TEAD4
gene geneOn this page
Also known as TEF-3TEFR-1EFTR-2RTEF-1
Summary
TEAD4 (TEA domain transcription factor 4, HGNC:11717) is a protein-coding gene on chromosome 12p13.33, encoding Transcriptional enhancer factor TEF-3 (Q15561). Transcription factor which plays a key role in the Hippo signaling pathway, a pathway involved in organ size control and tumor suppression by restricting proliferation and promoting apoptosis.
This gene product is a member of the transcriptional enhancer factor (TEF) family of transcription factors, which contain the TEA/ATTS DNA-binding domain. It is preferentially expressed in the skeletal muscle, and binds to the M-CAT regulatory element found in promoters of muscle-specific genes to direct their gene expression. Alternatively spliced transcripts encoding distinct isoforms, some of which are translated through the use of a non-AUG (UUG) initiation codon, have been described for this gene.
Source: NCBI Gene 7004 — RefSeq curated summary.
At a glance
- GWAS associations: 1
- Clinical variants (ClinVar): 82 total
- Druggable target: yes — 3 molecules with ChEMBL bioactivity
- Transcription factor: yes — 14 downstream targets (CollecTRI)
- MANE Select transcript:
NM_003213
Identifiers
Gene identifiers
| Field | Value |
|---|---|
| HGNC ID | HGNC:11717 |
| Approved symbol | TEAD4 |
| Name | TEA domain transcription factor 4 |
| Location | 12p13.33 |
| Locus type | gene with protein product |
| Status | Approved |
| Aliases | TEF-3, TEFR-1, EFTR-2, RTEF-1 |
| Ensembl gene | ENSG00000197905 |
| Ensembl biotype | protein_coding |
| OMIM | 601714 |
| Entrez | 7004 |
Gene structure
Transcript identifiers
Ensembl transcripts: 8 — 7 protein_coding, 1 nonsense_mediated_decay
ENST00000358409, ENST00000359864, ENST00000397122, ENST00000443986, ENST00000536826, ENST00000540314, ENST00000543035, ENST00000544666
RefSeq mRNA: 3 — MANE Select: NM_003213
NM_003213, NM_201441, NM_201443
CCDS: CCDS31729, CCDS31730, CCDS41737
Canonical transcript exons
ENST00000359864 — 13 exons
| Exon | Start | End |
|---|---|---|
| ENSE00001276069 | 3040107 | 3040259 |
| ENSE00001276077 | 3037968 | 3038108 |
| ENSE00001276084 | 3021844 | 3022017 |
| ENSE00001276090 | 3020634 | 3020773 |
| ENSE00001369261 | 2959948 | 2960040 |
| ENSE00001796160 | 2959397 | 2959481 |
| ENSE00002224630 | 2994738 | 2994992 |
| ENSE00002270937 | 3040365 | 3040676 |
| ENSE00003494634 | 3017398 | 3017526 |
| ENSE00003589946 | 3011004 | 3011068 |
| ENSE00003601570 | 3019115 | 3019170 |
| ENSE00003653885 | 3012170 | 3012232 |
| ENSE00003785144 | 3018545 | 3018588 |
Expression profiles
Bgee: expression breadth ubiquitous, 220 present calls, max score 96.21.
FANTOM5 (CAGE): breadth ubiquitous, TPM avg 19.4142 / max 250.6254, expressed in 1534 samples.
FANTOM5 promoters (12 alternative TSS)
| Promoter ID | TPM avg | Samples expressed |
|---|---|---|
| 123462 | 10.0621 | 1428 |
| 123469 | 3.4893 | 1241 |
| 123460 | 2.1819 | 1011 |
| 123461 | 1.6306 | 835 |
| 123463 | 0.4734 | 238 |
| 123467 | 0.4030 | 216 |
| 123464 | 0.3471 | 172 |
| 123459 | 0.3231 | 152 |
| 123468 | 0.2518 | 117 |
| 123466 | 0.1078 | 34 |
Top tissues by expression
283 total, by Bgee expression score (0-100, higher = more expressed):
| Tissue | Anatomy ID | Expression score | Quality |
|---|---|---|---|
| hindlimb stylopod muscle | UBERON:0004252 | 96.21 | gold quality |
| gastrocnemius | UBERON:0001388 | 96.03 | gold quality |
| muscle of leg | UBERON:0001383 | 94.86 | gold quality |
| muscle organ | UBERON:0001630 | 94.22 | gold quality |
| gluteal muscle | UBERON:0002000 | 93.57 | gold quality |
| triceps brachii | UBERON:0001509 | 93.37 | gold quality |
| tibialis anterior | UBERON:0001385 | 92.82 | gold quality |
| quadriceps femoris | UBERON:0001377 | 92.58 | gold quality |
| skeletal muscle tissue | UBERON:0001134 | 92.52 | gold quality |
| vastus lateralis | UBERON:0001379 | 92.35 | gold quality |
| body of pancreas | UBERON:0001150 | 91.81 | gold quality |
| biceps brachii | UBERON:0001507 | 91.47 | gold quality |
| primordial germ cell in gonad | CL:0000670 ∩ UBERON:0000991 | 91.20 | gold quality |
| skeletal muscle tissue of biceps brachii | UBERON:0004502 | 90.24 | gold quality |
| skeletal muscle tissue of rectus abdominis | UBERON:0004511 | 90.19 | gold quality |
| muscle tissue | UBERON:0002385 | 90.01 | gold quality |
| diaphragm | UBERON:0001103 | 89.94 | gold quality |
| deltoid | UBERON:0001476 | 89.08 | gold quality |
| right lobe of thyroid gland | UBERON:0001119 | 88.35 | gold quality |
| right lung | UBERON:0002167 | 88.21 | gold quality |
| left lobe of thyroid gland | UBERON:0001120 | 87.80 | gold quality |
| upper lobe of left lung | UBERON:0008952 | 87.79 | gold quality |
| upper lobe of lung | UBERON:0008948 | 87.19 | gold quality |
| cartilage tissue | UBERON:0002418 | 87.17 | gold quality |
| pancreas | UBERON:0001264 | 86.92 | gold quality |
| thyroid gland | UBERON:0002046 | 86.59 | gold quality |
| tendon of biceps brachii | UBERON:0008188 | 86.21 | gold quality |
| endometrium epithelium | UBERON:0004811 | 85.35 | gold quality |
| sural nerve | UBERON:0015488 | 84.51 | gold quality |
| apex of heart | UBERON:0002098 | 83.94 | gold quality |
Single-cell (SCXA)
Detected in 1 experiment(s), a significant marker in 1.
| Experiment | Marker? | Max mean expression |
|---|---|---|
| E-ANND-3 | yes | 9.12 |
Regulation
Is transcription factor: yes
Downstream targets (CollecTRI)
14 targets.
| Target | Regulation |
|---|---|
| ACTA1 | |
| ADAM2 | |
| CCN2 | Unknown |
| CDX2 | Unknown |
| EIF3K | |
| FGFR1 | Activation |
| HIF1A | Activation |
| IGFBP1 | Activation |
| MYH7 | Activation |
| PPP1CB | Activation |
| S100B | Repression |
| S1PR1 | Activation |
| VEGFA | Repression |
| VEGFB | Unknown |
JASPAR motifs
| Motif | Name | Family |
|---|---|---|
| MA0809.1 | TEAD4 | TEF-1-related factors |
| MA0809.2 | TEAD4 | TEF-1-related factors |
| MA0809.3 | TEAD4 | TEF-1-related factors |
JASPAR matrix evidence (PMIDs): PMID:9571041, PMID:23332764
miRNA regulators (miRDB)
13 targeting TEAD4, 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-6783-3P | 99.89 | 67.92 | 2059 |
| HSA-MIR-1343-3P | 99.89 | 66.78 | 1815 |
| HSA-MIR-4766-5P | 99.75 | 69.23 | 2662 |
| HSA-MIR-6887-3P | 99.66 | 67.83 | 1778 |
| HSA-MIR-6715B-5P | 99.64 | 69.63 | 1420 |
| HSA-MIR-4269 | 99.55 | 69.89 | 1373 |
| HSA-MIR-6839-3P | 99.39 | 68.86 | 1301 |
| HSA-MIR-3940-5P | 99.14 | 65.26 | 493 |
| HSA-MIR-4507 | 99.14 | 65.27 | 515 |
| HSA-MIR-146A-3P | 99.13 | 68.99 | 1881 |
| HSA-MIR-3074-5P | 98.82 | 66.56 | 1414 |
| HSA-MIR-629-5P | 98.78 | 68.72 | 1032 |
| HSA-MIR-6742-3P | 97.95 | 64.50 | 1490 |
Literature-anchored findings (GeneRIF, showing 40)
- Constitutive activation of alpha1-adrenergic signaling through the RTEF-1 transcription factor results in chronic elevation of PP1beta expression and connexin dephosphorylation. This mechanism may underlie some defects in cardiac conduction. (PMID:15520314)
- Novel RTEF-1 transcripts are present within human ocular vascular endothelial cells and mouse neural retina during normal and retinopathy of prematurity development, and alternatively spliced products are produced under hyperoxic and hypoxic conditions (PMID:17652751)
- The gain of function studies indicated that TEA domain family member 4 activate NR5A1 gene expression. (PMID:18579725)
- TEF3 mediates the expression of Down syndrome candidate region 1 isoform 1 (DSCR1-1L) in endothelial cells (PMID:18840614)
- the RTEF-1-driven increase of VEGF-B plays an important role in communication between the endothelium and myocardium (PMID:21169295)
- TEF3, mainly its nuclear localization, is required for VEGF-A(165)-induced endothelial proliferation, migration, tube formation, and in vivo Matrigel angiogenesis. (PMID:21169383)
- RTEF-1 as a regulator of HIF-1alpha transcription (PMID:21540178)
- RTEF-1 plays an important role in FGFR1- stimulated vasodilatation. (PMID:22433836)
- Blocking connexin 43 function inhibited RTEF-1-induced endothelial cell connections and aggregation (PMID:22652601)
- High TEAD4 expression is associated with Age-Related Macular Degeneration. (PMID:22761647)
- These results show that RTEF-1-stimulated IGFBP-1 expression may be central to the mechanism by which RTEF-1 attenuates blood glucose levels. (PMID:22843786)
- These data suggest that TFF3 and survivin expressions play a vital role in gastric cancer development, and these two proteins are important markers for prognosis in gastric cancer. (PMID:22996285)
- Data indicate that knockdown of TEAD1/3/4 induces an almost identical cellular senescent phenotype as YAP silencing. (PMID:23576552)
- convergent optimization of the YAP/TAZ TEAD binding site suggests that the similarity in the affinities of binding of YAP to TEAD and of TAZ to TEAD is important for Hippo pathway functionality. (PMID:23780915)
- the multilevel perturbations of TEAD4 at epigenetic, transcriptional and posttranslational levels may contribute to GC development. (PMID:24325916)
- Edg-1 is a potential target gene of RTEF-1 and is involved in RTEF-1-induced angiogenesis in endothelial cells. (PMID:24520353)
- Our findings suggest that genetic variants of Hippo pathway genes, particularly YAP1 rs11225163, TEAD1 rs7944031 and TEAD4 rs1990330, may independently or jointly modulate survival of CM patients. (PMID:25628125)
- the peptides TEF3-11-66 and TEF3-1197-434 functioned as two independent activation domains, suggesting that N-terminal domain of TEF3-1 also has transcriptional activation capacity (PMID:25687649)
- TEAD4 and KLF5, in collaboration, promoted triple negative breast cancer cell proliferation and tumor growth in part by inhibiting p27 gene transcription (PMID:25970772)
- TAZ negatively regulate transcription of DeltaNp63 through TEAD1,2,3 and 4 transcription factors. (PMID:25995450)
- potential anti-oxidation gene and can prevent H2O2-induced endothelial cell oxidative damage by activating Klotho (PMID:26041389)
- The transcription factor TEAD4 regulates a pro-metastasis transcription program in a YAP-independent manner in CRC, thus providing a novel mechanism of TEAD4 transcriptional regulation and its oncogenic role in CRC, independently of the Hippo pathway. (PMID:26387538)
- TEAD4 overexpression induced p16 in HAoSMCs homozygous for the nonrisk coronary disease allele, but not for the risk allele. (PMID:26487755)
- Tead4 cooperates with AP1 transcription factors to coordinate target gene transcription. (PMID:26832411)
- High TEF3 expression is associated with cell cycle progression and angiogenesis in colon cancer. (PMID:26885617)
- TEAD4, the transcription factor that mediates Hippo-YAP signalling, undergoes alternative splicing facilitated by the tumour suppressor RBM4. (PMID:27291620)
- Our results suggest that TEAD4 plays a role in the pathophysiology of atypical teratoid/rhabdoid tumor, which represents a new insight into the biology of this aggressive tumor (PMID:27966820)
- Hippo pathway transcription factor TEAD4 directly associates with the Wnt pathway transcription factor TCF4 via their DNA-binding domains, forming a complex on target genes. VGLL4 binds to this TEAD4-TCF4 complex to inhibit transactivation of both TCF4 and TEAD4. (PMID:28051067)
- Collectively, these results indicate that human papillomavirus 16 E6 induces upregulation of APOBEC3B through increased levels of TEADs, highlighting the importance of the TEAD-APOBEC3B axis in carcinogenesis. (PMID:28077648)
- It was found that the TEAD4-YAP complex in the nuclei may be related closely to transcriptions of G1 arrest-related genes. (PMID:28315328)
- our work provides a structural basis for understanding the regulatory mechanism of TEAD4-mediated gene transcription (PMID:28368398)
- Combining single site-directed mutagenesis and double mutant analyses, the authors conduct a detailed analysis on the role of several residues located at the YAP:TEAD interface. The results provide quantitative understanding of the interactions taking place at the YAP:TEAD interface and give insights into the formation of the YAP:TEAD complex and more particularly on the interaction between TEAD and the ohm-loop found … (PMID:28430104)
- Osmotic stress promotes TEAD4 cytoplasmic translocation via p38 MAPK in a Hippo-independent manner. Stress-induced TEAD inhibition predominates YAP-activating signals and selectively suppresses YAP-driven cancer cell growth. (PMID:28752853)
- TEAD1 and TEAD4 are oncogenic factors, whose aberrant activation are, in part, mediated by the silence of miR-377-3p, miR-1343-3p and miR-4269. (PMID:28759040)
- Studied the effect of TEAD4 acylation on its interaction with YAP and TAZ; found YAP and TAZ bind in a similar manner to both acylated and non-acylated TEAD4. Also found TEAD4 acylation significantly enhances its stability. (PMID:28960584)
- TEAD4 plays an important tumor-promoting role in colorectal cancer by directly targeting the YAP1. (PMID:29157094)
- TEAD4 is up-regulated in lung adenocarcinoma and its expression is an unfavourable prognostic factor.TEAD4 expression is regulated by miR-6839-3p. (PMID:29667772)
- LOX nuclear localization was significantly associated with poor survival in patients with Colorectal cancer (CRC). Nuclear LOX expression was correlated with synchronous or postoperative lung/hepatic metastasis. LOX may prove to be a potential target gene of YAP and TEAD4. (PMID:29766649)
- To analyze the clinical characteristics, treatment methods and prognosis of renal cell carcinoma associated with Xp11.2 translocation/TFE3 gene fusions (PMID:30392265)
- High TEAD4 expression is associated with Hepatoblastoma. (PMID:30794805)
Cross-species orthologs
3 orthologs
| Organism | Symbol | Gene ID |
|---|---|---|
| mus_musculus | Tead4 | ENSMUSG00000030353 |
| rattus_norvegicus | Tead4 | ENSRNOG00000005608 |
| drosophila_melanogaster | sd | FBGN0003345 |
Paralogs (3): TEAD3 (ENSG00000007866), TEAD2 (ENSG00000074219), TEAD1 (ENSG00000187079)
Protein
Protein identifiers
Transcriptional enhancer factor TEF-3 — Q15561 (reviewed: Q15561)
Alternative names: TEA domain family member 4, Transcription factor 13-like 1, Transcription factor RTEF-1
All UniProt accessions (8): A0A0A0MRF3, Q15561, H0Y7B0, H0YFF9, H0YFK0, H0YG62, H0YGS2, Q53GI4
UniProt curated annotations — full annotation on UniProt →
Function. Transcription factor which plays a key role in the Hippo signaling pathway, a pathway involved in organ size control and tumor suppression by restricting proliferation and promoting apoptosis. The core of this pathway is composed of a kinase cascade wherein MST1/MST2, in complex with its regulatory protein SAV1, phosphorylates and activates LATS1/2 in complex with its regulatory protein MOB1, which in turn phosphorylates and inactivates YAP1 oncoprotein and WWTR1/TAZ. Acts by mediating gene expression of YAP1 and WWTR1/TAZ, thereby regulating cell proliferation, migration and epithelial mesenchymal transition (EMT) induction. Binds specifically and non-cooperatively to the Sph and GT-IIC ’enhansons’ (5’-GTGGAATGT-3’) and activates transcription. Binds to the M-CAT motif.
Subunit / interactions. Interacts with YAP1 and WWTR1/TAZ.
Subcellular location. Nucleus.
Tissue specificity. Preferentially expressed in skeletal muscle. Lower levels in pancreas, placenta, and heart.
Isoforms (3)
| UniProt ID | Names | Canonical? |
|---|---|---|
| Q15561-1 | 1 | yes |
| Q15561-2 | 2 | |
| Q15561-3 | 3 |
RefSeq proteins (3): NP_003204, NP_958849, NP_958851 (=MANE)
Domains & families (InterPro)
| ID | Name | Type |
|---|---|---|
| IPR000818 | TEA/ATTS_dom | Domain |
| IPR016361 | TEF_metazoa | Family |
| IPR027255 | TEF-3 | Family |
| IPR038096 | TEA/ATTS_sf | Homologous_superfamily |
| IPR041086 | YBD | Domain |
| IPR050937 |
Pfam: PF01285, PF17725
UniProt features (54 total): strand 16, helix 12, mutagenesis site 11, sequence conflict 5, region of interest 2, compositionally biased region 2, splice variant 2, chain 1, DNA-binding region 1, turn 1, sequence variant 1
Structure
Experimental structures (PDB)
23 structures.
| PDB | Method | Resolution (Å) |
|---|---|---|
| 9SYN | X-RAY DIFFRACTION | 1.3 |
| 6GEI | X-RAY DIFFRACTION | 1.65 |
| 6HIK | X-RAY DIFFRACTION | 1.65 |
| 6SEN | X-RAY DIFFRACTION | 1.65 |
| 8A8R | X-RAY DIFFRACTION | 1.7 |
| 6GEC | X-RAY DIFFRACTION | 1.7 |
| 9QKQ | X-RAY DIFFRACTION | 1.74 |
| 6GE6 | X-RAY DIFFRACTION | 1.8 |
| 6GE3 | X-RAY DIFFRACTION | 1.85 |
| 5OAQ | X-RAY DIFFRACTION | 1.95 |
| 6GEE | X-RAY DIFFRACTION | 1.96 |
| 6GE4 | X-RAY DIFFRACTION | 1.97 |
| 8CAA | X-RAY DIFFRACTION | 2 |
| 6Q36 | X-RAY DIFFRACTION | 2.01 |
| 6GE5 | X-RAY DIFFRACTION | 2.05 |
| 6Q2X | X-RAY DIFFRACTION | 2.1 |
| 9SYI | X-RAY DIFFRACTION | 2.1 |
| 6GEG | X-RAY DIFFRACTION | 2.23 |
| 8C17 | X-RAY DIFFRACTION | 2.25 |
| 6GEK | X-RAY DIFFRACTION | 2.28 |
| 6SEO | X-RAY DIFFRACTION | 2.55 |
| 5GZB | X-RAY DIFFRACTION | 2.7 |
| 5NO6 | X-RAY DIFFRACTION | 2.88 |
Predicted structure (AlphaFold)
| Model | pLDDT | Fraction very-high |
|---|---|---|
| AF-Q15561-F1 | 76.75 | 0.50 |
Functional residue map
Curated UniProt residues grouped by drug-discovery relevance — catalytic, ligand-binding, modification, and mutation-validated positions. Source: UniProtKB sequence features.
Mutagenesis-validated functional residues (11):
| Position | Phenotype |
|---|---|
| 297 | important loss of interaction with yap1 and complete loss of transforming ability. |
| 299 | important loss of interaction with yap1 and complete loss of transforming ability. |
| 337 | reduced interaction with yap1. |
| 373 | reduced transforming ability. |
| 380 | reduced transforming ability. |
| 391 | reduced transforming ability. |
| 393 | reduced transforming ability. |
| 427 | reduced transforming ability. |
| 429 | loss of interaction with yap1 and also activation by yap1. |
| 429 | important loss of interaction with yap1 and complete loss of transforming ability. |
| 266 | reduced transforming ability. |
Function
Pathways and Gene Ontology
Reactome pathways
12 pathways
| ID | Pathway |
|---|---|
| R-HSA-2032785 | YAP1- and WWTR1 (TAZ)-stimulated gene expression |
| R-HSA-8951671 | RUNX3 regulates YAP1-mediated transcription |
| R-HSA-9796292 | Formation of axial mesoderm |
| R-HSA-9819196 | Zygotic genome activation (ZGA) |
| R-HSA-9909649 | Regulation of PD-L1(CD274) transcription |
| R-HSA-1266738 | Developmental Biology |
| R-HSA-212436 | Generic Transcription Pathway |
| R-HSA-73857 | RNA Polymerase II Transcription |
| R-HSA-74160 | Gene expression (Transcription) |
| R-HSA-8878159 | Transcriptional regulation by RUNX3 |
| R-HSA-9758941 | Gastrulation |
| R-HSA-9816359 | Maternal to zygotic transition (MZT) |
MSigDB gene sets: 171 (showing top):
GOBP_EMBRYO_DEVELOPMENT_ENDING_IN_BIRTH_OR_EGG_HATCHING, MYOGENIN_Q6, REACTOME_ADAPTIVE_IMMUNE_SYSTEM, GOBP_SKELETAL_SYSTEM_DEVELOPMENT, GRAESSMANN_APOPTOSIS_BY_SERUM_DEPRIVATION_UP, GOBP_HIPPO_SIGNALING, GOBP_BLASTOCYST_FORMATION, WEI_MYCN_TARGETS_WITH_E_BOX, DAUER_STAT3_TARGETS_UP, CREIGHTON_ENDOCRINE_THERAPY_RESISTANCE_1, GOBP_IN_UTERO_EMBRYONIC_DEVELOPMENT, GOBP_MUSCLE_STRUCTURE_DEVELOPMENT, WOO_LIVER_CANCER_RECURRENCE_UP, KORKOLA_EMBRYONAL_CARCINOMA_UP, BILD_E2F3_ONCOGENIC_SIGNATURE
GO Biological Process (16): skeletal system development (GO:0001501), cell fate specification (GO:0001708), trophectodermal cell fate commitment (GO:0001830), DNA-templated transcription (GO:0006351), regulation of transcription by RNA polymerase II (GO:0006357), muscle organ development (GO:0007517), embryo implantation (GO:0007566), hippo signaling (GO:0035329), embryonic organ development (GO:0048568), positive regulation of stem cell population maintenance (GO:1902459), in utero embryonic development (GO:0001701), blastocyst formation (GO:0001825), regulation of DNA-templated transcription (GO:0006355), cell fate commitment (GO:0045165), positive regulation of DNA-templated transcription (GO:0045893), positive regulation of transcription by RNA polymerase II (GO:0045944)
GO Molecular Function (7): RNA polymerase II cis-regulatory region sequence-specific DNA binding (GO:0000978), DNA-binding transcription factor activity, RNA polymerase II-specific (GO:0000981), DNA-binding transcription activator activity, RNA polymerase II-specific (GO:0001228), DNA-binding transcription factor activity (GO:0003700), DNA binding (GO:0003677), protein binding (GO:0005515), sequence-specific DNA binding (GO:0043565)
GO Cellular Component (6): chromatin (GO:0000785), nucleus (GO:0005634), nucleoplasm (GO:0005654), transcription regulator complex (GO:0005667), cytoplasm (GO:0005737), protein-DNA complex (GO:0032993)
Reactome top-level categories
Rollup of top-8 pathways:
| Category | Pathways |
|---|---|
| Generic Transcription Pathway | 2 |
| Developmental Biology | 2 |
| Transcriptional regulation by RUNX3 | 1 |
| Gastrulation | 1 |
| Maternal to zygotic transition (MZT) | 1 |
| Regulation of PD-L1(CD274) expression | 1 |
| RNA Polymerase II Transcription | 1 |
| Gene expression (Transcription) | 1 |
GO top-level categories
Rollup of top GO terms by namespace:
| Category | Terms |
|---|---|
| regulation of DNA-templated transcription | 3 |
| RNA polymerase II transcription regulatory region sequence-specific DNA binding | 3 |
| cellular anatomical structure | 3 |
| cell fate commitment | 2 |
| cellular developmental process | 2 |
| transcription by RNA polymerase II | 2 |
| animal organ development | 2 |
| DNA-templated transcription | 2 |
| regulation of transcription by RNA polymerase II | 2 |
| protein-containing complex | 2 |
| system development | 1 |
| trophectodermal cell differentiation | 1 |
| gene expression | 1 |
| RNA biosynthetic process | 1 |
| muscle structure development | 1 |
| multicellular organism development | 1 |
| female pregnancy | 1 |
| reproductive process | 1 |
| intracellular signal transduction | 1 |
| embryo development | 1 |
| stem cell population maintenance | 1 |
| positive regulation of developmental process | 1 |
| positive regulation of multicellular organismal process | 1 |
| regulation of stem cell population maintenance | 1 |
| chordate embryonic development | 1 |
| blastocyst development | 1 |
| anatomical structure formation involved in morphogenesis | 1 |
| regulation of gene expression | 1 |
| regulation of RNA biosynthetic process | 1 |
| cell differentiation | 1 |
| positive regulation of RNA biosynthetic process | 1 |
| positive regulation of DNA-templated transcription | 1 |
| cis-regulatory region sequence-specific DNA binding | 1 |
| chromatin | 1 |
| DNA-binding transcription factor activity | 1 |
| DNA-binding transcription factor activity, RNA polymerase II-specific | 1 |
| DNA-binding transcription activator activity | 1 |
| positive regulation of transcription by RNA polymerase II | 1 |
| transcription cis-regulatory region binding | 1 |
| transcription regulator activity | 1 |
Protein interactions and networks
STRING
2086 interactions, top by confidence (×1000):
| Protein A | Protein B | Partner UniProt | Score |
|---|---|---|---|
| TEAD4 | YAP1 | P46937 | 992 |
| TEAD4 | MCAT | Q8IVS2 | 885 |
| TEAD4 | VGLL4 | Q14135 | 881 |
| TEAD4 | VGLL1 | Q99990 | 879 |
| TEAD4 | EP300 | Q09472 | 844 |
| TEAD4 | SMAD3 | P84022 | 802 |
| TEAD4 | CDX2 | Q99626 | 799 |
| TEAD4 | WWTR1 | Q9GZV5 | 786 |
| TEAD4 | ELF5 | Q9UKW6 | 734 |
| TEAD4 | GATA3 | P23771 | 709 |
| TEAD4 | LATS1 | O95835 | 708 |
| TEAD4 | POU5F1 | P31359 | 705 |
| TEAD4 | EOMES | O95936 | 663 |
| TEAD4 | VGLL3 | A8MV65 | 660 |
| TEAD4 | LATS2 | Q9NRM7 | 650 |
IntAct
181 interactions, top by confidence:
| A | B | Type | Score |
|---|---|---|---|
| YAP1 | TEAD4 | psi-mi:“MI:0915”(physical association) | 0.930 |
| TEAD4 | YAP1 | psi-mi:“MI:0407”(direct interaction) | 0.930 |
| TEAD4 | YAP1 | psi-mi:“MI:0914”(association) | 0.930 |
| YAP1 | TEAD4 | psi-mi:“MI:0407”(direct interaction) | 0.930 |
| TEAD4 | WWTR1 | psi-mi:“MI:0915”(physical association) | 0.920 |
| VGLL4 | TEAD4 | psi-mi:“MI:0407”(direct interaction) | 0.760 |
| TEAD4 | VGLL4 | psi-mi:“MI:0915”(physical association) | 0.760 |
| TEAD4 | CEP55 | psi-mi:“MI:0915”(physical association) | 0.740 |
| TEAD4 | TRIM27 | psi-mi:“MI:0915”(physical association) | 0.720 |
| TEAD4 | TRAF1 | psi-mi:“MI:0915”(physical association) | 0.720 |
| TEAD4 | KRT40 | psi-mi:“MI:0915”(physical association) | 0.720 |
| TEAD4 | GOLGA2 | psi-mi:“MI:0915”(physical association) | 0.720 |
| TEAD4 | MTUS2 | psi-mi:“MI:0915”(physical association) | 0.720 |
BioGRID (165): TEAD4 (Two-hybrid), TEAD4 (Two-hybrid), TEAD4 (Two-hybrid), TRAF1 (Two-hybrid), PNMA1 (Two-hybrid), KIAA0753 (Two-hybrid), CCNDBP1 (Two-hybrid), RABGEF1 (Two-hybrid), CEP55 (Two-hybrid), CEP70 (Two-hybrid), LZTS2 (Two-hybrid), SSX2IP (Two-hybrid), CCDC172 (Two-hybrid), TEAD4 (Affinity Capture-MS), AMOTL1 (Affinity Capture-MS)
ESM2 similar proteins: B5DF93, D2HNW6, O14896, P52633, P56477, P70671, P97431, Q08DD6, Q13568, Q14653, Q15561, Q15562, Q1JPG0, Q3B7M3, Q3TC46, Q3ZBK7, Q4JF28, Q4KLN4, Q53GS7, Q58DJ0, Q5DTY9, Q5R8Q4, Q5RAS2, Q62717, Q68DU8, Q6A0A9, Q6DEZ2, Q6NUQ4, Q7L4E1, Q86TB9, Q86UW7, Q86UW9, Q8AVJ1, Q8BK03, Q8BYR5, Q8CDG3, Q8CF97, Q8CID0, Q8HWS3, Q8IY22
Diamond homologs: A0A0A7HMS2, B6H7F3, C0STD9, E9EMI7, E9RD40, I1S4T3, K9GDC6, P18412, P20945, P28347, P30051, P30052, P48301, P48984, P70210, Q15561, Q15562, Q19849, Q2U9L6, Q5ANJ4, Q62296, Q90701, Q99594, W6PQG8, Q25214
SIGNOR signaling
4 interactions.
| A | Effect | B | Mechanism |
|---|---|---|---|
| WWTR1 | up-regulates | TEAD4 | binding |
| YAP1 | up-regulates | TEAD4 | binding |
| YAP1 | “up-regulates activity” | TEAD4 | binding |
| TEAD4 | “up-regulates quantity by expression” | CCN2 | “transcriptional regulation” |
Disease & clinical
Clinical variants and AI predictions
ClinVar
82 variants total. Per-class counts are floors (≥ shown; pagination cap):
| Classification | Count (floor) |
|---|---|
| Pathogenic | 0 |
| Likely pathogenic | 0 |
| Uncertain significance | 65 |
| Likely benign | 4 |
| Benign | 0 |
Top pathogenic / likely-pathogenic (0)
SpliceAI
3139 predictions. Top by Δscore:
| Variant | Effect | Δscore |
|---|---|---|
| 12:2994988:GTATG:G | donor_gain | 1.0000 |
| 12:2994990:ATGGT:A | donor_loss | 1.0000 |
| 12:2994991:TGGT:T | donor_loss | 1.0000 |
| 12:2994992:GGT:G | donor_loss | 1.0000 |
| 12:2994993:GT:G | donor_loss | 1.0000 |
| 12:2994994:T:A | donor_loss | 1.0000 |
| 12:3011062:G:GT | donor_gain | 1.0000 |
| 12:3012229:AAAGG:A | donor_loss | 1.0000 |
| 12:3012231:AGGTA:A | donor_loss | 1.0000 |
| 12:3012234:T:A | donor_loss | 1.0000 |
| 12:3014410:G:T | donor_gain | 1.0000 |
| 12:3017523:AGGGG:A | donor_loss | 1.0000 |
| 12:3017524:GGG:G | donor_gain | 1.0000 |
| 12:3017525:GGG:G | donor_gain | 1.0000 |
| 12:3017527:GTAA:G | donor_loss | 1.0000 |
| 12:3017528:T:TC | donor_loss | 1.0000 |
| 12:3018543:A:AG | acceptor_gain | 1.0000 |
| 12:3018544:G:GG | acceptor_gain | 1.0000 |
| 12:3018544:GTTTT:G | acceptor_gain | 1.0000 |
| 12:3018587:GA:G | donor_gain | 1.0000 |
| 12:3018589:G:GG | donor_gain | 1.0000 |
| 12:3019113:A:AG | acceptor_gain | 1.0000 |
| 12:3019114:G:GG | acceptor_gain | 1.0000 |
| 12:3020632:AG:A | acceptor_gain | 1.0000 |
| 12:3020633:GG:G | acceptor_gain | 1.0000 |
| 12:3020633:GGGTT:G | acceptor_gain | 1.0000 |
| 12:3020772:CGG:C | donor_loss | 1.0000 |
| 12:3020774:G:GG | donor_gain | 1.0000 |
| 12:3020775:T:G | donor_loss | 1.0000 |
| 12:3021826:GACCC:G | acceptor_gain | 1.0000 |
AlphaMissense
2871 scored. Top likely-pathogenic:
| Variant | Protein change | am_pathogenicity |
|---|---|---|
| 12:2994893:T:A | W43R | 1.000 |
| 12:2994893:T:C | W43R | 1.000 |
| 12:2994894:G:C | W43S | 1.000 |
| 12:2994895:G:C | W43C | 1.000 |
| 12:2994895:G:T | W43C | 1.000 |
| 12:2994917:T:C | F51L | 1.000 |
| 12:2994918:T:C | F51S | 1.000 |
| 12:2994918:T:G | F51C | 1.000 |
| 12:2994919:C:A | F51L | 1.000 |
| 12:2994919:C:G | F51L | 1.000 |
| 12:2994926:G:C | A54P | 1.000 |
| 12:2994927:C:A | A54D | 1.000 |
| 12:2994930:T:C | L55P | 1.000 |
| 12:2994938:T:C | Y58H | 1.000 |
| 12:2994938:T:G | Y58D | 1.000 |
| 12:2994947:T:C | C61R | 1.000 |
| 12:2994948:G:A | C61Y | 1.000 |
| 12:2994949:T:G | C61W | 1.000 |
| 12:2994950:G:C | G62R | 1.000 |
| 12:2994950:G:T | G62C | 1.000 |
| 12:2994951:G:A | G62D | 1.000 |
| 12:2994951:G:T | G62V | 1.000 |
| 12:2994953:A:G | R63G | 1.000 |
| 12:2994953:A:T | R63W | 1.000 |
| 12:2994954:G:C | R63T | 1.000 |
| 12:2994954:G:T | R63M | 1.000 |
| 12:2994955:G:C | R63S | 1.000 |
| 12:2994955:G:T | R63S | 1.000 |
| 12:2994956:C:A | R64S | 1.000 |
| 12:2994956:C:T | R64C | 1.000 |
dbSNP variants (sampled 300 via entrez): RS1000012605 (12:2999293 C>G,T), RS1000128262 (12:3039217 A>G), RS1000140991 (12:2969344 G>A,T), RS1000142410 (12:3026988 C>T), RS1000148523 (12:2974056 G>A,C), RS1000175200 (12:2957552 C>G,T), RS1000177089 (12:3027193 A>G), RS1000190431 (12:3013297 C>G,T), RS1000205431 (12:2993842 C>A,T), RS1000232996 (12:2988393 C>T), RS1000274526 (12:2968232 A>G,T), RS1000286702 (12:2988669 A>G), RS1000287189 (12:3021606 C>T), RS1000313874 (12:3004237 G>A), RS1000410583 (12:3016162 G>T)
Disease associations
OMIM: gene MIM:601714 | disease phenotypes:
GenCC curated gene-disease
Mondo (0):
Orphanet (0):
HPO phenotypes
0 total (0 of 0 shown, HPO-id order):
GWAS associations
1 associations (top):
| Study | Trait | p-value |
|---|---|---|
| GCST001909_3 | Narcolepsy with cataplexy | 2.000000e-07 |
Drugs & pharmacology
Drug and pharmacology data
Is drug target: yes
ChEMBL targets (5): CHEMBL4295828 (SINGLE PROTEIN), CHEMBL5465250 (PROTEIN COMPLEX), CHEMBL6066038 (PROTEIN-PROTEIN INTERACTION), CHEMBL6193819 (PROTEIN-PROTEIN INTERACTION), CHEMBL6195574 (PROTEIN-PROTEIN INTERACTION)
Molecules with ChEMBL bioactivity
3 molecules (phase ≥1), by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 51,894 (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 |
|---|---|---|---|
| CHEMBL23588 | FLUFENAMIC ACID | 2 | 34,797 |
| CHEMBL32350 | PIRLINDOLE | 2 | 1,928 |
| CHEMBL63323 | NIFLUMIC ACID | 2 | 15,169 |
PharmGKB: 1 entry (VIP=true, CPIC=false)
GtoPdb / IUPHAR curated pharmacology
(IUPHAR/BPS Guide to Pharmacology — expert-curated)
Target class: other protein — TEAD (transcriptional enhanced associate domain) transcription factors
Most potent curated ligand interactions (1 total), top 1:
| Ligand | Action | Affinity | Parameter |
|---|---|---|---|
| GNE-7883 | Binding | 7.52 | pIC50 |
Binding affinities (BindingDB)
104 measured of 110 human assays (110 total across all organisms); most potent 50 below. Values come from heterogeneous assays and are not directly comparable.
| Ligand | Measure | Value | Patent |
|---|---|---|---|
| US12083101, Example 71b | IC50 | 1 nM | US-12083101: Biaryl derivatives as YAP/TAZ-TEAD protein-protein interaction inhibitors |
| US12083101, Example 110 | IC50 | 1 nM | US-12083101: Biaryl derivatives as YAP/TAZ-TEAD protein-protein interaction inhibitors |
| US12083101, Example 112 | IC50 | 1 nM | US-12083101: Biaryl derivatives as YAP/TAZ-TEAD protein-protein interaction inhibitors |
| US12083101, Example 147 | IC50 | 1 nM | US-12083101: Biaryl derivatives as YAP/TAZ-TEAD protein-protein interaction inhibitors |
| US12083101, Example 170 | IC50 | 1 nM | US-12083101: Biaryl derivatives as YAP/TAZ-TEAD protein-protein interaction inhibitors |
| US12083101, Example 12 | IC50 | 1.5 nM | US-12083101: Biaryl derivatives as YAP/TAZ-TEAD protein-protein interaction inhibitors |
| US12083101, Example 38 | IC50 | 2 nM | US-12083101: Biaryl derivatives as YAP/TAZ-TEAD protein-protein interaction inhibitors |
| US12083101, Example 56b | IC50 | 2 nM | US-12083101: Biaryl derivatives as YAP/TAZ-TEAD protein-protein interaction inhibitors |
| US12083101, Example 66a | IC50 | 2 nM | US-12083101: Biaryl derivatives as YAP/TAZ-TEAD protein-protein interaction inhibitors |
| US12083101, Example 66b | IC50 | 2 nM | US-12083101: Biaryl derivatives as YAP/TAZ-TEAD protein-protein interaction inhibitors |
| US12083101, Example 67a | IC50 | 2 nM | US-12083101: Biaryl derivatives as YAP/TAZ-TEAD protein-protein interaction inhibitors |
| US12083101, Example 71a | IC50 | 2 nM | US-12083101: Biaryl derivatives as YAP/TAZ-TEAD protein-protein interaction inhibitors |
| US12083101, Example 94a | IC50 | 2 nM | US-12083101: Biaryl derivatives as YAP/TAZ-TEAD protein-protein interaction inhibitors |
| US12083101, Example 99 | IC50 | 2 nM | US-12083101: Biaryl derivatives as YAP/TAZ-TEAD protein-protein interaction inhibitors |
| US12083101, Example 100a | IC50 | 2 nM | US-12083101: Biaryl derivatives as YAP/TAZ-TEAD protein-protein interaction inhibitors |
| US12083101, Example 104b | IC50 | 2 nM | US-12083101: Biaryl derivatives as YAP/TAZ-TEAD protein-protein interaction inhibitors |
| US12083101, Example 108 | IC50 | 2 nM | US-12083101: Biaryl derivatives as YAP/TAZ-TEAD protein-protein interaction inhibitors |
| US12083101, Example 113 | IC50 | 2 nM | US-12083101: Biaryl derivatives as YAP/TAZ-TEAD protein-protein interaction inhibitors |
| US12083101, Example 115a | IC50 | 2 nM | US-12083101: Biaryl derivatives as YAP/TAZ-TEAD protein-protein interaction inhibitors |
| US12083101, Example 115b | IC50 | 2 nM | US-12083101: Biaryl derivatives as YAP/TAZ-TEAD protein-protein interaction inhibitors |
| US12083101, Example 121 | IC50 | 2 nM | US-12083101: Biaryl derivatives as YAP/TAZ-TEAD protein-protein interaction inhibitors |
| US12083101, Example 126 | IC50 | 2 nM | US-12083101: Biaryl derivatives as YAP/TAZ-TEAD protein-protein interaction inhibitors |
| US12083101, Example 151 | IC50 | 2 nM | US-12083101: Biaryl derivatives as YAP/TAZ-TEAD protein-protein interaction inhibitors |
| US12083101, Example 152 | IC50 | 2 nM | US-12083101: Biaryl derivatives as YAP/TAZ-TEAD protein-protein interaction inhibitors |
| US12083101, Example 171 | IC50 | 2 nM | US-12083101: Biaryl derivatives as YAP/TAZ-TEAD protein-protein interaction inhibitors |
| US12083101, Example 31 | IC50 | 3 nM | US-12083101: Biaryl derivatives as YAP/TAZ-TEAD protein-protein interaction inhibitors |
| US12083101, Example 33 | IC50 | 3 nM | US-12083101: Biaryl derivatives as YAP/TAZ-TEAD protein-protein interaction inhibitors |
| US12083101, Example 51 | IC50 | 3 nM | US-12083101: Biaryl derivatives as YAP/TAZ-TEAD protein-protein interaction inhibitors |
| US12083101, Example 57b | IC50 | 3 nM | US-12083101: Biaryl derivatives as YAP/TAZ-TEAD protein-protein interaction inhibitors |
| US12083101, Example 86 | IC50 | 3 nM | US-12083101: Biaryl derivatives as YAP/TAZ-TEAD protein-protein interaction inhibitors |
| US12083101, Example 94b | IC50 | 3 nM | US-12083101: Biaryl derivatives as YAP/TAZ-TEAD protein-protein interaction inhibitors |
| US12083101, Example 102a | IC50 | 3 nM | US-12083101: Biaryl derivatives as YAP/TAZ-TEAD protein-protein interaction inhibitors |
| US12083101, Example 120 | IC50 | 3 nM | US-12083101: Biaryl derivatives as YAP/TAZ-TEAD protein-protein interaction inhibitors |
| US12083101, Example 143 | IC50 | 3 nM | US-12083101: Biaryl derivatives as YAP/TAZ-TEAD protein-protein interaction inhibitors |
| US12083101, Example 146 | IC50 | 3 nM | US-12083101: Biaryl derivatives as YAP/TAZ-TEAD protein-protein interaction inhibitors |
| US12083101, Example 8 | IC50 | 4 nM | US-12083101: Biaryl derivatives as YAP/TAZ-TEAD protein-protein interaction inhibitors |
| US12083101, Example 58b | IC50 | 4 nM | US-12083101: Biaryl derivatives as YAP/TAZ-TEAD protein-protein interaction inhibitors |
| US12083101, Example 69b | IC50 | 4 nM | US-12083101: Biaryl derivatives as YAP/TAZ-TEAD protein-protein interaction inhibitors |
| US12083101, Example 85a | IC50 | 4 nM | US-12083101: Biaryl derivatives as YAP/TAZ-TEAD protein-protein interaction inhibitors |
| US12083101, Example 97 | IC50 | 4 nM | US-12083101: Biaryl derivatives as YAP/TAZ-TEAD protein-protein interaction inhibitors |
| US12083101, Example 111 | IC50 | 4 nM | US-12083101: Biaryl derivatives as YAP/TAZ-TEAD protein-protein interaction inhibitors |
| US12083101, Example 140a | IC50 | 4 nM | US-12083101: Biaryl derivatives as YAP/TAZ-TEAD protein-protein interaction inhibitors |
| US12083101, Example 150 | IC50 | 4 nM | US-12083101: Biaryl derivatives as YAP/TAZ-TEAD protein-protein interaction inhibitors |
| US12083101, Example 164 | IC50 | 4 nM | US-12083101: Biaryl derivatives as YAP/TAZ-TEAD protein-protein interaction inhibitors |
| US12083101, Example 49 | IC50 | 5 nM | US-12083101: Biaryl derivatives as YAP/TAZ-TEAD protein-protein interaction inhibitors |
| US12083101, Example 69a | IC50 | 5 nM | US-12083101: Biaryl derivatives as YAP/TAZ-TEAD protein-protein interaction inhibitors |
| US12083101, Example 96 | IC50 | 5 nM | US-12083101: Biaryl derivatives as YAP/TAZ-TEAD protein-protein interaction inhibitors |
| US12083101, Example 98 | IC50 | 5 nM | US-12083101: Biaryl derivatives as YAP/TAZ-TEAD protein-protein interaction inhibitors |
| US12083101, Example 103 | IC50 | 5 nM | US-12083101: Biaryl derivatives as YAP/TAZ-TEAD protein-protein interaction inhibitors |
| US12083101, Example 141 | IC50 | 5 nM | US-12083101: Biaryl derivatives as YAP/TAZ-TEAD protein-protein interaction inhibitors |
ChEMBL bioactivities
121 potent at pChembl≥5 of 177 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).
PubChem BioAssay actives
122 with measured affinity, of 591 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 |
|---|---|---|---|---|
| 2-[(2S,3S)-5-chloro-6-fluoro-3-methyl-2-(methylaminomethyl)-2-phenyl-3H-1-benzofuran-4-yl]-3-fluoro-4-methoxybenzamide | 2007263: Inhibition of Avi-His-tagged human TEAD4 (217 to 434 residues)/N-biotinylated-N-terminal Cy5-labelled human YAP (60 to 100 residues) incubated for 1 hr by TR FRET assay | ic50 | 0.0020 | uM |
| 2-[(2S,3S)-2-(aminomethyl)-5-chloro-6-fluoro-3-methyl-2-phenyl-3H-1-benzofuran-4-yl]-3-fluoro-4-(2-methoxyethoxy)benzamide | 2007263: Inhibition of Avi-His-tagged human TEAD4 (217 to 434 residues)/N-biotinylated-N-terminal Cy5-labelled human YAP (60 to 100 residues) incubated for 1 hr by TR FRET assay | ic50 | 0.0020 | uM |
| N-[[4-(hydroxymethyl)-1-[4-(trifluoromethoxy)phenyl]pyrazolo[3,4-b]pyridin-3-yl]methyl]prop-2-ynamide | 2020151: Inhibition of His-tagged TEAD4 (unknown origin) preincubated for 0.5 to 4 hrs followed by biotinylated lipid pocket probe addition and measured after 60 min by TR-FRET assay | ic50 | 0.0020 | uM |
| 2-chloro-N-[[4-(hydroxymethyl)-1-[4-(trifluoromethoxy)phenyl]pyrazolo[3,4-b]pyridin-3-yl]methyl]prop-2-enamide | 2020151: Inhibition of His-tagged TEAD4 (unknown origin) preincubated for 0.5 to 4 hrs followed by biotinylated lipid pocket probe addition and measured after 60 min by TR-FRET assay | ic50 | 0.0020 | uM |
| cyclobuten-1-yl-[3-[9-methyl-6-[4-(trifluoromethoxy)phenyl]purin-2-yl]azetidin-1-yl]methanone | 2015512: Displacement of biotinylated lipid pocket probes from His-tagged TEAD4 (unknown origin) preincubated for 4 hrs followed by lipid pocket probe addition and measured after 60 mins by TR-FRET assay | ic50 | 0.0020 | uM |
| 1-[3-[7-[4-(trifluoromethoxy)phenyl]-[1,3]thiazolo[5,4-d]pyrimidin-5-yl]azetidin-1-yl]prop-2-en-1-one | 2015512: Displacement of biotinylated lipid pocket probes from His-tagged TEAD4 (unknown origin) preincubated for 4 hrs followed by lipid pocket probe addition and measured after 60 mins by TR-FRET assay | ic50 | 0.0020 | uM |
| 1-[3-[9-methyl-6-[4-(trifluoromethoxy)phenyl]purin-2-yl]azetidin-1-yl]prop-2-en-1-one | 2015512: Displacement of biotinylated lipid pocket probes from His-tagged TEAD4 (unknown origin) preincubated for 4 hrs followed by lipid pocket probe addition and measured after 60 mins by TR-FRET assay | ic50 | 0.0020 | uM |
| 2-[(2S,3R)-2-(aminomethyl)-5-chloro-6-fluoro-3-(hydroxymethyl)-2-phenyl-3H-1-benzofuran-4-yl]-3-fluoro-4-methoxybenzamide | 2007263: Inhibition of Avi-His-tagged human TEAD4 (217 to 434 residues)/N-biotinylated-N-terminal Cy5-labelled human YAP (60 to 100 residues) incubated for 1 hr by TR FRET assay | ic50 | 0.0020 | uM |
| 2-chloro-N-methyl-N-[[1-[4-(trifluoromethoxy)phenyl]indazol-3-yl]methyl]acetamide | 2020151: Inhibition of His-tagged TEAD4 (unknown origin) preincubated for 0.5 to 4 hrs followed by biotinylated lipid pocket probe addition and measured after 60 min by TR-FRET assay | ic50 | 0.0030 | uM |
| (E)-1-[3-[4-chloro-1-[4-(trifluoromethoxy)phenyl]pyrazolo[3,4-b]pyridin-3-yl]azetidin-1-yl]-4-hydroxybut-2-en-1-one | 2020151: Inhibition of His-tagged TEAD4 (unknown origin) preincubated for 0.5 to 4 hrs followed by biotinylated lipid pocket probe addition and measured after 60 min by TR-FRET assay | ic50 | 0.0030 | uM |
| 1-[3-[4-(hydroxymethyl)-1-[4-(trifluoromethoxy)phenyl]pyrazolo[3,4-b]pyridin-3-yl]azetidin-1-yl]prop-2-en-1-one | 2020151: Inhibition of His-tagged TEAD4 (unknown origin) preincubated for 0.5 to 4 hrs followed by biotinylated lipid pocket probe addition and measured after 60 min by TR-FRET assay | ic50 | 0.0030 | uM |
| N-[[4-(hydroxymethyl)-7-[4-(trifluoromethoxy)phenyl]-2,3-dihydro-1-benzofuran-5-yl]methyl]ethenesulfonamide | 2015512: Displacement of biotinylated lipid pocket probes from His-tagged TEAD4 (unknown origin) preincubated for 4 hrs followed by lipid pocket probe addition and measured after 60 mins by TR-FRET assay | ic50 | 0.0030 | uM |
| N-[[4-(3-hydroxyprop-1-ynyl)-3-methyl-7-[4-(trifluoromethoxy)phenyl]benzimidazol-5-yl]methyl]prop-2-enamide | 2015512: Displacement of biotinylated lipid pocket probes from His-tagged TEAD4 (unknown origin) preincubated for 4 hrs followed by lipid pocket probe addition and measured after 60 mins by TR-FRET assay | ic50 | 0.0030 | uM |
| N-[[4-(hydroxymethyl)-7-[4-(trifluoromethoxy)phenyl]-2,3-dihydro-1-benzofuran-5-yl]methyl]-N-methylprop-2-enamide | 2015512: Displacement of biotinylated lipid pocket probes from His-tagged TEAD4 (unknown origin) preincubated for 4 hrs followed by lipid pocket probe addition and measured after 60 mins by TR-FRET assay | ic50 | 0.0030 | uM |
| (2S)-1-[(2S)-2-[[(2S)-6-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S,4R)-1-[(2S)-2-[[(2S)-6-amino-2-[[(2S)-5-carbamimidamido-2-[[1-[[(2S)-5-carbamimidamido-2-[[(2S)-3-(6-chloro-1H-indol-3-yl)-2-[[(2S)-pyrrolidine-2-carbonyl]amino]propanoyl]amino]pentanoyl]amino]cyclopropanecarbonyl]amino]pentanoyl]amino]hexanoyl]amino]-3-cyclobutylpropanoyl]-4-hydroxypyrrolidine-2-carbonyl]amino]-3-carboxypropanoyl]amino]-3-hydroxypropanoyl]amino]-3-phenylpropanoyl]amino]-3-naphthalen-1-ylpropanoyl]amino]hexanoyl]amino]-4-carboxybutanoyl]pyrrolidine-2-carboxylic acid | 1634096: Inhibition of human TEAD4 (217 to 434 residues) expressed in Escherichia coli BL21 (DE3) interaction with N-biotinylated YAP (60 to 100 residues) incubated for 2 hrs by by TR-FRET assay | ic50 | 0.0090 | uM |
| 1-[3-[4-ethynyl-1-[4-(trifluoromethoxy)phenyl]pyrazolo[3,4-b]pyridin-3-yl]azetidin-1-yl]prop-2-en-1-one | 2020151: Inhibition of His-tagged TEAD4 (unknown origin) preincubated for 0.5 to 4 hrs followed by biotinylated lipid pocket probe addition and measured after 60 min by TR-FRET assay | ic50 | 0.0090 | uM |
| (2S)-1-[(2S)-2-[[(2S)-6-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S,4R)-1-[(2S)-2-[[(2S)-6-amino-2-[[(2S)-5-carbamimidamido-2-[[(2S)-2-[[(2S)-5-carbamimidamido-2-[[(2S)-3-(6-chloro-1H-indol-3-yl)-2-[[(2S)-pyrrolidine-2-carbonyl]amino]propanoyl]amino]pentanoyl]amino]-4-methylpentanoyl]amino]pentanoyl]amino]hexanoyl]amino]-3-cyclobutylpropanoyl]-4-hydroxypyrrolidine-2-carbonyl]amino]-3-carboxypropanoyl]amino]-3-hydroxypropanoyl]amino]-3-phenylpropanoyl]amino]-3-naphthalen-1-ylpropanoyl]amino]hexanoyl]amino]-4-carboxybutanoyl]pyrrolidine-2-carboxylic acid | 1634096: Inhibition of human TEAD4 (217 to 434 residues) expressed in Escherichia coli BL21 (DE3) interaction with N-biotinylated YAP (60 to 100 residues) incubated for 2 hrs by by TR-FRET assay | ic50 | 0.0160 | uM |
| (2S)-1-[(2S)-2-[[(2S)-6-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-1-[(2S)-2-[[(2S)-6-amino-2-[[(2S)-5-carbamimidamido-2-[[(2S)-2-[[(2S)-5-carbamimidamido-2-[[(2S)-3-(6-chloro-1H-indol-3-yl)-2-[[(2S)-pyrrolidine-2-carbonyl]amino]propanoyl]amino]pentanoyl]amino]-4-methylpentanoyl]amino]pentanoyl]amino]hexanoyl]amino]-3-cyclobutylpropanoyl]pyrrolidine-2-carbonyl]amino]-3-carboxypropanoyl]amino]-3-hydroxypropanoyl]amino]-3-phenylpropanoyl]amino]-3-naphthalen-1-ylpropanoyl]amino]hexanoyl]amino]-4-carboxybutanoyl]pyrrolidine-2-carboxylic acid | 1634096: Inhibition of human TEAD4 (217 to 434 residues) expressed in Escherichia coli BL21 (DE3) interaction with N-biotinylated YAP (60 to 100 residues) incubated for 2 hrs by by TR-FRET assay | ic50 | 0.0450 | uM |
| (2S)-1-[(2S)-1-[(2S)-6-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-1-[(2S)-2-[[(2S)-6-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-1-[(2S)-2-[[(2S,3R)-2-[[(2S)-5-amino-2-[[(2S)-1-[(2S)-2-[[(2S)-4-amino-2-[[(2S)-2-[[(2S,3R)-2-[[(2S)-6-amino-2-[[(2S)-1-[(2S)-4-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-4-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S,3R)-2-[[(2S)-2-[[(2S)-2-amino-3-hydroxypropanoyl]amino]-4-carboxybutanoyl]amino]-3-hydroxybutanoyl]amino]-3-carboxypropanoyl]amino]-4-methylpentanoyl]amino]-4-carboxybutanoyl]amino]propanoyl]amino]-4-methylpentanoyl]amino]-3-phenylpropanoyl]amino]-4-oxobutanoyl]amino]propanoyl]amino]-3-methylbutanoyl]amino]hexanoyl]amino]-4-oxobutanoyl]pyrrolidine-2-carbonyl]amino]hexanoyl]amino]-3-hydroxybutanoyl]amino]propanoyl]amino]-4-oxobutanoyl]amino]-3-methylbutanoyl]pyrrolidine-2-carbonyl]amino]-5-oxopentanoyl]amino]-3-hydroxybutanoyl]amino]-3-methylbutanoyl]pyrrolidine-2-carbonyl]amino]hexanoyl]amino]-5-carbamimidamidopentanoyl]amino]-4-methylpentanoyl]amino]-5-carbamimidamidopentanoyl]amino]hexanoyl]amino]-4-methylpentanoyl]pyrrolidine-2-carbonyl]amino]-3-carboxypropanoyl]amino]-3-hydroxypropanoyl]amino]-3-phenylpropanoyl]amino]-3-phenylpropanoyl]amino]hexanoyl]pyrrolidine-2-carbonyl]pyrrolidine-2-carboxylic acid | 1634096: Inhibition of human TEAD4 (217 to 434 residues) expressed in Escherichia coli BL21 (DE3) interaction with N-biotinylated YAP (60 to 100 residues) incubated for 2 hrs by by TR-FRET assay | ic50 | 0.0560 | uM |
| 2-[anilino(phenyl)methyl]-3-hydroxy-6-(hydroxymethyl)pyran-4-one | 1676394: Binding affinity to nonacylated N-terminal His6-tagged human TEAD4 (217 to 434 residues) expressed in Escherichia coli BL21-CodonPlus (DE3)-RIPL cells assessed as inhibition of protein-FAM-YAP (50 to 100 residues) interaction preincubated for 10 mins followed by FAM YAP addition and measured after 1 hr by fluorescence assay | ic50 | 0.0700 | uM |
| N-[5-cyano-4-[(E)-2-(4,4-difluorocyclohexyl)ethenyl]-2-pyridinyl]prop-2-enamide | 2007283: Inhibition of His-tagged TEAD4 (unknown origin) preincubated for 30 mins followed by biotinylated lipid pocket addition and measured after 60 mins by TR-FRET assay | ic50 | 0.1000 | uM |
| N-[7-[(E)-2-(4,4-difluorocyclohexyl)ethenyl]-4-fluoro-2,3-dihydro-1-benzofuran-5-yl]prop-2-enamide | 2007283: Inhibition of His-tagged TEAD4 (unknown origin) preincubated for 30 mins followed by biotinylated lipid pocket addition and measured after 60 mins by TR-FRET assay | ic50 | 0.1000 | uM |
| N-[6-methoxy-5-[(E)-2-[4-(trifluoromethyl)cyclohexyl]ethenyl]pyridazin-3-yl]prop-2-enamide | 2007283: Inhibition of His-tagged TEAD4 (unknown origin) preincubated for 30 mins followed by biotinylated lipid pocket addition and measured after 60 mins by TR-FRET assay | ic50 | 0.1000 | uM |
| 2-[anilino-(2-fluorophenyl)methyl]-3-hydroxy-6-(hydroxymethyl)pyran-4-one | 1676399: Inhibition of FITC-labeled palmitate tracer binding to N-terminal His6-tagged human TEAD4 (217 to 434 residues) expressed in Escherichia coli BL21-CodonPlus (DE3)-RIPL cells preincubated for 10 mins followed by FITC-labeled palmitate tracer addition and measured after 1 hr by fluorescence assay | ic50 | 0.1000 | uM |
| N-[4-(naphthalen-2-ylmethyl)phenyl]ethenesulfonamide | 1580415: Inhibition of N-terminal His6 tagged human TEAD4-YBD (217 to 434 residues) expressed in Escherichia coli C43 (DE3) cells assessed as reduction in autopalmitoylation preincubated for 2 hrs followed by palmitoyl alkyne-coenzyme A addition and measured after 30 mins by immunoblot analysis | ic50 | 0.1970 | uM |
| 2-[anilino(naphthalen-2-yl)methyl]-3-hydroxy-6-(hydroxymethyl)pyran-4-one | 1676399: Inhibition of FITC-labeled palmitate tracer binding to N-terminal His6-tagged human TEAD4 (217 to 434 residues) expressed in Escherichia coli BL21-CodonPlus (DE3)-RIPL cells preincubated for 10 mins followed by FITC-labeled palmitate tracer addition and measured after 1 hr by fluorescence assay | ic50 | 0.2000 | uM |
| 2-[(3-fluoroanilino)-phenylmethyl]-3-hydroxy-6-(hydroxymethyl)pyran-4-one | 1676399: Inhibition of FITC-labeled palmitate tracer binding to N-terminal His6-tagged human TEAD4 (217 to 434 residues) expressed in Escherichia coli BL21-CodonPlus (DE3)-RIPL cells preincubated for 10 mins followed by FITC-labeled palmitate tracer addition and measured after 1 hr by fluorescence assay | ic50 | 0.2000 | uM |
| 2-[anilino-(4-bromophenyl)methyl]-3-hydroxy-6-(hydroxymethyl)pyran-4-one | 1676399: Inhibition of FITC-labeled palmitate tracer binding to N-terminal His6-tagged human TEAD4 (217 to 434 residues) expressed in Escherichia coli BL21-CodonPlus (DE3)-RIPL cells preincubated for 10 mins followed by FITC-labeled palmitate tracer addition and measured after 1 hr by fluorescence assay | ic50 | 0.2000 | uM |
| 2-[anilino-(4-propan-2-ylphenyl)methyl]-3-hydroxy-6-(hydroxymethyl)pyran-4-one | 1676399: Inhibition of FITC-labeled palmitate tracer binding to N-terminal His6-tagged human TEAD4 (217 to 434 residues) expressed in Escherichia coli BL21-CodonPlus (DE3)-RIPL cells preincubated for 10 mins followed by FITC-labeled palmitate tracer addition and measured after 1 hr by fluorescence assay | ic50 | 0.2000 | uM |
| 2-[anilino-(4-methylphenyl)methyl]-3-hydroxy-6-(hydroxymethyl)pyran-4-one | 1676399: Inhibition of FITC-labeled palmitate tracer binding to N-terminal His6-tagged human TEAD4 (217 to 434 residues) expressed in Escherichia coli BL21-CodonPlus (DE3)-RIPL cells preincubated for 10 mins followed by FITC-labeled palmitate tracer addition and measured after 1 hr by fluorescence assay | ic50 | 0.2000 | uM |
| 5-methoxy-4-[3-(trifluoromethyl)anilino]-1,3-dihydroisoindole-2-carbonitrile | 1964894: Displacement of FAM- labeled YAP1 peptide (60 to 99 residues) from human TEAD4 (217 to 434 residues) expressed in Escherichia coli BL21 (DE3) cells incubated for 24 hrs by fluorescence polarization-based competitive binding assay | ic50 | 0.2000 | uM |
| (2S)-1-[(2S)-1-[(2S)-6-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-1-[(2S)-2-[[(2S)-6-amino-2-[[(2S)-5-carbamimidamido-2-[[(2S)-2-[[(2S)-5-carbamimidamido-2-[[(2S)-3-(6-chloro-1H-indol-3-yl)-2-[[(2S)-pyrrolidine-2-carbonyl]amino]propanoyl]amino]pentanoyl]amino]-4-methylpentanoyl]amino]pentanoyl]amino]hexanoyl]amino]-3-cyclobutylpropanoyl]pyrrolidine-2-carbonyl]amino]-3-carboxypropanoyl]amino]-3-hydroxypropanoyl]amino]-3-phenylpropanoyl]amino]-3-naphthalen-1-ylpropanoyl]amino]hexanoyl]pyrrolidine-2-carbonyl]pyrrolidine-2-carboxylic acid | 1634096: Inhibition of human TEAD4 (217 to 434 residues) expressed in Escherichia coli BL21 (DE3) interaction with N-biotinylated YAP (60 to 100 residues) incubated for 2 hrs by by TR-FRET assay | ic50 | 0.2160 | uM |
| 3-hydroxy-6-(hydroxymethyl)-2-[phenyl-(pyridin-2-ylamino)methyl]pyran-4-one | 1676399: Inhibition of FITC-labeled palmitate tracer binding to N-terminal His6-tagged human TEAD4 (217 to 434 residues) expressed in Escherichia coli BL21-CodonPlus (DE3)-RIPL cells preincubated for 10 mins followed by FITC-labeled palmitate tracer addition and measured after 1 hr by fluorescence assay | ic50 | 0.3000 | uM |
| 4-[[[3-hydroxy-6-(hydroxymethyl)-4-oxopyran-2-yl]-phenylmethyl]amino]benzamide | 1676399: Inhibition of FITC-labeled palmitate tracer binding to N-terminal His6-tagged human TEAD4 (217 to 434 residues) expressed in Escherichia coli BL21-CodonPlus (DE3)-RIPL cells preincubated for 10 mins followed by FITC-labeled palmitate tracer addition and measured after 1 hr by fluorescence assay | ic50 | 0.3000 | uM |
| 3-hydroxy-6-(hydroxymethyl)-2-[[(4-methyl-2-pyridinyl)amino]-phenylmethyl]pyran-4-one | 1676399: Inhibition of FITC-labeled palmitate tracer binding to N-terminal His6-tagged human TEAD4 (217 to 434 residues) expressed in Escherichia coli BL21-CodonPlus (DE3)-RIPL cells preincubated for 10 mins followed by FITC-labeled palmitate tracer addition and measured after 1 hr by fluorescence assay | ic50 | 0.3000 | uM |
| 2-[anilino-(4-fluorophenyl)methyl]-3-hydroxy-6-(hydroxymethyl)pyran-4-one | 1676399: Inhibition of FITC-labeled palmitate tracer binding to N-terminal His6-tagged human TEAD4 (217 to 434 residues) expressed in Escherichia coli BL21-CodonPlus (DE3)-RIPL cells preincubated for 10 mins followed by FITC-labeled palmitate tracer addition and measured after 1 hr by fluorescence assay | ic50 | 0.3000 | uM |
| 4-[anilino-[3-hydroxy-6-(hydroxymethyl)-4-oxopyran-2-yl]methyl]benzamide | 1676399: Inhibition of FITC-labeled palmitate tracer binding to N-terminal His6-tagged human TEAD4 (217 to 434 residues) expressed in Escherichia coli BL21-CodonPlus (DE3)-RIPL cells preincubated for 10 mins followed by FITC-labeled palmitate tracer addition and measured after 1 hr by fluorescence assay | ic50 | 0.3000 | uM |
| 2-[(2-fluorophenyl)-(pyridin-2-ylamino)methyl]-3-hydroxy-6-(hydroxymethyl)pyran-4-one | 1676399: Inhibition of FITC-labeled palmitate tracer binding to N-terminal His6-tagged human TEAD4 (217 to 434 residues) expressed in Escherichia coli BL21-CodonPlus (DE3)-RIPL cells preincubated for 10 mins followed by FITC-labeled palmitate tracer addition and measured after 1 hr by fluorescence assay | ic50 | 0.3000 | uM |
| 2-[(benzylamino)-phenylmethyl]-3-hydroxy-6-(hydroxymethyl)pyran-4-one | 1676399: Inhibition of FITC-labeled palmitate tracer binding to N-terminal His6-tagged human TEAD4 (217 to 434 residues) expressed in Escherichia coli BL21-CodonPlus (DE3)-RIPL cells preincubated for 10 mins followed by FITC-labeled palmitate tracer addition and measured after 1 hr by fluorescence assay | ic50 | 0.4000 | uM |
| 2-[(4-bromophenyl)-(pyridin-2-ylamino)methyl]-3-hydroxy-6-(hydroxymethyl)pyran-4-one | 1676399: Inhibition of FITC-labeled palmitate tracer binding to N-terminal His6-tagged human TEAD4 (217 to 434 residues) expressed in Escherichia coli BL21-CodonPlus (DE3)-RIPL cells preincubated for 10 mins followed by FITC-labeled palmitate tracer addition and measured after 1 hr by fluorescence assay | ic50 | 0.4000 | uM |
| 4-[3-(trifluoromethyl)anilino]-1,3,3a,4,5,6,7,7a-octahydroisoindole-2-carbonitrile | 1964903: Inhibition of TEAD4 (unknown origin) transfected in human HEK293 cells co-transfected with renilla plasmid assessed as inhibition of transcriptional activity incubated for 24 hrs by dual Glo-luciferase reporter assay | ic50 | 0.4000 | uM |
| (2S)-1-[(2S)-1-[(2S)-6-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-1-[(2S)-2-[[(2S)-6-amino-2-[[(2S)-5-carbamimidamido-2-[[(2S)-2-[[(2S)-5-carbamimidamido-2-[[(2S)-3-(6-chloro-1H-indol-3-yl)-2-[[(2S)-pyrrolidine-2-carbonyl]amino]propanoyl]amino]pentanoyl]amino]-4-methylpentanoyl]amino]pentanoyl]amino]hexanoyl]amino]hexanoyl]pyrrolidine-2-carbonyl]amino]-3-carboxypropanoyl]amino]-3-hydroxypropanoyl]amino]-3-phenylpropanoyl]amino]-3-naphthalen-1-ylpropanoyl]amino]hexanoyl]pyrrolidine-2-carbonyl]pyrrolidine-2-carboxylic acid | 1634096: Inhibition of human TEAD4 (217 to 434 residues) expressed in Escherichia coli BL21 (DE3) interaction with N-biotinylated YAP (60 to 100 residues) incubated for 2 hrs by by TR-FRET assay | ic50 | 0.4090 | uM |
| tert-butyl 4-[[1-(6-chloro-1H-indol-3-yl)-2-oxo-2-[[(1S,2S,4S)-1,7,7-trimethyl-2-bicyclo[2.2.1]heptanyl]amino]ethyl]-[[1-[(6-methylimidazo[1,2-a]pyridin-2-yl)methyl]triazol-4-yl]methyl]amino]-4-oxobutanoate | 2007261: Inhibition of N-terminal His-tagged human TEAD4 (217 to 434 residues) expressed in Escherichia coli BL21-codonPlus (DE3)-RIPL cells by fluorescence polarisation assay | ic50 | 0.4100 | uM |
| 2-[anilino(pyridin-2-yl)methyl]-3-hydroxy-6-(hydroxymethyl)pyran-4-one | 1676399: Inhibition of FITC-labeled palmitate tracer binding to N-terminal His6-tagged human TEAD4 (217 to 434 residues) expressed in Escherichia coli BL21-CodonPlus (DE3)-RIPL cells preincubated for 10 mins followed by FITC-labeled palmitate tracer addition and measured after 1 hr by fluorescence assay | ic50 | 0.5000 | uM |
| tert-butyl 4-[[1-(6-chloro-1H-indol-3-yl)-2-oxo-2-[(1,7,7-trimethyl-2-bicyclo[2.2.1]heptanyl)amino]ethyl]-[[1-[(7-methylimidazo[1,2-a]pyridin-2-yl)methyl]triazol-4-yl]methyl]amino]-4-oxobutanoate | 1916164: Inhibition of YAP binding to human TEAD4 by fluorescence polarization assay | ic50 | 0.5100 | uM |
| 5-fluoro-4-[3-(trifluoromethyl)anilino]-1,3-dihydroisoindole-2-carbonitrile | 1964894: Displacement of FAM- labeled YAP1 peptide (60 to 99 residues) from human TEAD4 (217 to 434 residues) expressed in Escherichia coli BL21 (DE3) cells incubated for 24 hrs by fluorescence polarization-based competitive binding assay | ic50 | 0.6000 | uM |
| 2-chloro-1-[2-[3-(trifluoromethyl)anilino]phenyl]ethanone | 1676397: Inhibition of CPM binding to N-terminal His6-tagged human TEAD4 (217 to 434 residues) expressed in Escherichia coli BL21-CodonPlus (DE3)-RIPL cells preincubated for 10 mins followed by CPM addition and measured after 1 hr by fluorescence assay | ic50 | 0.8000 | uM |
| 2-[1,3-dihydroisoindol-2-yl(phenyl)methyl]-3-hydroxy-6-(hydroxymethyl)pyran-4-one | 1676399: Inhibition of FITC-labeled palmitate tracer binding to N-terminal His6-tagged human TEAD4 (217 to 434 residues) expressed in Escherichia coli BL21-CodonPlus (DE3)-RIPL cells preincubated for 10 mins followed by FITC-labeled palmitate tracer addition and measured after 1 hr by fluorescence assay | ic50 | 0.9000 | uM |
| 2-(3-chloro-N-(2-chloroacetyl)anilino)-N-(2-phenylethyl)-2-thiophen-2-ylacetamide | 1977251: Inhibition of GST-tagged TEAD4 (217 to 434 residues) (unknown origin) expressed in Escherichia coli BL21 (DE3) cells/FAM-labelled YAP1 (60 to 99 residues)(unknown origin) protein-protein interaction preincubated for 48 hrs at 4 degree C with TEAD4 followed by fluorescent labelled YAP1 addition by fluorescence polarization assay | ic50 | 0.9000 | uM |
| 3-[(2-chloroacetyl)amino]-1-benzofuran-2-carboxamide | 1977244: Inhibition of GST-tagged TEAD4 (217 to 434 residues) (unknown origin) expressed in Escherichia coli BL21 (DE3) cells/FAM-labelled YAP1 (60 to 99 residues)(unknown origin) protein-protein interaction preincubated for 24 hrs at 4 degree C with TEAD4 followed by fluorescent labelled YAP1 addition by fluorescence polarization assay | ic50 | 0.9000 | uM |
CTD chemical–gene interactions
54 total (human), top 30 by PubMed support.
| Chemical | Actions (top 5) | PubMed papers |
|---|---|---|
| Valproic Acid | increases expression, increases methylation | 3 |
| sodium arsenite | decreases expression, increases abundance | 2 |
| Air Pollutants | affects cotreatment, increases abundance, increases oxidation, decreases expression | 2 |
| Benzo(a)pyrene | affects methylation, decreases methylation | 2 |
| Nickel | increases expression | 2 |
| Tobacco Smoke Pollution | increases expression | 2 |
| Cyclosporine | decreases expression | 2 |
| Cadmium Chloride | decreases expression | 2 |
| tert-Butylhydroperoxide | affects expression, decreases expression | 2 |
| Particulate Matter | decreases expression, decreases reaction, increases abundance | 2 |
| alpha-pinene | affects cotreatment, increases oxidation, increases abundance | 1 |
| arsenite | affects binding, increases reaction | 1 |
| zinc chromate | decreases expression, increases abundance | 1 |
| benzo(e)pyrene | increases methylation | 1 |
| potassium chromate(VI) | affects cotreatment, decreases expression | 1 |
| aflatoxin B2 | decreases methylation, increases methylation | 1 |
| methacrylaldehyde | increases oxidation, increases abundance, affects cotreatment | 1 |
| S-(1,2-dichlorovinyl)cysteine | affects response to substance, increases expression | 1 |
| beta-methylcholine | affects expression | 1 |
| epigallocatechin gallate | decreases expression, affects cotreatment | 1 |
| chromium hexavalent ion | decreases expression, increases abundance | 1 |
| seocalcitol | decreases expression | 1 |
| rofecoxib | increases expression | 1 |
| 2-methyl-2H-pyrazole-3-carboxylic acid (2-methyl-4-o-tolylazophenyl)amide | decreases expression, decreases reaction | 1 |
| jinfukang | affects cotreatment, decreases expression | 1 |
| incobotulinumtoxinA | decreases expression | 1 |
| NSC 689534 | affects binding, decreases expression | 1 |
| theaflavin-3,3’-digallate | affects expression | 1 |
| Resveratrol | affects cotreatment, decreases expression | 1 |
| Sunitinib | increases expression | 1 |
ChEMBL screening assays
131 unique, capped per target: 131 binding
Representative assays (with source publication via chembl_document):
| Assay ID | Type | Description | Source paper |
|---|---|---|---|
| CHEMBL4120896 | Binding | Binding affinity to human His-tagged TEAD4 YBD (217 to 434 residues) expressed in Escherichia coli BL21(DE3) after 30 mins by ITC assay | Targeting Transcriptional Enhanced Associate Domains (TEADs). — J Med Chem |
Cellosaurus cell lines
8 cell lines: 4 embryonic stem cell, 3 cancer cell line, 1 transformed cell line
First 10 cell lines (id-ordered, not curated):
| Cellosaurus | Name | Category | Sex |
|---|---|---|---|
| CVCL_A7F8 | SEES3-1V human TEAD4, clone1 | Embryonic stem cell | Male |
| CVCL_A7F9 | SEES3-1V human TEAD4, clone2 | Embryonic stem cell | Male |
| CVCL_A7G0 | SEES3-1V human TEAD4, clone3 | Embryonic stem cell | Male |
| CVCL_A8RD | WAe001-A-68 | Embryonic stem cell | Male |
| CVCL_B1HX | Abcam A-549 TEAD4 KO | Cancer cell line | Male |
| CVCL_B3J5 | Abcam HEK293T TEAD4 KO | Transformed cell line | Female |
| CVCL_TR86 | HAP1 TEAD4 (-) 1 | Cancer cell line | Male |
| CVCL_XU16 | HAP1 TEAD4 (-) 2 | Cancer cell line | Male |
Clinical trials (associated diseases)
0 trials via MONDO — disease-level, not drug-specific.
Related Atlas pages
- Disease cohort memberships (association, not causation — diseases whose associated-gene cohort lists this gene; a subset are also under Associated diseases): narcolepsy-cataplexy syndrome