TEAD1

Summary

TEAD1 (TEA domain transcription factor 1, HGNC:11714) is a protein-coding gene on chromosome 11p15.3, encoding Transcriptional enhancer factor TEF-1 (P28347). 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. It is a selective cancer dependency (DepMap: 18.3% of cell lines).

This gene encodes a ubiquitous transcriptional enhancer factor that is a member of the TEA/ATTS domain family. This protein directs the transactivation of a wide variety of genes and, in placental cells, also acts as a transcriptional repressor. Mutations in this gene cause Sveinsson’s chorioretinal atrophy. Additional transcript variants have been described but their full-length natures have not been experimentally verified.

Source: NCBI Gene 7003 — RefSeq curated summary.

At a glance

• Gene–disease (curated): helicoid peripapillary chorioretinal degeneration (Strong, GenCC) — +1 more curated relationship
• GWAS associations: 19
• Clinical variants (ClinVar): 286 total — 1 pathogenic
• Phenotypes (HPO): 5
• Druggable target: yes — 1 molecules with ChEMBL bioactivity
• Cancer dependency (DepMap): dependent in 18.3% of screened cell lines
• Transcription factor: yes — 34 downstream targets (CollecTRI)
• MANE Select transcript: NM_021961

Identifiers

Gene identifiers

Field	Value
HGNC ID	HGNC:11714
Approved symbol	TEAD1
Name	TEA domain transcription factor 1
Location	11p15.3
Locus type	gene with protein product
Status	Approved
Aliases	TEF-1
Ensembl gene	ENSG00000187079
Ensembl biotype	protein_coding
OMIM	189967
Entrez	7003

Gene structure

Transcript identifiers

Ensembl transcripts: 6 — 5 protein_coding, 1 retained_intron

ENST00000334310, ENST00000525312, ENST00000526600, ENST00000527376, ENST00000527575, ENST00000527636

RefSeq mRNA: 1 — MANE Select: NM_021961 NM_021961

CCDS: CCDS7810

Canonical transcript exons

ENST00000527636 — 13 exons

Exon	Start	End
ENSE00000890040	12881005	12881051
ENSE00000890041	12881896	12881957
ENSE00001101300	12930174	12930326
ENSE00001101315	12924912	12925052
ENSE00001260282	12879708	12879842
ENSE00001260300	12864838	12864900
ENSE00001260349	12883001	12883125
ENSE00001260398	12901940	12902113
ENSE00001481782	12764179	12764434
ENSE00001564120	12675409	12675561
ENSE00002193739	12937109	12944737
ENSE00002199209	12674421	12674834
ENSE00003639365	12862250	12862314

Expression profiles

Bgee: expression breadth ubiquitous, 263 present calls, max score 98.67.

FANTOM5 (CAGE): breadth ubiquitous, TPM avg 38.5730 / max 250.2747, expressed in 1547 samples.

FANTOM5 promoters (10 alternative TSS)

Promoter ID	TPM avg	Samples expressed
113150	35.2369	1543
113152	1.0786	557
113149	0.6838	412
113154	0.3557	167
113148	0.3399	183
113153	0.3191	139
113164	0.2805	112
113160	0.1545	45
113159	0.1055	29
113158	0.0186	14

Top tissues by expression

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

Tissue	Anatomy ID	Expression score	Quality
skeletal muscle tissue of rectus abdominis	UBERON:0004511	98.67	gold quality
biceps brachii	UBERON:0001507	98.15	gold quality
skeletal muscle tissue of biceps brachii	UBERON:0004502	98.06	gold quality
body of tongue	UBERON:0011876	97.39	gold quality
cauda epididymis	UBERON:0004360	97.30	gold quality
trigeminal ganglion	UBERON:0001675	97.23	gold quality
bronchial epithelial cell	CL:0002328	96.98	gold quality
saphenous vein	UBERON:0007318	96.86	gold quality
sural nerve	UBERON:0015488	96.65	gold quality
renal medulla	UBERON:0000362	96.03	gold quality
nipple	UBERON:0002030	95.92	gold quality
mucosa of paranasal sinus	UBERON:0005030	95.81	gold quality
urethra	UBERON:0000057	95.76	gold quality
amniotic fluid	UBERON:0000173	95.65	gold quality
caput epididymis	UBERON:0004358	95.49	gold quality
skin of hip	UBERON:0001554	95.22	gold quality
vena cava	UBERON:0004087	95.12	gold quality
upper leg skin	UBERON:0004262	95.09	gold quality
oral cavity	UBERON:0000167	94.96	gold quality
seminal vesicle	UBERON:0000998	94.85	gold quality
stromal cell of endometrium	CL:0002255	94.69	gold quality
dorsal root ganglion	UBERON:0000044	94.63	gold quality
colonic epithelium	UBERON:0000397	94.43	gold quality
lower lobe of lung	UBERON:0008949	94.43	gold quality
heart right ventricle	UBERON:0002080	94.33	gold quality
pharyngeal mucosa	UBERON:0000355	94.21	gold quality
tongue	UBERON:0001723	94.02	gold quality
pylorus	UBERON:0001166	93.69	gold quality
hindlimb stylopod muscle	UBERON:0004252	93.69	gold quality
tibia	UBERON:0000979	93.41	gold quality

Single-cell (SCXA)

Detected in 3 experiment(s), a significant marker in 2.

Experiment	Marker?	Max mean expression
E-MTAB-6678	yes	17.08
E-CURD-11	no	412.18
E-ANND-3	no	0.00

Regulation

Is transcription factor: yes

Downstream targets (CollecTRI)

34 targets.

Target	Regulation
ACTA1
ADAM2
ADRA1A
ANKRD1	Unknown
ATP6V0A2	Activation
BMP4	Activation
CAT
CCL5	Unknown
CCND1	Unknown
CS	Unknown
CSH2	Repression
EIF3K
FGFR1	Activation
FOXM1	Activation
FOXO3	Activation
GH1	Repression
IFITM3	Unknown
IVL	Unknown
MRPL21
MSLN	Activation
MYF5	Unknown
MYH6
MYH7	Unknown
MYOCD
NAIP	Unknown
NDUFA6
PAX3	Unknown
PRL	Repression
SRF	Unknown
TBXT

JASPAR motifs

Motif	Name	Family
MA0090.1	TEAD1	TEF-1-related factors
MA0090.2	TEAD1	TEF-1-related factors
MA0090.3	TEAD1	TEF-1-related factors
MA0090.4	TEAD1	TEF-1-related factors

JASPAR matrix evidence (PMIDs): PMID:9571041, PMID:23332764

Upstream regulators (CollecTRI, top): GLI2, YAP1

miRNA regulators (miRDB)

510 targeting TEAD1, 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-6867-5P	100.00	82.21	3464
HSA-MIR-5011-5P	100.00	83.46	5820
HSA-MIR-5692A	100.00	74.40	6850
HSA-LET-7A-3P	100.00	74.03	3932
HSA-LET-7B-3P	100.00	74.08	3913
HSA-LET-7F-1-3P	100.00	74.02	3928
HSA-MIR-98-3P	100.00	74.08	3907
HSA-MIR-190A-3P	100.00	80.35	5520
HSA-MIR-513A-5P	100.00	69.77	2465
HSA-MIR-3163	100.00	77.23	8605
HSA-MIR-4747-5P	100.00	67.90	2681
HSA-MIR-5196-5P	100.00	67.98	2761
HSA-MIR-574-5P	100.00	66.01	989
HSA-MIR-518D-5P	100.00	67.51	979
HSA-MIR-518E-5P	100.00	67.66	954
HSA-MIR-518F-5P	100.00	67.51	979
HSA-MIR-519A-5P	100.00	67.66	954
HSA-MIR-519B-5P	100.00	67.66	954
HSA-MIR-519C-5P	100.00	67.66	954
HSA-MIR-520C-5P	100.00	67.51	979
HSA-MIR-522-5P	100.00	67.66	954
HSA-MIR-523-5P	100.00	67.66	954
HSA-MIR-526A-5P	100.00	67.51	979
HSA-MIR-3646	100.00	73.56	5283
HSA-MIR-6873-3P	100.00	71.42	2626
HSA-MIR-5193	100.00	67.26	1744
HSA-MIR-126-5P	100.00	72.71	3180
HSA-MIR-4510	100.00	66.60	2050
HSA-MIR-6127	100.00	66.76	2188
HSA-MIR-6129	100.00	66.46	2080

Functional genomics

DepMap (CRISPR cell-line fitness): dependent in 18.3% of screened cell lines.

Literature-anchored findings (GeneRIF, showing 40)

• These results are consistent with two plausible models of cryptic MCAT enhancer regulation by Pur alpha, Pur beta, and MSY1 involving either competitive single-stranded DNA binding or masking of MCAT-bound transcription enhancer factor-1. (PMID:11751932)
• TEAD1 (TEF-1) interacts with a muscle-specific cofactor to promote skeletal muscle gene expression. (PMID:12376544)
• Transcription enhancer factor 1 binds multiple muscle MEF2 and A/T-rich elements during fast-to-slow skeletal muscle fiber type transitions (PMID:12861002)
• A missense mutation (Y421H) in TEAD1 is tightly linked to Sveinsson’s chorioretinal atrophy (SCRA), an autosomal dominant eye disease characterized by symmetrical lesions radiating from the optic disc involving the retina and the choroid. (PMID:15016762)
• the mutation in the TEAD1 gene is the cause of Sveinsson’s chorioretinal atrophy. (PMID:15016762)
• regulation of IFITM3 by TEF-1 demonstrates that TEF-1 dependent regulation is more widespread than its previously established role in the expression of muscle specific genes (PMID:18177740)
• TEAD1 has non-AUG translation initiation (PMID:1851669)
• TEAD1 inhibits prolactin gene expression in cultured human uterine decidual cells. (PMID:18775765)
• TEAD1 and the ubiquitin ligase c-Cbl were identified as novel basal cell markers in prostate cancer (PMID:19002168)
• Here we show that during vertebrate neural tube development, the TEA domain transcription factor (TEAD) is the cognate DNA-binding partner of YAP. (PMID:19015275)
• The primary cellular origin of circumpapillary dysgenesis of the pigment epithelium is within the choroid instead of the pigment epithelium. (PMID:19410955)
• our data reveal a new, Livin-dependent, apoptotic role for TEAD1 in mammals and provide mechanistic insight downstream of TEAD1 deregulation in cancers. (PMID:23029054)
• Data indicate that knockdown of TEAD1/3/4 induces an almost identical cellular senescent phenotype as YAP silencing. (PMID:23576552)
• identified an intronic region of the NAIP gene responding to TEAD1/YAP activity, suggesting that regulation of NAIP by TEAD1/YAP is at the transcriptional level (PMID:23994529)
• the first evidence demonstrating that TEAD1 is a novel general repressor of smooth muscle-specific gene expression through interfering with myocardin binding to SRF. (PMID:24344135)
• TEAD1 causes the nuclear sequestration of p65 leading to a novel TEAD1/p65 complex that associates with the intronic enhancer and is necessary for cytokine induction of MnSOD. (PMID:24953189)
• the YAP-TEAD interaction can be disrupted using cyclic YAP-like peptides, which targets the HIPPO pathway (PMID:25384421)
• 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)
• Melanoma reprogramming involves thousands of genomic regulatory regions underlying the proliferative and invasive states, identifying SOX10/MITF and AP-1/TEAD as regulators, respectively. (PMID:25865119)
• Suggest central role for TEAD and YAP as signal-responsive regulators of multipotent pancreatic progenitors. (PMID:25915126)
• TAZ negatively regulate transcription of DeltaNp63 through TEAD1,2,3 and 4 transcription factors. (PMID:25995450)
• Our data suggest that AIC is a genetically heterogeneous disease and is not restricted to the X chromosome, and that TEAD1 mutations may be present in male patients. (PMID:26091538)
• show that the proangiogenic microfibrillar-associated protein 5 (MFAP5) is a direct transcriptional target of YAP/TEAD in cholangiocarcinoma cells transcription factors. (PMID:26173433)
• TEAD1 mediates YAP1 chromatin-binding genome-wide. (PMID:26295846)
• Yap1 post-translational modifications favoring its ubiquitination and apoptosis characterize hepatocellular carcinoma (HCC) with better prognosis, whereas conditions favoring the formation of YAP1-TEAD complexes are associated with aggressiveness and acquisition of stemness features by HCC cells (PMID:27359056)
• MYC and TEAD activity is able to stratify different breast cancer subtypes in large panels of breast cancer patients. (PMID:27433809)
• TEAD1 could enhance the expression levels of SP1, by directly binding to its promoter. (PMID:27434865)
• Here, the authors show that TEAD1-expressing skeletal muscle of transgenic mice features a dramatic hyperplasia of muscle stem cells (i.e. satellite cells, SCs) but surprisingly without affecting muscle tissue size. (PMID:27725085)
• The authors show MRTF family proteins bind YAP via a conserved PPXY motif that interacts with the YAP WW domain. This interaction allows MRTF to recruit NcoA3 to the TEAD-YAP transcriptional complex and potentiate its transcriptional activity. (PMID:28028053)
• 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)
• Upregulation of transcriptional enhancer activator domain 1 was found in hepatocellular carcinoma tissues and inversely correlated with miR-590-3p. Our results indicate a tumor suppressor role of miR-590-3p in hepatocellular carcinoma through targeting transcriptional enhancer activator domain 1 and suggest its use in the diagnosis and prognosis of liver cancer. (PMID:28349829)
• This identifies the YAP1/TEAD1 complex as the representative dysregulated profile of Hippo signaling in OS and provides proof-of-principle that targeting TEAD1 may be a therapeutic strategy of osteosarcoma. (PMID:28483529)
• 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)
• YAP1 interacted with TEAD1, exerted their transcriptional control of the functional target, glucose transporter 1 (Glut1). (PMID:28892790)
• adult human and mouse hearts had more Taz than Yap1 by mRNA and protein expression and their increases in diseased hearts were proportional and did not change Yap1/Taz ratio. Yap1, Taz, and Tead1 were accumulated in the nuclear fraction and cardiomyocyte nuclei of diseased hearts (PMID:29154888)
• YAP1-TEAD1 signaling induces mitochondrial biogenesis in endothelial cells and stimulates angiogenesis through PGC1alpha. (PMID:29680477)
• TEA domain family member 1 (TEAD1) expression is highly expressed in hepatocellular carcinoma (HCC). (PMID:29739039)
• Data show that hyperactivated WWTR1 (TAZ) protein induced substantial myeloid cell infiltration into the liver and the secretion of proinflammatory cytokines through a TEA domain transcription factor 1 (TEAD)-dependent mechanism. (PMID:30206136)
• TEA domain transcription factor1 (TEAD1) trans occupies at accessibility sites within AQP4, EGFR, and CDH4. TEAD1 knockout in patient-derived glioblastoma (GBM) lines diminishes migration, in vitro and in vivo, and alters migratory and epithelial-to-mesenchymal transition (EMT) transcriptome signatures with downregulation of its target AQP4. (PMID:30275445)
• High TEAD1 expression is associated with bladder cancer progression. (PMID:30417565)

Cross-species orthologs

4 orthologs

Organism	Symbol	Gene ID
danio_rerio	tead1b	ENSDARG00000059483
mus_musculus	Tead1	ENSMUSG00000055320
rattus_norvegicus	Tead1	ENSRNOG00000015488
drosophila_melanogaster	sd	FBGN0003345

Paralogs (3): TEAD3 (ENSG00000007866), TEAD2 (ENSG00000074219), TEAD4 (ENSG00000197905)

Protein

Protein identifiers

Transcriptional enhancer factor TEF-1 — P28347 (reviewed: P28347)

Alternative names: NTEF-1, Protein GT-IIC, TEA domain family member 1, Transcription factor 13

All UniProt accessions (5): E9PKB7, H0YCZ6, H0YE88, H0YEJ9, P28347

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 cooperatively to the SPH and GT-IIC ’enhansons’ (5’-GTGGAATGT-3’) and activates transcription in vivo in a cell-specific manner. The activation function appears to be mediated by a limiting cell-specific transcriptional intermediary factor (TIF). Involved in cardiac development. 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.

Post-translational modifications. Lactylation by AARS1 promotes nuclear localization and stabilization of YAP1, leading to increased Hippo signaling pathway. Delactylated by SIRT1.

Disease relevance. Sveinsson chorioretinal atrophy (SCRA) [MIM:108985] Characterized by symmetrical lesions radiating from the optic disk involving the retina and the choroid. The disease is caused by variants affecting the gene represented in this entry.

Isoforms (2)

UniProt ID	Names	Canonical?
P28347-1	1	yes
P28347-2	2

RefSeq proteins (1): NP_068780* (*=MANE)

Domains & families (InterPro)

ID	Name	Type
IPR000818	TEA/ATTS_dom	Domain
IPR016361	TEF_metazoa	Family
IPR038096	TEA/ATTS_sf	Homologous_superfamily
IPR041086	YBD	Domain
IPR050937

Pfam: PF01285, PF17725

UniProt features (43 total): strand 16, helix 10, splice variant 3, modified residue 3, mutagenesis site 2, turn 2, region of interest 2, compositionally biased region 2, chain 1, DNA-binding region 1, sequence variant 1

Structure

Experimental structures (PDB)

14 structures.

PDB	Method	Resolution (Å)
8Q68	X-RAY DIFFRACTION	1.58
6IM5	X-RAY DIFFRACTION	1.7
9S64	X-RAY DIFFRACTION	1.85
9GAX	X-RAY DIFFRACTION	1.93
8S6Y	X-RAY DIFFRACTION	2.03
4Z8E	X-RAY DIFFRACTION	2.09
7ZJP	X-RAY DIFFRACTION	2.19
4RE1	X-RAY DIFFRACTION	2.2
9FZA	X-RAY DIFFRACTION	2.21
6HIL	X-RAY DIFFRACTION	2.3
3KYS	X-RAY DIFFRACTION	2.8
5NNX	X-RAY DIFFRACTION	3.29
7CMM	X-RAY DIFFRACTION	3.5
2HZD	SOLUTION NMR

Predicted structure (AlphaFold)

Model	pLDDT	Fraction very-high
AF-P28347-F1	77.43	0.48

Functional residue map

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

Post-translational modifications (3): 1, 11, 108

Mutagenesis-validated functional residues (2):

Position	Phenotype
108	nearly abolished lactylation.
421	important loss of interaction with yap1.

Function

Pathways and Gene Ontology

Reactome pathways

10 pathways

ID	Pathway
R-HSA-2032785	YAP1- and WWTR1 (TAZ)-stimulated gene expression
R-HSA-8951671	RUNX3 regulates YAP1-mediated transcription
R-HSA-9619665	EGR2 and SOX10-mediated initiation of Schwann cell myelination
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-9675108	Nervous system development

MSigDB gene sets: 368 (showing top): GSE18804_SPLEEN_MACROPHAGE_VS_COLON_TUMORAL_MACROPHAGE_DN, REACTOME_ADAPTIVE_IMMUNE_SYSTEM, TGCACTT_MIR519C_MIR519B_MIR519A, TTTGTAG_MIR520D, GOBP_GROWTH, GOBP_HIPPO_SIGNALING, ATGTTAA_MIR302C, GTGCCTT_MIR506, SOX9_B1, GOBP_POSITIVE_REGULATION_OF_CELL_GROWTH, DACOSTA_UV_RESPONSE_VIA_ERCC3_TTD_DN, TGCTGAY_UNKNOWN, WTGAAAT_UNKNOWN, TGTGTGA_MIR377, HFH4_01

GO Biological Process (9): regulation of transcription by RNA polymerase II (GO:0006357), positive regulation of cell growth (GO:0030307), hippo signaling (GO:0035329), positive regulation of DNA-templated transcription (GO:0045893), positive regulation of transcription by RNA polymerase II (GO:0045944), embryonic organ development (GO:0048568), protein-containing complex assembly (GO:0065003), positive regulation of miRNA transcription (GO:1902895), regulation of DNA-templated transcription (GO:0006355)

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 (GO:0003677), DNA-binding transcription factor activity (GO:0003700), sequence-specific double-stranded DNA binding (GO:1990837), protein binding (GO:0005515)

GO Cellular Component (5): chromatin (GO:0000785), nucleus (GO:0005634), nucleoplasm (GO:0005654), transcription regulator complex (GO:0005667), TEAD-YAP complex (GO:0140552)

Reactome top-level categories

Rollup of top-7 pathways:

Category	Pathways
Generic Transcription Pathway	2
Transcriptional regulation by RUNX3	1
Nervous system development	1
Regulation of PD-L1(CD274) expression	1
RNA Polymerase II Transcription	1
Gene expression (Transcription)	1
Developmental Biology	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
transcription by RNA polymerase II	2
DNA-templated transcription	2
regulation of transcription by RNA polymerase II	2
positive regulation of DNA-templated transcription	2
cellular anatomical structure	2
regulation of cell growth	1
cell growth	1
positive regulation of growth	1
positive regulation of cellular process	1
intracellular signal transduction	1
positive regulation of RNA biosynthetic process	1
embryo development	1
animal organ development	1
cellular component assembly	1
protein-containing complex organization	1
miRNA transcription	1
regulation of miRNA transcription	1
positive regulation of miRNA metabolic process	1
regulation of gene expression	1
regulation of RNA biosynthetic process	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
nucleic acid binding	1
transcription cis-regulatory region binding	1
transcription regulator activity	1
double-stranded DNA binding	1
sequence-specific DNA binding	1
binding	1
chromosome	1
intracellular membrane-bounded organelle	1
nuclear lumen	1
protein-containing complex	1
RNA polymerase II transcription regulator complex	1

Protein interactions and networks

STRING

2234 interactions, top by confidence (×1000):

Protein A	Protein B	Partner UniProt	Score
TEAD1	YAP1	P46937	999
TEAD1	VGLL1	Q99990	961
TEAD1	WWTR1	Q9GZV5	960
TEAD1	VGLL2	Q8N8G2	915
TEAD1	VGLL3	A8MV65	898
TEAD1	MCAT	Q8IVS2	891
TEAD1	VGLL4	Q14135	837
TEAD1	SAV1	Q9H4B6	803
TEAD1	LATS1	O95835	802
TEAD1	AMOT	Q4VCS5	728
TEAD1	LATS2	Q9NRM7	711
TEAD1	NF2	P35240	707
TEAD1	CCN1	O00622	677
TEAD1	SRF	P11831	676
TEAD1	CCN2	P29279	662

IntAct

79 interactions, top by confidence:

A	B	Type	Score
YAP1	TEAD1	psi-mi:“MI:0915”(physical association)	0.940
TEAD1	YAP1	psi-mi:“MI:0915”(physical association)	0.940
YAP1	YWHAQ	psi-mi:“MI:0914”(association)	0.920
FOSL1	JUN	psi-mi:“MI:0914”(association)	0.850
JUND	FOSL1	psi-mi:“MI:0914”(association)	0.730
TEAD1		psi-mi:“MI:0407”(direct interaction)	0.620
	TEAD1	psi-mi:“MI:0407”(direct interaction)	0.620
MPDZ	SMCHD1	psi-mi:“MI:0914”(association)	0.590
TEAD1	RAD51	psi-mi:“MI:0915”(physical association)	0.560
TEAD1	RAD51	psi-mi:“MI:0914”(association)	0.560
YAP1	CCDC85C	psi-mi:“MI:0914”(association)	0.530
TEAD2	TEAD1	psi-mi:“MI:0914”(association)	0.530
WWTR1	TEAD1	psi-mi:“MI:0914”(association)	0.530
TEAD4	PARN	psi-mi:“MI:0914”(association)	0.530
vg	TEAD1	psi-mi:“MI:0915”(physical association)	0.520
TEAD1	JUN	psi-mi:“MI:0914”(association)	0.480
VGLL4	TEAD1	psi-mi:“MI:0914”(association)	0.480
TEAD1	BRAF	psi-mi:“MI:2364”(proximity)	0.470

BioGRID (231): TEAD1 (Two-hybrid), TEAD1 (Affinity Capture-MS), TEAD1 (Affinity Capture-MS), RAD51 (Affinity Capture-MS), TEAD1 (Affinity Capture-MS), TEAD1 (Co-fractionation), TEAD1 (Affinity Capture-MS), TEAD1 (Affinity Capture-Western), TEAD1 (Affinity Capture-MS), TEAD1 (Affinity Capture-MS), TEAD1 (Affinity Capture-MS), TEAD1 (Affinity Capture-MS), RAD51 (Affinity Capture-MS), TEAD1 (Affinity Capture-RNA), YAP1 (Reconstituted Complex)

ESM2 similar proteins: O15350, O42132, O42252, O43679, O55203, O73715, O88898, P03372, P06211, P06212, P12349, P19785, P28347, P30051, P30052, P49884, P57753, P70060, P70662, Q03297, Q15561, Q15648, Q1EQW7, Q29040, Q53AD2, Q56R14, Q5RES4, Q5RJA1, Q5U4T7, Q60520, Q6DEZ2, Q6NVL6, Q6ZPQ6, Q86U70, Q8C7R7, Q8CFE5, Q90701, Q91250, Q925J9, Q96ST3

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

12 interactions.

A	Effect	B	Mechanism
TEAD1	“up-regulates quantity by expression”	FOXO3	“transcriptional regulation”
TEAD1	“up-regulates quantity by expression”	MYF5	“transcriptional regulation”
WWTR1	up-regulates	TEAD1	binding
TEAD1	“up-regulates quantity by expression”	FOXM1	“transcriptional regulation”
TEAD1	“up-regulates quantity by expression”	CCND1	“transcriptional regulation”
YAP1	up-regulates	TEAD1	binding
TEAD1	“up-regulates quantity by expression”	BMP4	“transcriptional regulation”
TEAD1	“up-regulates quantity by expression”	FOXO	“transcriptional regulation”
TEAD1	“up-regulates quantity by expression”	MSLN	“transcriptional regulation”
hsa-miR-30a-3p	“down-regulates quantity by destabilization”	TEAD1	“post transcriptional regulation”

Enriched among interaction partners

Reactome pathways and GO biological processes over-represented among this gene’s 48 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
Regulation of PD-L1(CD274) transcription	6	16.7×	1e-04
ESR-mediated signaling	5	16.4×	7e-04
Signaling by Nuclear Receptors	5	13.1×	2e-03
Diseases of signal transduction by growth factor receptors and second messengers	6	8.7×	2e-03
PIP3 activates AKT signaling	5	8.6×	7e-03
Transcriptional Regulation by TP53	5	8.0×	8e-03

GO biological processes:

GO term	Partners	Fold	FDR
positive regulation of miRNA transcription	7	46.2×	1e-07
negative regulation of cell growth	5	16.4×	1e-03
osteoblast differentiation	5	13.8×	2e-03
positive regulation of ERK1 and ERK2 cascade	5	9.7×	6e-03

Disease & clinical

Clinical variants and AI predictions

ClinVar

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

Classification	Count (floor)
Pathogenic	1
Likely pathogenic	0
Uncertain significance	146
Likely benign	110
Benign	11

Top pathogenic / likely-pathogenic (1)

Variant ID	HGVS	Classification
12630	NM_021961.6(TEAD1):c.1261T>C (p.Tyr421His)	Pathogenic

SpliceAI

2941 predictions. Top by Δscore:

Variant	Effect	Δscore
11:12764177:A:AG	acceptor_gain	1.0000
11:12764177:AG:A	acceptor_gain	1.0000
11:12764178:G:GA	acceptor_gain	1.0000
11:12764178:G:GC	acceptor_loss	1.0000
11:12764178:GG:G	acceptor_gain	1.0000
11:12764178:GGT:G	acceptor_gain	1.0000
11:12764178:GGTT:G	acceptor_gain	1.0000
11:12764178:GGTTT:G	acceptor_gain	1.0000
11:12764430:GTATG:G	donor_gain	1.0000
11:12764434:GGT:G	donor_loss	1.0000
11:12764435:G:GA	donor_loss	1.0000
11:12764435:G:GG	donor_gain	1.0000
11:12764436:T:G	donor_loss	1.0000
11:12879839:GGGG:G	donor_gain	1.0000
11:12879840:GGGG:G	donor_gain	1.0000
11:12881887:T:TA	acceptor_gain	1.0000
11:12881894:A:AG	acceptor_gain	1.0000
11:12881895:G:GG	acceptor_gain	1.0000
11:12881895:GC:G	acceptor_gain	1.0000
11:12881954:CCAGG:C	donor_loss	1.0000
11:12881956:AGG:A	donor_loss	1.0000
11:12881957:GGTG:G	donor_loss	1.0000
11:12881958:G:GA	donor_loss	1.0000
11:12881959:T:G	donor_loss	1.0000
11:12882999:AG:A	acceptor_gain	1.0000
11:12883000:GG:G	acceptor_gain	1.0000
11:12901934:TTACA:T	acceptor_loss	1.0000
11:12901935:TACAG:T	acceptor_loss	1.0000
11:12901936:ACAG:A	acceptor_loss	1.0000
11:12901937:CAG:C	acceptor_loss	1.0000

AlphaMissense

2840 scored. Top likely-pathogenic:

Variant	Protein change	am_pathogenicity
11:12764335:T:A	W35R	1.000
11:12764335:T:C	W35R	1.000
11:12764336:G:C	W35S	1.000
11:12764337:G:C	W35C	1.000
11:12764337:G:T	W35C	1.000
11:12764348:T:A	I39N	1.000
11:12764356:A:C	S42R	1.000
11:12764358:C:A	S42R	1.000
11:12764358:C:G	S42R	1.000
11:12764359:T:A	F43I	1.000
11:12764359:T:C	F43L	1.000
11:12764359:T:G	F43V	1.000
11:12764360:T:C	F43S	1.000
11:12764360:T:G	F43C	1.000
11:12764361:T:A	F43L	1.000
11:12764361:T:G	F43L	1.000
11:12764368:G:A	A46T	1.000
11:12764368:G:C	A46P	1.000
11:12764369:C:A	A46D	1.000
11:12764369:C:T	A46V	1.000
11:12764372:T:C	L47P	1.000
11:12764380:T:A	Y50N	1.000
11:12764380:T:C	Y50H	1.000
11:12764380:T:G	Y50D	1.000
11:12764387:C:A	P52Q	1.000
11:12764389:T:C	C53R	1.000
11:12764390:G:A	C53Y	1.000
11:12764391:T:G	C53W	1.000
11:12764392:G:A	G54R	1.000
11:12764392:G:C	G54R	1.000

dbSNP variants (sampled 300 via entrez): RS1000017292 (11:12879112 A>C), RS1000050539 (11:12719548 C>T), RS1000056868 (11:12839382 G>A,C), RS1000062936 (11:12819658 A>G), RS1000065432 (11:12936110 A>G), RS1000074257 (11:12697214 T>C), RS1000087370 (11:12774817 A>G), RS1000099186 (11:12735862 A>G), RS1000099714 (11:12763968 T>C), RS1000110486 (11:12698795 C>T), RS1000129228 (11:12748712 C>G), RS1000150737 (11:12719524 C>A,T), RS1000153856 (11:12920087 A>C), RS1000180921 (11:12710528 C>T), RS1000187707 (11:12872891 A>C)

Disease associations

OMIM: gene MIM:189967 | disease phenotypes: MIM:108985

GenCC curated gene-disease

Disease	Classification	Inheritance
helicoid peripapillary chorioretinal degeneration	Strong	Autosomal dominant
Aicardi syndrome	Limited	Autosomal dominant

Mondo (3): helicoid peripapillary chorioretinal degeneration (MONDO:0007176), inherited retinal dystrophy (MONDO:0019118), Aicardi syndrome (MONDO:0010568)

Orphanet (2): Helicoid peripapillary chorioretinal degeneration (Orphanet:86813), OBSOLETE: Inherited retinal disorder (Orphanet:71862)

HPO phenotypes

5 total (6 of 5 shown, HPO-id order):

HPO	Term
HP:0000006	Autosomal dominant inheritance
HP:0000483	Astigmatism
HP:0000545	Myopia
HP:0003677	Slowly progressive
HP:0007950	Peripapillary chorioretinal atrophy
HP:0000556	Retinal dystrophy

GWAS associations

19 associations (top):

Study	Trait	p-value
GCST000817_50	Height	4.000000e-10
GCST002647_40	Height	1.000000e-15
GCST002875_36	Diisocyanate-induced asthma	2.000000e-06
GCST005316_355	Intelligence (MTAG)	5.000000e-10
GCST005316_356	Intelligence (MTAG)	7.000000e-09
GCST006979_619	Heel bone mineral density	2.000000e-10
GCST008163_449	Height	4.000000e-06
GCST008595_148	Cognitive ability, years of educational attainment or schizophrenia (pleiotropy)	4.000000e-11
GCST009474_1	Central retinal vein equivalent	3.000000e-11
GCST009524_20	Household income (MTAG)	3.000000e-10
GCST009524_295	Household income (MTAG)	1.000000e-09
GCST009524_32	Household income (MTAG)	1.000000e-10
GCST009613_4	HDL cholesterol levels x loop diuretics use interaction	6.000000e-07
GCST010724_20	HOMA-B (corrected for HOMA-IR)	5.000000e-08
GCST012116_3	Rheumatic heart disease	3.000000e-06
GCST90000047_215	Age at first sexual intercourse	2.000000e-10
GCST90002398_194	Neutrophil count	4.000000e-09
GCST90007011_4	Gut microbiota relative abundance (unclassified genus belonging to family Erysipelotrichaceae)	8.000000e-06
GCST90020028_1821	Hip circumference adjusted for BMI	5.000000e-08

EFO canonical traits (12, from GWAS)

EFO ID	Trait name
EFO:0006995	response to diisocyanate
EFO:0004337	intelligence
EFO:0009270	heel bone mineral density
EFO:0004784	self reported educational attainment
EFO:0010554	retinal vasculature measurement
EFO:0009695	household income
EFO:0004612	high density lipoprotein cholesterol measurement
EFO:0004469	HOMA-B
EFO:0009749	age at first sexual intercourse measurement
EFO:0004833	neutrophil count
EFO:0007874	gut microbiome measurement
EFO:0008039	BMI-adjusted hip circumference

MeSH disease descriptors (3)

Descriptor	Name	Tree numbers
D058540	Aicardi Syndrome	C10.500.034.687; C11.270.019; C16.131.162; C16.131.666.034.687; C16.320.290.019; C16.320.322.030
D058499	Retinal Dystrophies	C11.768.585.658
C566236	Sveinsson Chorioretinal Atrophy (supp.)

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (5): CHEMBL3334416 (SINGLE PROTEIN), CHEMBL3430909 (PROTEIN-PROTEIN INTERACTION), CHEMBL6066051 (PROTEIN-PROTEIN INTERACTION), CHEMBL6193819 (PROTEIN-PROTEIN INTERACTION), CHEMBL6195504 (PROTEIN-PROTEIN INTERACTION)

Molecules with ChEMBL bioactivity

1 molecules (phase ≥1), by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 1,928 (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
CHEMBL32350	PIRLINDOLE	2	1,928

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	7.3	pIC50

Binding affinities (BindingDB)

1 measured of 1 human assays (1 total across all organisms); most potent 1 below. Values come from heterogeneous assays and are not directly comparable.

Ligand	Measure	Value
CHEMBL4129172	IC50	83 nM

ChEMBL bioactivities

171 potent at pChembl≥5 of 180 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).

pChembl	Type	Value	Unit	Molecule
9.52	Ki	0.3	nM	CHEMBL6147038
9.10	Ki	0.8	nM	CHEMBL6162390
8.99	IC50	1.02	nM	CHEMBL5198469
8.96	Ki	1.1	nM	CHEMBL6163072
8.96	Ki	1.1	nM	CHEMBL6162987
8.92	Ki	1.2	nM	CHEMBL6165193
8.89	Ki	1.3	nM	CHEMBL6161233
8.60	Ki	2.5	nM	CHEMBL6142714
8.60	Ki	2.5	nM	CHEMBL6160130
8.52	IC50	3	nM	CHEMBL5401444
8.52	IC50	3	nM	CHEMBL5422959
8.52	IC50	3	nM	CHEMBL5438256
8.52	IC50	3	nM	CHEMBL5408536
8.48	Ki	3.3	nM	CHEMBL6167591
8.42	Ki	3.8	nM	CHEMBL6152197
8.40	IC50	4	nM	CHEMBL5419829
8.40	IC50	4	nM	CHEMBL5415215
8.40	IC50	4	nM	CHEMBL5411200
8.40	IC50	4	nM	CHEMBL5403826
8.38	Ki	4.2	nM	CHEMBL6160358
8.38	Ki	4.2	nM	CHEMBL6168354
8.22	IC50	6	nM	CHEMBL5416415
8.15	IC50	7	nM	CHEMBL5400400
8.10	IC50	8	nM	CHEMBL5428867
8.01	Ki	9.7	nM	CHEMBL6150768
8.00	IC50	10	nM	CHEMBL5432828
8.00	Ki	10	nM	CHEMBL6164141
7.98	Ki	10.4	nM	CHEMBL6168179
7.96	IC50	11	nM	CHEMBL5433922
7.94	Ki	11.6	nM	CHEMBL6171778
7.87	Ki	13.4	nM	CHEMBL6147615
7.85	Ki	14.1	nM	CHEMBL6134537
7.82	Kd	15	nM	CHEMBL3335461
7.82	Kd	15	nM	CHEMBL4130196
7.80	Ki	15.8	nM	CHEMBL6142314
7.78	Ki	16.5	nM	CHEMBL6149136
7.75	Kd	18	nM	CHEMBL3335453
7.73	Ki	18.6	nM	CHEMBL6148765
7.71	Ki	19.7	nM	CHEMBL6160885
7.71	Ki	19.7	nM	CHEMBL6149521
7.60	IC50	25	nM	CHEMBL3335461
7.60	IC50	25	nM	CHEMBL4130196
7.60	EC50	25	nM	CHEMBL6082980
7.52	EC50	30	nM	CHEMBL6103206
7.50	Ki	31.6	nM	CHEMBL6169845
7.42	EC50	38	nM	CHEMBL6102579
7.41	Kd	39	nM	CHEMBL3335452
7.41	EC50	39	nM	CHEMBL6078219
7.39	IC50	41	nM	CHEMBL3335458
7.39	Ki	40.5	nM	CHEMBL6150386

PubChem BioAssay actives

63 with measured affinity, of 187 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-methyl-3-(1-methylimidazol-4-yl)-4-[4-(trifluoromethyl)anilino]benzenesulfonamide	2084127: Inhibition of N-terminal His-tagged TEAD1 (unknown origin) (209 to 426 residues) expressed in Escherichia coli BL21 by chromatography analysis	ic50	0.0010	uM
2-chloro-N-methyl-N-[[1-[4-(trifluoromethoxy)phenyl]indazol-3-yl]methyl]acetamide	2020148: Inhibition of His-tagged TEAD1 (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
2-chloro-N-[[4-(hydroxymethyl)-1-[4-(trifluoromethoxy)phenyl]pyrazolo[3,4-b]pyridin-3-yl]methyl]prop-2-enamide	2020148: Inhibition of His-tagged TEAD1 (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-[7-[4-(trifluoromethoxy)phenyl]-[1,3]thiazolo[5,4-d]pyrimidin-5-yl]azetidin-1-yl]prop-2-en-1-one	2015509: Displacement of biotinylated lipid pocket probes from His-tagged TEAD1 (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
1-[3-[9-methyl-6-[4-(trifluoromethoxy)phenyl]purin-2-yl]azetidin-1-yl]prop-2-en-1-one	2015509: Displacement of biotinylated lipid pocket probes from His-tagged TEAD1 (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)-1-[4-(trifluoromethoxy)phenyl]pyrazolo[3,4-b]pyridin-3-yl]methyl]prop-2-ynamide	2020148: Inhibition of His-tagged TEAD1 (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	0.0040	uM
1-[3-[4-ethynyl-1-[4-(trifluoromethoxy)phenyl]pyrazolo[3,4-b]pyridin-3-yl]azetidin-1-yl]prop-2-en-1-one	2020148: Inhibition of His-tagged TEAD1 (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	0.0040	uM
N-[[4-(hydroxymethyl)-7-[4-(trifluoromethoxy)phenyl]-2,3-dihydro-1-benzofuran-5-yl]methyl]ethenesulfonamide	2015509: Displacement of biotinylated lipid pocket probes from His-tagged TEAD1 (unknown origin) preincubated for 4 hrs followed by lipid pocket probe addition and measured after 60 mins by TR-FRET assay	ic50	0.0040	uM
N-[[4-(hydroxymethyl)-7-[4-(trifluoromethoxy)phenyl]-2,3-dihydro-1-benzofuran-5-yl]methyl]-N-methylprop-2-enamide	2015509: Displacement of biotinylated lipid pocket probes from His-tagged TEAD1 (unknown origin) preincubated for 4 hrs followed by lipid pocket probe addition and measured after 60 mins by TR-FRET assay	ic50	0.0040	uM
N-[[4-(3-hydroxyprop-1-ynyl)-3-methyl-7-[4-(trifluoromethoxy)phenyl]benzimidazol-5-yl]methyl]prop-2-enamide	2015509: Displacement of biotinylated lipid pocket probes from His-tagged TEAD1 (unknown origin) preincubated for 4 hrs followed by lipid pocket probe addition and measured after 60 mins by TR-FRET assay	ic50	0.0060	uM
cyclobuten-1-yl-[3-[9-methyl-6-[4-(trifluoromethoxy)phenyl]purin-2-yl]azetidin-1-yl]methanone	2015509: Displacement of biotinylated lipid pocket probes from His-tagged TEAD1 (unknown origin) preincubated for 4 hrs followed by lipid pocket probe addition and measured after 60 mins by TR-FRET assay	ic50	0.0070	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	2020148: Inhibition of His-tagged TEAD1 (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	0.0080	uM
1-[3-[4-(hydroxymethyl)-1-[4-(trifluoromethoxy)phenyl]pyrazolo[3,4-b]pyridin-3-yl]azetidin-1-yl]prop-2-en-1-one	2020148: Inhibition of His-tagged TEAD1 (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	0.0100	uM
2-fluoro-1-[(3R,4R)-3-(pyrimidin-2-ylamino)-4-[[4-(trifluoromethyl)phenyl]methoxy]pyrrolidin-1-yl]prop-2-en-1-one	2084131: Inhibition of N-terminal His-tagged human TEAD1 expressed in Escherichia coli BL21 (DE3) (209 to 424 residues) by affinity chromatography analysis	ic50	0.0110	uM
(4S)-4-[[(2S)-1-[(2S)-1-[(2S)-2-[[(3S,6S,9S,12S,15S,21R,24S,27S,30S,33S)-15-[[(2S)-2-[[(2S)-1-[(2S)-2-acetamido-3-methylbutanoyl]pyrrolidine-2-carbonyl]amino]-3-(3-chlorophenyl)propanoyl]amino]-6-(4-aminobutyl)-24-benzyl-3-butyl-9-(3-carbamimidamidopropyl)-27-(hydroxymethyl)-30-methyl-12-(2-methylpropyl)-2,5,8,11,14,23,26,29,32-nonaoxo-18,19-dithia-1,4,7,10,13,22,25,28,31-nonazabicyclo[31.3.0]hexatriacontane-21-carbonyl]amino]-6-aminohexanoyl]pyrrolidine-2-carbonyl]pyrrolidine-2-carbonyl]amino]-5-amino-5-oxopentanoic acid	1164243: Inhibition of YAP/ GST-TEAD1 interaction in human Bel-7404 cells by GST pull-down assay	kd	0.0150	uM
(4S)-4-[[(2S)-1-[(2S)-1-[(2S)-2-[[(3S,6S,9S,12S,15S,21R,24R,27S,30S,33S)-15-[[(2S)-2-[1-[(2S)-1-[(2S)-2-acetamido-3-methylbutanoyl]pyrrolidin-2-yl]ethylamino]-3-(3-chlorophenyl)propanoyl]amino]-6-(4-aminobutyl)-24-benzyl-3-butyl-9-(3-carbamimidamidopropyl)-27-(hydroxymethyl)-30-methyl-12-(2-methylpropyl)-2,5,8,11,14,23,26,29,32-nonaoxo-18,19-dithia-1,4,7,10,13,22,25,28,31-nonazabicyclo[31.3.0]hexatriacontane-21-carbonyl]amino]-6-aminohexanoyl]pyrrolidine-2-carbonyl]pyrrolidine-2-carbonyl]amino]-5-amino-5-oxopentanoic acid	1494159: Binding affinity to human GST-tagged TEAD1 (194 to 411) expressed in Escherichia coli BL21(DE3) by SPR assay	kd	0.0150	uM
(4S)-4-[[(2S)-1-[(2S)-1-[(2S)-2-[[(3S,6S,9S,12S,15S,21R,24S,27S,30S,33S)-15-[[(2S)-2-[[(2S)-1-[(2S)-2-acetamido-3-methylbutanoyl]pyrrolidine-2-carbonyl]amino]-4-methylsulfanylbutanoyl]amino]-6-(4-aminobutyl)-24-benzyl-9-[3-(diaminomethylideneamino)propyl]-27-(hydroxymethyl)-30-methyl-12-(2-methylpropyl)-2,5,8,11,14,23,26,29,32-nonaoxo-3-pentyl-18,19-dithia-1,4,7,10,13,22,25,28,31-nonazabicyclo[31.3.0]hexatriacontane-21-carbonyl]amino]-6-aminohexanoyl]pyrrolidine-2-carbonyl]pyrrolidine-2-carbonyl]amino]-5-amino-5-oxopentanoic acid	1164243: Inhibition of YAP/ GST-TEAD1 interaction in human Bel-7404 cells by GST pull-down assay	kd	0.0180	uM
(4S)-4-[[(2S)-1-[(2S)-1-[(2S)-2-[[(3S,6S,9S,12S,15S,21R,24S,27S,30S,33S)-15-[[(2S)-2-[[(2S)-1-[(2S)-2-acetamido-3-methylbutanoyl]pyrrolidine-2-carbonyl]amino]-4-methylsulfanylbutanoyl]amino]-6-(4-aminobutyl)-24-benzyl-3-butyl-9-[3-(diaminomethylideneamino)propyl]-27-(hydroxymethyl)-30-methyl-12-(2-methylpropyl)-2,5,8,11,14,23,26,29,32-nonaoxo-18,19-dithia-1,4,7,10,13,22,25,28,31-nonazabicyclo[31.3.0]hexatriacontane-21-carbonyl]amino]-6-aminohexanoyl]pyrrolidine-2-carbonyl]pyrrolidine-2-carbonyl]amino]-5-amino-5-oxopentanoic acid	1164243: Inhibition of YAP/ GST-TEAD1 interaction in human Bel-7404 cells by GST pull-down assay	kd	0.0390	uM
(4S)-4-[[(2S)-1-[(2S)-1-[(2S)-2-[[(3S,6S,9S,12S,15S,21R,24S,27S,30S,33S)-15-[[(2S)-2-[[(2S)-1-[(2S)-2-acetamido-3-methylbutanoyl]pyrrolidine-2-carbonyl]amino]heptanoyl]amino]-6-(4-aminobutyl)-24-benzyl-3-butyl-9-[3-(diaminomethylideneamino)propyl]-27-(hydroxymethyl)-30-methyl-12-(2-methylpropyl)-2,5,8,11,14,23,26,29,32-nonaoxo-18,19-dithia-1,4,7,10,13,22,25,28,31-nonazabicyclo[31.3.0]hexatriacontane-21-carbonyl]amino]-6-aminohexanoyl]pyrrolidine-2-carbonyl]pyrrolidine-2-carbonyl]amino]-5-amino-5-oxopentanoic acid	1164242: Inhibition of YAP/ GST-TEAD1 (unknown origin) interaction by surface plasmon resonance assay	ic50	0.0410	uM
1-[(3R,4R)-3-[4-(oxan-4-yl)triazol-1-yl]-4-[[4-(trifluoromethyl)phenyl]methoxy]pyrrolidin-1-yl]prop-2-en-1-one	2084131: Inhibition of N-terminal His-tagged human TEAD1 expressed in Escherichia coli BL21 (DE3) (209 to 424 residues) by affinity chromatography analysis	ic50	0.0450	uM
(4S)-4-[[(2S)-1-[(2S)-1-[(2S)-2-[[(3S,6S,9S,12S,15S,21R,24S,27S,30S,33S)-15-[[(2S)-2-[[(2S)-1-[(2S)-2-acetamido-3-methylbutanoyl]pyrrolidine-2-carbonyl]amino]-4-methylsulfanylbutanoyl]amino]-6-(4-aminobutyl)-3-butyl-9-[3-(diaminomethylideneamino)propyl]-24-[(4-fluorophenyl)methyl]-27-(hydroxymethyl)-30-methyl-12-(2-methylpropyl)-2,5,8,11,14,23,26,29,32-nonaoxo-18,19-dithia-1,4,7,10,13,22,25,28,31-nonazabicyclo[31.3.0]hexatriacontane-21-carbonyl]amino]-6-aminohexanoyl]pyrrolidine-2-carbonyl]pyrrolidine-2-carbonyl]amino]-5-amino-5-oxopentanoic acid	1164242: Inhibition of YAP/ GST-TEAD1 (unknown origin) interaction by surface plasmon resonance assay	ic50	0.0750	uM
N-[4-(2-adamantyl)phenyl]-2-(1H-1,2,4-triazol-5-ylsulfanyl)acetamide	1494162: Inhibition of Gal4-fused TEAD 1 (unknown origin) interaction with YAP expressed in human 293T cells by Dual-Glo luciferase reporter gene assay	ic50	0.0830	uM
N-[5-cyano-4-[(E)-2-(4,4-difluorocyclohexyl)ethenyl]-2-pyridinyl]prop-2-enamide	2007280: Inhibition of His-tagged TEAD1 (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	2007280: Inhibition of His-tagged TEAD1 (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	2007280: Inhibition of His-tagged TEAD1 (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-[3-[[3-(trifluoromethyl)phenoxy]methyl]cyclobutyl]prop-2-enamide	2007288: Inhibition of TEAD1 mediated gene transcription in human MCF7 cells incubated overnight by luciferase reporter assay	ic50	0.1000	uM
N-[6-[[3-(trifluoromethyl)phenyl]methylamino]spiro[3.3]heptan-2-yl]prop-2-enamide	2007288: Inhibition of TEAD1 mediated gene transcription in human MCF7 cells incubated overnight by luciferase reporter assay	ic50	0.1000	uM
N-[4-(5-butyl-1,2-oxazol-3-yl)phenyl]prop-2-enamide	2007284: Inhibition of TEAD1 mediating gene expression in human MCF7 cells incubated overnight by luciferase reporter assay	ic50	0.1000	uM
N-[4-(1-pentylpyrazol-3-yl)phenyl]prop-2-enamide	2007284: Inhibition of TEAD1 mediating gene expression in human MCF7 cells incubated overnight by luciferase reporter assay	ic50	0.1000	uM
N-[3-chloro-4-[5-(trifluoromethyl)-1,2,4-oxadiazol-3-yl]phenyl]prop-2-enamide	2007284: Inhibition of TEAD1 mediating gene expression in human MCF7 cells incubated overnight by luciferase reporter assay	ic50	0.1000	uM
N-[3-[[3-(trifluoromethyl)phenoxy]methyl]-1-bicyclo[1.1.1]pentanyl]prop-2-enamide	2007288: Inhibition of TEAD1 mediated gene transcription in human MCF7 cells incubated overnight by luciferase reporter assay	ic50	0.1000	uM
2-methyl-4-[4-(trifluoromethyl)phenyl]pyrazolo[3,4-b]indole-7-carboxylic acid	1892894: Binding affinity to human TEAD1 (209 to 426 residues) expressed in Escherichia coli BL21 Star (DE3) by surface plasmon resonance assay	kd	0.1200	uM
2-fluoro-1-[(3R,4R)-3-(4-pyridin-3-yltriazol-1-yl)-4-[[4-(trifluoromethyl)phenyl]methoxy]pyrrolidin-1-yl]prop-2-en-1-one	2088626: Binding affinity to human recombinant N-terminal His-tagged TEAD1 (residues 209 to 424) expressed in Escherichia coli BL21 (DE3) assessed as dissociation constant	kd	0.1700	uM
4-[4-(trifluoromethyl)anilino]-1,3-dihydroisoindole-2-carbonitrile	1964891: Displacement of FAM- labeled YAP1 peptide (60 to 99 residues) from human TEAD1 (209 to 426 residues) expressed in Escherichia coli BL21 (DE3) cells incubated for 24 hrs by fluorescence polarization-based competitive binding assay	ic50	0.2000	uM
5-fluoro-4-[3-(trifluoromethyl)anilino]-1,3-dihydroisoindole-2-carbonitrile	1964891: Displacement of FAM- labeled YAP1 peptide (60 to 99 residues) from human TEAD1 (209 to 426 residues) expressed in Escherichia coli BL21 (DE3) cells incubated for 24 hrs by fluorescence polarization-based competitive binding assay	ic50	0.2000	uM
(4S)-4-[[(2S)-1-[(2S)-1-[(2S)-2-[[(3S,6S,9S,12S,15S,21R,24S,27S,30S,33S)-15-[[(2S)-2-[[(2S)-1-[(2S)-2-acetamido-3-methylbutanoyl]pyrrolidine-2-carbonyl]amino]-4-methylsulfanylbutanoyl]amino]-6-(4-aminobutyl)-24-benzyl-3-butyl-9-(3-carbamimidamidopropyl)-30-(carboxymethyl)-27-(hydroxymethyl)-12-(2-methylpropyl)-2,5,8,11,14,23,26,29,32-nonaoxo-18,19-dithia-1,4,7,10,13,22,25,28,31-nonazabicyclo[31.3.0]hexatriacontane-21-carbonyl]amino]-6-aminohexanoyl]pyrrolidine-2-carbonyl]pyrrolidine-2-carbonyl]amino]-5-amino-5-oxopentanoic acid	1164243: Inhibition of YAP/ GST-TEAD1 interaction in human Bel-7404 cells by GST pull-down assay	kd	0.2110	uM
5-methoxy-4-[3-(trifluoromethyl)anilino]-1,3-dihydroisoindole-2-carbonitrile	1964891: Displacement of FAM- labeled YAP1 peptide (60 to 99 residues) from human TEAD1 (209 to 426 residues) expressed in Escherichia coli BL21 (DE3) cells incubated for 24 hrs by fluorescence polarization-based competitive binding assay	ic50	0.3000	uM
(4S)-4-[[(2S)-1-[(2S)-1-[(2S)-2-[[(3S,6S,9S,12S,15S,21R,24S,27S,30S,33S)-15-[[(2S)-2-[[(2S)-1-[(2S)-2-acetamido-3-methylbutanoyl]pyrrolidine-2-carbonyl]amino]-4-methylsulfanylbutanoyl]amino]-6-(4-aminobutyl)-24-benzyl-9-[3-(diaminomethylideneamino)propyl]-27-(hydroxymethyl)-30-methyl-3-(4-methylpentyl)-12-(2-methylpropyl)-2,5,8,11,14,23,26,29,32-nonaoxo-18,19-dithia-1,4,7,10,13,22,25,28,31-nonazabicyclo[31.3.0]hexatriacontane-21-carbonyl]amino]-6-aminohexanoyl]pyrrolidine-2-carbonyl]pyrrolidine-2-carbonyl]amino]-5-amino-5-oxopentanoic acid	1164242: Inhibition of YAP/ GST-TEAD1 (unknown origin) interaction by surface plasmon resonance assay	ic50	0.3100	uM
(4S)-4-[[(2S)-1-[(2S)-1-[(2S)-2-[[(3S,6S,9S,12S,15S,21R,24S,27S,30S,33S)-15-[[(2S)-2-[[(2S)-1-[(2S)-2-acetamido-3-methylbutanoyl]pyrrolidine-2-carbonyl]amino]hexanoyl]amino]-6-(4-aminobutyl)-24-benzyl-3-butyl-9-[3-(diaminomethylideneamino)propyl]-27-(hydroxymethyl)-30-methyl-12-(2-methylpropyl)-2,5,8,11,14,23,26,29,32-nonaoxo-18,19-dithia-1,4,7,10,13,22,25,28,31-nonazabicyclo[31.3.0]hexatriacontane-21-carbonyl]amino]-6-aminohexanoyl]pyrrolidine-2-carbonyl]pyrrolidine-2-carbonyl]amino]-5-amino-5-oxopentanoic acid	1164242: Inhibition of YAP/ GST-TEAD1 (unknown origin) interaction by surface plasmon resonance assay	ic50	0.3400	uM
(4S)-4-[[(2S)-1-[(2S)-1-[(2S)-2-[[(3S,6S,9S,12S,15S,21R,24S,27S,30S,33S)-15-[[(2S)-2-[[(2S)-1-[(2S)-2-acetamido-3-methylbutanoyl]pyrrolidine-2-carbonyl]amino]-3-phenylpropanoyl]amino]-6-(4-aminobutyl)-24-benzyl-3-butyl-9-(3-carbamimidamidopropyl)-27-(hydroxymethyl)-30-methyl-12-(2-methylpropyl)-2,5,8,11,14,23,26,29,32-nonaoxo-18,19-dithia-1,4,7,10,13,22,25,28,31-nonazabicyclo[31.3.0]hexatriacontane-21-carbonyl]amino]-6-aminohexanoyl]pyrrolidine-2-carbonyl]pyrrolidine-2-carbonyl]amino]-5-amino-5-oxopentanoic acid	1164242: Inhibition of YAP/ GST-TEAD1 (unknown origin) interaction by surface plasmon resonance assay	ic50	0.3500	uM
(4S)-4-[[(2S)-1-[(2S)-1-[(2S)-2-[[(3S,6S,9S,12S,15S,21R,24S,27S,30S,33S)-15-[[(2S)-2-[[(2S)-1-[(2S)-2-acetamido-3-methylbutanoyl]pyrrolidine-2-carbonyl]amino]-4-methylsulfanylbutanoyl]amino]-6-(4-aminobutyl)-24-benzyl-9-[3-(diaminomethylideneamino)propyl]-3-hexyl-27-(hydroxymethyl)-30-methyl-12-(2-methylpropyl)-2,5,8,11,14,23,26,29,32-nonaoxo-18,19-dithia-1,4,7,10,13,22,25,28,31-nonazabicyclo[31.3.0]hexatriacontane-21-carbonyl]amino]-6-aminohexanoyl]pyrrolidine-2-carbonyl]pyrrolidine-2-carbonyl]amino]-5-amino-5-oxopentanoic acid	1164242: Inhibition of YAP/ GST-TEAD1 (unknown origin) interaction by surface plasmon resonance assay	ic50	0.3700	uM
(4S)-4-[[(2S)-1-[(2S)-1-[(2S)-2-[[(3S,6S,9S,12S,15S,21R,24S,27S,30S,33S)-15-[[(2S)-2-[[(2S)-1-[(2S)-2-acetamido-3-methylbutanoyl]pyrrolidine-2-carbonyl]amino]-3-(2-chlorophenyl)propanoyl]amino]-6-(4-aminobutyl)-24-benzyl-3-butyl-9-(3-carbamimidamidopropyl)-27-(hydroxymethyl)-30-methyl-12-(2-methylpropyl)-2,5,8,11,14,23,26,29,32-nonaoxo-18,19-dithia-1,4,7,10,13,22,25,28,31-nonazabicyclo[31.3.0]hexatriacontane-21-carbonyl]amino]-6-aminohexanoyl]pyrrolidine-2-carbonyl]pyrrolidine-2-carbonyl]amino]-5-amino-5-oxopentanoic acid	1164242: Inhibition of YAP/ GST-TEAD1 (unknown origin) interaction by surface plasmon resonance assay	ic50	0.3800	uM
(4S)-4-[[(2S)-1-[(2S)-1-[(2S)-2-[[(3S,6S,9S,12S,15S,21R,24S,27S,30S,33S)-15-[[(2S)-2-[[(2S)-1-[(2S)-2-acetamido-3-methylbutanoyl]pyrrolidine-2-carbonyl]amino]-3-(4-chlorophenyl)propanoyl]amino]-6-(4-aminobutyl)-24-benzyl-3-butyl-9-(3-carbamimidamidopropyl)-27-(hydroxymethyl)-30-methyl-12-(2-methylpropyl)-2,5,8,11,14,23,26,29,32-nonaoxo-18,19-dithia-1,4,7,10,13,22,25,28,31-nonazabicyclo[31.3.0]hexatriacontane-21-carbonyl]amino]-6-aminohexanoyl]pyrrolidine-2-carbonyl]pyrrolidine-2-carbonyl]amino]-5-amino-5-oxopentanoic acid	1164242: Inhibition of YAP/ GST-TEAD1 (unknown origin) interaction by surface plasmon resonance assay	ic50	0.5300	uM
1-[4-(2-phenoxyethyl)piperidin-1-yl]prop-2-en-1-one	2007286: Inhibition of N-terminal 6xHis-tagged human TEAD1 auto palmitoylation (209 to 426 residues) expressed in Escherichia coli BL21 (DE3) cells by ABPP assay	ic50	0.5800	uM
(4S)-4-[[(2S)-1-[(2S)-1-[(2S)-2-[[(3S,6S,9S,12S,15S,21R,24S,27S,30S,33S)-15-[[(2S)-2-[[(2S)-1-[(2S)-2-acetamido-3-methylbutanoyl]pyrrolidine-2-carbonyl]amino]-4-methylsulfanylbutanoyl]amino]-6-(4-aminobutyl)-24-benzyl-9-[3-(diaminomethylideneamino)propyl]-27-(hydroxymethyl)-30-methyl-3-(3-methylbutyl)-12-(2-methylpropyl)-2,5,8,11,14,23,26,29,32-nonaoxo-18,19-dithia-1,4,7,10,13,22,25,28,31-nonazabicyclo[31.3.0]hexatriacontane-21-carbonyl]amino]-6-aminohexanoyl]pyrrolidine-2-carbonyl]pyrrolidine-2-carbonyl]amino]-5-amino-5-oxopentanoic acid	1164242: Inhibition of YAP/ GST-TEAD1 (unknown origin) interaction by surface plasmon resonance assay	ic50	0.6200	uM
4-[3-(trifluoromethyl)anilino]-1,3-dihydroisoindole-2-carbonitrile	1964891: Displacement of FAM- labeled YAP1 peptide (60 to 99 residues) from human TEAD1 (209 to 426 residues) expressed in Escherichia coli BL21 (DE3) cells incubated for 24 hrs by fluorescence polarization-based competitive binding assay	ic50	0.9000	uM
4-[2-(trifluoromethyl)anilino]-1,3-dihydroisoindole-2-carbonitrile	1964891: Displacement of FAM- labeled YAP1 peptide (60 to 99 residues) from human TEAD1 (209 to 426 residues) expressed in Escherichia coli BL21 (DE3) cells incubated for 24 hrs by fluorescence polarization-based competitive binding assay	ic50	1.3000	uM
(4S)-4-[[(2S)-1-[(2S)-1-[(2S)-2-[[(3S,6S,9S,12S,15S,21R,24S,27S,30S,33S)-15-[[(2S)-2-[[(2S)-1-[(2S)-2-acetamido-3-methylbutanoyl]pyrrolidine-2-carbonyl]amino]-4-methylsulfanylbutanoyl]amino]-6-(4-aminobutyl)-24-benzyl-9-[3-(diaminomethylideneamino)propyl]-27-(hydroxymethyl)-30-methyl-3,12-bis(2-methylpropyl)-2,5,8,11,14,23,26,29,32-nonaoxo-18,19-dithia-1,4,7,10,13,22,25,28,31-nonazabicyclo[31.3.0]hexatriacontane-21-carbonyl]amino]-6-aminohexanoyl]pyrrolidine-2-carbonyl]pyrrolidine-2-carbonyl]amino]-5-amino-5-oxopentanoic acid	1164242: Inhibition of YAP/ GST-TEAD1 (unknown origin) interaction by surface plasmon resonance assay	ic50	1.5000	uM
4-[4-(trifluoromethyl)anilino]-1,3,3a,4,5,6,7,7a-octahydroisoindole-2-carbonitrile	1964891: Displacement of FAM- labeled YAP1 peptide (60 to 99 residues) from human TEAD1 (209 to 426 residues) expressed in Escherichia coli BL21 (DE3) cells incubated for 24 hrs by fluorescence polarization-based competitive binding assay	ic50	1.5000	uM
4-[3-(trifluoromethyl)anilino]-1,3,3a,4,5,6,7,7a-octahydroisoindole-2-carbonitrile	1964891: Displacement of FAM- labeled YAP1 peptide (60 to 99 residues) from human TEAD1 (209 to 426 residues) expressed in Escherichia coli BL21 (DE3) cells incubated for 24 hrs by fluorescence polarization-based competitive binding assay	ic50	1.6000	uM

CTD chemical–gene interactions

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

Chemical	Actions (top 5)	PubMed papers
Benzo(a)pyrene	affects methylation, decreases expression	3
bisphenol A	affects cotreatment, decreases methylation, decreases expression	2
Arsenic	affects methylation	2
Valproic Acid	decreases expression	2
7,8-Dihydro-7,8-dihydroxybenzo(a)pyrene 9,10-oxide	decreases expression	2
Cadmium Chloride	decreases reaction, increases abundance, increases palmitoylation, decreases expression	2
aristolochic acid I	decreases expression	1
FR900359	decreases phosphorylation	1
geldanamycin	increases expression	1
trichostatin A	decreases expression	1
beta-lapachone	decreases expression	1
arsenite	affects binding, decreases reaction	1
2-bromopalmitate	decreases reaction, increases abundance, increases palmitoylation	1
doxifluridine	decreases response to substance	1
coumarin	increases phosphorylation	1
cupric oxide	increases expression	1
1-UFT protocol	decreases response to substance	1
evodiamine	increases expression	1
perfluorooctane sulfonic acid	decreases expression	1
CGP 52608	affects binding, increases reaction	1
bisphenol S	decreases expression, affects cotreatment	1
jinfukang	affects cotreatment, decreases expression	1
Capecitabine	decreases response to substance	1
Sunitinib	increases expression	1
Fulvestrant	affects cotreatment, decreases methylation	1
Vorinostat	decreases expression	1
Cadmium	decreases reaction, increases abundance, increases palmitoylation	1
Cisplatin	affects cotreatment, decreases expression	1
Dichlorodiphenyl Dichloroethylene	decreases expression	1
Dexamethasone	affects cotreatment, decreases expression	1

ChEMBL screening assays

85 unique, capped per target: 82 binding, 3 functional

Representative assays (with source publication via chembl_document):

Assay ID	Type	Description	Source paper
CHEMBL4120894	Binding	Binding affinity to human GST-tagged TEAD1 (194 to 411) expressed in Escherichia coli BL21(DE3) by SPR assay	Targeting Transcriptional Enhanced Associate Domains (TEADs). — J Med Chem
CHEMBL6104673	Functional	In vivo PROTAC activity at CRBN/TEAD1 in human MSTO-211H cells xenografted in BALB/c nude mouse assessed as induction of TEAD1 degradation at 50 mg/kg, ip administered as single dose measured for 4 hrs by Western blot analysis	Selective Degradation of TEADs by a PROTAC Molecule Exhibited Robust Anticancer Efficacy In Vitro and In Vivo. — J Med Chem

Cellosaurus cell lines

2 cell lines: 1 embryonic stem cell, 1 cancer cell line

First 10 cell lines (id-ordered, not curated):

Cellosaurus	Name	Category	Sex
CVCL_A8RC	WAe001-A-67	Embryonic stem cell	Male
CVCL_B1HW	Abcam A-549 TEAD1 KO	Cancer cell line	Male

Clinical trials (associated diseases)

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

Trial	Phase	Status	Title
NCT04224207	PHASE3	COMPLETED	Management of Retinitis Pigmentosa by Mesenchymal Stem Cells by Wharton’s Jelly Derived Mesenchymal Stem Cells
NCT07082855	PHASE3	NOT_YET_RECRUITING	A Multicenter, Randomized, Double-Blind, Controlled Clinical Study of Minocycline for the Treatment of Retinitis Pigmentosa
NCT03763227	PHASE2	COMPLETED	Intravitreal Ranibizumab (Lucentis®) in the Treatment of Non-leaking Macular Cysts in Retinal Dystrophy
NCT04068207	PHASE2	COMPLETED	Minocycline Treatment in Retinitis Pigmentosa
NCT04945772	PHASE2	COMPLETED	Efficacy and Safety of MCO-010 Optogenetic Therapy in Adults With Retinitis Pigmentosa [RESTORE]
NCT05902962	PHASE1	COMPLETED	SAD of IVT VP-001 in PRPF31 Mutation-Associated Retinal Dystrophy Subjects
NCT06319872	PHASE1	RECRUITING	The Effects of Disulfiram (Antabuse®) on Visual Acuity in Patients With Retinal Degeneration
NCT06455826	PHASE1	COMPLETED	MAD of IVT VP-001 in PRPF31 Mutation-Associated Retinal Dystrophy Subjects (Wallaby)
NCT00305305	Not specified	UNKNOWN	Brain Development Research Program
NCT00697411	Not specified	RECRUITING	Study of Selected X-Linked Disorders: Aicardi Syndrome
NCT04855045	PHASE2/PHASE3	UNKNOWN	An Open-label, Dose Escalation and Double-masked, Randomized, Controlled Trial Evaluating Safety and Tolerability of Sepofarsen in Children (<8 Years of Age) With LCA10 Caused by Mutations in the CEP290 Gene.
NCT03872479	PHASE1/PHASE2	UNKNOWN	Single Ascending Dose Study in Participants With LCA10
NCT04123626	PHASE1/PHASE2	ACTIVE_NOT_RECRUITING	A Study to Evaluate the Safety and Tolerability of QR-1123 in Subjects With Autosomal Dominant Retinitis Pigmentosa Due to the P23H Mutation in the RHO Gene
NCT04545736	PHASE1/PHASE2	RECRUITING	Oral Metformin for Treatment of ABCA4 Retinopathy
NCT06212297	PHASE1/PHASE2	ACTIVE_NOT_RECRUITING	Fellow-eye Study (FE) of LX101 in Subjects With Inherited Retinal Dystrophy
NCT06852963	PHASE1/PHASE2	ACTIVE_NOT_RECRUITING	A Repeat-Dose, Open-Label, Two Arm Safety and Efficacy Study of Two Doses of VP-001 Administered Intravitreally in Participants With Confirmed PRPF31 Mutation-Associated Retinal Dystrophy, Including Participants Previously Treated With VP001
NCT07177196	PHASE1/PHASE2	ACTIVE_NOT_RECRUITING	Personalized Antisense Oligonucleotide Therapy for a Single Participant With PRPH2 Mutation Associated With Retinal Dystrophy
NCT07063030	EARLY_PHASE1	RECRUITING	A Study of LX107 Gene Therapy in AIPL1-IRD Patients
NCT01546181	Not specified	COMPLETED	Retinal Imaging by Adaptive Optics in Healthy Eyes and During Retinal and General Diseases
NCT01876147	Not specified	COMPLETED	Visual and Functional Assessment in Low Vision Patients
NCT01920867	Not specified	UNKNOWN	Stem Cell Ophthalmology Treatment Study
NCT02014389	Not specified	RECRUITING	Evaluation of Objective Perimetry Using Chromatic Multifocal Pupillometer
NCT02983305	Not specified	COMPLETED	Optical Head-Mounted Display Technology for Low Vision Rehabilitation
NCT03592017	Not specified	COMPLETED	Performance of Long-wavelength Autofluorescence Imaging
NCT03662386	Not specified	TERMINATED	Prospective Analysis of Genotype-phenotype Correlations Observed in a Large Cohort of Patients With Hereditary Retinal Dystrophies - GEPHIRD
NCT03691168	Not specified	UNKNOWN	Multi-center Observation of the Natural Course of Inherited Retinal Dystrophies
NCT03843840	Not specified	COMPLETED	Dual Wavelength OCT
NCT03853252	Not specified	COMPLETED	iPS Cells of Patients for Models of Retinal Dystrophies
NCT05130385	Not specified	UNKNOWN	High Resolution Optical Coherence Tomography
NCT05294978	Not specified	RECRUITING	EyeConic: Qualification for Cone-Optogenetics
NCT05573984	Not specified	ACTIVE_NOT_RECRUITING	Natural History of PRPF31 Mutation-Associated Retinal Dystrophy
NCT05793515	Not specified	COMPLETED	Mechanisms of Inherited Retinal Dystrophies Using Whole Genome Sequencing and in Vitro and in Vivo Models
NCT05820100	Not specified	COMPLETED	Observational Study to Assess the Reliability and Validity of the MLYMT and MLSDT
NCT05976139	Not specified	RECRUITING	Micropulsed Laser in Patients With Macular Oedema in Retinal Dystrophies
NCT06162585	Not specified	ACTIVE_NOT_RECRUITING	Non-Interventional Long Term Follow-up Study of Participants Previously Enrolled in the RESTORE Study
NCT06177977	Not specified	RECRUITING	SS-HH-OCT as a Novel Diagnostic Modality for Early-Onset Retinal Dystrophies (EORDs)
NCT06375239	Not specified	RECRUITING	Observational Study to Assess Endpoint Operational Feasibility & Measurement Properties in Patients with Retinal Degeneration
NCT06908161	Not specified	NOT_YET_RECRUITING	Functional Assessments in Vision Impairment
NCT07085533	Not specified	RECRUITING	Natural History Study of Inherited Retinal Diseases
NCT07502664	Not specified	RECRUITING	Development and Evaluation of Functional Visual Field and Navigation Endpoints in Moderate to Profound Inherited Retinal Disease (DEFINE-IRD)