 >50,000
CDK7/cyclin H 115 160 >100,000 11,300 >100,000
CDK8/cyclin C 0.22 95 470 4,100 >100,000
CDK9/cyclin K 7.2 <1.0 5,600 6,300 >100,000
CDK9/cyclin T1 14 10 8,500 12,000 n.a.
CDK9/cyclin T2 6.4 <1.0 5,000 5,400 17,000
CDK12/cyclin K 120 20 28,000 1,100 >100,000
CDK12 (R722C)/cyclin K 70 16.3 >100,000 1,500 >100,000
CDK13/cyclin K 180 90 >100,000 990 >100,000
CDK14/cyclin Y 22 17 25,000 9,300 >50,000
CDK16/cyclin Y 14 15.3 72,000 11,800 30,000
CDK17/cyclin Y 15 0.4 18,000 12,000 >100,000
CDK18/cyclin Y 27 1.8 27,000 8,000 21,000
CDK19/cyclin C 0.3 94 1,000 4,800 >100,000
Screening Location

Malvern, PA, USA

Further information

More information can be found on our website Kinase Assays.