WDR5

Summary

WDR5 (WD repeat domain 5, HGNC:12757) is a protein-coding gene on chromosome 9q34.2, encoding WD repeat-containing protein 5 (P61964). Contributes to histone modification. It is a common-essential gene (DepMap: required in 98.3% of cancer cell lines).

This gene encodes a member of the WD repeat protein family. WD repeats are minimally conserved regions of approximately 40 amino acids typically bracketed by gly-his and trp-asp (GH-WD), which may facilitate formation of heterotrimeric or multiprotein complexes. Members of this family are involved in a variety of cellular processes, including cell cycle progression, signal transduction, apoptosis, and gene regulation. This protein contains 7 WD repeats. Alternatively spliced transcript variants encoding the same protein have been identified.

Source: NCBI Gene 11091 — RefSeq curated summary.

At a glance

• Gene–disease (curated): neurodevelopmental disorder (Strong, GenCC) — +1 more curated relationship
• GWAS associations: 2
• Clinical variants (ClinVar): 60 total — 2 pathogenic, 1 likely-pathogenic
• Druggable target: yes — 6 molecules with ChEMBL bioactivity
• Cancer dependency (DepMap): dependent in 98.3% of screened cell lines (common-essential)
• MANE Select transcript: NM_017588

Identifiers

Gene identifiers

Field	Value
HGNC ID	HGNC:12757
Approved symbol	WDR5
Name	WD repeat domain 5
Location	9q34.2
Locus type	gene with protein product
Status	Approved
Aliases	SWD3, CFAP89, BIG-3
Ensembl gene	ENSG00000196363
Ensembl biotype	protein_coding
OMIM	609012
Entrez	11091

Gene structure

Transcript identifiers

Ensembl transcripts: 14 — 14 protein_coding

ENST00000358625, ENST00000608739, ENST00000608937, ENST00000907894, ENST00000907895, ENST00000907896, ENST00000907897, ENST00000907898, ENST00000924659, ENST00000924660, ENST00000924661, ENST00000924662, ENST00000924663, ENST00000957642

RefSeq mRNA: 13 — MANE Select: NM_017588 NM_001384409, NM_001384410, NM_001384411, NM_001384412, NM_001384413, NM_001384414, NM_001384415, NM_001384416, NM_001384417, NM_001384418, NM_001384419, NM_017588, NM_052821

CCDS: CCDS6981

Canonical transcript exons

ENST00000358625 — 14 exons

Exon	Start	End
ENSE00001370072	134141510	134141583
ENSE00001378987	134140703	134140811
ENSE00001399325	134139820	134139958
ENSE00001401373	134148288	134148343
ENSE00001411527	134154466	134154541
ENSE00001415339	134142333	134142422
ENSE00001416091	134142636	134142719
ENSE00001417345	134156506	134156593
ENSE00001422107	134141949	134142038
ENSE00001422154	134136082	134136200
ENSE00001429531	134155340	134155373
ENSE00001430459	134151983	134152029
ENSE00001431152	134155693	134155767
ENSE00001833493	134157893	134159968

Expression profiles

Bgee: expression breadth ubiquitous, 245 present calls, max score 91.94.

FANTOM5 (CAGE): breadth ubiquitous, TPM avg 57.9494 / max 391.5425, expressed in 1815 samples.

FANTOM5 promoters (4 alternative TSS)

Promoter ID	TPM avg	Samples expressed
99306	42.3169	1809
99307	14.2833	1780
99305	1.3104	796
99308	0.0388	5

Top tissues by expression

254 total, by Bgee expression score (0-100, higher = more expressed):

Tissue	Anatomy ID	Expression score	Quality
upper arm skin	UBERON:0004263	91.94	gold quality
left testis	UBERON:0004533	91.57	gold quality
right testis	UBERON:0004534	91.26	gold quality
sperm	CL:0000019	91.21	gold quality
testis	UBERON:0000473	90.36	gold quality
gastrocnemius	UBERON:0001388	90.07	gold quality
cerebellar hemisphere	UBERON:0002245	89.57	gold quality
right hemisphere of cerebellum	UBERON:0014890	89.57	gold quality
cerebellar cortex	UBERON:0002129	89.49	gold quality
muscle of leg	UBERON:0001383	89.27	gold quality
cerebellum	UBERON:0002037	89.11	gold quality
adenohypophysis	UBERON:0002196	89.07	gold quality
secondary oocyte	CL:0000655	88.96	gold quality
lower esophagus mucosa	UBERON:0035834	88.77	gold quality
primordial germ cell in gonad	CL:0000670 ∩ UBERON:0000991	88.69	gold quality
mucosa of transverse colon	UBERON:0004991	88.56	gold quality
right lobe of liver	UBERON:0001114	88.55	gold quality
pituitary gland	UBERON:0000007	88.53	gold quality
ganglionic eminence	UBERON:0004023	88.27	gold quality
apex of heart	UBERON:0002098	88.23	gold quality
ventricular zone	UBERON:0003053	88.23	gold quality
body of pancreas	UBERON:0001150	88.20	gold quality
esophagus mucosa	UBERON:0002469	87.64	gold quality
lower esophagus	UBERON:0013473	87.33	gold quality
lower esophagus muscularis layer	UBERON:0035833	87.33	gold quality
body of stomach	UBERON:0001161	87.31	gold quality
right ovary	UBERON:0002118	87.31	gold quality
esophagus	UBERON:0001043	87.28	gold quality
granulocyte	CL:0000094	87.21	gold quality
cortical plate	UBERON:0005343	87.17	gold quality

Single-cell (SCXA)

Detected in 1 experiment(s), a significant marker in 1.

Experiment	Marker?	Max mean expression
E-ANND-3	yes	3.81

Regulation

Is transcription factor: yes

Downstream targets (CollecTRI)

1 targets.

Target	Regulation
MYC	Unknown

Upstream regulators (CollecTRI, top): DLX5, ESRRG, FOXC1, MSX2, MYC, SMAD6, SRY

miRNA regulators (miRDB)

46 targeting WDR5, top 30 by miRDB confidence (max_score; target_count = how many genes the miRNA targets in total — lower means more specific):

miRNA	Max score	Avg score	miRNA target_count
HSA-MIR-6758-5P	100.00	66.21	1470
HSA-MIR-6856-5P	100.00	65.47	1298
HSA-MIR-4282	99.99	75.36	6408
HSA-MIR-607	99.97	73.62	5593
HSA-MIR-548AJ-3P	99.96	73.38	5345
HSA-MIR-548X-3P	99.96	73.38	5345
HSA-MIR-548J-3P	99.94	72.61	4881
HSA-MIR-6721-5P	99.93	68.92	2981
HSA-MIR-548AE-3P	99.93	72.66	4867
HSA-MIR-548AH-3P	99.93	72.54	4872
HSA-MIR-548AM-3P	99.93	72.54	4872
HSA-MIR-548AQ-3P	99.93	72.66	4867
HSA-MIR-3686	99.90	70.53	2432
HSA-MIR-3529-3P	99.90	73.55	3045
HSA-MIR-9902	99.89	69.15	2250
HSA-MIR-3919	99.87	69.45	2489
HSA-MIR-3180-5P	99.82	69.12	2422
HSA-MIR-4319	99.76	69.83	2586
HSA-MIR-2681-5P	99.75	67.64	1655
HSA-MIR-1283	99.69	72.42	3009
HSA-MIR-7844-5P	99.55	68.56	1428
HSA-MIR-4672	99.50	71.58	2893
HSA-MIR-5695	99.41	67.48	1047
HSA-MIR-125A-5P	99.36	70.59	1640
HSA-MIR-125B-5P	99.36	70.36	1662
HSA-MIR-520A-5P	99.35	66.72	1632
HSA-MIR-525-5P	99.35	66.85	1615
HSA-MIR-361-3P	99.19	66.45	1381
HSA-MIR-423-5P	98.69	67.48	1522
HSA-MIR-31-5P	98.58	68.35	1239

Functional genomics

DepMap (CRISPR cell-line fitness): dependent in 98.3% of screened cell lines, common-essential.

Literature-anchored findings (GeneRIF, showing 40)

• The WDR5 is required for binding of the methyltransferase complex to the K4-dimethylated H3 tail as well as for global H3 K4 trimethylation and HOX gene activation in human cells. (PMID:15960974)
• Wdr5 has a funcitonal role in endocondral bone formation (PMID:16340128)
• the high-resolution X-ray structures of WDR5 in the unliganded form and complexed with histone H3 peptides having unmodified and mono-, di- and trimethylated K4 (PMID:16829959)
• the crystal structure of WDR5 bound to a histone H3 (PMID:16829960)
• WDR5 mediates interactions of the MLL1 catalytic unit both with the common structural platform and with the histone substrate. (PMID:16878130)
• involvement of WDR5 in binding and presenting histone H3K4 for further methylation (PMID:16946699)
• WDR5’s recognition of arginine 3765 of MLL1 is essential for the assembly and enzymatic activity of the MLL1 core complex in vitro (PMID:18829457)
• WDR5 recognizes Arg-3765 of MLL1, which is essential for the assembly and enzymatic activity of the MLL1 core complex (PMID:18829459)
• analysis of interactions between WDR5, the catalytic subunit, MLL, and the substrate, histone H3, of the MLL complex (PMID:18840606)
• The identified components revealed factors involved in histone methylation and cell cycle control and include Ash2L, RbBP5, WDR5, HCF-1, DBC-1, and EMSY. (PMID:19131338)
• Activation of an estrogen/estrogen receptor signaling by BIG3 through its inhibitory effect on nuclear transport of PHB2/REA in breast cancer is reported. (PMID:19496786)
• NSL is composed of nine subunits. Two of its subunits, WD repeat domain 5 (WDR5) and host cell factor 1 (HCF1), are shared with members of the MLL/SET family of histone H3 lysine 4 (H3K4) methyltransferase complexes. (PMID:20018852)
• WDR5 is essential in assembling a virus-induced VISA-associated complex and plays an important role in virus-triggered induction of type I interferons. (PMID:20080758)
• Results show that Depletion of CHD8 enhances HOXA2 expression and a loss of the WDR5/Ash2L/RbBP5 subcomplex. (PMID:20085832)
• the change of folding free energy by mutations mainly corresponds to the deletion of hydrogen bonds. (PMID:20939513)
• crystal structure of WDR5 in ternary complex with RbBP5 and MLL1 (PMID:21220120)
• WDR5 as a critical substrate of CUL4B in regulating neuronal gene expression. (PMID:21816345)
• findings show that WDR5 is a direct target of SRY; the interaction of WDR5 and SRY activates Sox9 expression; results suggest that, in conjunction with SRY, WDR5 plays an important role in sex determination (PMID:22523547)
• WDR5-Win motif interaction is important for the assembly of the MLL1 core complex in vivo. (PMID:22665483)
• data are consistent with a model in which WDR5 binds the gamma-globin promoter in a PRMT5-dependent manner. (PMID:22689669)
• we defined a role for Trithorax proteins WDR5 and MLL2 in activating the differentiation gene program in epidermal progenitor cells (PMID:22829784)
• A small molecule antagonist binds to WDR5 in the peptide-binding pocket which inhibits the catalytic activity of mixed-lineage leukemia protein. (PMID:22989411)
• BIG3(WRD5)-PHB2 interaction is critical for the tamoxifen resistance of breast cancer cells; its targeting reverses the resistance. (PMID:24051437)
• Data indicate that MLL1 methylates Ash2L in the absence of histone H3, but only when assembled within a complex with WDR5 and RbBP5. (PMID:24235145)
• results identify WDR5 as a critical epigenomic integrator of histone phosphorylation and methylation and as a major driver of androgen-dependent prostate cancer cell proliferation (PMID:24793694)
• we have discovered that WDR5 plays an important role in bladder cancer suggesting that WDR5 is a potential biomarker and a promising target in the treatment of bladder cancer. (PMID:25656485)
• findings prove that the TSP-1/CD47/SIRP-alpha signal axis is important to the evolution of tumor cells in the microenvironment of immunotherapy and identify thrombospondin-1 as a key signal (PMID:25666610)
• BIG3 may block the KPNAs (KPNA1, KPNA5, and KPNA6) binding region(s) of PHB2. (PMID:26052702)
• Wdr5-MLL interaction in C/EBPA N-terminal leukemia is a promising pharmacological target. (PMID:26167872)
• solution structures of the MLL3 core complex assembled with and without WDR5 by small angle x-ray scattering show similar overall topologies (PMID:26324722)
• WDR5 over-expression is associated with poor breast cancer clinical outcome. (PMID:26355959)
• Target gene recognition by MYC depends on its interaction with WDR5. This interaction could create an avidity-based chromatin recognition mechanism allowing MYC to select its target genes in response to both genetic and epigenetic determinants. Review. (PMID:26383167)
• Results identify WDR5 as a key cofactor for N-Myc-regulated transcriptional activation and tumorigenesis and as a novel therapeutic target for MYCN-amplified neuroblastomas. (PMID:26471359)
• This report documents a novel lncRNA, GClnc1, which may act as a scaffold to recruit the WDR5 and KAT2A complex and modify the transcription of target genes. This study reveals that GClnc1 is an oncogenic lncRNA in human gastric cancer. (PMID:27147598)
• WDR5 may have oncogenic effect and WDR5-mediated H3K4 methylation plays an important role in leukemogenesis (PMID:27192115)
• WDR5 functions to sustain proper execution of DNA replication in pancreatic ductal adenocarcinoma cells, as previously suggested by replication stress studies involving MLL1, and c-Myc, also found to interact with WDR5. (PMID:27320920)
• Targeted Disruption of the Interaction between WD-40 Repeat Protein 5 (WDR5) and Mixed Lineage Leukemia (MLL)/SET1 Family Proteins Specifically Inhibits MLL1 and SETd1A Methyltransferase Complexes. (PMID:27563068)
• we demonstrate for the first time that targeted expression of miR-31-5p using a nonviral minicircle vector can serve as a novel approach for tumor miRNA therapy. Moreover, WDR5 may be a promising therapeutic target for NPC treatment. (PMID:28042945)
• different cancer mutations in MLL1 lead to a loss or increase in activity, illustrating the complex and tumor-specific role of MLL1 in carcinogenesis. (PMID:28182322)
• WDR5 shows a direct binding to the ZNF407 promoter. (PMID:28300833)

Cross-species orthologs

5 orthologs

Organism	Symbol	Gene ID
danio_rerio	wdr5	ENSDARG00000016903
mus_musculus	Wdr5	ENSMUSG00000026917
rattus_norvegicus	Wdr5	ENSRNOG00000008212
drosophila_melanogaster	CG10931	FBGN0034274
drosophila_melanogaster	wds	FBGN0040066

Paralogs (26): PAFAH1B1 (ENSG00000007168), SNRNP40 (ENSG00000060688), WDR62 (ENSG00000075702), WDR7 (ENSG00000091157), TBL2 (ENSG00000106638), PAK1IP1 (ENSG00000111845), WDR75 (ENSG00000115368), DCAF4 (ENSG00000119599), DAW1 (ENSG00000123977), TEP1 (ENSG00000129566), AHI1 (ENSG00000135541), WDR38 (ENSG00000136918), MAPKBP1 (ENSG00000137802), POC1B (ENSG00000139323), NEDD1 (ENSG00000139350), COP1 (ENSG00000143207), WDR17 (ENSG00000150627), WDR43 (ENSG00000163811), POC1A (ENSG00000164087), WDR88 (ENSG00000166359), WDR81 (ENSG00000167716), DCAF4L2 (ENSG00000176566), DCAF4L1 (ENSG00000182308), WDR27 (ENSG00000184465), NWD1 (ENSG00000188039), WDR5B (ENSG00000196981)

Protein

Protein identifiers

WD repeat-containing protein 5 — P61964 (reviewed: P61964)

Alternative names: BMP2-induced 3-kb gene protein

All UniProt accessions (3): P61964, V9GYQ5, V9GZ59

UniProt curated annotations — full annotation on UniProt →

Function. Contributes to histone modification. May position the N-terminus of histone H3 for efficient trimethylation at ‘Lys-4’. As part of the MLL1/MLL complex it is involved in methylation and dimethylation at ‘Lys-4’ of histone H3. H3 ‘Lys-4’ methylation represents a specific tag for epigenetic transcriptional activation. As part of the NSL complex it may be involved in acetylation of nucleosomal histone H4 on several lysine residues. May regulate osteoblasts differentiation. In association with RBBP5 and ASH2L, stimulates the histone methyltransferase activities of KMT2A, KMT2B, KMT2C, KMT2D, SETD1A and SETD1B.

Subunit / interactions. Interacts with PAXBP1; the interaction is direct and links a WDR5-containing histone methyltransferase complex to PAX7 and PAX3. Interacts with HCFC1. Component of the ATAC complex, a complex with histone acetyltransferase activity on histones H3 and H4. Component of the SET1 complex, at least composed of the catalytic subunit (SETD1A or SETD1B), WDR5, WDR82, RBBP5, ASH2L/ASH2, CXXC1/CFP1, HCFC1 and DPY30. Core component of several methyltransferase-containing complexes including MLL1/MLL, MLL2/3 (also named ASCOM complex) and MLL4/WBP7. Each complex is at least composed of ASH2L, RBBP5, WDR5, DPY30, one or more specific histone methyltransferases (KMT2A/MLL1, KMT2D/MLL2, KMT2C/MLL3 and KMT2B/MLL4), and the facultative components PAGR1, BACC1, CHD8, E2F6, HCFC1, HCFC2, HSP70, INO80C, KDM6A, KANSL1, LAS1L, MAX, MCRS1, MEN1, MGA, MYST1/MOF, NCOA6, PAXIP1/PTIP, PELP1, PHF20, PRP31, RING2, RUVB1/TIP49A, RUVB2/TIP49B, SENP3, TAF1, TAF4, TAF6, TAF7, TAF9, TEX10 and alpha- and beta-tubulin. Component of the NSL complex at least composed of MOF/KAT8, KANSL1, KANSL2, KANSL3, MCRS1, PHF20, OGT1/OGT, WDR5 and HCFC1. Interacts with KMT2A/MLL1 (via WIN motif) and RBBP5; the interaction is direct. Component of the ADA2A-containing complex (ATAC), composed of KAT14, KAT2A, TADA2L, TADA3L, ZZ3, MBIP, WDR5, YEATS2, CCDC101 and DR1. In the complex, it probably interacts directly with KAT2A, MBIP and KAT14. Interacts with histone H3. Interacts with SETD1A (via WIN motif). Component of a histone methylation complex composed of at least ZNF335, RBBP5, ASH2L and WDR5; the complex may have histone H3-specific methyltransferase activity, however does not have specificity for ‘Lys-4’ of histone H3. Interacts with ZNF335. Components of this complex may associate with components of the ZNF335-CCAR2-EMSY nuclear receptor-mediated transcription complex to form a complex at least composed of ZNF335, HCFC1, CCAR2, EMSY, MKI67, RBBP5, ASH2L and WDR5. Interacts with PER1. Interacts with KMT2B (via WIN motif), KMT2C (via WIN motif), KMT2D (via WIN motif) and SETD1B (via WIN motif). (Microbial infection) Interacts with herpes virus 8/HHV-8 protein LANA1; this interaction regulates the MLL1 histone methyltransferase activity on viral DNA.

Subcellular location. Nucleus.

Similarity. Belongs to the WD repeat WDR5/wds family.

RefSeq proteins (13): NP_001371338, NP_001371339, NP_001371340, NP_001371341, NP_001371342, NP_001371343, NP_001371344, NP_001371345, NP_001371346, NP_001371347, NP_001371348, NP_060058, NP_438172 (=MANE)

Domains & families (InterPro)

ID	Name	Type
IPR001680	WD40_rpt	Repeat
IPR015943	WD40/YVTN_repeat-like_dom_sf	Homologous_superfamily
IPR019775	WD40_repeat_CS	Conserved_site
IPR020472	WD40_PAC1	Repeat
IPR036322	WD40_repeat_dom_sf	Homologous_superfamily
IPR059122	Beta-prop_WDR5-like	Domain

Pfam: PF25175

UniProt features (80 total): strand 34, mutagenesis site 15, turn 8, repeat 7, site 4, cross-link 3, compositionally biased region 2, modified residue 2, initiator methionine 1, chain 1, sequence variant 1, helix 1, region of interest 1

Structure

Experimental structures (PDB)

199 structures, top 30 by resolution.

PDB	Method	Resolution (Å)
6E1Z	X-RAY DIFFRACTION	1.1
6U6W	X-RAY DIFFRACTION	1.2
6E1Y	X-RAY DIFFRACTION	1.22
6UHZ	X-RAY DIFFRACTION	1.26
6UHY	X-RAY DIFFRACTION	1.26
7BED	X-RAY DIFFRACTION	1.26
6U8B	X-RAY DIFFRACTION	1.26
4ERY	X-RAY DIFFRACTION	1.3
24XP	X-RAY DIFFRACTION	1.3
8G3E	X-RAY DIFFRACTION	1.33
3EMH	X-RAY DIFFRACTION	1.37
3UVK	X-RAY DIFFRACTION	1.4
7WVK	X-RAY DIFFRACTION	1.42
2H14	X-RAY DIFFRACTION	1.48
9UXM	X-RAY DIFFRACTION	1.48
6UJH	X-RAY DIFFRACTION	1.49
2H6N	X-RAY DIFFRACTION	1.5
4CY1	X-RAY DIFFRACTION	1.5
4QL1	X-RAY DIFFRACTION	1.5
6PGD	X-RAY DIFFRACTION	1.5
7BCY	X-RAY DIFFRACTION	1.5
4EWR	X-RAY DIFFRACTION	1.5
6IAM	X-RAY DIFFRACTION	1.51
6UJ4	X-RAY DIFFRACTION	1.53
6U5Y	X-RAY DIFFRACTION	1.53
6UOZ	X-RAY DIFFRACTION	1.53
6PGF	X-RAY DIFFRACTION	1.54
6U80	X-RAY DIFFRACTION	1.55
8E9F	X-RAY DIFFRACTION	1.55
9LWY	X-RAY DIFFRACTION	1.55

Predicted structure (AlphaFold)

Model	pLDDT	Fraction very-high
AF-P61964-F1	93.66	0.90

Functional residue map

Curated UniProt residues grouped by drug-discovery relevance — catalytic, ligand-binding, modification, and mutation-validated positions. Source: UniProtKB sequence features.

Catalytic / active sites (4): 107 (important for interaction with histone h3); 133 (important for interaction with histone h3); 263 (important for interaction with histone h3); 322 (important for interaction with histone h3)

Post-translational modifications (5): 2, 112, 7, 27, 46

Mutagenesis-validated functional residues (15):

Position	Phenotype
47	strongly reduced affinity for histone h3.
91	strongly reduced affinity for histone h3.
107	strongly reduced affinity for histone h3. significant decrease in interaction with kmt2a.
107	strongly reduced affinity for histone h3.
133	strongly reduced affinity for histone h3. significant decrease in interaction with kmt2a.
133	strongly reduced affinity for histone h3.
149	significant decrease in interaction with kmt2a.
225	loss of interaction with rbbp5 and reduced ability to stimulate kmt2a methyltransferase activity in association with rbb
240	loss of interaction with rbbp5 and reduced ability to stimulate kmt2a methyltransferase activity in association with rbb
263	strongly reduced affinity for histone h3. significant decrease in interaction with kmt2a.
263	strongly reduced affinity for histone h3.
289	reduced interaction with rbbp5 and reduced ability to stimulate kmt2a methyltransferase activity in association with rbb
321	abolishes histone h3 binding.
322	strongly reduced affinity for histone h3. no effect on interaction with kmt2a.

Function

Pathways and Gene Ontology

Reactome pathways

16 pathways

ID	Pathway
R-HSA-201722	Formation of the beta-catenin:TCF transactivating complex
R-HSA-3214841	PKMTs methylate histone lysines
R-HSA-3214847	HATs acetylate histones
R-HSA-3214858	RMTs methylate histone arginines
R-HSA-3769402	Deactivation of the beta-catenin transactivating complex
R-HSA-5617472	Activation of anterior HOX genes in hindbrain development during early embryogenesis
R-HSA-8936459	RUNX1 regulates genes involved in megakaryocyte differentiation and platelet function
R-HSA-8951664	Neddylation
R-HSA-9733709	Cardiogenesis
R-HSA-9772755	Formation of WDR5-containing histone-modifying complexes
R-HSA-9818564	Epigenetic regulation of gene expression by MLL3 and MLL4 complexes
R-HSA-9841922	MLL4 and MLL3 complexes regulate expression of PPARG target genes in adipogenesis and hepatic steatosis
R-HSA-9909649	Regulation of PD-L1(CD274) transcription
R-HSA-9943962	CHD6, CHD7, CHD8, CHD9 subfamily
R-HSA-9944997	Loss of Function of KMT2D in MLL4 Complex Formation in Kabuki Syndrome
R-HSA-9976102	Differentiation of naive CD4+ T cells to T helper 2 cells (Th2 cells)

MSigDB gene sets: 180 (showing top): REACTOME_ADAPTIVE_IMMUNE_SYSTEM, GOBP_SKELETAL_SYSTEM_DEVELOPMENT, GOBP_REGULATION_OF_PROTEIN_DEACETYLATION, AREB6_03, GOBP_MACROMOLECULE_DEACYLATION, GOBP_POSITIVE_REGULATION_OF_CARBOHYDRATE_METABOLIC_PROCESS, GOBP_SMALL_MOLECULE_BIOSYNTHETIC_PROCESS, GOBP_REGULATION_OF_CARBOHYDRATE_METABOLIC_PROCESS, GOBP_MONOSACCHARIDE_BIOSYNTHETIC_PROCESS, GOBP_REGULATION_OF_CELL_CYCLE, GOBP_CARBOHYDRATE_METABOLIC_PROCESS, GOBP_REGULATION_OF_CELL_DIVISION, GOBP_REGULATION_OF_GLUCOSE_METABOLIC_PROCESS, LIAO_METASTASIS, GOBP_DNA_TEMPLATED_TRANSCRIPTION_INITIATION

GO Biological Process (12): negative regulation of transcription by RNA polymerase II (GO:0000122), skeletal system development (GO:0001501), gluconeogenesis (GO:0006094), regulation of DNA-templated transcription (GO:0006355), regulation of transcription by RNA polymerase II (GO:0006357), positive regulation of gluconeogenesis (GO:0045722), transcription initiation-coupled chromatin remodeling (GO:0045815), positive regulation of DNA-templated transcription (GO:0045893), regulation of embryonic development (GO:0045995), regulation of cell division (GO:0051302), regulation of cell cycle (GO:0051726), chromatin organization (GO:0006325)

GO Molecular Function (5): histone binding (GO:0042393), histone H3K4 methyltransferase activity (GO:0042800), histone H3Q5ser reader activity (GO:0140004), histone H3K4me1 reader activity (GO:0140109), protein binding (GO:0005515)

GO Cellular Component (12): histone acetyltransferase complex (GO:0000123), nucleus (GO:0005634), nucleoplasm (GO:0005654), histone methyltransferase complex (GO:0035097), NSL complex (GO:0044545), MLL1/2 complex (GO:0044665), MLL3/4 complex (GO:0044666), Set1C/COMPASS complex (GO:0048188), MLL1 complex (GO:0071339), mitotic spindle (GO:0072686), sperm principal piece (GO:0097228), ATAC complex (GO:0140672)

Reactome top-level categories

Rollup of top-12 pathways:

Category	Pathways
Chromatin modifying enzymes	3
TCF dependent signaling in response to WNT	2
Epigenetic regulation by WDR5-containing histone modifying complexes	2
Activation of HOX genes during differentiation	1
Transcriptional regulation by RUNX1	1
Post-translational protein modification	1
Developmental Biology	1
Epigenetic regulation of adipogenesis genes by MLL3 and MLL4 complexes	1
Regulation of PD-L1(CD274) expression	1
CHD chromatin remodelers	1
Loss of Function of KMT2D in Kabuki Syndrome	1
Differentiation of T cells	1

GO top-level categories

Rollup of top GO terms by namespace:

Category	Terms
histone methyltransferase complex	3
transcription by RNA polymerase II	2
DNA-templated transcription	2
regulation of DNA-templated transcription	2
regulation of cellular process	2
histone H3 reader activity	2
cellular anatomical structure	2
regulation of transcription by RNA polymerase II	1
negative regulation of DNA-templated transcription	1
system development	1
glucose metabolic process	1
hexose biosynthetic process	1
regulation of gene expression	1
regulation of RNA biosynthetic process	1
gluconeogenesis	1
regulation of gluconeogenesis	1
positive regulation of biosynthetic process	1
positive regulation of glucose metabolic process	1
transcription initiation at RNA polymerase II promoter	1
positive regulation of gene expression, epigenetic	1
positive regulation of RNA biosynthetic process	1
embryo development	1
regulation of multicellular organismal development	1
cell division	1
cell cycle	1
cellular component organization	1
protein binding	1
protein-lysine N-methyltransferase activity	1
histone H3 methyltransferase activity	1
binding	1
chromatin	1
protein acetyltransferase complex	1
intracellular membrane-bounded organelle	1
nuclear lumen	1
nucleoplasm	1
methyltransferase complex	1
nuclear protein-containing complex	1
H4 histone acetyltransferase complex	1
MLL1/2 complex	1
spindle	1

Protein interactions and networks

STRING

4117 interactions, top by confidence (×1000):

Protein A	Protein B	Partner UniProt	Score
WDR5	ASH2L	Q9UBL3	999
WDR5	DPY30	Q9C005	999
WDR5	H3-3A	P06351	997
WDR5	SETD1A	O15047	997
WDR5	H3C14	Q71DI3	997
WDR5	H3-5	Q6NXT2	997
WDR5	H3C1	P02295	997
WDR5	H3-4	Q16695	997
WDR5	H3-7	Q5TEC6	997
WDR5	CXXC1	Q9P0U4	995
WDR5	KMT2C	Q8NEZ4	994
WDR5	RBBP5	Q15291	993
WDR5	HCFC1	P51610	991
WDR5	KAT2A	Q92830	989
WDR5	WDR82	Q6UXN9	989

IntAct

375 interactions, top by confidence:

A	B	Type	Score
WDR5	RBBP5	psi-mi:“MI:0914”(association)	0.960
RBBP5	WDR5	psi-mi:“MI:0915”(physical association)	0.960
RBBP5	WDR5	psi-mi:“MI:0914”(association)	0.960
WDR5	RBBP5	psi-mi:“MI:0915”(physical association)	0.960
RBBP5	WDR5	psi-mi:“MI:0407”(direct interaction)	0.960
KMT2A	WDR5	psi-mi:“MI:0915”(physical association)	0.960
ASH2L	WDR5	psi-mi:“MI:0915”(physical association)	0.950
ASH2L	WDR5	psi-mi:“MI:0914”(association)	0.950
NCOA6	WDR5	psi-mi:“MI:0914”(association)	0.920
WDR5	NCOA6	psi-mi:“MI:0915”(physical association)	0.920
KMT2D	WDR5	psi-mi:“MI:0914”(association)	0.910
WDR5	KMT2D	psi-mi:“MI:0915”(physical association)	0.910
KMT2D	WDR5	psi-mi:“MI:0915”(physical association)	0.910
PAXIP1	WDR5	psi-mi:“MI:0915”(physical association)	0.900
PAXIP1	WDR5	psi-mi:“MI:0914”(association)	0.900
WDR5	MBIP	psi-mi:“MI:0915”(physical association)	0.880
DPY30	WDR5	psi-mi:“MI:0914”(association)	0.860
CDK8	MED19	psi-mi:“MI:2364”(proximity)	0.850
RBBP5	KMT2D	psi-mi:“MI:0914”(association)	0.840
WDR5	ZXDC	psi-mi:“MI:0915”(physical association)	0.800
WDR5	HSF2	psi-mi:“MI:0915”(physical association)	0.780

BioGRID (2104): WDR5 (Affinity Capture-Western), WDR5 (Reconstituted Complex), WDR5 (Two-hybrid), MBIP (Two-hybrid), ZXDC (Two-hybrid), SSX2IP (Two-hybrid), RUSC1-AS1 (Two-hybrid), WDR5 (Affinity Capture-MS), WDR5 (Reconstituted Complex), HIST3H3 (Affinity Capture-Western), WDR5 (Co-localization), WDR5 (Affinity Capture-Western), WDR5 (Affinity Capture-Western), WDR5 (Affinity Capture-Western), WDR5 (Affinity Capture-Western)

ESM2 similar proteins: A0JMG1, F6RQL9, O43791, O77676, P00516, P0C605, P31321, P35250, P49407, P53033, P61157, P61158, P61964, P61965, Q05B83, Q09028, Q0IHH9, Q0VC00, Q0VCW1, Q13126, Q13976, Q15382, Q2KIG2, Q2M2N2, Q3MHL3, Q498M4, Q4V7C7, Q56JV3, Q5BL35, Q5M7K4, Q5NVK7, Q5RF92, Q5SP67, Q60972, Q62639, Q6ICL3, Q6INH0, Q6IQ16, Q6P8B3, Q6ZWS8

Diamond homologs: A8X8C6, B6QC56, B8N9H4, C0S902, C1GB49, C5FWH1, C5GVJ9, C5JD40, C5PFX0, F1LTR1, O42937, O74184, O74309, P14197, P20484, P25569, P61964, P61965, P87314, P90794, Q17963, Q23256, Q28D01, Q2KIG2, Q2UGU1, Q498M4, Q4P4R3, Q4V8C4, Q54H44, Q54KL5, Q58WW2, Q5M786, Q5R9B8, Q5RE95, Q5SP67, Q7K0L4, Q7ZXK9, Q80ZK9, Q86VZ2, Q8C6G8

SIGNOR signaling

4 interactions.

A	Effect	B	Mechanism
WDR5	“form complex”	HMT	binding
WDR5	“form complex”	“Set1-Ash2 HMT complex”	binding
WDR5	“form complex”	“NSL histone acetyltransferase”	binding
PASK	“up-regulates activity”	WDR5	phosphorylation

Enriched among interaction partners

Reactome pathways and GO biological processes over-represented among this gene’s 117 IntAct physical interaction partners (hypergeometric vs the genome-wide background, BH-FDR, gene-set size 15–500, ranked by fold). A functional readout of the neighbourhood — distinct from this gene’s own memberships above, and biased toward well-studied / hub proteins, so read it as themes rather than proof.

Reactome pathways:

Pathway	Partners	Fold	FDR
Formation of WDR5-containing histone-modifying complexes	20	69.9×	8e-31
Activation of HOX genes during differentiation	6	34.7×	7e-07
Epigenetic regulation by WDR5-containing histone modifying complexes	13	26.4×	3e-13
Epigenetic regulation of gene expression by MLL3 and MLL4 complexes	10	25.9×	5e-10
Transcriptional Regulation by E2F6	5	19.3×	1e-04
Deactivation of the beta-catenin transactivating complex	6	18.4×	2e-05
Epigenetic regulation of adipogenesis genes by MLL3 and MLL4 complexes	6	17.0×	3e-05
PKMTs methylate histone lysines	8	16.9×	9e-07

GO biological processes:

GO term	Partners	Fold	FDR
transcription initiation-coupled chromatin remodeling	7	27.4×	2e-06
intrinsic apoptotic signaling pathway	5	18.3×	1e-03
cellular response to UV	5	15.1×	2e-03
G1/S transition of mitotic cell cycle	7	14.3×	1e-04
rhythmic process	5	12.8×	3e-03
DNA damage response	15	8.2×	3e-07
regulation of cell cycle	9	6.8×	1e-03
chromatin remodeling	8	6.0×	4e-03

Disease & clinical

Clinical variants and AI predictions

ClinVar

60 variants total. Per-class counts are floors (≥ shown; pagination cap):

Classification	Count (floor)
Pathogenic	2
Likely pathogenic	1
Uncertain significance	32
Likely benign	3
Benign	0

Top pathogenic / likely-pathogenic (3)

Variant ID	HGVS	Classification
3026292	NM_017588.3(WDR5):c.623C>T (p.Thr208Met)	Pathogenic
3369045	NM_017588.3(WDR5):c.586C>T (p.Arg196Cys)	Pathogenic
3375461	NM_017588.3(WDR5):c.175T>C (p.Trp59Arg)	Likely pathogenic

SpliceAI

2920 predictions. Top by Δscore:

Variant	Effect	Δscore
9:134139807:T:G	acceptor_gain	1.0000
9:134139954:GCAAG:G	donor_gain	1.0000
9:134139955:CAAGG:C	donor_loss	1.0000
9:134139957:AGGT:A	donor_loss	1.0000
9:134139959:G:GA	donor_loss	1.0000
9:134139959:G:GG	donor_gain	1.0000
9:134140792:A:T	donor_gain	1.0000
9:134140812:G:GG	donor_gain	1.0000
9:134141580:GCTG:G	donor_gain	1.0000
9:134141946:AAG:A	acceptor_gain	1.0000
9:134141947:AG:A	acceptor_gain	1.0000
9:134141948:G:A	acceptor_gain	1.0000
9:134141948:GGGA:G	acceptor_gain	1.0000
9:134142034:GCTCG:G	donor_gain	1.0000
9:134142038:GGTA:G	donor_loss	1.0000
9:134142039:G:GG	donor_gain	1.0000
9:134142039:GTAA:G	donor_loss	1.0000
9:134142040:T:A	donor_loss	1.0000
9:134142633:CA:C	acceptor_loss	1.0000
9:134142634:A:AG	acceptor_gain	1.0000
9:134142634:AGT:A	acceptor_loss	1.0000
9:134142634:AGTTT:A	acceptor_gain	1.0000
9:134142635:G:GG	acceptor_gain	1.0000
9:134142635:GT:G	acceptor_gain	1.0000
9:134142635:GTT:G	acceptor_gain	1.0000
9:134142635:GTTT:G	acceptor_gain	1.0000
9:134142635:GTTTG:G	acceptor_gain	1.0000
9:134142717:GCC:G	donor_gain	1.0000
9:134151973:T:TA	acceptor_gain	1.0000
9:134151981:A:AG	acceptor_gain	1.0000

AlphaMissense

2187 scored. Top likely-pathogenic:

Variant	Protein change	am_pathogenicity
9:134140800:T:C	L60P	1.000
9:134140805:A:C	S62R	1.000
9:134140807:T:A	S62R	1.000
9:134140807:T:G	S62R	1.000
9:134141533:T:A	W72R	1.000
9:134141533:T:C	W72R	1.000
9:134141967:T:A	W95R	1.000
9:134141967:T:C	W95R	1.000
9:134142006:G:C	D108H	1.000
9:134142373:T:A	V132D	1.000
9:134142412:T:A	V145D	1.000
9:134142414:T:C	S146P	1.000
9:134142417:G:A	G147R	1.000
9:134142417:G:C	G147R	1.000
9:134142418:G:A	G147E	1.000
9:134142420:T:C	S148P	1.000
9:134142421:C:T	S148F	1.000
9:134142636:T:C	F149L	1.000
9:134142638:T:A	F149L	1.000
9:134142638:T:G	F149L	1.000
9:134142639:G:C	D150H	1.000
9:134142640:A:C	D150A	1.000
9:134142640:A:T	D150V	1.000
9:134142657:T:A	W156R	1.000
9:134142657:T:C	W156R	1.000
9:134142697:C:A	A169D	1.000
9:134142699:C:G	H170D	1.000
9:134142701:C:A	H170Q	1.000
9:134142701:C:G	H170Q	1.000
9:134142712:T:A	V174D	1.000

dbSNP variants (sampled 300 via entrez): RS1000190511 (9:134158391 C>G), RS1000207618 (9:134159615 G>A,T), RS1000248238 (9:134135880 T>C), RS1000253775 (9:134134966 C>G), RS1000503903 (9:134139087 A>C), RS1000521214 (9:134159349 C>G,T), RS1000552087 (9:134159575 C>G), RS1000582571 (9:134157439 T>C), RS1000809925 (9:134151171 C>A,T), RS1000895908 (9:134142950 C>G), RS1000947821 (9:134143209 A>T), RS1000973841 (9:134140909 G>A), RS1001058290 (9:134146439 T>C), RS1001067740 (9:134155271 G>A), RS1001160433 (9:134136977 T>C)

Disease associations

OMIM: gene MIM:609012 | disease phenotypes:

GenCC curated gene-disease

Disease	Classification	Inheritance
neurodevelopmental disorder	Strong	Autosomal dominant
congenital heart disease	Limited	Autosomal dominant

ClinGen Gene-Disease Validity (1)

Expert-panel classifications — Definitive > Strong > Moderate > Limited > Disputed > Refuted.

Disease	Classification	Inheritance
congenital heart disease	Limited	AD

Mondo (2): congenital heart disease (MONDO:0005453), neurodevelopmental disorder (MONDO:0700092)

Orphanet (0):

HPO phenotypes

0 total (0 of 0 shown, HPO-id order):

GWAS associations

2 associations (top):

Study	Trait	p-value
GCST007002_4	Cerebrospinal fluid t-tau levels in normal cognition	6.000000e-07
GCST007998_28	Intraocular pressure	9.000000e-07

EFO canonical traits (2, from GWAS)

EFO ID	Trait name
EFO:0004760	t-tau measurement
EFO:0004695	intraocular pressure measurement

MeSH disease descriptors (2)

Descriptor	Name	Tree numbers
D006330	Heart Defects, Congenital	C14.240.400; C14.280.400; C16.131.240.400
D065886	Neurodevelopmental Disorders	F03.625

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (7): CHEMBL1075317 (SINGLE PROTEIN), CHEMBL3137282 (PROTEIN COMPLEX), CHEMBL3883320 (PROTEIN-PROTEIN INTERACTION), CHEMBL4106124 (PROTEIN-PROTEIN INTERACTION), CHEMBL5169069 (PROTEIN-PROTEIN INTERACTION), CHEMBL5465211 (PROTEIN-PROTEIN INTERACTION), CHEMBL5465553 (PROTEIN-PROTEIN INTERACTION)

Molecules with ChEMBL bioactivity

6 molecules (phase ≥1), by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 129,681 (via chembl_molecule»patent_compound — counts attach to the compound, not the gene–compound relationship, so off-target/promiscuous molecules can dominate).

Molecule	Name	Phase	Patents
CHEMBL1201320	ESOMEPRAZOLE	4	37,518
CHEMBL1201863	DEXLANSOPRAZOLE	4	1,583
CHEMBL1219	RABEPRAZOLE	4	12,441
CHEMBL1503	OMEPRAZOLE	4	52,284
CHEMBL480	LANSOPRAZOLE	4	24,317
CHEMBL1232461	MOLIBRESIB	2	1,538

PharmGKB: 1 entry (VIP=true, CPIC=false)

GtoPdb / IUPHAR curated pharmacology

(IUPHAR/BPS Guide to Pharmacology — expert-curated)

Target class: other protein — WD repeat-containing proteins

Most potent curated ligand interactions (6 total), top 6:

Ligand	Action	Affinity	Parameter
compound 41 [PMID: 35436124]	Binding	10.7	pKi
compound 22 [PMID: 38085679]	Inhibition	10.7	pKi
HBI-2375	Binding	8.3	pKi
OICR-9429	Binding	7.62	pKd
MS132	Binding	6.91	pKd
MS40	Binding	6.9	pKd

Binding affinities (BindingDB)

527 measured of 631 human assays (631 total across all organisms); most potent 50 below. Values come from heterogeneous assays and are not directly comparable.

Ligand	Measure	Value	Patent
N-[2-[(3S)-3,4- dimethylpiperazin-1-yl]- 4-fluoro-5-(2-morpholin- 4-ylpyrimidin-5- yl)phenyl]-6-oxo-4- (trifluoromethyl)-1H- pyridine-3-carboxamide	KD	0.06 nM	US-11319299: Substituted carboxamides as inhibitors of WDR5 protein-protein binding
N-[4-fluoro-5-(1-pyrimidin-2-yl-3,6-dihydro-2H-pyridin-5-yl)-2-[(3R,5S)-3,4,5-trimethylpiperazin-1-yl]phenyl]-6-oxo-4-(trifluoromethyl)piperidine-3-carboxamide	KD	0.095 nM	US-11319299: Substituted carboxamides as inhibitors of WDR5 protein-protein binding
N-[5-[1-[5-[(dimethylamino) methyl]pyrimidin-2-yl]-3,6- dihydro-2H-pyridin-4-yl]- 4-fluoro-2-[rac-(3R,5S)- 3,4,5-trimethylpiperazin- 1-yl]phenyl]-6-oxo-4- (trifluoromethyl)-1H- pyridine-3-carboxamide	KD	0.095 nM	US-11319299: Substituted carboxamides as inhibitors of WDR5 protein-protein binding
4-(difluoromethyl)-N-[4- fluoro-5-(2-morpholin-4- ylpyrimidin-5-yl)-2- [(3S,5R)-3,4,5- trimethylpiperazin-1- yl]phenyl]-6-oxo-1H- pyridine-3-carboxamide	KD	0.1 nM	US-11319299: Substituted carboxamides as inhibitors of WDR5 protein-protein binding
N-[4-fluoro-5-[1-[5-[(4- methylpiperazin-1- yl)methyl]pyrimidin-2- yl]-3,6-dihydro-2H- pyridin-5-yl]-2-[rac- (3R,5S)-3,4,5- trimethylpiperazin-1- yl]phenyl]-6-oxo-4- (trifluoromethyl)-1H- pyridine-3-carboxamide	KD	0.108 nM	US-11319299: Substituted carboxamides as inhibitors of WDR5 protein-protein binding
2-fluoro-N-[(1S)-1-(5-fluoro-6-methyl-2-pyridinyl)ethyl]-5-[(2-imino-3-methylimidazol-1-yl)methyl]-3-[1-(trifluoromethyl)pyridin-1-ium-2-yl]benzamide	KI	0.13 nM	US-10844044: WDR5 inhibitors and modulators
4-(difluoromethyl)-N-[4- fluoro-5-[2-[rac-(2R,6S)- 2,6-dimethylmorpholin-4- yl]pyrimidin-5-yl]-2-[rac- (3S)-3,4-dimethylpiperazin-1- yl]phenyl]-6-oxo-1H- pyridine-3-carboxamide	KD	0.152 nM	US-11319299: Substituted carboxamides as inhibitors of WDR5 protein-protein binding
N-[5-[2-(dimethylamino) pyrimidin-5-yl]-4-fluoro-2- [rac-(3R,5S)-3,4,5- trimethylpiperazin-1- yl]phenyl]-6-oxo-4- (trifluoromethyl)-1H- pyridine-3-carboxamide	KD	0.168 nM	US-11319299: Substituted carboxamides as inhibitors of WDR5 protein-protein binding
N-[5-(6-acetamidopyridin- 3-yl)-4-fluoro-2-[rac-(3R,5S)- 3,4,5-trimethylpiperazin- 1-yl]phenyl]-6-oxo-4- (trifluoromethyl)-1H- pyridine-3-carboxamide	KD	0.199 nM	US-11319299: Substituted carboxamides as inhibitors of WDR5 protein-protein binding
N-[2-[(3R)-3- (dimethylamino)pyrrolidin- 1-yl]-4-fluoro-5-(2- morpholin-4-ylpyrimidin- 5-yl)phenyl]-6-oxo-4- (trifluoromethyl)-1H- pyridine-3-carboxamide	KD	0.2 nM	US-11319299: Substituted carboxamides as inhibitors of WDR5 protein-protein binding
N-[5-(3,4-dihydro-2H- 1,5-benzodioxepin-7-yl)- 4-fluoro-2-[rac-(3R,5S)- 3,4,5-trimethylpiperazin- 1-yl]phenyl]-6-oxo-4- (trifluoromethyl)-1H- pyridine-3-carboxamide	KD	0.225 nM	US-11319299: Substituted carboxamides as inhibitors of WDR5 protein-protein binding
N-[4-fluoro-5-[1-(5- formylpyrimidin-2-yl)-3,6- dihydro-2H-pyridin-5-yl]-2- [rac-(3R,5S)-3,4,5- trimethylpiperazin- 1-yl]phenyl]-6-oxo-4- (trifluoromethyl)-1H- pyridine-3-carboxamide	KD	0.229 nM	US-11319299: Substituted carboxamides as inhibitors of WDR5 protein-protein binding
N-[4-fluoro-5-[1-[[4-(4- methylpiperazin-1- yl)phenyl]methyl]-3,6- dihydro-2H-pyridin-4-yl]- 2-[rac-(3R,5S)-3,4,5- trimethylpiperazin-1- yl]phenyl]-6-oxo-4- (trifluoromethyl)-1H- pyridine-3-carboxamide	KD	0.23 nM	US-11319299: Substituted carboxamides as inhibitors of WDR5 protein-protein binding
N-[4-fluoro-5-[1-[5-[(4- methylpiperazin-1-yl)methyl] pyrimidin-2-yl]-3,6-dihydro- 2H-pyridin-4-yl]-2-[rac- (3R,5S)-3,4,5- trimethylpiperazin-1-yl]phenyl]- 6-oxo-4-(trifluoromethyl)-1H- pyridine-3-carboxamide	KD	0.231 nM	US-11319299: Substituted carboxamides as inhibitors of WDR5 protein-protein binding
N-[5-(6- acetamidopyridin-3-yl)-4- fluoro-2-[rac-(3R)-3,4- dimethylpiperazin-1- yl]phenyl]-6-oxo-4- (trifluoromethyl)-1H- pyridine-3-carboxamide	KD	0.24 nM	US-11319299: Substituted carboxamides as inhibitors of WDR5 protein-protein binding
N-[4-fluoro-5-[2-[methyl- [rac-(3R)-oxolan-3- yl]amino]pyrimidin-5-yl]- 2-[rac-(3R)-3,4- dimethylpiperazin-1- yl]phenyl]-6-oxo-4- (trifluoromethyl)-1H- pyridine-3-carboxamide	KD	0.244 nM	US-11319299: Substituted carboxamides as inhibitors of WDR5 protein-protein binding
N-[4-fluoro-5-[1-(6- methoxypyrimidin-4-yl)- 3,6-dihydro-2H-pyridin- 5-yl]-2-[rac-(3R,5S)- 3,4,5-trimethylpiperazin- 1-yl]phenyl]-6-oxo-4- (trifluoromethyl)-1H- pyridine-3-carboxamide	KD	0.246 nM	US-11319299: Substituted carboxamides as inhibitors of WDR5 protein-protein binding
propan-2-yl 5-[2-fluoro- 5-[[6-oxo-4-(trifluoromethyl)- 1H-pyridine-3-carbonyl] amino]-4-[rac-(3R,5S)-3,4,5- trimethylpiperazin-1- yl]phenyl]-3,6-dihydro- 2H-pyridine-1-carboxylate	KD	0.271 nM	US-11319299: Substituted carboxamides as inhibitors of WDR5 protein-protein binding
N-[5-[6- (cyclopropylmethoxy) pyridin-3-yl]-4-fluoro-2- [(3S,5R)-3,4,5- trimethylpiperazin-1- yl]phenyl]-6-oxo-4- (trifluoromethyl)-1H- pyridine-3-carboxamide	KD	0.3 nM	US-11319299: Substituted carboxamides as inhibitors of WDR5 protein-protein binding
N-[4-fluoro-5-[1-[5- (hydroxymethyl)pyrimidin-2-yl]- 3,6-dihydro-2H-pyridin-5-yl]-2- [rac-(3R,5S)-3,4,5- trimethylpiperazin-1-yl)phenyl]- 6-oxo-4-(trifluoromethyl)-1H- pyridine-3-carboxamide	KD	0.302 nM	US-11319299: Substituted carboxamides as inhibitors of WDR5 protein-protein binding
N-[4-fluoro-5-[6-(oxan-4- yloxy)pyridin-3-yl]-2- [rac-(3R,5S)-3,4,5- trimethylpiperazin-1- yl]phenyl]-6-oxo-4- (trifluoromethyl)-1H- pyridine-3-carboxamide	KD	0.32 nM	US-11319299: Substituted carboxamides as inhibitors of WDR5 protein-protein binding
N-[4-fluoro-5-[6-(2- methoxyethoxy)pyridin- 3-yl]-2-[rac-(3R,5S)- 3,4,5-trimethylpiperazin- 1-yl]phenyl]-6-oxo-4- (trifluoromethyl)-1H- pyridine-3-carboxamide	KD	0.338 nM	US-11319299: Substituted carboxamides as inhibitors of WDR5 protein-protein binding
N-[4-fluoro-5-(2- piperazin-1-ylpyrimidin- 5-yl)-2-[rac-(3R,5S)- 3,4,5-trimethylpiperazin- 1-yl]phenyl]-6-oxo-4- (trifluoromethyl)-1H- pyridine-3-carboxamide	KD	0.345 nM	US-11319299: Substituted carboxamides as inhibitors of WDR5 protein-protein binding
N-[5-[1-(5-cyano-1,3- thiazol-2-yl)-3,6-dihydro- 2H-pyridin-5-yl]-4- fluoro-2-[rac-(3R,5S)- 3,4,5-trimethylpiperazin- 1-yl]phenyl]-6-oxo-4- (trifluoromethyl)-1H- pyridine-3-carboxamide	KD	0.375 nM	US-11319299: Substituted carboxamides as inhibitors of WDR5 protein-protein binding
N-[4-fluoro-5-(2- morpholin-4-ylpyridin-4- yl)-2-[rac-(3R,5S)-3,4,5- trimethylpiperazin-1- yl]phenyl]-6-oxo-4- (trifluoromethyl)-1H- pyridine-3-carboxamide	KD	0.391 nM	US-11319299: Substituted carboxamides as inhibitors of WDR5 protein-protein binding
N-[4-fluoro-5-[1-[5-[(4- methylpiperazin-1- yl)methyl]pyrimidin-2- yl]-2,5-dihydropyrrol-3- yl]-2-[rac-(3R,5S)-3,4,5- trimethylpiperazin-1- yl]phenyl]-6-oxo-4- (trifluoromethyl)-1H- pyridine-3-carboxamide	KD	0.392 nM	US-11319299: Substituted carboxamides as inhibitors of WDR5 protein-protein binding
N-[4-fluoro-5-(6- morpholin-4-ylpyridin-3- yl)-2-[(3S,5R)-3,4,5- trimethylpiperazin-1- yl]phenyl]-6-oxo-4- (trifluoromethyl)-1H- pyridine-3-carboxamide	KD	0.4 nM	US-11319299: Substituted carboxamides as inhibitors of WDR5 protein-protein binding
(1-methylcyclobutyl) 3- [2-fluoro-5-[[6-oxo-4- (trifluoromethyl)-1H- pyridine-3- carbonyl]amino]-4-[rac- (3R,5S)-3,4,5- trimethylpiperazin-1- yl]phenyl]-2,5- dihydropyrrole-1- carboxylate	KD	0.407 nM	US-11319299: Substituted carboxamides as inhibitors of WDR5 protein-protein binding
N-[5-(2,3-dihydro-1,4- benzodioxin-6-yl)-4- fluoro-2-[rac-(3R,5S)- 3,4,5-trimethylpiperazin- 1-yl]phenyl]-6-oxo-4- (trifluoromethyl)-1H- pyridine-3-carboxamide	KD	0.429 nM	US-11319299: Substituted carboxamides as inhibitors of WDR5 protein-protein binding
N-[4-fluoro-5-[2-[rac- (2R,6S)-2,6- dimethylmorpholin-4- yl]pyrimidin-5-yl]-2-[rac- (3R)-3,4-dimethylpiperazin-1- yl]phenyl]-6-oxo-4- (trifluoromethyl)-1H- pyridine-3-carboxamide	KD	0.434 nM	US-11319299: Substituted carboxamides as inhibitors of WDR5 protein-protein binding
N-[4-fluoro-5-(3-fluoro- 4-morpholin-4-ylphenyl)- 2-[rac-(3R,5S)-3,4,5- trimethylpiperazin-1- yl]phenyl]-6-oxo-4- (trifluoromethyl)-1H- pyridine-3-carboxamide	KD	0.439 nM	US-11319299: Substituted carboxamides as inhibitors of WDR5 protein-protein binding
N-[4-fluoro-5-[4-(2- methoxyethoxy)phenyl]- 2-[rac-(3R,5S)-3,4,5- trimethylpiperazin-1- yl]phenyl]-6-oxo-4- (trifluoromethyl)-1H- pyridine-3-carboxamide	KD	0.441 nM	US-11319299: Substituted carboxamides as inhibitors of WDR5 protein-protein binding
N-[4-fIuoro-5-[1-[5- (morpholin-4-ylmethyl) pyrimidin-2-yl]-3,6-dihydro-2H- pyridin-4-yl]-2-[rac-(3R,5S)- 3,4,5-trimethylpiperazin- 1-yl]phenyl]-6-oxo-4- (trifluoromethyl)-1H- pyridine-3-carboxamide	KD	0.457 nM	US-11319299: Substituted carboxamides as inhibitors of WDR5 protein-protein binding
N-[4-fluoro-5-[6- methoxy-5-(trifluoromethyl) pyridin-3-yl]-2-[rac-(3R,5S)- 3,4,5-trimethylpiperazin- 1-yl]phenyl]-6-oxo-4- (trifluoromethyl)-1H- pyridine-3-carboxamide	KD	0.463 nM	US-11319299: Substituted carboxamides as inhibitors of WDR5 protein-protein binding
N-[4-fluoro-5-(3-fluoro- 4-morpholin-4-ylphenyl)- 2-[rac-(3R)-3,4- dimethylpiperazin-1- yl]phenyl]-6-oxo-4- (trifluoromethyl)-1H- pyridine-3-carboxamide	KD	0.466 nM	US-11319299: Substituted carboxamides as inhibitors of WDR5 protein-protein binding
N-[4-fluoro-5-[1-[5- (morpholin-4- ylmethyl)pyrimidin-2-yl]- 2,5-dihydropyrrol-3-yl]- 2-[rac-(3R,5S)-3,4,5- trimethylpiperazin-1- yl]phenyl]-6-oxo-4- (trifluoromethyl)-1H- pyridine-3-carboxamide	KD	0.474 nM	US-11319299: Substituted carboxamides as inhibitors of WDR5 protein-protein binding
propan-2-yl 4-[2-fluoro- 5-[[6-oxo-4-(trifluoromethyl)- 1H-pyridine-3- carbonyl]amino]-4-[rac- (3R,5S)-3,4,5- trimethylpiperazin-1- yl]phenyl]-3,6-dihydro- 2H-pyridine-1-carboxylate	KD	0.475 nM	US-11319299: Substituted carboxamides as inhibitors of WDR5 protein-protein binding
(1-methylcyclobutyl) 5- [2-fluoro-5-[[6-oxo-4- (trifluoromethyl)-1H- pyridine-3-carbonyl]amino]- 4-[rac-(3R,5S)-3,4,5- trimethylpiperazin-1- yl]phenyl]-3,6-dihydro- 2H-pyridine-1-carboxylate	KD	0.494 nM	US-11319299: Substituted carboxamides as inhibitors of WDR5 protein-protein binding
N-[4-fluoro-5-[1-(5- methylpyrimidin-2-yl)- 3,6-dihydro-2H-pyridin- 4-yl]-2-[rac-(3R,5S)- 3,4,5-trimethylpiperazin- 1-yl]phenyl]-6-oxo-4- (trifluoromethyl)-1H- pyridine-3-carboxamide	KD	0.499 nM	US-11319299: Substituted carboxamides as inhibitors of WDR5 protein-protein binding
N-[4-fluoro-5-(2- methylpyrimidin-5-yl)-2- [(3S,5R)-3,4,5- trimethylpiperazin-1- yl]phenyl]-6-oxo-4- (trifluoromethyl)-1H- pyridine-3-carboxamide	KD	0.5 nM	US-11319299: Substituted carboxamides as inhibitors of WDR5 protein-protein binding
N-[4-fluoro-5-(6- piperazin-1-ylpyridin-3- yl)-2-[rac-(3R,5S)-3,4,5- trimethylpiperazin-1- yl]phenyl]-6-oxo-4- (trifluoromethyl)-1H- pyridine-3-carboxamide	KD	0.5 nM	US-11319299: Substituted carboxamides as inhibitors of WDR5 protein-protein binding
N-[5-(4-cyanophenyl)-4- fluoro-2-[rac-(3R,5S)- 3,4,5-trimethylpiperazin- 1-yl]phenyl]-6-oxo-4- (trifluoromethyl)-1H- pyridine-3-carboxamide	KD	0.508 nM	US-11319299: Substituted carboxamides as inhibitors of WDR5 protein-protein binding
N-[4-fluoro-2-[rac-(3R)- 3,4-dimethylpiperazin-1- yl]-5-[2-[rac-(2R)-2- methylmorpholin-4- yl]pyrimidin-5-yl]phenyl]-6- oxo-4-(trifluoromethyl)-1H- pyridine-3-carboxamide	KD	0.522 nM	US-11319299: Substituted carboxamides as inhibitors of WDR5 protein-protein binding
N-[4-fluoro-5-[6-[rac- (2R,6S)-2,6- dimethylmorpholin-4- yl]pyridin-3-yl]-2-[rac- (3S,5R)-3,4,5- trimethylpiperazin-1- yl]phenyl]-6-oxo-4- (trifluoromethyl)-1H- pyridine-3-carboxamide	KD	0.532 nM	US-11319299: Substituted carboxamides as inhibitors of WDR5 protein-protein binding
N-[4-fluoro-5-(6- morpholin-4-ylpyridin-2- yl)-2-[rac-(3R,5S)-3,4,5- trimethylpiperazin-1- yl]phenyl]-6-oxo-4- (trifluoromethyl)-1H- pyridine-3-carboxamide	KD	0.533 nM	US-11319299: Substituted carboxamides as inhibitors of WDR5 protein-protein binding
N-[4-fluoro-5-[1-[(4- methoxyphenyl)methyl]- 3,6-dihydro-2H-pyridin- 4-yl]-2-[rac-(3R,5S)- 3,4,5-trimethylpiperazin- 1-yl]phenyl]-6-oxo-4- (trifluoromethyl)-1H- pyridine-3-carboxamide	KD	0.54 nM	US-11319299: Substituted carboxamides as inhibitors of WDR5 protein-protein binding
N-[4-fluoro-2-[rac-(3S)-3,4- dimethylpiperazin-1-yl]-5-[2- [rac-(2R)-2-methylmorpholin-4- yl]pyrimidin-5-yl]phenyl]-6-oxo- 4-(trifluoromethyl)-1H- pyridine-3-carboxamide	KD	0.551 nM	US-11319299: Substituted carboxamides as inhibitors of WDR5 protein-protein binding
N-[-4-fluoro-2-[rac-(3R)- 3,4-dimethylpiperazin-1- yl]-5-[6-(trifluoromethyl) pyridin-2-yl]phenyl]-6-oxo- 4-(trifluoromethyl)-1H- pyridine-3-carboxamide	KD	0.552 nM	US-11319299: Substituted carboxamides as inhibitors of WDR5 protein-protein binding
4-(difluoromethyl)-N-[4- fluoro-2-[rac-(3S)-3,4- dimethylpiperazin-1-yl]- 5-[2-[rac-(2R)-2- methylmorpholin-4- yl]pyrimidin-5-yl]phenyl]- 6-oxo-1H-pyridine-3- carboxamide	KD	0.564 nM	US-11319299: Substituted carboxamides as inhibitors of WDR5 protein-protein binding
N-[4-fluoro-5-[1-[2-(4- methoxyphenyl)acetyl]- 3,6-dihydro-2H-pyridin- 4-yl]-2-[rac-(3R,5S)- 3,4,5-trimethylpiperazin- 1-yl]phenyl]-6-oxo-4- (trifluoromethyl)-1H- pyridine-3-carboxamide	KD	0.57 nM	US-11319299: Substituted carboxamides as inhibitors of WDR5 protein-protein binding

ChEMBL bioactivities

1944 potent at pChembl≥5 of 2042 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).

pChembl	Type	Value	Unit	Molecule
10.70	Ki	0.02	nM	CHEMBL5190556
10.70	Ki	0.02	nM	CHEMBL5422217
10.70	Ki	0.02	nM	CHEMBL5414839
10.70	Ki	0.02	nM	CHEMBL5888524
10.70	Ki	0.02	nM	CHEMBL5871401
10.68	Ki	0.021	nM	CHEMBL5998450
10.66	Ki	0.022	nM	CHEMBL5169425
10.64	Kd	0.023	nM	CHEMBL4463486
10.64	Ki	0.023	nM	CHEMBL5181314
10.64	Ki	0.023	nM	CHEMBL5398730
10.60	Ki	0.025	nM	CHEMBL5186072
10.59	Ki	0.026	nM	CHEMBL5398302
10.57	Kd	0.027	nM	CHEMBL4476662
10.57	Ki	0.027	nM	CHEMBL5405792
10.55	Ki	0.028	nM	CHEMBL5192283
10.55	Ki	0.028	nM	CHEMBL5171051
10.55	Ki	0.028	nM	CHEMBL5179388
10.54	Ki	0.029	nM	CHEMBL5182982
10.54	Ki	0.029	nM	CHEMBL5180435
10.52	Kd	0.03	nM	CHEMBL4557848
10.52	Kd	0.03	nM	CHEMBL4534270
10.51	Ki	0.031	nM	CHEMBL5978035
10.49	Kd	0.032	nM	CHEMBL4585441
10.48	Kd	0.033	nM	CHEMBL4530969
10.48	Ki	0.033	nM	CHEMBL5171315
10.48	Ki	0.033	nM	CHEMBL5401138
10.48	Ki	0.033	nM	CHEMBL5939864
10.46	Kd	0.035	nM	CHEMBL4439051
10.46	Ki	0.035	nM	CHEMBL5171953
10.44	Ki	0.036	nM	CHEMBL5202878
10.43	Ki	0.037	nM	CHEMBL5431390
10.42	Ki	0.038	nM	CHEMBL5747419
10.41	Ki	0.039	nM	CHEMBL5194215
10.41	Ki	0.039	nM	CHEMBL5440128
10.37	Kd	0.043	nM	CHEMBL4453355
10.36	Ki	0.044	nM	CHEMBL4441671
10.34	Ki	0.046	nM	CHEMBL5206455
10.33	Ki	0.047	nM	CHEMBL5425914
10.31	Kd	0.049	nM	CHEMBL4435250
10.31	Ki	0.049	nM	CHEMBL4435250
10.30	Ki	0.05	nM	CHEMBL5890838
10.29	Ki	0.051	nM	CHEMBL5401714
10.26	Kd	0.055	nM	CHEMBL4555492
10.26	Ki	0.055	nM	CHEMBL5182077
10.22	Kd	0.06	nM	CHEMBL5182613
10.22	Ki	0.06	nM	CHEMBL5974946
10.22	Ki	0.06	nM	CHEMBL5856268
10.22	Ki	0.06	nM	CHEMBL5860062
10.21	Kd	0.061	nM	CHEMBL4593719
10.20	Kd	0.063	nM	CHEMBL4556167

PubChem BioAssay actives

623 with measured affinity, of 1346 total; 50 most potent distinct compounds. Largely complementary to BindingDB; screening values are coarse (µM, 4 dp), so sub-nM hits tie at the floor.

Compound	Assay	Type	Value	Unit
N-[(3,4-dichlorophenyl)methyl]-3-(6-fluoro-2-methyl-3-pyridinyl)-5-[(2-imino-3-methylimidazol-1-yl)methyl]benzamide	1582122: Competitive inhibition of human N-terminal His6-SUMO tagged WDR5 (22 to 334 residues) expressed in Escherichia coli BL21-Gold(DE3) cells using 10-mer-Thr-FAM peptide as substrate after 1 hr by TR-FRET assay	ki	<0.0001	uM
N-[(3,5-dimethoxyphenyl)methyl]-3-(4-fluoro-2-methylphenyl)-5-[(2-imino-3-methylimidazol-1-yl)methyl]benzamide	1582122: Competitive inhibition of human N-terminal His6-SUMO tagged WDR5 (22 to 334 residues) expressed in Escherichia coli BL21-Gold(DE3) cells using 10-mer-Thr-FAM peptide as substrate after 1 hr by TR-FRET assay	kd	<0.0001	uM
2-[(3,5-dimethoxyphenyl)methyl]-5-(4-fluoro-2-methylphenyl)-7-[(2-imino-3-methylimidazol-1-yl)methyl]-3,4-dihydroisoquinolin-1-one	1582122: Competitive inhibition of human N-terminal His6-SUMO tagged WDR5 (22 to 334 residues) expressed in Escherichia coli BL21-Gold(DE3) cells using 10-mer-Thr-FAM peptide as substrate after 1 hr by TR-FRET assay	kd	<0.0001	uM
3-(4-fluoro-2-methylphenyl)-N-[(4-fluoro-3-methylphenyl)methyl]-5-[(2-imino-3-methylimidazol-1-yl)methyl]benzamide	1582122: Competitive inhibition of human N-terminal His6-SUMO tagged WDR5 (22 to 334 residues) expressed in Escherichia coli BL21-Gold(DE3) cells using 10-mer-Thr-FAM peptide as substrate after 1 hr by TR-FRET assay	kd	<0.0001	uM
2-[(3,5-dimethoxyphenyl)methyl]-6-(4-fluoro-2-methylphenyl)-8-[(2-imino-3-methylimidazol-1-yl)methyl]-4,5-dihydro-3H-2-benzazepin-1-one	2025265: Inhibition of 6His-SUMO tagged human WDR5 (22 to 334 residues) expressed in Escherichia coli BL21-Gold (DE3) cells incubated for 1 hr by TR-FRET assay	ki	<0.0001	uM
5-[1-ethyl-3-(trifluoromethyl)pyrazol-4-yl]-2-[(1S)-1-(4-methoxy-2-pyridinyl)ethyl]-7-[(2-methylimidazol-1-yl)methyl]-3,4-dihydroisoquinolin-1-one	1908631: Competitive binding affinity to N-terminal 6xHis-SUMO-tagged human WDR5 (22 to 334 residues) expressed in Escherichia coli BL21-Gold (DE3) cells assessed as inhibition constant using 10-mer-Thr-FAM peptide as substrate incubated for 1 hr by Lantha Screen based TR-FRET assay	ki	<0.0001	uM
2-[(3,5-dimethoxyphenyl)methyl]-5-(1,3-dimethylpyrazol-4-yl)-7-[(2-imino-3-methylimidazol-1-yl)methyl]-3,4-dihydroisoquinolin-1-one	1908631: Competitive binding affinity to N-terminal 6xHis-SUMO-tagged human WDR5 (22 to 334 residues) expressed in Escherichia coli BL21-Gold (DE3) cells assessed as inhibition constant using 10-mer-Thr-FAM peptide as substrate incubated for 1 hr by Lantha Screen based TR-FRET assay	ki	<0.0001	uM
2-[(4-ethyl-2-pyridinyl)methyl]-5-[1-ethyl-3-(trifluoromethyl)pyrazol-4-yl]-7-[(2-methylimidazol-1-yl)methyl]-3,4-dihydroisoquinolin-1-one	1908631: Competitive binding affinity to N-terminal 6xHis-SUMO-tagged human WDR5 (22 to 334 residues) expressed in Escherichia coli BL21-Gold (DE3) cells assessed as inhibition constant using 10-mer-Thr-FAM peptide as substrate incubated for 1 hr by Lantha Screen based TR-FRET assay	ki	<0.0001	uM
7-[(2-methylimidazol-1-yl)methyl]-2-[(4-methyl-2-pyridinyl)methyl]-5-[1-methyl-3-(trifluoromethyl)pyrazol-4-yl]-3,4-dihydroisoquinolin-1-one	1908631: Competitive binding affinity to N-terminal 6xHis-SUMO-tagged human WDR5 (22 to 334 residues) expressed in Escherichia coli BL21-Gold (DE3) cells assessed as inhibition constant using 10-mer-Thr-FAM peptide as substrate incubated for 1 hr by Lantha Screen based TR-FRET assay	ki	<0.0001	uM
2-[(3,5-dimethoxyphenyl)methyl]-5-(4-fluoro-2-methylphenyl)-7-[(2-imino-1,3-oxazol-3-yl)methyl]-3,4-dihydroisoquinolin-1-one	1582122: Competitive inhibition of human N-terminal His6-SUMO tagged WDR5 (22 to 334 residues) expressed in Escherichia coli BL21-Gold(DE3) cells using 10-mer-Thr-FAM peptide as substrate after 1 hr by TR-FRET assay	kd	<0.0001	uM
2-[(3,5-dimethoxyphenyl)methyl]-5-(4-fluoro-2-methylphenyl)-7-[(5-imino-1-methyl-1,2,4-triazol-4-yl)methyl]-3,4-dihydroisoquinolin-1-one	1582122: Competitive inhibition of human N-terminal His6-SUMO tagged WDR5 (22 to 334 residues) expressed in Escherichia coli BL21-Gold(DE3) cells using 10-mer-Thr-FAM peptide as substrate after 1 hr by TR-FRET assay	kd	<0.0001	uM
2-[(S)-cyclopropyl-(4-methyl-2-pyridinyl)methyl]-5-[1-ethyl-3-(trifluoromethyl)pyrazol-4-yl]-7-[(2-methylimidazol-1-yl)methyl]-3,4-dihydroisoquinolin-1-one	1908631: Competitive binding affinity to N-terminal 6xHis-SUMO-tagged human WDR5 (22 to 334 residues) expressed in Escherichia coli BL21-Gold (DE3) cells assessed as inhibition constant using 10-mer-Thr-FAM peptide as substrate incubated for 1 hr by Lantha Screen based TR-FRET assay	ki	<0.0001	uM
2-[(3,5-dimethoxyphenyl)methyl]-7-[(2-imino-3-methylimidazol-1-yl)methyl]-5-[2-(trifluoromethyl)-3-pyridinyl]-3,4-dihydroisoquinolin-1-one	1908631: Competitive binding affinity to N-terminal 6xHis-SUMO-tagged human WDR5 (22 to 334 residues) expressed in Escherichia coli BL21-Gold (DE3) cells assessed as inhibition constant using 10-mer-Thr-FAM peptide as substrate incubated for 1 hr by Lantha Screen based TR-FRET assay	ki	<0.0001	uM
2-[(3,5-dimethoxyphenyl)methyl]-7-[(2-imino-3-methylimidazol-1-yl)methyl]-5-[1-methyl-3-(trifluoromethyl)pyrazol-4-yl]-3,4-dihydroisoquinolin-1-one	1908631: Competitive binding affinity to N-terminal 6xHis-SUMO-tagged human WDR5 (22 to 334 residues) expressed in Escherichia coli BL21-Gold (DE3) cells assessed as inhibition constant using 10-mer-Thr-FAM peptide as substrate incubated for 1 hr by Lantha Screen based TR-FRET assay	ki	<0.0001	uM
2-[(3,5-dimethoxyphenyl)methyl]-7-[(2-methylimidazol-1-yl)methyl]-5-[1-methyl-3-(trifluoromethyl)pyrazol-4-yl]-3,4-dihydroisoquinolin-1-one	1908631: Competitive binding affinity to N-terminal 6xHis-SUMO-tagged human WDR5 (22 to 334 residues) expressed in Escherichia coli BL21-Gold (DE3) cells assessed as inhibition constant using 10-mer-Thr-FAM peptide as substrate incubated for 1 hr by Lantha Screen based TR-FRET assay	ki	<0.0001	uM
2-[(4-methoxy-2-pyridinyl)methyl]-7-[(2-methylimidazol-1-yl)methyl]-5-[1-methyl-3-(trifluoromethyl)pyrazol-4-yl]-3,4-dihydroisoquinolin-1-one	1908631: Competitive binding affinity to N-terminal 6xHis-SUMO-tagged human WDR5 (22 to 334 residues) expressed in Escherichia coli BL21-Gold (DE3) cells assessed as inhibition constant using 10-mer-Thr-FAM peptide as substrate incubated for 1 hr by Lantha Screen based TR-FRET assay	ki	<0.0001	uM
5-(4-fluoro-2-methylphenyl)-2-[(4-fluoro-3-methylphenyl)methyl]-7-[(2-imino-3-methylimidazol-1-yl)methyl]-3,4-dihydroisoquinolin-1-one	1582122: Competitive inhibition of human N-terminal His6-SUMO tagged WDR5 (22 to 334 residues) expressed in Escherichia coli BL21-Gold(DE3) cells using 10-mer-Thr-FAM peptide as substrate after 1 hr by TR-FRET assay	kd	<0.0001	uM
2-[(S)-cyclopropyl-(4-methoxy-2-pyridinyl)methyl]-5-[1-ethyl-3-(trifluoromethyl)pyrazol-4-yl]-7-(imidazol-1-ylmethyl)-3,4-dihydroisoquinolin-1-one	1908631: Competitive binding affinity to N-terminal 6xHis-SUMO-tagged human WDR5 (22 to 334 residues) expressed in Escherichia coli BL21-Gold (DE3) cells assessed as inhibition constant using 10-mer-Thr-FAM peptide as substrate incubated for 1 hr by Lantha Screen based TR-FRET assay	ki	<0.0001	uM
7-[(2-methylimidazol-1-yl)methyl]-2-[(6-methyl-2-pyridinyl)methyl]-5-[1-methyl-3-(trifluoromethyl)pyrazol-4-yl]-3,4-dihydroisoquinolin-1-one	1908631: Competitive binding affinity to N-terminal 6xHis-SUMO-tagged human WDR5 (22 to 334 residues) expressed in Escherichia coli BL21-Gold (DE3) cells assessed as inhibition constant using 10-mer-Thr-FAM peptide as substrate incubated for 1 hr by Lantha Screen based TR-FRET assay	ki	<0.0001	uM
2-[(3,5-dimethoxyphenyl)methyl]-5-(4-fluoro-2-methylphenyl)-7-[(2-imino-1,3-thiazolidin-3-yl)methyl]-3,4-dihydroisoquinolin-1-one	1582122: Competitive inhibition of human N-terminal His6-SUMO tagged WDR5 (22 to 334 residues) expressed in Escherichia coli BL21-Gold(DE3) cells using 10-mer-Thr-FAM peptide as substrate after 1 hr by TR-FRET assay	kd	<0.0001	uM
7-[(3-cyclopropyl-2-iminoimidazol-1-yl)methyl]-2-[(3,5-dimethoxyphenyl)methyl]-5-(4-fluoro-2-methylphenyl)-3,4-dihydroisoquinolin-1-one	1582122: Competitive inhibition of human N-terminal His6-SUMO tagged WDR5 (22 to 334 residues) expressed in Escherichia coli BL21-Gold(DE3) cells using 10-mer-Thr-FAM peptide as substrate after 1 hr by TR-FRET assay	kd	<0.0001	uM
N’-[[2-[(3,5-dimethoxyphenyl)methyl]-5-(4-fluoro-2-methylphenyl)-1-oxo-3,4-dihydroisoquinolin-7-yl]methyl]cyclopropanecarboximidamide	1582122: Competitive inhibition of human N-terminal His6-SUMO tagged WDR5 (22 to 334 residues) expressed in Escherichia coli BL21-Gold(DE3) cells using 10-mer-Thr-FAM peptide as substrate after 1 hr by TR-FRET assay	kd	<0.0001	uM
2-[(4-chloro-3-methylphenyl)methyl]-5-(4-fluoro-2-methylphenyl)-7-[(2-imino-3-methylimidazol-1-yl)methyl]-3,4-dihydroisoquinolin-1-one	1582122: Competitive inhibition of human N-terminal His6-SUMO tagged WDR5 (22 to 334 residues) expressed in Escherichia coli BL21-Gold(DE3) cells using 10-mer-Thr-FAM peptide as substrate after 1 hr by TR-FRET assay	kd	<0.0001	uM
9-[1-ethyl-3-(trifluoromethyl)pyrazol-4-yl]-7-(imidazol-1-ylmethyl)-4-[(4S)-6-methoxy-3,4-dihydro-2H-chromen-4-yl]-2,3-dihydro-1,4-benzoxazepin-5-one	2025265: Inhibition of 6His-SUMO tagged human WDR5 (22 to 334 residues) expressed in Escherichia coli BL21-Gold (DE3) cells incubated for 1 hr by TR-FRET assay	ki	<0.0001	uM
4-[(S)-cyclopropyl-(4-methoxy-2-pyridinyl)methyl]-9-[1-ethyl-3-(trifluoromethyl)pyrazol-4-yl]-7-(imidazol-1-ylmethyl)-2,3-dihydro-1,4-benzoxazepin-5-one	2025265: Inhibition of 6His-SUMO tagged human WDR5 (22 to 334 residues) expressed in Escherichia coli BL21-Gold (DE3) cells incubated for 1 hr by TR-FRET assay	ki	<0.0001	uM
4-[(3,5-dimethoxyphenyl)methyl]-9-(4-fluoro-2-methylphenyl)-7-[(2-imino-3-methylimidazol-1-yl)methyl]-2,3-dihydro-1H-1,4-benzodiazepin-5-one	2025265: Inhibition of 6His-SUMO tagged human WDR5 (22 to 334 residues) expressed in Escherichia coli BL21-Gold (DE3) cells incubated for 1 hr by TR-FRET assay	ki	<0.0001	uM
4-(7-methoxy-1,2,3,4-tetrahydronaphthalen-1-yl)-7-[(2-methylimidazol-1-yl)methyl]-9-[1-methyl-3-(trifluoromethyl)pyrazol-4-yl]-2,3-dihydro-1,4-benzoxazepin-5-one	2025265: Inhibition of 6His-SUMO tagged human WDR5 (22 to 334 residues) expressed in Escherichia coli BL21-Gold (DE3) cells incubated for 1 hr by TR-FRET assay	ki	<0.0001	uM
4-(6-ethyl-8-methoxyquinolin-4-yl)-7-(imidazol-1-ylmethyl)-9-[1-methyl-3-(trifluoromethyl)pyrazol-4-yl]-2,3-dihydro-1,4-benzoxazepin-5-one	2025265: Inhibition of 6His-SUMO tagged human WDR5 (22 to 334 residues) expressed in Escherichia coli BL21-Gold (DE3) cells incubated for 1 hr by TR-FRET assay	ki	<0.0001	uM
9-[1-ethyl-3-(trifluoromethyl)pyrazol-4-yl]-4-[(4S)-6-methoxy-3,4-dihydro-2H-chromen-4-yl]-7-[(2-methylimidazol-1-yl)methyl]-2,3-dihydro-1,4-benzoxazepin-5-one	2025265: Inhibition of 6His-SUMO tagged human WDR5 (22 to 334 residues) expressed in Escherichia coli BL21-Gold (DE3) cells incubated for 1 hr by TR-FRET assay	ki	<0.0001	uM
3-[(3,5-dimethoxyphenyl)methyl]-8-(4-fluoro-2-methylphenyl)-6-[(2-imino-3-methylimidazol-1-yl)methyl]-1,2-dihydroquinazolin-4-one	2025265: Inhibition of 6His-SUMO tagged human WDR5 (22 to 334 residues) expressed in Escherichia coli BL21-Gold (DE3) cells incubated for 1 hr by TR-FRET assay	ki	<0.0001	uM
7-(imidazol-1-ylmethyl)-4-(3-methoxyquinolin-5-yl)-9-[1-methyl-3-(trifluoromethyl)pyrazol-4-yl]-2,3-dihydro-1,4-benzoxazepin-5-one	2025265: Inhibition of 6His-SUMO tagged human WDR5 (22 to 334 residues) expressed in Escherichia coli BL21-Gold (DE3) cells incubated for 1 hr by TR-FRET assay	ki	<0.0001	uM
4-[(3,5-dimethoxyphenyl)methyl]-9-(4-fluoro-2-methylphenyl)-7-[(2-imino-3-methylimidazol-1-yl)methyl]-2,3-dihydro-1,4-benzoxazepin-5-one	2025265: Inhibition of 6His-SUMO tagged human WDR5 (22 to 334 residues) expressed in Escherichia coli BL21-Gold (DE3) cells incubated for 1 hr by TR-FRET assay	ki	<0.0001	uM
N-[(4-fluoro-3-methoxyphenyl)methyl]-3-(4-fluoro-2-methylphenyl)-5-[(2-imino-3-methylimidazol-1-yl)methyl]benzamide	1582122: Competitive inhibition of human N-terminal His6-SUMO tagged WDR5 (22 to 334 residues) expressed in Escherichia coli BL21-Gold(DE3) cells using 10-mer-Thr-FAM peptide as substrate after 1 hr by TR-FRET assay	kd	<0.0001	uM
N-[(3,4-dichlorophenyl)methyl]-3-(4-fluoro-2-methylphenyl)-5-[(2-imino-3-methylimidazol-1-yl)methyl]benzamide	1582122: Competitive inhibition of human N-terminal His6-SUMO tagged WDR5 (22 to 334 residues) expressed in Escherichia coli BL21-Gold(DE3) cells using 10-mer-Thr-FAM peptide as substrate after 1 hr by TR-FRET assay	kd	<0.0001	uM
6-ethyl-4-[7-(imidazol-1-ylmethyl)-5-[1-methyl-3-(trifluoromethyl)pyrazol-4-yl]-1-oxo-3,4-dihydroisoquinolin-2-yl]-N-methylquinoline-8-carboxamide	2025265: Inhibition of 6His-SUMO tagged human WDR5 (22 to 334 residues) expressed in Escherichia coli BL21-Gold (DE3) cells incubated for 1 hr by TR-FRET assay	ki	<0.0001	uM
7-(imidazol-1-ylmethyl)-2-(3-methoxyquinolin-5-yl)-5-[1-methyl-3-(trifluoromethyl)pyrazol-4-yl]-3,4-dihydroisoquinolin-1-one	2025265: Inhibition of 6His-SUMO tagged human WDR5 (22 to 334 residues) expressed in Escherichia coli BL21-Gold (DE3) cells incubated for 1 hr by TR-FRET assay	ki	<0.0001	uM
2-(6-ethyl-8-methoxyquinolin-4-yl)-7-(imidazol-1-ylmethyl)-5-[1-methyl-3-(trifluoromethyl)pyrazol-4-yl]-3,4-dihydroisoquinolin-1-one	2025265: Inhibition of 6His-SUMO tagged human WDR5 (22 to 334 residues) expressed in Escherichia coli BL21-Gold (DE3) cells incubated for 1 hr by TR-FRET assay	ki	<0.0001	uM
2-[(R)-cyclopropyl-(4-methoxy-2-pyridinyl)methyl]-5-[1-ethyl-3-(trifluoromethyl)pyrazol-4-yl]-7-(imidazol-1-ylmethyl)-3,4-dihydroisoquinolin-1-one	1908631: Competitive binding affinity to N-terminal 6xHis-SUMO-tagged human WDR5 (22 to 334 residues) expressed in Escherichia coli BL21-Gold (DE3) cells assessed as inhibition constant using 10-mer-Thr-FAM peptide as substrate incubated for 1 hr by Lantha Screen based TR-FRET assay	ki	<0.0001	uM
2-[(3,5-dimethoxyphenyl)methyl]-5-(4-fluoro-2-methoxyphenyl)-7-[(2-imino-3-methylimidazol-1-yl)methyl]-3,4-dihydroisoquinolin-1-one	1908631: Competitive binding affinity to N-terminal 6xHis-SUMO-tagged human WDR5 (22 to 334 residues) expressed in Escherichia coli BL21-Gold (DE3) cells assessed as inhibition constant using 10-mer-Thr-FAM peptide as substrate incubated for 1 hr by Lantha Screen based TR-FRET assay	ki	<0.0001	uM
7-[(2-cyclopropylimidazol-1-yl)methyl]-2-[(3,5-dimethoxyphenyl)methyl]-5-[1-methyl-3-(trifluoromethyl)pyrazol-4-yl]-3,4-dihydroisoquinolin-1-one	1908631: Competitive binding affinity to N-terminal 6xHis-SUMO-tagged human WDR5 (22 to 334 residues) expressed in Escherichia coli BL21-Gold (DE3) cells assessed as inhibition constant using 10-mer-Thr-FAM peptide as substrate incubated for 1 hr by Lantha Screen based TR-FRET assay	ki	<0.0001	uM
2-[(3,5-dimethoxyphenyl)methyl]-5-(4-fluoro-2-hydroxyphenyl)-7-[(2-imino-3-methylimidazol-1-yl)methyl]-3,4-dihydroisoquinolin-1-one	1908631: Competitive binding affinity to N-terminal 6xHis-SUMO-tagged human WDR5 (22 to 334 residues) expressed in Escherichia coli BL21-Gold (DE3) cells assessed as inhibition constant using 10-mer-Thr-FAM peptide as substrate incubated for 1 hr by Lantha Screen based TR-FRET assay	ki	<0.0001	uM
2-[(3,5-dimethoxyphenyl)methyl]-5-(2,5-dimethyl-3-pyridinyl)-7-[(2-imino-3-methylimidazol-1-yl)methyl]-3,4-dihydroisoquinolin-1-one	1908631: Competitive binding affinity to N-terminal 6xHis-SUMO-tagged human WDR5 (22 to 334 residues) expressed in Escherichia coli BL21-Gold (DE3) cells assessed as inhibition constant using 10-mer-Thr-FAM peptide as substrate incubated for 1 hr by Lantha Screen based TR-FRET assay	ki	<0.0001	uM
2-[(4-ethyl-2-pyridinyl)methyl]-7-[(2-methylimidazol-1-yl)methyl]-5-[1-methyl-3-(trifluoromethyl)pyrazol-4-yl]-3,4-dihydroisoquinolin-1-one	1908631: Competitive binding affinity to N-terminal 6xHis-SUMO-tagged human WDR5 (22 to 334 residues) expressed in Escherichia coli BL21-Gold (DE3) cells assessed as inhibition constant using 10-mer-Thr-FAM peptide as substrate incubated for 1 hr by Lantha Screen based TR-FRET assay	ki	<0.0001	uM
5-[1-ethyl-3-(trifluoromethyl)pyrazol-4-yl]-7-(imidazol-1-ylmethyl)-2-[(1R)-1-(4-methoxy-2-pyridinyl)ethyl]-3,4-dihydroisoquinolin-1-one	1908631: Competitive binding affinity to N-terminal 6xHis-SUMO-tagged human WDR5 (22 to 334 residues) expressed in Escherichia coli BL21-Gold (DE3) cells assessed as inhibition constant using 10-mer-Thr-FAM peptide as substrate incubated for 1 hr by Lantha Screen based TR-FRET assay	ki	<0.0001	uM
5-[1-ethyl-3-(trifluoromethyl)pyrazol-4-yl]-2-[(1R)-1-(4-methoxy-2-pyridinyl)ethyl]-7-[(2-methylimidazol-1-yl)methyl]-3,4-dihydroisoquinolin-1-one	1908631: Competitive binding affinity to N-terminal 6xHis-SUMO-tagged human WDR5 (22 to 334 residues) expressed in Escherichia coli BL21-Gold (DE3) cells assessed as inhibition constant using 10-mer-Thr-FAM peptide as substrate incubated for 1 hr by Lantha Screen based TR-FRET assay	ki	<0.0001	uM
2-[(3,5-dimethoxyphenyl)methyl]-5-(2,5-dimethylpyrazol-3-yl)-7-[(2-imino-3-methylimidazol-1-yl)methyl]-3,4-dihydroisoquinolin-1-one	1908631: Competitive binding affinity to N-terminal 6xHis-SUMO-tagged human WDR5 (22 to 334 residues) expressed in Escherichia coli BL21-Gold (DE3) cells assessed as inhibition constant using 10-mer-Thr-FAM peptide as substrate incubated for 1 hr by Lantha Screen based TR-FRET assay	ki	<0.0001	uM
2-[(3,5-dimethoxyphenyl)methyl]-5-[1-ethyl-3-(trifluoromethyl)pyrazol-4-yl]-7-[(2-imino-3-methylimidazol-1-yl)methyl]-3,4-dihydroisoquinolin-1-one	1908631: Competitive binding affinity to N-terminal 6xHis-SUMO-tagged human WDR5 (22 to 334 residues) expressed in Escherichia coli BL21-Gold (DE3) cells assessed as inhibition constant using 10-mer-Thr-FAM peptide as substrate incubated for 1 hr by Lantha Screen based TR-FRET assay	ki	<0.0001	uM
2-[(3,5-dimethoxyphenyl)methyl]-7-[(2-imino-3-methylimidazol-1-yl)methyl]-5-(3-methyl-4-pyridinyl)-3,4-dihydroisoquinolin-1-one	1908631: Competitive binding affinity to N-terminal 6xHis-SUMO-tagged human WDR5 (22 to 334 residues) expressed in Escherichia coli BL21-Gold (DE3) cells assessed as inhibition constant using 10-mer-Thr-FAM peptide as substrate incubated for 1 hr by Lantha Screen based TR-FRET assay	ki	<0.0001	uM
5-[1-ethyl-3-(trifluoromethyl)pyrazol-4-yl]-2-[(4-methoxy-2-pyridinyl)methyl]-7-[(2-methylimidazol-1-yl)methyl]-3,4-dihydroisoquinolin-1-one	1908631: Competitive binding affinity to N-terminal 6xHis-SUMO-tagged human WDR5 (22 to 334 residues) expressed in Escherichia coli BL21-Gold (DE3) cells assessed as inhibition constant using 10-mer-Thr-FAM peptide as substrate incubated for 1 hr by Lantha Screen based TR-FRET assay	ki	<0.0001	uM
2-[(R)-cyclopropyl-(4-methoxy-2-pyridinyl)methyl]-5-[1-ethyl-3-(trifluoromethyl)pyrazol-4-yl]-7-[(2-methylimidazol-1-yl)methyl]-3,4-dihydroisoquinolin-1-one	1908631: Competitive binding affinity to N-terminal 6xHis-SUMO-tagged human WDR5 (22 to 334 residues) expressed in Escherichia coli BL21-Gold (DE3) cells assessed as inhibition constant using 10-mer-Thr-FAM peptide as substrate incubated for 1 hr by Lantha Screen based TR-FRET assay	ki	<0.0001	uM

CTD chemical–gene interactions

37 total (human), top 30 by PubMed support.

Chemical	Actions (top 5)	PubMed papers
bisphenol A	decreases reaction, affects binding, increases reaction, decreases expression, increases expression (+1 more)	3
arsenite	affects binding, increases reaction, increases methylation	2
sodium arsenite	decreases expression, increases expression	2
Nickel	increases expression	2
Valproic Acid	affects expression, increases expression	2
Cadmium Chloride	decreases reaction, increases abundance, increases palmitoylation, decreases expression	2
dicrotophos	increases expression	1
deoxynivalenol	increases expression	1
sodium arsenate	decreases expression	1
decabromobiphenyl ether	increases expression	1
tetrabromobisphenol A	decreases expression	1
2-bromopalmitate	decreases reaction, increases abundance, increases palmitoylation	1
zinc chromate	decreases expression, increases abundance	1
nonylphenol	increases expression	1
beta-methylcholine	affects expression	1
gadodiamide	increases expression	1
di-n-butylphosphoric acid	affects expression	1
chromium hexavalent ion	decreases expression, increases abundance	1
4-octylphenol	increases expression	1
4-(5-benzo(1,3)dioxol-5-yl-4-pyridin-2-yl-1H-imidazol-2-yl)benzamide	affects cotreatment, increases expression	1
abrine	decreases expression	1
2,2’,4,4’-tetrabromodiphenyl ether	decreases expression	1
pentabrominated diphenyl ether 100	increases expression	1
hexabrominated diphenyl ether 153	increases expression	1
2-(1H-indazol-4-yl)-6-(4-methanesulfonylpiperazin-1-ylmethyl)-4-morpholin-4-ylthieno(3,2-d)pyrimidine	decreases expression, increases response to substance	1
bisphenol S	affects expression	1
LDN 193189	affects cotreatment, increases expression	1
Arsenic	affects methylation	1
Cadmium	increases abundance, increases palmitoylation, decreases reaction	1
Doxorubicin	decreases expression	1

ChEMBL screening assays

314 unique, capped per target: 311 binding, 3 functional

Representative assays (with source publication via chembl_document):

Assay ID	Type	Description	Source paper
CHEMBL1118768	Binding	Binding affinity to WDR5 expressed in pLysS cells by optimized fluorescent polarization based competitive binding assay	Analysis of the binding of mixed lineage leukemia 1 (MLL1) and histone 3 peptides to WD repeat domain 5 (WDR5) for the design of inhibitors of the MLL1-WDR5 interaction. — J Med Chem
CHEMBL5723088	Functional	Affinity Biochemical interaction: (Fluorescence polarisation anisotropy) EUB0002166aAD WDR5	Affinity Biochemical Literature for EUbOPEN Chemogenomic Library

Clinical trials (associated diseases)

300 trials via MONDO — disease-level, not drug-specific.

Trial	Phase	Status	Title
NCT00668824	PHASE4	UNKNOWN	Improved Diagnosis of Congenital Heart Disease by Magnetic Resonance Imaging Using Vasovist
NCT01368705	PHASE4	COMPLETED	Nitrogen Balance in Infants After Post Cardiothoracic Surgery
NCT01619982	PHASE4	COMPLETED	Pre-operative Prophylaxis With Vancomycin and Cefazolin in Pediatric Cardiovascular Surgery Patients
NCT02122679	PHASE4	WITHDRAWN	Tranexamic Acid Effect on Platelet Aggregation Following Infant Cardiopulmonary Bypass
NCT02527811	PHASE4	UNKNOWN	Ulinastatin Injection in in Pediatric Patients Undergoing Open Heart Surgery
NCT03014700	PHASE4	COMPLETED	Fibrinogen Concentrate vs Cryoprecipitate
NCT03408340	PHASE4	TERMINATED	Paravertebral Nerve Blocks in Neonates
NCT03630796	PHASE4	UNKNOWN	Effect of Sevoflurane in Postoperative Troponin I Levels in Children Undergoing Congenital Heart Defects Surgery
NCT03667703	PHASE4	COMPLETED	Stress Ulcer Prophylaxis Versus Placebo in Critically Ill Infants With Congenital Heart Disease
NCT04453761	PHASE4	UNKNOWN	Thiamine Influenced on Substrate Energy Effectiveness in Indonesian Children Undergoing Cardiopulmonary Bypass
NCT06668389	PHASE4	RECRUITING	Sodium-Glucose Cotransporter 2 Inhibitors for Repaired Tetralogy of Fallot Patients for Enhancement of Cardio-Pulmonary Status Trial
NCT07499154	PHASE4	NOT_YET_RECRUITING	Perioperative Lidocaine for Lung Protection in Infants Undergoing Cardiac Surgery
NCT00000470	PHASE3	COMPLETED	Infant Heart Surgery: Central Nervous System Sequelae of Circulatory Arrest
NCT00000494	PHASE3	COMPLETED	Management of Patent Ductus in Premature Infants
NCT01134302	PHASE3	UNKNOWN	Hybrid Versus Norwood Management Strategies in Infants Undergoing Single Ventricle Palliation
NCT01607983	PHASE3	WITHDRAWN	Effects of Pulmonary Vasodilation Upon VA Coupling in Fontan Patients
NCT01662011	PHASE3	UNKNOWN	Application of Neurally Adjusted Ventilatory Assist to Children After Congenital Cardiac Surgery
NCT02320669	PHASE3	COMPLETED	Phase 3 Triiodothyronine Supplementation for Infants After Cardiopulmonary Bypass
NCT02615262	PHASE3	COMPLETED	Intraoperative Dexamethasone in Pediatric Cardiac Surgery
NCT03153137	PHASE3	COMPLETED	Clinical Study Assessing the Efficacy and Safety of Macitentan in Fontan-palliated Subjects
NCT03154476	PHASE3	COMPLETED	Role of Sildenafil for Fontan Associated Liver Disease (SiFALD) Study
NCT04536194	PHASE3	COMPLETED	Dopamine Versus Norepinephrine Under General Anesthesia
NCT04702373	PHASE3	ACTIVE_NOT_RECRUITING	Training in Exercise Activities and Motion for Growth (TEAM 4 Growth) RCT
NCT05049590	PHASE3	COMPLETED	Acute Normovolemic Hemodilution in Complex Cardiac Surgery
NCT06406517	PHASE3	UNKNOWN	Comparative Effectiveness of Gadopiclenol for Evaluation of Adult Congenital Heart Anatomy and Hemodynamics
NCT06693674	PHASE3	RECRUITING	Effect of Sacubitril-Valsartan on Cardiac Structure and Function
NCT06955260	PHASE3	NOT_YET_RECRUITING	SGLT2 Inhibition With Empagliflozin in Fontan Circulatory Failure
NCT00115375	PHASE2	COMPLETED	Platelet Aggregation Inhibition in Children on Clopidogrel (PICOLO)
NCT00350220	PHASE2	COMPLETED	Transfusion Strategies in Pediatric Cardiothoracic Surgery
NCT00374088	PHASE2	COMPLETED	N-Acetylcysteine in Neonatal Congenital Heart Surgery (INACT Study)
NCT00538785	PHASE2	COMPLETED	A Study to Evaluate MEDI-524 In Children With Hemodynamically Significant Congenital Heart Disease
NCT00770705	PHASE2	WITHDRAWN	Parenteral Phenoxybenzamine During Congenital Heart Disease Surgery
NCT00919945	PHASE2	TERMINATED	Impact of Early Enteral Feeding on Splanchnic Blood Flow After Surgery for Critical Heart Disease in the Newborn
NCT01063712	PHASE2	COMPLETED	Safety and Effectiveness of the Device Nit-Occlud® PDA-R
NCT01069510	PHASE2	COMPLETED	Spironolactone in Adult Congenital Heart Disease
NCT01189981	PHASE2	COMPLETED	Effect of eHealth Encouragements to Intensive Exercise in Adolescents With Congenital Heart Disease
NCT01330433	PHASE2	COMPLETED	Effects of CoSeal on Bleeding & Adhesions in Pediatric Heart Surgery
NCT01662037	PHASE2	COMPLETED	Bosentan Therapy in Children With Functional Single Ventricle
NCT01668264	PHASE2	UNKNOWN	Imaging Assessment of Diastolic Function
NCT01827059	PHASE2	UNKNOWN	Bosentan In Exercise Induced Pulmonary Arterial Hypertension in CongenitaL Heart diseasE