PEF1

Summary

PEF1 (penta-EF-hand domain containing 1, HGNC:30009) is a protein-coding gene on chromosome 1p35.2, encoding Peflin (Q9UBV8). Calcium-binding protein that acts as an adapter that bridges unrelated proteins or stabilizes weak protein-protein complexes in response to calcium. It is a selective cancer dependency (DepMap: 27.8% of cell lines).

This gene encodes a calcium-binding protein belonging to the penta-EF-hand protein family. The encoded protein has been shown to form a heterodimer with the programmed cell death 6 gene product and may modulate its function in Ca(2+) signaling. Alternative splicing results in multiple transcript variants and a pseudogene has been identified on chromosome 1.

Source: NCBI Gene 553115 — RefSeq curated summary.

At a glance

• GWAS associations: 9
• Clinical variants (ClinVar): 17 total
• Druggable target: yes
• Cancer dependency (DepMap): dependent in 27.8% of screened cell lines
• MANE Select transcript: NM_012392

Identifiers

Gene identifiers

Field	Value
HGNC ID	HGNC:30009
Approved symbol	PEF1
Name	penta-EF-hand domain containing 1
Location	1p35.2
Locus type	gene with protein product
Status	Approved
Aliases	PEF1A
Ensembl gene	ENSG00000162517
Ensembl biotype	protein_coding
OMIM	610033
Entrez	553115

Gene structure

Transcript identifiers

Ensembl transcripts: 13 — 7 protein_coding_CDS_not_defined, 6 protein_coding

ENST00000373703, ENST00000461006, ENST00000471219, ENST00000472443, ENST00000478502, ENST00000489164, ENST00000492061, ENST00000496805, ENST00000859307, ENST00000859308, ENST00000859309, ENST00000911438, ENST00000966434

RefSeq mRNA: 2 — MANE Select: NM_012392 NM_001359651, NM_012392

CCDS: CCDS345

Canonical transcript exons

ENST00000373703 — 5 exons

Exon	Start	End
ENSE00001461333	31629866	31630842
ENSE00001838580	31644841	31644876
ENSE00003519178	31632495	31632638
ENSE00003589334	31633159	31633314
ENSE00003635225	31635222	31635522

Expression profiles

Bgee: expression breadth ubiquitous, 285 present calls, max score 98.18.

FANTOM5 (CAGE): breadth ubiquitous, TPM avg 39.7121 / max 250.6897, expressed in 1812 samples.

FANTOM5 promoters (2 alternative TSS)

Promoter ID	TPM avg	Samples expressed
11470	39.5995	1812
201451	0.1125	26

Top tissues by expression

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

Tissue	Anatomy ID	Expression score	Quality
left lobe of thyroid gland	UBERON:0001120	98.18	gold quality
right lobe of thyroid gland	UBERON:0001119	98.16	gold quality
thyroid gland	UBERON:0002046	97.69	gold quality
ascending aorta	UBERON:0001496	97.18	gold quality
skin of leg	UBERON:0001511	97.17	gold quality
thoracic aorta	UBERON:0001515	97.17	gold quality
aorta	UBERON:0000947	97.00	gold quality
skin of abdomen	UBERON:0001416	96.99	gold quality
popliteal artery	UBERON:0002250	96.93	gold quality
tibial artery	UBERON:0007610	96.92	gold quality
descending thoracic aorta	UBERON:0002345	96.87	gold quality
right coronary artery	UBERON:0001625	96.62	gold quality
left coronary artery	UBERON:0001626	96.56	gold quality
coronary artery	UBERON:0001621	96.38	gold quality
lower esophagus	UBERON:0013473	96.30	gold quality
lower esophagus muscularis layer	UBERON:0035833	96.30	gold quality
esophagogastric junction muscularis propria	UBERON:0035841	96.30	gold quality
upper lobe of left lung	UBERON:0008952	96.24	gold quality
prefrontal cortex	UBERON:0000451	96.13	gold quality
right adrenal gland	UBERON:0001233	96.02	gold quality
right adrenal gland cortex	UBERON:0035827	95.99	gold quality
body of uterus	UBERON:0009853	95.97	gold quality
apex of heart	UBERON:0002098	95.94	gold quality
zone of skin	UBERON:0000014	95.92	gold quality
upper lobe of lung	UBERON:0008948	95.92	gold quality
left uterine tube	UBERON:0001303	95.88	gold quality
right lung	UBERON:0002167	95.83	gold quality
right frontal lobe	UBERON:0002810	95.83	gold quality
ectocervix	UBERON:0012249	95.83	gold quality
left adrenal gland	UBERON:0001234	95.73	gold quality

Single-cell (SCXA)

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

Experiment	Marker?	Max mean expression
E-ANND-3	no	0.00

Regulation

Is transcription factor: no

miRNA regulators (miRDB)

35 targeting PEF1, 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-4455	100.00	65.48	1587
HSA-MIR-7110-3P	100.00	73.18	2486
HSA-MIR-4531	99.99	69.70	3181
HSA-MIR-12136	99.98	72.81	5713
HSA-MIR-6124	99.87	69.78	3551
HSA-MIR-7150	99.62	66.80	1322
HSA-MIR-4516	99.61	67.78	3390
HSA-MIR-885-5P	99.59	68.59	879
HSA-MIR-1207-5P	99.49	69.11	2983
HSA-MIR-4441	99.49	66.56	3216
HSA-MIR-12131	99.48	68.72	1673
HSA-MIR-6081	99.48	66.07	1446
HSA-MIR-4254	99.11	65.15	1315
HSA-MIR-4763-3P	99.10	67.83	2649
HSA-MIR-4270	99.02	66.26	1987
HSA-MIR-6760-5P	98.87	66.73	1515
HSA-MIR-5000-3P	98.79	65.63	1251
HSA-MIR-6754-5P	98.60	65.54	1627
HSA-MIR-12125	98.59	67.54	1044
HSA-MIR-7843-3P	98.31	67.94	803
HSA-MIR-653-3P	98.31	67.71	1542
HSA-MIR-4457	98.09	67.12	1274
HSA-MIR-4436A	98.05	64.83	1140
HSA-MIR-4468	98.01	66.85	1187
HSA-MIR-4736	97.96	65.89	1287
HSA-MIR-127-5P	97.78	67.64	869
HSA-MIR-4799-3P	97.78	65.97	893
HSA-MIR-22-5P	97.67	68.92	1355
HSA-MIR-4720-5P	97.46	65.67	893
HSA-MIR-5588-5P	97.46	65.70	913

Functional genomics

DepMap (CRISPR cell-line fitness): dependent in 27.8% of screened cell lines.

Literature-anchored findings (GeneRIF, showing 2)

• peflin is stabilized by dimerization through its fifth EF-hand region (PMID:11883899)
• This work identifies for the first time a clear steady state role for a PEF protein in ER-to-Golgi transport-peflin is a negative regulator of transport. (PMID:27276012)

Cross-species orthologs

11 orthologs

Organism	Symbol	Gene ID
danio_rerio	pef1	ENSDARG00000023989
mus_musculus	Pef1	ENSMUSG00000028779
rattus_norvegicus	Pef1	ENSRNOG00000013972
caenorhabditis_elegans		WBGENE00000542
caenorhabditis_elegans	clp-3	WBGENE00000544
caenorhabditis_elegans		WBGENE00000546
caenorhabditis_elegans		WBGENE00000547
caenorhabditis_elegans	clp-8	WBGENE00009695
caenorhabditis_elegans	clpr-3	WBGENE00010417
caenorhabditis_elegans	clpr-1	WBGENE00012233
caenorhabditis_elegans	clpr-3	WBGENE00013184

Paralogs (20): CAPN1 (ENSG00000014216), SRI (ENSG00000075142), CAPN6 (ENSG00000077274), CAPN3 (ENSG00000092529), CAPN15 (ENSG00000103326), GCA (ENSG00000115271), ADGB (ENSG00000118492), CAPNS1 (ENSG00000126247), CAPN7 (ENSG00000131375), CAPN9 (ENSG00000135773), CAPN11 (ENSG00000137225), CAPN10 (ENSG00000142330), CAPN5 (ENSG00000149260), CAPN2 (ENSG00000162909), CAPN13 (ENSG00000162949), CAPN12 (ENSG00000182472), CAPN8 (ENSG00000203697), CAPN14 (ENSG00000214711), PDCD6 (ENSG00000249915), CAPNS2 (ENSG00000256812)

Protein

Protein identifiers

Peflin — Q9UBV8 (reviewed: Q9UBV8)

Alternative names: PEF protein with a long N-terminal hydrophobic domain, Penta-EF hand domain-containing protein 1

All UniProt accessions (2): A0A384MQX5, Q9UBV8

UniProt curated annotations — full annotation on UniProt →

Function. Calcium-binding protein that acts as an adapter that bridges unrelated proteins or stabilizes weak protein-protein complexes in response to calcium. Together with PDCD6, acts as a calcium-dependent adapter for the BCR(KLHL12) complex, a complex involved in endoplasmic reticulum (ER)-Golgi transport by regulating the size of COPII coats. In response to cytosolic calcium increase, the heterodimer formed with PDCD6 interacts with, and bridges together the BCR(KLHL12) complex and SEC31 (SEC31A or SEC31B), promoting monoubiquitination of SEC31 and subsequent collagen export, which is required for neural crest specification. Its role in the heterodimer formed with PDCD6 is however unclear: some evidence shows that PEF1 and PDCD6 work together and promote association between PDCD6 and SEC31 in presence of calcium. Other reports show that PEF1 dissociates from PDCD6 in presence of calcium, and may act as a negative regulator of PDCD6. Also acts as a negative regulator of ER-Golgi transport; possibly by inhibiting interaction between PDCD6 and SEC31.

Subunit / interactions. Heterodimer; heterodimerizes (via the EF-hand 5) with PDCD6. Dissociates from PDCD6 in presence of calcium.

Subcellular location. Cytoplasm. Endoplasmic reticulum. Membrane. Cytoplasmic vesicle. COPII-coated vesicle membrane.

Post-translational modifications. Ubiquitinated by the BCR(KLHL12) E3 ubiquitin ligase complex.

RefSeq proteins (2): NP_001346580, NP_036524* (*=MANE)

Domains & families (InterPro)

ID	Name	Type
IPR002048	EF_hand_dom	Domain
IPR011992	EF-hand-dom_pair	Homologous_superfamily
IPR018247	EF_Hand_1_Ca_BS	Binding_site
IPR051426	Peflin/Sorcin_CaBP	Family

Pfam: PF13405, PF13499

UniProt features (36 total): binding site 10, repeat 9, domain 5, compositionally biased region 4, region of interest 3, mutagenesis site 3, chain 1, cross-link 1

Structure

Experimental structures (PDB)

1 structures.

PDB	Method	Resolution (Å)
8RBH	X-RAY DIFFRACTION	1.88

Predicted structure (AlphaFold)

Model	pLDDT	Fraction very-high
AF-Q9UBV8-F1	75.78	0.60

Functional residue map

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

Ligand- & substrate-binding residues (10): 127; 129; 131; 133; 138; 194; 196; 198; 200; 205

Post-translational modifications (1): 137

Mutagenesis-validated functional residues (3):

Position	Phenotype
137	decreased ubiquitination by the bcr(klhl12) e3 ubiquitin ligase complex.
165	does not affect ubiquitination by the bcr(klhl12) e3 ubiquitin ligase complex.
167	does not affect ubiquitination by the bcr(klhl12) e3 ubiquitin ligase complex.

Function

Pathways and Gene Ontology

Reactome pathways

0 pathways

MSigDB gene sets: 171 (showing top): GOBP_EMBRYO_DEVELOPMENT_ENDING_IN_BIRTH_OR_EGG_HATCHING, CHIARADONNA_NEOPLASTIC_TRANSFORMATION_KRAS_DN, GOBP_VESICLE_LOCALIZATION, GOBP_VESICLE_ORGANIZATION, GOBP_VESICLE_TARGETING, GOBP_VESICLE_MEDIATED_TRANSPORT, GOBP_RESPONSE_TO_METAL_ION, GOBP_ENDOPLASMIC_RETICULUM_TO_GOLGI_VESICLE_MEDIATED_TRANSPORT, GOBP_MESENCHYMAL_CELL_DIFFERENTIATION, GOCC_COATED_VESICLE, GOBP_PROTEIN_MONOUBIQUITINATION, GOBP_POST_TRANSLATIONAL_PROTEIN_MODIFICATION, GOCC_VESICLE_COAT, LASTOWSKA_NEUROBLASTOMA_COPY_NUMBER_DN, GOBP_MESENCHYME_DEVELOPMENT

GO Biological Process (6): endoplasmic reticulum to Golgi vesicle-mediated transport (GO:0006888), neural crest formation (GO:0014029), neural crest cell development (GO:0014032), COPII vesicle coat assembly (GO:0048208), response to calcium ion (GO:0051592), positive regulation of protein monoubiquitination (GO:1902527)

GO Molecular Function (9): RNA binding (GO:0003723), calcium ion binding (GO:0005509), identical protein binding (GO:0042802), protein heterodimerization activity (GO:0046982), protein dimerization activity (GO:0046983), calcium-dependent protein binding (GO:0048306), ubiquitin-like ligase-substrate adaptor activity (GO:1990756), protein binding (GO:0005515), metal ion binding (GO:0046872)

GO Cellular Component (8): cytoplasm (GO:0005737), endoplasmic reticulum (GO:0005783), COPII vesicle coat (GO:0030127), Cul3-RING ubiquitin ligase complex (GO:0031463), extracellular exosome (GO:0070062), ER to Golgi transport vesicle membrane (GO:0012507), membrane (GO:0016020), cytoplasmic vesicle (GO:0031410)

GO top-level categories

Rollup of top GO terms by namespace:

Category	Terms
cytoplasm	3
protein binding	3
cellular anatomical structure	2
intercellular transport	1
intracellular transport	1
Golgi vesicle transport	1
epithelial to mesenchymal transition	1
chordate embryonic development	1
anatomical structure formation involved in morphogenesis	1
neural crest cell differentiation	1
stem cell development	1
vesicle coat assembly	1
protein-containing complex assembly	1
COPII-coated vesicle budding	1
response to metal ion	1
protein monoubiquitination	1
positive regulation of protein ubiquitination	1
regulation of protein monoubiquitination	1
nucleic acid binding	1
metal ion binding	1
protein dimerization activity	1
calcium ion binding	1
enzyme-substrate adaptor activity	1
binding	1
cation binding	1
intracellular anatomical structure	1
endomembrane system	1
intracellular membrane-bounded organelle	1
ER to Golgi transport vesicle membrane	1
vesicle coat	1
cullin-RING ubiquitin ligase complex	1
extracellular vesicle	1
COPII-coated ER to Golgi transport vesicle	1
transport vesicle membrane	1
coated vesicle membrane	1
intracellular vesicle	1

Protein interactions and networks

STRING

1068 interactions, top by confidence (×1000):

Protein A	Protein B	Partner UniProt	Score
PEF1	KLHL12	Q53G59	882
PEF1	CUL3	Q13618	690
PEF1	ALG1	Q9BT22	652
PEF1	SEC13	P55735	635
PEF1	ANXA11	P50995	603
PEF1	SEC31A	O94979	599
PEF1	ALG6	Q9Y672	585
PEF1	MYC	P01106	531
PEF1	ANXA7	P20073	522
PEF1	PLTP	P55058	467
PEF1	SLCO6A1	Q86UG4	461
PEF1	EEF1A2	P54266	416
PEF1	EEF1A1	P04719	406
PEF1	SACK1B	Q5T0W9	398
PEF1	TINAGL1	Q9GZM7	385

IntAct

179 interactions, top by confidence:

A	B	Type	Score
KLHL12	CUL3	psi-mi:“MI:0914”(association)	0.920
PEF1	PDCD6	psi-mi:“MI:0915”(physical association)	0.900
PDCD6	PEF1	psi-mi:“MI:0915”(physical association)	0.900
PEF1	PDCD6	psi-mi:“MI:0914”(association)	0.900
KLHL12	PEF1	psi-mi:“MI:0915”(physical association)	0.880
PEF1	KLHL12	psi-mi:“MI:0915”(physical association)	0.880
PEF1	KLHL12	psi-mi:“MI:0914”(association)	0.880
KLHL12	KLHL2	psi-mi:“MI:0914”(association)	0.850
H2AX	PARP1	psi-mi:“MI:0914”(association)	0.840
FOXR2	PEF1	psi-mi:“MI:0915”(physical association)	0.780
PEF1	FOXR2	psi-mi:“MI:0915”(physical association)	0.780
PEF1	DAZAP2	psi-mi:“MI:0915”(physical association)	0.760
DAZAP2	PEF1	psi-mi:“MI:0915”(physical association)	0.760

BioGRID (163): PEF1 (Two-hybrid), PEF1 (Two-hybrid), PEF1 (Two-hybrid), PEF1 (Two-hybrid), PEF1 (Two-hybrid), PEF1 (Two-hybrid), PEF1 (Two-hybrid), PEF1 (Two-hybrid), KIAA0930 (Affinity Capture-MS), HIST2H2AB (Affinity Capture-MS), FASN (Co-fractionation), PDCD6 (Co-fractionation), PDCD6IP (Co-fractionation), PEF1 (Co-fractionation), PEF1 (Co-fractionation)

ESM2 similar proteins: A0A0D1C8Z4, A5A6H4, A7VJC2, O88569, P04256, P07909, P09651, P09867, P17130, P19198, P21522, P22626, P35637, P48810, P49312, P51968, P51989, P51990, P51991, P51992, P56959, Q01844, Q08473, Q13151, Q22037, Q28009, Q28521, Q2HJ60, Q32P51, Q43472, Q5PQ53, Q5RBU8, Q61545, Q640A2, Q641Z8, Q6DC93, Q6URK4, Q7ZX83, Q8BG05, Q8EA81

Diamond homologs: A6NHC0, G3V7W1, O75340, O88456, P02627, P04574, P04632, P05044, P06704, P06813, P07290, P07291, P12815, P13135, P28676, P30626, P42322, P48451, Q06BI3, Q12798, Q1PFH8, Q24214, Q2QY10, Q38868, Q39584, Q5PQ53, Q5R4U9, Q5RAI6, Q641Z8, Q64537, Q6DC93, Q6F334, Q6P069, Q8BFY6, Q8VC88, Q8W4L0, Q94743, Q95YL5, Q96L46, Q9BXU9

SIGNOR signaling

0 interactions.

Enriched among interaction partners

Reactome pathways and GO biological processes over-represented among this gene’s 80 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.

GO biological processes:

GO term	Partners	Fold	FDR
macroautophagy	5	16.9×	2e-03
endoplasmic reticulum to Golgi vesicle-mediated transport	8	15.3×	3e-05

Disease & clinical

Clinical variants and AI predictions

ClinVar

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

Classification	Count (floor)
Pathogenic	0
Likely pathogenic	0
Uncertain significance	13
Likely benign	2
Benign	0

Top pathogenic / likely-pathogenic (0)

SpliceAI

967 predictions. Top by Δscore:

Variant	Effect	Δscore
1:31632489:CCGCA:C	donor_loss	1.0000
1:31632490:CGCA:C	donor_loss	1.0000
1:31632491:GCACC:G	donor_loss	1.0000
1:31632492:CACCT:C	donor_loss	1.0000
1:31632493:ACC:A	donor_loss	1.0000
1:31632494:C:CA	donor_loss	1.0000
1:31632494:CCTTG:C	donor_gain	1.0000
1:31632543:A:AC	donor_gain	1.0000
1:31632544:C:CC	donor_gain	1.0000
1:31632544:CTG:C	donor_gain	1.0000
1:31632634:CATGT:C	acceptor_gain	1.0000
1:31632635:ATGT:A	acceptor_gain	1.0000
1:31632636:TGT:T	acceptor_gain	1.0000
1:31632637:GT:G	acceptor_gain	1.0000
1:31632639:C:CC	acceptor_gain	1.0000
1:31632639:CTGA:C	acceptor_loss	1.0000
1:31632640:T:C	acceptor_loss	1.0000
1:31632645:G:C	acceptor_gain	1.0000
1:31632645:G:GC	acceptor_gain	1.0000
1:31633157:A:AC	donor_gain	1.0000
1:31633158:C:CT	donor_gain	1.0000
1:31633158:CTT:C	donor_gain	1.0000
1:31633158:CTTAT:C	donor_gain	1.0000
1:31633161:A:AC	donor_gain	1.0000
1:31633161:AT:A	donor_gain	1.0000
1:31633161:ATCAT:A	donor_gain	1.0000
1:31633162:T:C	donor_gain	1.0000
1:31634828:CAGTA:C	donor_gain	1.0000
1:31635218:TTACC:T	donor_loss	1.0000
1:31635219:TACCC:T	donor_loss	1.0000

AlphaMissense

1829 scored. Top likely-pathogenic:

Variant	Protein change	am_pathogenicity
1:31632592:G:C	F176L	0.999
1:31632592:G:T	F176L	0.999
1:31632594:A:G	F176L	0.999
1:31632631:A:C	F163L	0.999
1:31632631:A:T	F163L	0.999
1:31632633:A:G	F163L	0.999
1:31630697:G:C	F257L	0.998
1:31630697:G:T	F257L	0.998
1:31630699:A:G	F257L	0.998
1:31630739:G:C	F243L	0.998
1:31630739:G:T	F243L	0.998
1:31630741:A:G	F243L	0.998
1:31632503:A:G	L206P	0.998
1:31633187:G:C	F151L	0.998
1:31633187:G:T	F151L	0.998
1:31633189:A:G	F151L	0.998
1:31633224:A:G	L139P	0.998
1:31633271:G:C	F123L	0.998
1:31633271:G:T	F123L	0.998
1:31633272:A:G	F123S	0.998
1:31633273:A:G	F123L	0.998
1:31630641:A:T	V276D	0.997
1:31630740:A:G	F243S	0.997
1:31632550:G:C	F190L	0.997
1:31632550:G:T	F190L	0.997
1:31632552:A:G	F190L	0.997
1:31632593:A:G	F176S	0.997
1:31633239:A:T	I134N	0.997
1:31630698:A:G	F257S	0.996
1:31630719:A:G	L250P	0.996

dbSNP variants (sampled 300 via entrez): RS1000078239 (1:31638873 C>T), RS1000251485 (1:31634903 T>C), RS1000298287 (1:31642193 A>G), RS1000683782 (1:31640566 C>A,T), RS1000849736 (1:31635572 C>A), RS1000901823 (1:31635284 C>A,T), RS1001072444 (1:31642381 A>G), RS1001181042 (1:31637241 G>A), RS1001233361 (1:31636940 C>T), RS1001250792 (1:31630248 C>T), RS1001410802 (1:31642692 T>C), RS1001706818 (1:31630075 C>T), RS1001796840 (1:31643992 A>G), RS1002251182 (1:31643864 C>G), RS1002366476 (1:31629637 G>C,T)

Disease associations

OMIM: gene MIM:610033 | disease phenotypes:

GenCC curated gene-disease

Mondo (0):

Orphanet (0):

HPO phenotypes

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

GWAS associations

9 associations (top):

Study	Trait	p-value
GCST005141_37	Cognitive ability (MTAG)	8.000000e-10
GCST005142_60	Cognitive ability	5.000000e-08
GCST005142_61	Cognitive ability	3.000000e-08
GCST005316_274	Intelligence (MTAG)	2.000000e-13
GCST005951_36	Body mass index	9.000000e-10
GCST006269_516	General cognitive ability	6.000000e-15
GCST006957_1	Severe aortic features in Marfan syndrome	9.000000e-06
GCST009798_61	Asthma	3.000000e-08
GCST012007_3	Hypoalbuminemia	7.000000e-07

EFO canonical traits (3, from GWAS)

EFO ID	Trait name
EFO:0004337	intelligence
EFO:0004784	self reported educational attainment
EFO:0004340	body mass index

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (1): CHEMBL4105771 (SINGLE PROTEIN)

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

ChEMBL bioactivities

2 potent at pChembl≥5 of 4 total, top 2 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).

pChembl	Type	Value	Unit	Molecule
5.19	Kd	6519	nM	CHEMBL3752910
5.19	ED50	6519	nM	CHEMBL3752910

PubChem BioAssay actives

1 with measured affinity, of 12 total; 1 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
4-methyl-3-[(1-methyl-6-pyridin-3-ylpyrazolo[3,4-d]pyrimidin-4-yl)amino]-N-[3-(trifluoromethyl)phenyl]benzamide	2148975: Binding affinity to human PEF1 incubated for 45 mins by Kinobead based pull down assay	kd	6.5190	uM

CTD chemical–gene interactions

27 total (human), top 27 by PubMed support.

Chemical	Actions (top 5)	PubMed papers
Valproic Acid	decreases expression	2
triphenyl phosphate	affects expression	1
sodium arsenate	decreases expression	1
pyrogallol 1,3-dimethyl ether	affects cotreatment, increases expression	1
trichostatin A	decreases expression	1
sodium arsenite	increases expression	1
di-n-butylphosphoric acid	affects expression	1
CGP 52608	affects binding, increases reaction	1
abrine	increases expression	1
3-(2-hydroxy-4-(2-methylnonan-2-yl)phenyl)cyclohexan-1-ol	increases expression	1
Decitabine	affects expression	1
Vorinostat	decreases expression	1
Aspirin	decreases expression	1
Cisplatin	affects expression	1
Doxorubicin	decreases expression	1
Enzyme Inhibitors	decreases activity, increases O-linked glycosylation	1
Lead	decreases expression	1
Menthol	increases expression	1
Ribonucleotides	affects binding	1
Selenium	increases expression	1
Smoke	decreases expression	1
Sodium Chloride	affects cotreatment, increases expression	1
Thiram	decreases expression	1
Tobacco Smoke Pollution	increases expression	1
Vitamin E	increases expression	1
Aflatoxin B1	increases methylation	1
Cadmium Chloride	increases expression	1

ChEMBL screening assays

8 unique, capped per target: 8 binding

Representative assays (with source publication via chembl_document):

Assay ID	Type	Description	Source paper
CHEMBL4012570	Binding	Binding affinity to PEF1 protein in human INA-6 cells after 3 hrs by nanoLC-MS/MS method	Ugi Reaction-Derived α-Acyl Aminocarboxamides Bind to Phosphatidylinositol 3-Kinase-Related Kinases, Inhibit HSF1-Dependent Heat Shock Response, and Induce Apoptosis in Multiple Myeloma Cells. — J Med Chem

Cellosaurus cell lines

3 cell lines: 3 cancer cell line

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

Cellosaurus	Name	Category	Sex
CVCL_D1PP	Abcam K-562 PEF1 KO	Cancer cell line	Female
CVCL_D2LA	Abcam Raji PEF1 KO	Cancer cell line	Male
CVCL_WQ25	Abcam Jurkat PEF1 KO	Cancer cell line	Male

Clinical trials (associated diseases)

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