PURB

Summary

PURB (purine rich element binding protein B, HGNC:9702) is a protein-coding gene on chromosome 7p13, encoding Transcriptional regulator protein Pur-beta (Q96QR8). Transcriptional regulator which can act as an activator or a repressor.

This gene product is a sequence-specific, single-stranded DNA-binding protein. It binds preferentially to the single strand of the purine-rich element termed PUR, which is present at origins of replication and in gene flanking regions in a variety of eukaryotes from yeasts through humans. Thus, it is implicated in the control of both DNA replication and transcription. Deletion of this gene has been associated with myelodysplastic syndrome and acute myelogenous leukemia.

Source: NCBI Gene 5814 — RefSeq curated summary.

At a glance

• GWAS associations: 1
• Clinical variants (ClinVar): 33 total
• Druggable target: yes
• MANE Select transcript: NM_033224

Identifiers

Gene identifiers

Field	Value
HGNC ID	HGNC:9702
Approved symbol	PURB
Name	purine rich element binding protein B
Location	7p13
Locus type	gene with protein product
Status	Approved
Aliases	PURBETA
Ensembl gene	ENSG00000146676
Ensembl biotype	protein_coding
OMIM	608887
Entrez	5814

Gene structure

Transcript identifiers

Ensembl transcripts: 1 — 1 protein_coding

ENST00000395699

RefSeq mRNA: 1 — MANE Select: NM_033224 NM_033224

CCDS: CCDS5499

Canonical transcript exons

ENST00000395699 — 1 exons

Exon	Start	End
ENSE00001522527	44876299	44885530

Expression profiles

Bgee: expression breadth ubiquitous, 254 present calls, max score 97.62.

FANTOM5 (CAGE): breadth ubiquitous, TPM avg 7.9388 / max 252.8718, expressed in 1743 samples.

FANTOM5 promoters (2 alternative TSS)

Promoter ID	TPM avg	Samples expressed
83905	6.4605	1723
83904	1.4783	766

Top tissues by expression

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

Tissue	Anatomy ID	Expression score	Quality
upper arm skin	UBERON:0004263	97.62	gold quality
cerebellar vermis	UBERON:0004720	96.58	gold quality
epithelial cell of pancreas	CL:0000083	96.32	gold quality
kidney epithelium	UBERON:0004819	95.71	gold quality
gingival epithelium	UBERON:0001949	95.68	gold quality
oviduct epithelium	UBERON:0004804	95.57	gold quality
pancreatic ductal cell	CL:0002079	95.40	gold quality
visceral pleura	UBERON:0002401	95.20	gold quality
gingiva	UBERON:0001828	95.06	gold quality
tibialis anterior	UBERON:0001385	95.03	gold quality
Brodmann (1909) area 23	UBERON:0013554	95.03	gold quality
epithelium of nasopharynx	UBERON:0001951	94.83	gold quality
left ventricle myocardium	UBERON:0006566	94.78	gold quality
mammalian vulva	UBERON:0000997	94.77	gold quality
cardiac muscle of right atrium	UBERON:0003379	94.70	gold quality
middle temporal gyrus	UBERON:0002771	94.33	gold quality
saphenous vein	UBERON:0007318	94.03	gold quality
parietal pleura	UBERON:0002400	93.95	gold quality
deltoid	UBERON:0001476	93.80	gold quality
lower lobe of lung	UBERON:0008949	93.60	gold quality
seminal vesicle	UBERON:0000998	93.48	gold quality
Brodmann (1909) area 46	UBERON:0006483	93.39	gold quality
parietal lobe	UBERON:0001872	93.28	gold quality
cartilage tissue	UBERON:0002418	93.19	gold quality
thymus	UBERON:0002370	93.17	gold quality
postcentral gyrus	UBERON:0002581	93.15	gold quality
epithelium of mammary gland	UBERON:0003244	93.12	gold quality
mammary duct	UBERON:0001765	93.08	gold quality
nipple	UBERON:0002030	93.06	gold quality
upper leg skin	UBERON:0004262	93.05	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: yes

Downstream targets (CollecTRI)

5 targets.

Target	Regulation
CFC1
GNRH1	Repression
MCAT
MYH6	Repression
TPM1

miRNA regulators (miRDB)

408 targeting PURB, 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-3163	100.00	77.23	8605
HSA-MIR-3613-3P	100.00	76.36	7965
HSA-MIR-3689D	100.00	66.14	1181
HSA-MIR-6851-5P	100.00	65.63	1294
HSA-MIR-4262	100.00	73.26	3931
HSA-MIR-3646	100.00	73.56	5283
HSA-MIR-5692A	100.00	74.40	6850
HSA-MIR-4668-3P	100.00	68.74	2635
HSA-MIR-6740-5P	100.00	65.64	932
HSA-MIR-3134	100.00	66.43	777
HSA-MIR-548C-3P	99.99	74.01	7587
HSA-MIR-34A-5P	99.99	71.21	1784
HSA-MIR-449A	99.99	71.05	1776
HSA-MIR-371B-5P	99.99	75.34	4759
HSA-MIR-548AW	99.99	72.57	3559
HSA-MIR-4282	99.99	75.36	6408
HSA-MIR-181C-5P	99.99	72.95	2996
HSA-MIR-181A-5P	99.99	72.96	2995
HSA-MIR-181B-5P	99.99	72.97	2996
HSA-MIR-181D-5P	99.99	73.04	2997
HSA-MIR-3662	99.99	73.82	5684
HSA-MIR-223-3P	99.99	70.14	1140
HSA-MIR-186-5P	99.99	70.83	3707
HSA-MIR-4531	99.99	69.70	3181
HSA-MIR-373-5P	99.98	75.36	4753
HSA-MIR-616-5P	99.98	75.58	4775
HSA-MIR-8068	99.98	73.85	2376
HSA-MIR-103A-3P	99.98	69.14	1595
HSA-MIR-107	99.98	69.14	1595
HSA-MIR-499A-5P	99.98	70.79	1323

Literature-anchored findings (GeneRIF, showing 5)

• results show that PUR proteins are capable of binding to alpha-MHC mRNA and attenuate its translational efficiency; also show robust expression of PUR proteins in failing hearts where alpha-MHC mRNA levels are suppressed (PMID:12933792)
• findings offer insights into mechanism, energetics, and sequence of Purbeta repressor binding to a biologically relevant, contractile phenotype-regulating cis-element while revealing the thermodynamic confines of Purbeta-mediated effects on DNA structure (PMID:19496623)
• Suggest dynamic interplay between transcriptional activators Pur-alpha/Pur-beta and repressors in regulating SMalphaA gene output during myofibroblast differentiation. (PMID:24446247)
• site-directed mutagenesis revealed several basic amino acid residues in the intermolecular (R267) and intramolecular (K82 and R159) subdomains that are essential for Purbeta transcriptional repressor function in Acta2 promoter-reporter assays. In keeping with their diminished Acta2 repressor activity in fibroblasts, purified Purbeta variants containing an R267A mutation exhibited reduced binding affinity for purine-ric… (PMID:27064749)
• Results showed that Purbeta ssDNA-binding activity was significantly increased in myeloid cells from AML patients suggesting that the enhanced ssDNA-binding activity of Purbeta in transformed myeloid cells may serve as a unique and measurable phenotypic trait for improving prognostic risk stratification in AML. (PMID:28834593)

Cross-species orthologs

7 orthologs

Organism	Symbol	Gene ID
danio_rerio	purba	ENSDARG00000068822
danio_rerio	purbb	ENSDARG00000103546
mus_musculus	Purb	ENSMUSG00000094483
rattus_norvegicus	Purb	ENSRNOG00000062895
drosophila_melanogaster	Pur-alpha	FBGN0022361
caenorhabditis_elegans		WBGENE00004046
caenorhabditis_elegans		WBGENE00008976

Paralogs (2): PURG (ENSG00000172733), PURA (ENSG00000185129)

Protein

Protein identifiers

Transcriptional regulator protein Pur-beta — Q96QR8 (reviewed: Q96QR8)

Alternative names: Purine-rich element-binding protein B

All UniProt accessions (1): Q96QR8

UniProt curated annotations — full annotation on UniProt →

Function. Transcriptional regulator which can act as an activator or a repressor. Represses the transcription of ACTA2 in fibroblasts and smooth muscle cells via its ability to interact with the purine-rich strand of a MCAT- containing element in the 5’ flanking region of the gene. Represses the transcription of MYOCD, capable of repressing all isoforms of MYOCD but the magnitude of the repressive effects is most notable for the SMC- specific isoforms. Promotes hepatic glucose production by activating the transcription of ADCY6, leading to cAMP accumulation, increased PKA activity, CREB activation, and increased transcription of PCK1 and G6PC genes. Has capacity to bind repeated elements in single-stranded DNA such as the purine-rich single strand of the PUR element located upstream of the MYC gene. Participates in transcriptional and translational regulation of alpha-MHC expression in cardiac myocytes by binding to the purine-rich negative regulatory (PNR) element Modulates constitutive liver galectin-3 gene transcription by binding to its promoter. May play a role in the dendritic transport of a subset of mRNAs.

Subunit / interactions. Homodimer, heterodimer with PURA and heterotrimer with PURA and YBX1/Y-box protein 1. Interacts with MYOCD and SRF.

Subcellular location. Nucleus.

Tissue specificity. Expressed in myocardium of heart failure patients.

Miscellaneous. Defects in PURB may be a cause of progression of myelodysplastic syndrome (MDS) towards acute myelogenous leukemia (AML). MDS refers to a heterogeneous group of closely related hematopoietic disorders. All are characterized by a cellular marrow with impaired morphology and maturation (dysmyelopoiesis) and peripheral blood cytopenias, resulting from ineffective blood cell production. Some patients with MDS develop acute myelogenous leukemia (AML), a malignant disease in which hematopoietic precursors are arrested in an early stage of development.

Similarity. Belongs to the PUR DNA-binding protein family.

RefSeq proteins (1): NP_150093* (*=MANE)

Domains & families (InterPro)

ID	Name	Type
IPR006628	PUR-bd_fam	Family

Pfam: PF04845

UniProt features (18 total): modified residue 11, region of interest 3, compositionally biased region 2, initiator methionine 1, chain 1

Structure

Experimental structures (PDB)

0 structures.

Predicted structure (AlphaFold)

Model	pLDDT	Fraction very-high
AF-Q96QR8-F1	75.79	0.42

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 (11): 24, 31, 101, 152, 267, 294, 298, 304, 2, 6, 8

Function

Pathways and Gene Ontology

Reactome pathways

0 pathways

MSigDB gene sets: 268 (showing top): GOBP_MYELOID_CELL_DIFFERENTIATION, GCACCTT_MIR18A_MIR18B, HORIUCHI_WTAP_TARGETS_DN, TAATAAT_MIR126, TGCTGCT_MIR15A_MIR16_MIR15B_MIR195_MIR424_MIR497, TGCACTT_MIR519C_MIR519B_MIR519A, TTTGTAG_MIR520D, GTTAAAG_MIR302B, TACAATC_MIR508, AP2_Q3, CAGGTCC_MIR492, AATGGAG_MIR136, GOBP_NEGATIVE_REGULATION_OF_TRANSLATION, GOBP_TRANSLATION, GOBP_POST_TRANSCRIPTIONAL_REGULATION_OF_GENE_EXPRESSION

GO Biological Process (6): negative regulation of transcription by RNA polymerase II (GO:0000122), regulation of transcription by RNA polymerase II (GO:0006357), regulation of myeloid cell differentiation (GO:0045637), positive regulation of transcription by RNA polymerase II (GO:0045944), negative regulation of translation (GO:0017148), negative regulation of DNA-templated transcription (GO:0045892)

GO Molecular Function (14): mRNA regulatory element binding translation repressor activity (GO:0000900), RNA polymerase II transcription regulatory region sequence-specific DNA binding (GO:0000977), DNA-binding transcription factor activity, RNA polymerase II-specific (GO:0000981), DNA-binding transcription repressor activity, RNA polymerase II-specific (GO:0001227), single-stranded DNA binding (GO:0003697), RNA binding (GO:0003723), mRNA binding (GO:0003729), purine-rich negative regulatory element binding (GO:0032422), SMAD binding (GO:0046332), DNA-binding transcription factor binding (GO:0140297), DNA binding (GO:0003677), double-stranded DNA binding (GO:0003690), DNA-binding transcription factor activity (GO:0003700), protein binding (GO:0005515)

GO Cellular Component (2): nucleus (GO:0005634), nucleoplasm (GO:0005654)

GO top-level categories

Rollup of top GO terms by namespace:

Category	Terms
regulation of transcription by RNA polymerase II	3
transcription by RNA polymerase II	3
regulation of DNA-templated transcription	3
transcription cis-regulatory region binding	3
RNA polymerase II transcription regulatory region sequence-specific DNA binding	2
DNA binding	2
nucleic acid binding	2
negative regulation of DNA-templated transcription	1
myeloid cell differentiation	1
regulation of hemopoiesis	1
positive regulation of DNA-templated transcription	1
translation	1
regulation of translation	1
negative regulation of gene expression	1
negative regulation of protein metabolic process	1
DNA-templated transcription	1
negative regulation of RNA biosynthetic process	1
mRNA binding	1
translation repressor activity	1
chromatin	1
DNA-binding transcription factor activity	1
negative regulation of transcription by RNA polymerase II	1
DNA-binding transcription factor activity, RNA polymerase II-specific	1
DNA-binding transcription repressor activity	1
RNA binding	1
protein binding	1
transcription factor binding	1
transcription regulator activity	1
binding	1
intracellular membrane-bounded organelle	1
nuclear lumen	1
cellular anatomical structure	1

Protein interactions and networks

STRING

752 interactions, top by confidence (×1000):

Protein A	Protein B	Partner UniProt	Score
PURB	MYH7B	A7E2Y1	872
PURB	SOX6	P35712	870
PURB	POLDIP3	Q9BY77	793
PURB	YBX1	P16990	648
PURB	MYH6	P13533	622
PURB	MYH7	P12883	617
PURB	BCL2	P10415	465
PURB	MED13	Q9UHV7	441
PURB	OTUD4	Q01804	427
PURB	FOXJ2	Q9P0K8	422
PURB	CC2D1B	Q5T0F9	414
PURB	ENO1	P06733	396
PURB	SEPTIN14	Q6ZU15	394
PURB	PURA	Q00577	392
PURB	NUFIP2	Q7Z417	385

IntAct

114 interactions, top by confidence:

A	B	Type	Score
CNOT7	CNOT1	psi-mi:“MI:0914”(association)	0.880
CFTR	ESYT2	psi-mi:“MI:0914”(association)	0.710
LIN28A	IGF2BP3	psi-mi:“MI:0914”(association)	0.640
CFTR	HAX1	psi-mi:“MI:0914”(association)	0.610
PURB	AP1M1	psi-mi:“MI:0915”(physical association)	0.560
PURB	PCDHB14	psi-mi:“MI:0915”(physical association)	0.560
ZNF497	PURB	psi-mi:“MI:0915”(physical association)	0.560
NABP1	PURB	psi-mi:“MI:0915”(physical association)	0.560
PURB	MBD2	psi-mi:“MI:0915”(physical association)	0.560
LNX1	PURB	psi-mi:“MI:0915”(physical association)	0.560
RPS6	IPO7	psi-mi:“MI:0914”(association)	0.530
H1-6	ZNF724	psi-mi:“MI:0914”(association)	0.530
RPS2	MPHOSPH10	psi-mi:“MI:0914”(association)	0.530
MACROH2A2	PPM1G	psi-mi:“MI:0914”(association)	0.530
RPSA	DKC1	psi-mi:“MI:0914”(association)	0.530
RPS3	ZNF316	psi-mi:“MI:0914”(association)	0.530
MAGEB2	POLRMT	psi-mi:“MI:0914”(association)	0.530
RPSA	RPS17	psi-mi:“MI:0914”(association)	0.530
MAGEB2	GTPBP10	psi-mi:“MI:0914”(association)	0.530
KRR1	MPHOSPH10	psi-mi:“MI:0914”(association)	0.530
ABT1	ZNF316	psi-mi:“MI:0914”(association)	0.530
KIF1C	KIF1B	psi-mi:“MI:2364”(proximity)	0.480

BioGRID (184): PURB (Affinity Capture-MS), PURB (Affinity Capture-MS), PURB (Affinity Capture-MS), PURB (Affinity Capture-MS), PURB (Affinity Capture-MS), PURB (Co-fractionation), PURB (Affinity Capture-MS), PURB (Affinity Capture-MS), PURB (Affinity Capture-MS), PURB (Affinity Capture-MS), PURB (Affinity Capture-MS), PURB (Affinity Capture-MS), PURB (Affinity Capture-MS), PURB (Affinity Capture-MS), PURB (Affinity Capture-MS)

ESM2 similar proteins: A2AWA9, A6QL63, F1LQ48, O35295, O43242, O75446, O88506, P09851, P14685, P14866, P20936, P42669, P50904, Q00577, Q13330, Q2KJ46, Q503N9, Q5EAD0, Q5RAN1, Q5SQF8, Q60437, Q62599, Q62771, Q640Q5, Q68A21, Q6GMN2, Q6GQW0, Q6NT76, Q6P5H6, Q6PAC9, Q6PHK6, Q6ZVM7, Q8AVS4, Q8BKX1, Q8K4B0, Q8N122, Q8R081, Q8R3S6, Q8VHW5, Q8WXS5

Diamond homologs: O35295, P42669, P86252, Q00577, Q68A21, Q6PAC9, Q6PHK6, Q8AVS4, Q8R4E6, Q94230, Q96QR8, Q9UJV8

SIGNOR signaling

1 interactions.

A	Effect	B	Mechanism
PURB	“down-regulates quantity by repression”	MYH6	“transcriptional regulation”

Enriched among interaction partners

Reactome pathways and GO biological processes over-represented among this gene’s 112 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
Eukaryotic Translation Initiation	9	37.0×	4e-11
Cap-dependent Translation Initiation	9	37.0×	4e-11
SARS-CoV-1 modulates host translation machinery	9	37.0×	4e-11
Eukaryotic Translation Elongation	9	33.4×	9e-11
Activation of the mRNA upon binding of the cap-binding complex and eIFs, and subsequent binding to 43S	9	32.6×	1e-10
Nonsense-Mediated Decay (NMD)	9	28.0×	5e-10
Peptide chain elongation	16	27.1×	5e-17
Viral mRNA Translation	16	27.1×	5e-17

GO biological processes:

GO term	Partners	Fold	FDR
cytoplasmic translation	17	31.2×	2e-18
negative regulation of translation	9	17.5×	5e-07
translation	16	16.3×	8e-13
ribosomal small subunit biogenesis	6	13.5×	5e-04
RNA processing	5	10.8×	7e-03
rRNA processing	6	8.4×	7e-03

Disease & clinical

Clinical variants and AI predictions

ClinVar

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

Classification	Count (floor)
Pathogenic	0
Likely pathogenic	0
Uncertain significance	33
Likely benign	0
Benign	0

Top pathogenic / likely-pathogenic (0)

SpliceAI

247 predictions. Top by Δscore:

Variant	Effect	Δscore
7:44884485:ATC:A	donor_gain	0.9900
7:44884432:CCCT:C	donor_gain	0.9700
7:44884485:AT:A	donor_gain	0.9700
7:44884498:T:TA	donor_gain	0.9700
7:44884486:T:C	donor_gain	0.9600
7:44884426:T:TA	donor_gain	0.9200
7:44884431:AC:A	donor_gain	0.8700
7:44884432:CC:C	donor_gain	0.8700
7:44884487:C:A	donor_gain	0.8200
7:44884551:G:A	donor_gain	0.7900
7:44884598:TC:T	donor_gain	0.7900
7:44884417:TCATC:T	donor_gain	0.7700
7:44884418:CATCC:C	donor_gain	0.7700
7:44884419:ATCCA:A	donor_gain	0.7700
7:44884421:C:CT	donor_gain	0.7700
7:44884427:CCTCA:C	donor_loss	0.7700
7:44884428:CTCA:C	donor_loss	0.7700
7:44884429:TCA:T	donor_loss	0.7700
7:44884430:C:CG	donor_loss	0.7700
7:44884431:ACCC:A	donor_loss	0.7700
7:44884432:C:CA	donor_loss	0.7700
7:44884593:CGGCT:C	donor_gain	0.7600
7:44884426:TCC:T	donor_loss	0.7500
7:44884433:C:G	donor_loss	0.7300
7:44884153:CAATT:C	donor_gain	0.7200
7:44884420:TCC:T	donor_gain	0.7000
7:44884465:C:CT	donor_gain	0.6800
7:44884422:C:CT	donor_gain	0.6600
7:44884485:ATCC:A	donor_gain	0.6400
7:44884451:CGCCG:C	donor_loss	0.6100

AlphaMissense

2018 scored. Top likely-pathogenic:

Variant	Protein change	am_pathogenicity
7:44884556:A:G	W265R	1.000
7:44884556:A:T	W265R	1.000
7:44884570:A:T	V260E	1.000
7:44884576:A:T	I258N	1.000
7:44884586:G:T	R255S	1.000
7:44884602:C:A	E249D	1.000
7:44884602:C:G	E249D	1.000
7:44884604:C:T	E249K	1.000
7:44884605:G:C	S248R	1.000
7:44884605:G:T	S248R	1.000
7:44884607:T:G	S248R	1.000
7:44884615:A:G	L245P	1.000
7:44884617:A:C	F244L	1.000
7:44884617:A:T	F244L	1.000
7:44884618:A:G	F244S	1.000
7:44884619:A:C	F244V	1.000
7:44884619:A:G	F244L	1.000
7:44884619:A:T	F244I	1.000
7:44884624:C:A	G242V	1.000
7:44884624:C:T	G242E	1.000
7:44884625:C:A	G242W	1.000
7:44884625:C:G	G242R	1.000
7:44884625:C:T	G242R	1.000
7:44884632:G:C	N239K	1.000
7:44884632:G:T	N239K	1.000
7:44884633:T:A	N239I	1.000
7:44884648:A:G	F234S	1.000
7:44884650:G:C	F233L	1.000
7:44884650:G:T	F233L	1.000
7:44884652:A:G	F233L	1.000

dbSNP variants (sampled 300 via entrez): RS1000077259 (7:44877003 A>G), RS1000168378 (7:44884995 C>A,G), RS1000302089 (7:44882993 G>A), RS1000485322 (7:44882714 A>T), RS1000615092 (7:44881411 CTGGAG>C), RS1000682069 (7:44882630 T>C), RS1000798424 (7:44886395 G>A), RS1000844159 (7:44882391 A>T), RS1000878041 (7:44877579 G>A,C), RS1000931328 (7:44877755 G>C,T), RS1001225751 (7:44882059 T>C), RS1002212736 (7:44876923 A>G), RS1002280234 (7:44883519 A>G), RS1002289665 (7:44880205 G>A,C), RS1002432231 (7:44877225 C>G)

Disease associations

OMIM: gene MIM:608887 | 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
GCST004603_37	Platelet count	8.000000e-23

EFO canonical traits (1, from GWAS)

EFO ID	Trait name
EFO:0004309	platelet count

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (1): CHEMBL6066334 (SINGLE PROTEIN)

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

ChEMBL bioactivities

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

pChembl	Type	Value	Unit	Molecule
8.10	Kd	7.964	nM	CHEMBL3752910
8.10	ED50	7.964	nM	CHEMBL3752910
7.70	Kd	20.18	nM	CHEMBL5653589
7.70	ED50	20.18	nM	CHEMBL5653589

PubChem BioAssay actives

2 with measured affinity, of 4 total; 2 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	2149155: Binding affinity to human PURB incubated for 45 mins by Kinobead based pull down assay	kd	0.0080	uM
4-methyl-3-[(2-methyl-6-pyridin-3-ylpyrazolo[3,4-d]pyrimidin-4-yl)amino]-N-[3-(trifluoromethyl)phenyl]benzamide	2149155: Binding affinity to human PURB incubated for 45 mins by Kinobead based pull down assay	kd	0.0202	uM

CTD chemical–gene interactions

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

Chemical	Actions (top 5)	PubMed papers
bisphenol A	decreases expression, increases expression	3
Phenylmercuric Acetate	affects cotreatment, decreases expression	2
Tobacco Smoke Pollution	increases expression	2
Valproic Acid	affects expression, decreases expression	2
GSK-J4	decreases expression	1
FR900359	increases phosphorylation	1
sodium arsenite	increases expression	1
coumarin	increases phosphorylation	1
di-n-butylphosphoric acid	affects expression	1
CD 437	decreases expression	1
chloropicrin	decreases expression	1
4-(5-benzo(1,3)dioxol-5-yl-4-pyridin-2-yl-1H-imidazol-2-yl)benzamide	affects cotreatment, decreases expression	1
3-(4’-hydroxy-3’-adamantylbiphenyl-4-yl)acrylic acid	decreases expression	1
torcetrapib	increases expression	1
ICG 001	increases expression	1
abrine	increases expression	1
dorsomorphin	affects cotreatment, decreases expression	1
jinfukang	decreases expression	1
PCI 5002	affects cotreatment, increases expression	1
4-(4-((5-(4,5-dimethyl-2-nitrophenyl)-2-furanyl)methylene)-4,5-dihydro-3-methyl-5-oxo-1H-pyrazol-1-yl)benzoic acid	increases expression	1
Leflunomide	decreases expression	1
Atrazine	increases expression	1
Benzene	increases expression	1
Benzo(a)pyrene	decreases expression	1
Caffeine	increases phosphorylation	1
Haloperidol	decreases expression	1
Ribonucleotides	affects binding	1
Thimerosal	decreases expression	1
Urethane	decreases expression	1
Zinc	affects cotreatment, increases expression	1

ChEMBL screening assays

1 unique, capped per target: 1 binding

Representative assays (with source publication via chembl_document):

Assay ID	Type	Description	Source paper
CHEMBL5652197	Binding	Binding affinity to human PURB incubated for 45 mins by Kinobead based pull down assay	NVP-BHG712: Effects of Regioisomers on the Affinity and Selectivity toward the EPHrin Family. — ChemMedChem

Clinical trials (associated diseases)

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