OncoSignal
Live from Open Targets Platform, fetched 2026-11-11 15:33 UTC. Every row links to its source record.

WDR5 WD repeat domain 5

ENSG00000196363 · protein coding · Open Targets profile

Contributes to histone modification (PubMed:16600877, PubMed:16829960, PubMed:19103755, PubMed:19131338, PubMed:19556245, PubMed:20018852). May position the N-terminus of histone H3 for efficient trimethylation at 'Lys-4' (PubMed:16829960). As part of the MLL1/MLL complex it is involved in methylation and dimethylation at 'Lys-4' of histone H3 (PubMed:19556245). H3 'Lys-4' methylation represents a specific tag for epigenetic transcriptional activation (PubMed:18840606). As part of the NSL complex it may be involved in acetylation of nucleosomal histone H4 on several lysine residues (PubMed:19103755, PubMed:20018852). May regulate osteoblasts differentiation (By similarity). In association with RBBP5 and ASH2L, stimulates the histone methyltransferase activities of KMT2A, KMT2B, KMT2C, KMT2D, SETD1A and SETD1B (PubMed:21220120, PubMed:22266653). {ECO:0000250|UniProtKB:P61965, ECO:0000269|PubMed:16600877, ECO:0000269|PubMed:16829960, ECO:0000269|PubMed:18840606, ECO:0000269|PubMed:19103755, ECO:0000269|PubMed:19131338, ECO:0000269|PubMed:19556245, ECO:0000269|PubMed:20018852, ECO:0000269|PubMed:21220120, ECO:0000269|PubMed:22266653}.

In 1 of 15 cancers, the evidence for WDR5 comes mainly from inherited variants

Each row is a cancer, strongest overall evidence first. The two dots show how strong the inherited (germline) and tumour-mutation (somatic) evidence is; the line between them is the gap.

Inherited (germline) variantsMutations in tumours (somatic)
00.250.50.751cervical carcinomacervical carcinomacervical carcinoma: germline 0.23neuroblastomaneuroblastomabreast cancerbreast cancerhepatocellular carcinomahepatocellular carcinomacolorectal carcinomacolorectal carcinomabreast carcinomabreast carcinomaacute lymphoblastic leukemiaacute lymphoblastic leukemiaacute myeloid leukemiaacute myeloid leukemiapancreatic neoplasmpancreatic neoplasmleukemialeukemiacolonic neoplasmcolonic neoplasmurinary bladder carcinomaurinary bladder carcinomaurinary bladder cancerurinary bladder cancermalignant colon neoplasmmalignant colon neoplasmcholangiocarcinomacholangiocarcinoma

Scores run from 0 (no evidence) to 1 (strongest). A missing dot at 0 means Open Targets holds no evidence of that kind. Source: Open Targets Platform, fetched live.

Tractability

Small molecule
Structure with Ligand, High-Quality Ligand, High-Quality Pocket, Druggable Family
PROTAC
UniProt Ubiquitination, Database Ubiquitination, Half-life Data, Small Molecule Binder

gnomAD loss of function constraint: o/e – (upper bound –). Low values mean loss of function is poorly tolerated, a safety flag for inhibition.

Who runs trials of these drugs

No named investigators on registry trials of WDR5's approved or late-stage drugs in the last three years.

No terminated, withdrawn or suspended trials of WDR5's drugs are registered

All 0 drugs and clinical candidates as a table

Each drug, stage and indication links to its Open Targets record, where the trials and approvals behind it are listed. Salt forms (for example a mesylate) are listed as Open Targets records them, as separate entries.

DrugTypeHighest stageIndicationsSource records
No drugs or clinical candidates recorded.