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TargetEnzymes

Cyclin-dependent kinase 8

Named enzymes, including the metabolising cytochromes and the monoamine oxidases.

Measurements
2
Compounds
1
Binding constants
0
Median pX
—

I · Identity

What this target is

Its function as UniProt states it, where in a cell the protein is found, and which cell types and tissues transcribe its gene.

Protein

CDK8_HUMANCDK8Homo sapiens

Cyclin-dependent kinase 8

Component of the Mediator complex, a coactivator involved in regulated gene transcription of nearly all RNA polymerase II-dependent genes. Mediator functions as a bridge to convey information from gene-specific regulatory proteins to the basal RNA polymerase II transcription machinery. Mediator is recruited to promoters by direct interactions with regulatory proteins and serves as a scaffold for the assembly of a functional pre-initiation complex with RNA polymerase II and the general transcription factors. Phosphorylates the CTD (C-terminal domain) of the large subunit of RNA polymerase II (RNAp II), which may inhibit the formation of a transcription initiation complex. Phosphorylates CCNH leading to down-regulation of the TFIIH complex and transcriptional repression10993082. Recruited through interaction with MAML1 to hyperphosphorylate the intracellular domain of NOTCH, leading to its degradation15546612. Selectively regulates the interferon response by phosphorylating the transcription factor STAT1 transactivation domain (By similarity)

Quoted from UniProt’s FUNCTION annotation for P49336 (reviewed). The superscript numbers are UniProt’s own PubMed citations, kept in the sentence and in order, each linking to the paper it names.

What it acts with

STRING’s highest-confidence human functional partners. The combined score mixes several kinds of evidence, so each channel is shown separately — a partner supported by experiment is a different claim from one supported only by text mining, and for a receptor this is where its coupling appears as evidence rather than as assertion.

PartnerCombinedExperimentDatabaseText mining
MED120.9990.9310.9000.999
MED140.9990.9510.9000.866
MED60.9990.9250.9000.947
MED130.9990.9330.9000.996
MED170.9990.9170.9000.887
CCNC0.9990.9990.9000.999
MED80.9980.8770.9000.853
MED10.9980.9280.9000.731
MED210.9980.9060.9000.828
MED180.9980.8400.9000.913

Where it sits in the cell

  • Nucleoplasm

Human Protein Atlas, by antibody immunofluorescence in cell lines — a different assay from the expression figures below, which are RNA.

UniProt, curated Nucleus

Expression by cell type

Single cell type RNA, the 2 highest of those the Human Protein Atlas reports for this gene. Transcript, not protein, and a cell type rather than a tissue.

  • Myosatellite cells477.5 nCPM
  • Myonuclei427 nCPM

IV · Evidence

Every measurement at this target

Each row links to the ChEMBL assay it came from.

Other measurements 2

Everything else ChEMBL recorded for this compound — percentage inhibition, efficacy, half-life, cytotoxicity. Reported in the assay's own units, which is why no value is converted here.

TargetClassTypeValue (nM)pXOrganismAssay
Cyclin-dependent kinase 8EnzymesActivity— no normalized value— value does not convert to pXHomo sapiensCHEMBL4151445
Cyclin-dependent kinase 8EnzymesInhibition— no normalized value— value does not convert to pXHomo sapiensCHEMBL5046213
Cyclin-dependent kinase 8 · Psychedelia