Details of the Target

General Information of Target

Target ID LDTP05242
Target Name Cyclin-dependent kinase 3 (CDK3)
Gene Name CDK3
Gene ID 1018
Synonyms
CDKN3; Cyclin-dependent kinase 3; EC 2.7.11.22; Cell division protein kinase 3
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MDMFQKVEKIGEGTYGVVYKAKNRETGQLVALKKIRLDLEMEGVPSTAIREISLLKELKH
PNIVRLLDVVHNERKLYLVFEFLSQDLKKYMDSTPGSELPLHLIKSYLFQLLQGVSFCHS
HRVIHRDLKPQNLLINELGAIKLADFGLARAFGVPLRTYTHEVVTLWYRAPEILLGSKFY
TTAVDIWSIGCIFAEMVTRKALFPGDSEIDQLFRIFRMLGTPSEDTWPGVTQLPDYKGSF
PKWTRKGLEEIVPNLEPEGRDLLMQLLQYDPSQRITAKTALAHPYFSSPEPSPAARQYVL
QRFRH
Target Type
Clinical trial
Target Bioclass
Enzyme
Family
Protein kinase superfamily, CMGC Ser/Thr protein kinase family, CDC2/CDKX subfamily
Function
Serine/threonine-protein kinase that plays a critical role in the control of the eukaryotic cell cycle; involved in G0-G1 and G1-S cell cycle transitions. Interacts with CCNC/cyclin-C during interphase. Phosphorylates histone H1, ATF1, RB1 and CABLES1. ATF1 phosphorylation triggers ATF1 transactivation and transcriptional activities, and promotes cell proliferation and transformation. CDK3/cyclin-C mediated RB1 phosphorylation is required for G0-G1 transition. Promotes G1-S transition probably by contributing to the activation of E2F1, E2F2 and E2F3 in a RB1-independent manner.
TTD ID
T22956
Uniprot ID
Q00526
DrugMap ID
TTMYWL7
Ensemble ID
ENST00000425876.6
HGNC ID
HGNC:1772
ChEMBL ID
CHEMBL4442

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 3 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
Sulforaphane-probe2
 Probe Info  		1.95  LDD0160  [1]
HHS-475
 Probe Info  		Y159(1.04); Y19(1.04)  LDD0264  [2]
HHS-465
 Probe Info  		Y19(10.00)  LDD2237  [3]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0116  HHS-0101 DM93 Y159(1.04); Y19(1.04)  LDD0264  [2]
 LDCM0117  HHS-0201 DM93 Y19(0.57); Y159(0.87)  LDD0265  [2]
 LDCM0118  HHS-0301 DM93 Y159(0.63); Y19(0.64)  LDD0266  [2]
 LDCM0119  HHS-0401 DM93 Y159(0.66); Y19(0.78)  LDD0267  [2]
 LDCM0120  HHS-0701 DM93 Y159(0.90); Y19(1.07)  LDD0268  [2]
 LDCM0003  Sulforaphane MDA-MB-231 1.95  LDD0160  [1]

The Interaction Atlas With This Target

The Protein(s) Related To This Target

Transporter and channel
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Heat shock protein HSP 90-beta (HSP90AB1) Heat shock protein 90 family P08238
Transcription factor
Click To Hide/Show 5 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Paired box protein Pax-6 (PAX6) Paired homeobox family P26367
Forkhead box protein P2 (FOXP2) . O15409
LIM/homeobox protein Lhx4 (LHX4) . Q969G2
Paired box protein Pax-5 (PAX5) . Q02548
Paired box protein Pax-8 (PAX8) . Q06710
GPCR
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Olfactory receptor 2G6 (OR2G6) G-protein coupled receptor 1 family Q5TZ20
Other
Click To Hide/Show 10 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Cyclin-dependent kinase inhibitor 1 (CDKN1A) CDI family P38936
Cyclin-dependent kinases regulatory subunit 1 (CKS1B) CKS family P61024
Cyclin-dependent kinases regulatory subunit 2 (CKS2) CKS family P33552
Cyclin-I (CCNI) Cyclin family Q14094
Cyclin-C (CCNC) Cyclin family P24863
Cyclin-H (CCNH) Cyclin family P51946
G1/S-specific cyclin-D3 (CCND3) Cyclin family P30281
Negative elongation factor A (NELFA) NELF-A family Q9H3P2
Speedy protein E4 (SPDYE4) Speedy/Ringo family A6NLX3
Rac GTPase-activating protein 1 (RACGAP1) . Q9H0H5

The Drug(s) Related To This Target

Phase 1
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Rgb-286638 Small molecular drug D03DKV
Patented
Click To Hide/Show 3 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Nitrogen Mustard Derivative 1 Small molecular drug D0LK4L
Oxazolyl Methylthiothiazole Derivative 1 Small molecular drug D0M5DX
Pmid26161698-compound-17 Small molecular drug D0FQ6V

References

1 Competition-based, quantitative chemical proteomics in breast cancer cells identifies new target profiles for sulforaphane. Chem Commun (Camb). 2017 May 4;53(37):5182-5185. doi: 10.1039/c6cc08797c.
Mass spectrometry data entry: PXD006279
2 Discovery of a Cell-Active SuTEx Ligand of Prostaglandin Reductase 2. Chembiochem. 2021 Jun 15;22(12):2134-2139. doi: 10.1002/cbic.202000879. Epub 2021 Apr 29.
3 Global targeting of functional tyrosines using sulfur-triazole exchange chemistry. Nat Chem Biol. 2020 Feb;16(2):150-159. doi: 10.1038/s41589-019-0404-5. Epub 2019 Nov 25.