DERA

Summary

DERA (deoxyribose-phosphate aldolase, HGNC:24269) is a protein-coding gene on chromosome 12p12.3, encoding Deoxyribose-phosphate aldolase (Q9Y315). Catalyzes a reversible aldol reaction between acetaldehyde and D-glyceraldehyde 3-phosphate to generate 2-deoxy-D-ribose 5-phosphate.

Enables deoxyribose-phosphate aldolase activity. Involved in deoxyribonucleoside catabolic process. Located in nucleoplasm.

Source: NCBI Gene 51071 — RefSeq curated summary.

At a glance

• GWAS associations: 5
• Clinical variants (ClinVar): 72 total — 2 pathogenic
• Druggable target: yes
• MANE Select transcript: NM_015954

Identifiers

Gene identifiers

Field	Value
HGNC ID	HGNC:24269
Approved symbol	DERA
Name	deoxyribose-phosphate aldolase
Location	12p12.3
Locus type	gene with protein product
Status	Approved
Aliases	CGI-26, DEOC
Ensembl gene	ENSG00000023697
Ensembl biotype	protein_coding
OMIM	619668
Entrez	51071

Gene structure

Transcript identifiers

Ensembl transcripts: 15 — 11 protein_coding, 2 nonsense_mediated_decay, 1 retained_intron, 1 protein_coding_CDS_not_defined

ENST00000428559, ENST00000524480, ENST00000526521, ENST00000526530, ENST00000528821, ENST00000530274, ENST00000531803, ENST00000532573, ENST00000532964, ENST00000533447, ENST00000885122, ENST00000885123, ENST00000885124, ENST00000885125, ENST00000954121

RefSeq mRNA: 2 — MANE Select: NM_015954 NM_001300779, NM_015954

CCDS: CCDS44838, CCDS73451

Canonical transcript exons

ENST00000428559 — 9 exons

Exon	Start	End
ENSE00002147240	16036690	16037381
ENSE00002203313	15911332	15911414
ENSE00003511951	15958188	15958335
ENSE00003513705	15956936	15957033
ENSE00003518125	15982308	15982436
ENSE00003518735	16036232	16036381
ENSE00003566585	15959829	15959924
ENSE00003609405	15962813	15962947
ENSE00003691450	16032542	16032654

Expression profiles

Bgee: expression breadth ubiquitous, 288 present calls, max score 97.23.

FANTOM5 (CAGE): breadth ubiquitous, TPM avg 31.7398 / max 376.7165, expressed in 1799 samples.

FANTOM5 promoters (10 alternative TSS)

Promoter ID	TPM avg	Samples expressed
124509	29.3950	1797
124508	1.5309	1041
124507	0.6487	400
124514	0.0368	3
124513	0.0344	3
124511	0.0337	14
124510	0.0274	6
124512	0.0142	4
124515	0.0125	4
206636	0.0061	3

Top tissues by expression

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

Tissue	Anatomy ID	Expression score	Quality
secondary oocyte	CL:0000655	97.23	gold quality
jejunal mucosa	UBERON:0000399	97.05	gold quality
nephron tubule	UBERON:0001231	97.00	gold quality
pancreatic ductal cell	CL:0002079	96.66	gold quality
amniotic fluid	UBERON:0000173	96.38	gold quality
esophagus squamous epithelium	UBERON:0006920	95.66	gold quality
rectum	UBERON:0001052	95.33	gold quality
kidney epithelium	UBERON:0004819	95.17	gold quality
oocyte	CL:0000023	95.09	gold quality
duodenum	UBERON:0002114	94.97	gold quality
tongue squamous epithelium	UBERON:0006919	94.79	gold quality
renal glomerulus	UBERON:0000074	94.66	gold quality
palpebral conjunctiva	UBERON:0001812	94.66	gold quality
epithelium of esophagus	UBERON:0001976	94.60	gold quality
gingival epithelium	UBERON:0001949	94.57	gold quality
squamous epithelium	UBERON:0006914	94.49	gold quality
metanephric glomerulus	UBERON:0004736	94.44	gold quality
oral cavity	UBERON:0000167	94.40	gold quality
colonic mucosa	UBERON:0000317	93.98	gold quality
liver	UBERON:0002107	93.89	gold quality
endothelial cell	CL:0000115	93.83	gold quality
gingiva	UBERON:0001828	93.80	gold quality
mucosa of sigmoid colon	UBERON:0004993	93.57	gold quality
adult mammalian kidney	UBERON:0000082	93.52	gold quality
adrenal tissue	UBERON:0018303	93.49	gold quality
hair follicle	UBERON:0002073	93.31	gold quality
tibia	UBERON:0000979	93.11	gold quality
monocyte	CL:0000576	93.01	gold quality
kidney	UBERON:0002113	92.95	gold quality
mononuclear cell	CL:0000842	92.93	gold quality

Single-cell (SCXA)

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

Experiment	Marker?	Max mean expression
E-ANND-3	yes	12.44

Regulation

Is transcription factor: no

miRNA regulators (miRDB)

45 targeting DERA, 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-4795-3P	100.00	74.62	4024
HSA-MIR-5692A	100.00	74.40	6850
HSA-MIR-3924	100.00	72.09	2394
HSA-MIR-6758-5P	100.00	66.21	1470
HSA-MIR-6856-5P	100.00	65.47	1298
HSA-MIR-3646	100.00	73.56	5283
HSA-MIR-3662	99.99	73.82	5684
HSA-MIR-4775	99.98	75.00	6394
HSA-MIR-512-3P	99.97	67.35	1049
HSA-MIR-590-3P	99.96	74.34	6478
HSA-MIR-548AT-5P	99.96	70.83	2666
HSA-MIR-335-3P	99.93	73.36	4958
HSA-MIR-3143	99.93	71.96	3104
HSA-MIR-205-3P	99.92	69.92	3165
HSA-MIR-629-3P	99.85	67.99	1875
HSA-MIR-3133	99.81	70.92	3506
HSA-MIR-1299	99.77	71.24	2389
HSA-MIR-1255A	99.74	68.09	744
HSA-MIR-1255B-5P	99.74	68.16	741
HSA-MIR-561-3P	99.64	70.90	3647
HSA-MIR-3942-3P	99.57	69.03	2854
HSA-MIR-130A-5P	99.33	70.26	2623
HSA-MIR-628-3P	99.04	68.37	814
HSA-MIR-4650-3P	99.01	68.39	1062
HSA-MIR-3619-5P	99.00	68.87	2308
HSA-MIR-1911-5P	98.92	67.53	325
HSA-MIR-6512-5P	98.76	69.29	1195
HSA-MIR-3908	98.75	67.31	1160
HSA-MIR-214-3P	98.71	68.12	2128
HSA-MIR-761	98.71	68.07	2051

Literature-anchored findings (GeneRIF, showing 2)

• Genetic variants in TKT and DERA in the nicotinamide adenine dinucleotide phosphate pathway predict melanoma survival. (PMID:32659474)
• A case of pericytic neoplasm in the shoulder with a novel DERA-GLI1 gene fusion. (PMID:33067875)

Cross-species orthologs

5 orthologs

Organism	Symbol	Gene ID
danio_rerio	dera	ENSDARG00000005897
mus_musculus	Dera	ENSMUSG00000030225
rattus_norvegicus	Dera	ENSRNOG00000007570
drosophila_melanogaster	Dera	FBGN0033735
caenorhabditis_elegans		WBGENE00017283

Protein

Protein identifiers

Deoxyribose-phosphate aldolase — Q9Y315 (reviewed: Q9Y315)

Alternative names: 2-deoxy-D-ribose 5-phosphate aldolase, Phosphodeoxyriboaldolase

All UniProt accessions (8): E9PJ44, E9PJB9, E9PMH9, E9PML7, E9PPK3, E9PPM8, G3V158, Q9Y315

UniProt curated annotations — full annotation on UniProt →

Function. Catalyzes a reversible aldol reaction between acetaldehyde and D-glyceraldehyde 3-phosphate to generate 2-deoxy-D-ribose 5-phosphate. Participates in stress granule (SG) assembly. May allow ATP production from extracellular deoxyinosine in conditions of energy deprivation.

Subunit / interactions. Interacts with YBX1.

Subcellular location. Cytoplasm. Cytoplasmic granule. Nucleus.

Tissue specificity. Mainly expressed in liver, lung and colon.

Pathway. Carbohydrate degradation; 2-deoxy-D-ribose 1-phosphate degradation; D-glyceraldehyde 3-phosphate and acetaldehyde from 2-deoxy-alpha-D-ribose 1-phosphate: step 2/2.

Similarity. Belongs to the DeoC/FbaB aldolase family. DeoC type 2 subfamily.

RefSeq proteins (2): NP_001287708, NP_057038* (*=MANE)

Domains & families (InterPro)

ID	Name	Type
IPR002915	DeoC/FbaB/LacD_aldolase	Family
IPR011343	DeoC	Family
IPR013785	Aldolase_TIM	Homologous_superfamily

Pfam: PF01791

Enzyme classification (BRENDA):

• EC 4.1.2.4 — deoxyribose-phosphate aldolase (BRENDA: 48 organisms, 81 substrates, 28 inhibitors, 59 Km, 31 kcat entries)

Substrate kinetics (BRENDA)

7 substrates with measured Km, best-characterized 7. Km ranges are aggregated across organisms/conditions.

Substrate	Km (mM)	Measurements
2-DEOXY-D-RIBOSE 5-PHOSPHATE	0.02–145	37
D-2-DEOXYRIBOSE	33–67	5
ACETALDEHYDE	0.267–3.5	4
D-GLYCERALDEHYDE 3-PHOSPHATE	0.2–0.71	3
2-DEOXY-D-RIBOSE	24.77–418	2
CHLOROACETALDEHYDE	24–54.6	2
2-DEOXY-D-RIBOSE-5-PHOSPHATE	9.1	1

Catalyzed reactions (Rhea), 1 shown:

• 2-deoxy-D-ribose 5-phosphate = D-glyceraldehyde 3-phosphate + acetaldehyde (RHEA:12821)

UniProt features (9 total): active site 3, sequence conflict 3, mutagenesis site 2, chain 1

Structure

Experimental structures (PDB)

0 structures.

Predicted structure (AlphaFold)

Model	pLDDT	Fraction very-high
AF-Q9Y315-F1	95.99	0.93

Functional residue map

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

Catalytic / active sites (3): 155 (proton donor/acceptor); 218 (schiff-base intermediate with acetaldehyde); 254 (proton donor/acceptor)

Mutagenesis-validated functional residues (2):

Position	Phenotype
218	abolishes deoxyribose-phosphate aldolase activity.
254	abolishes deoxyribose-phosphate aldolase activity.

Function

Pathways and Gene Ontology

Reactome pathways

2 pathways

ID	Pathway
R-HSA-6798695	Neutrophil degranulation
R-HSA-71336	Pentose phosphate pathway

MSigDB gene sets: 147 (showing top): BUYTAERT_PHOTODYNAMIC_THERAPY_STRESS_DN, REACTOME_INNATE_IMMUNE_SYSTEM, GOCC_SECRETORY_GRANULE, GOBP_NADPPLUS_METABOLIC_PROCESS, GOBP_CARBOHYDRATE_DERIVATIVE_CATABOLIC_PROCESS, IVANOVA_HEMATOPOIESIS_LATE_PROGENITOR, GOBP_ORGANOPHOSPHATE_METABOLIC_PROCESS, LUCAS_HNF4A_TARGETS_UP, GOBP_CARBOHYDRATE_DERIVATIVE_METABOLIC_PROCESS, GOBP_GLUCOSE_6_PHOSPHATE_METABOLIC_PROCESS, GOBP_NUCLEOBASE_CONTAINING_SMALL_MOLECULE_METABOLIC_PROCESS, GOBP_GENERATION_OF_PRECURSOR_METABOLITES_AND_ENERGY, KORKOLA_EMBRYONAL_CARCINOMA_UP, GOBP_CARBOHYDRATE_METABOLIC_PROCESS, GOBP_ORGANOPHOSPHATE_CATABOLIC_PROCESS

GO Biological Process (5): pentose-phosphate shunt (GO:0006098), deoxyribonucleotide catabolic process (GO:0009264), carbohydrate catabolic process (GO:0016052), 2’-deoxyribonucleoside catabolic process (GO:0046121), deoxyribose phosphate catabolic process (GO:0046386)

GO Molecular Function (3): deoxyribose-phosphate aldolase activity (GO:0004139), protein binding (GO:0005515), lyase activity (GO:0016829)

GO Cellular Component (7): extracellular region (GO:0005576), nucleoplasm (GO:0005654), cytosol (GO:0005829), secretory granule lumen (GO:0034774), ficolin-1-rich granule lumen (GO:1904813), nucleus (GO:0005634), cytoplasm (GO:0005737)

Reactome top-level categories

Rollup of top-2 pathways:

Category	Pathways
Innate Immune System	1
Metabolism of carbohydrates and carbohydrate derivatives	1

GO top-level categories

Rollup of top GO terms by namespace:

Category	Terms
cellular anatomical structure	4
catabolic process	2
NADPH regeneration	1
pentose-phosphate shunt, oxidative branch	1
pentose-phosphate shunt, non-oxidative branch	1
glucose 6-phosphate metabolic process	1
deoxyribonucleotide metabolic process	1
carbohydrate metabolic process	1
2’-deoxyribonucleoside metabolic process	1
nucleoside catabolic process	1
organophosphate catabolic process	1
carbohydrate derivative catabolic process	1
aldehyde-lyase activity	1
binding	1
catalytic activity	1
nuclear lumen	1
cytoplasm	1
secretory granule	1
cytoplasmic vesicle lumen	1
intracellular organelle lumen	1
ficolin-1-rich granule	1
intracellular membrane-bounded organelle	1
intracellular anatomical structure	1

Protein interactions and networks

STRING

1561 interactions, top by confidence (×1000):

Protein A	Protein B	Partner UniProt	Score
DERA	RPIA	P49247	607
DERA	RBKS	Q9H477	593
DERA	RPE	Q96AT9	591
DERA	PGM2	Q96G03	547
DERA	GALE	Q14376	523
DERA	TPI1	P00938	522
DERA	MTFMT	Q96DP5	521
DERA	PNP	P00491	521
DERA	TKT	P29401	518
DERA	TKTL2	Q9H0I9	514
DERA	PHYKPL	Q8IUZ5	512
DERA	TALDO1	P37837	505
DERA	TKTL1	P51854	504
DERA	HEMK1	Q9Y5R4	497
DERA	UPRT	Q96BW1	491

IntAct

37 interactions, top by confidence:

A	B	Type	Score
PPIL1	SNW1	psi-mi:“MI:0914”(association)	0.930
ALDH16A1	DERA	psi-mi:“MI:0915”(physical association)	0.750
DERA	ALDH16A1	psi-mi:“MI:0915”(physical association)	0.750
ERP29	GLB1L	psi-mi:“MI:0914”(association)	0.640
DLGAP4	LIN7A	psi-mi:“MI:0914”(association)	0.590
HSF2	DERA	psi-mi:“MI:0915”(physical association)	0.560
ERP29	ARSB	psi-mi:“MI:0914”(association)	0.530
Rpl35	RPS6	psi-mi:“MI:0914”(association)	0.350
Lgals3bp	CS	psi-mi:“MI:0914”(association)	0.350
PCMT1	YDJC	psi-mi:“MI:0914”(association)	0.350
ERP29	EXOC5	psi-mi:“MI:0914”(association)	0.350
TLR1	PLXNB2	psi-mi:“MI:0914”(association)	0.350
LANCL1	MYO7A	psi-mi:“MI:0914”(association)	0.350
	TGFB1I1	psi-mi:“MI:0914”(association)	0.350
N	MRPL45	psi-mi:“MI:0914”(association)	0.350
NCAPD3	NDUFS8	psi-mi:“MI:0914”(association)	0.350
ERBB2	PGM3	psi-mi:“MI:0914”(association)	0.350
CEP63	CIT	psi-mi:“MI:0914”(association)	0.350
CEP192	WASL	psi-mi:“MI:0914”(association)	0.350
ALDH16A1	TRIAP1	psi-mi:“MI:0914”(association)	0.350
GSX1	YKT6	psi-mi:“MI:0914”(association)	0.350
TLR1	LRP6	psi-mi:“MI:0914”(association)	0.350

BioGRID (65): DERA (Affinity Capture-MS), DERA (Affinity Capture-MS), DERA (Affinity Capture-MS), AGL (Co-fractionation), ALDH16A1 (Co-fractionation), C6orf211 (Co-fractionation), ASPSCR1 (Co-fractionation), ATIC (Co-fractionation), PNP (Co-fractionation), PNPO (Co-fractionation), TYMP (Co-fractionation), DERA (Affinity Capture-MS), DERA (Affinity Capture-MS), DERA (Affinity Capture-MS), DERA (Affinity Capture-MS)

ESM2 similar proteins: A7M6E7, B8BJ39, B8BM17, B9I2J6, B9N1F9, O09171, O22216, O22718, O35490, O80526, O89000, P11029, P11497, P28173, P35433, Q01217, Q06203, Q12882, Q13085, Q15024, Q28007, Q28559, Q28943, Q2QNG7, Q2QXR8, Q2QZ86, Q2RAK2, Q3T0V9, Q5I597, Q5M8Z0, Q5R895, Q5RFG2, Q5SWU9, Q5XGM3, Q5XGS8, Q6NYG8, Q8CHR6, Q8CIH9, Q8IX04, Q8S0G4

Diamond homologs: A0KPE4, A0KU07, A1AJU8, A1RH87, A1S474, A3D7J4, A3N123, A3QGT3, A4IR26, A4SRU4, A4W698, A4Y9A8, A5F5S6, A6WRB8, A7MGB0, A7MUW7, A7ZVS4, A8A8B0, A8FYQ9, A8G9H6, A8H728, A9KZ80, A9VQK2, B0BPV4, B0TQ91, B1IS38, B1KRP8, B1LEI6, B1XFJ1, B2TZR4, B2VH50, B3H1P7, B4EWA4, B4TGZ9, B5FA98, B5FTC5, B5Y277, B5Z4R3, B6ENG3, B6I6M8

SIGNOR signaling

3 interactions.

A	Effect	B	Mechanism
DERA	“down-regulates quantity”	“2-deoxy-D-ribofuranose 5-phosphate(2-)”	“chemical modification”
DERA	“up-regulates quantity”	“D-glyceraldehyde 3-phosphate(2-)”	“chemical modification”
DERA	“up-regulates quantity”	acetaldehyde	“chemical modification”

Disease & clinical

Clinical variants and AI predictions

ClinVar

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

Classification	Count (floor)
Pathogenic	2
Likely pathogenic	0
Uncertain significance	55
Likely benign	4
Benign	0

Top pathogenic / likely-pathogenic (2)

Variant ID	HGVS	Classification
1711362	GRCh37/hg19 12p13.2-12.1(chr12:10853887-24103810)x1	Pathogenic
58987	GRCh38/hg38 12p12.3(chr12:16019165-17579501)x1	Pathogenic

SpliceAI

1760 predictions. Top by Δscore:

Variant	Effect	Δscore
12:15956931:TTTA:T	acceptor_loss	1.0000
12:15956931:TTTAG:T	acceptor_gain	1.0000
12:15956932:TTAGA:T	acceptor_gain	1.0000
12:15956933:TAGA:T	acceptor_gain	1.0000
12:15956934:A:AC	acceptor_gain	1.0000
12:15956934:A:AG	acceptor_gain	1.0000
12:15956935:G:A	acceptor_gain	1.0000
12:15956935:G:GT	acceptor_gain	1.0000
12:15956935:GA:G	acceptor_gain	1.0000
12:15956935:GACC:G	acceptor_gain	1.0000
12:15956935:GACCT:G	acceptor_gain	1.0000
12:15957029:GGCAG:G	donor_gain	1.0000
12:15957030:GCAGG:G	donor_gain	1.0000
12:15957031:CAGGT:C	donor_loss	1.0000
12:15957032:AGGT:A	donor_loss	1.0000
12:15957033:GGTA:G	donor_loss	1.0000
12:15957034:GT:G	donor_loss	1.0000
12:15957035:T:A	donor_loss	1.0000
12:15959826:TAGG:T	acceptor_loss	1.0000
12:15959827:A:AG	acceptor_gain	1.0000
12:15959827:AG:A	acceptor_gain	1.0000
12:15959828:G:GG	acceptor_gain	1.0000
12:15959828:G:GT	acceptor_loss	1.0000
12:15959828:GG:G	acceptor_gain	1.0000
12:15959828:GGC:G	acceptor_gain	1.0000
12:15959920:ATCAG:A	donor_loss	1.0000
12:15959921:TCAG:T	donor_loss	1.0000
12:15959922:CAG:C	donor_loss	1.0000
12:15959923:AGG:A	donor_loss	1.0000
12:15959924:G:GC	donor_loss	1.0000

AlphaMissense

2063 scored. Top likely-pathogenic:

Variant	Protein change	am_pathogenicity
12:15962824:T:C	F129L	0.999
12:15962826:T:A	F129L	0.999
12:15962826:T:G	F129L	0.999
12:16036243:A:C	K254N	0.998
12:16036243:A:T	K254N	0.998
12:15982415:A:C	S206R	0.997
12:15982417:T:A	S206R	0.997
12:15982417:T:G	S206R	0.997
12:16032558:G:C	K218N	0.997
12:16032558:G:T	K218N	0.997
12:15959851:T:G	C100W	0.996
12:15962825:T:G	F129C	0.996
12:16032556:A:G	K218E	0.996
12:16036241:A:G	K254E	0.996
12:16036251:G:A	G257E	0.996
12:16036347:G:A	G289D	0.996
12:15959843:G:C	A98P	0.995
12:15962825:T:C	F129S	0.995
12:15982368:T:A	I190K	0.995
12:16032569:G:A	G222E	0.995
12:16036283:T:A	W268R	0.995
12:16036283:T:C	W268R	0.995
12:16036352:A:C	S291R	0.995
12:16036354:T:A	S291R	0.995
12:16036354:T:G	S291R	0.995
12:15958198:T:C	L47P	0.994
12:15959847:T:A	V99D	0.994
12:15982362:A:T	K188I	0.994
12:15982363:A:C	K188N	0.994
12:15982363:A:T	K188N	0.994

dbSNP variants (sampled 300 via entrez): RS1000013391 (12:16008487 C>T), RS1000018454 (12:15990510 G>A,T), RS1000033884 (12:16034868 G>T), RS1000073933 (12:15949556 T>C), RS1000085207 (12:15944727 A>C), RS1000141231 (12:15930164 G>C,T), RS1000168868 (12:16001648 C>G), RS1000210231 (12:15914490 G>A,T), RS1000261428 (12:15984947 C>G,T), RS1000262500 (12:15965668 C>G), RS1000296948 (12:15997751 G>A,C,T), RS1000325469 (12:15936125 C>T), RS1000327089 (12:15939251 C>T), RS1000400448 (12:15923442 C>T), RS1000435268 (12:15921194 A>G)

Disease associations

OMIM: gene MIM:619668 | disease phenotypes:

GenCC curated gene-disease

Mondo (0):

Orphanet (0):

HPO phenotypes

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

GWAS associations

5 associations (top):

Study	Trait	p-value
GCST003102_4	Bone mineral density (hip) and age at menarche	3.000000e-06
GCST007576_214	Chronotype	3.000000e-08
GCST008514_19	Peginterferon alfa-2a treatment response in chronic hepatitis B infection	5.000000e-06
GCST008514_20	Peginterferon alfa-2a treatment response in chronic hepatitis B infection	5.000000e-06
GCST009153_3	Adverse response to chemotherapy (amenorrhea) in breast cancer	3.000000e-07

EFO canonical traits (4, from GWAS)

EFO ID	Trait name
EFO:0004703	age at menarche
EFO:0007702	hip bone mineral density
EFO:0008328	chronotype measurement
EFO:0010103	response to peginterferon alfa-2a

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (1): CHEMBL4295988 (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
5.62	Kd	2417	nM	CHEMBL5653589
5.61	ED50	2451	nM	CHEMBL5653589
5.51	Kd	3092	nM	CHEMBL3752910
5.50	ED50	3135	nM	CHEMBL3752910

PubChem BioAssay actives

2 with measured affinity, of 6 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-[(2-methyl-6-pyridin-3-ylpyrazolo[3,4-d]pyrimidin-4-yl)amino]-N-[3-(trifluoromethyl)phenyl]benzamide	2148230: Binding affinity to human DERA incubated for 45 mins by Kinobead based pull down assay	kd	2.4172	uM
4-methyl-3-[(1-methyl-6-pyridin-3-ylpyrazolo[3,4-d]pyrimidin-4-yl)amino]-N-[3-(trifluoromethyl)phenyl]benzamide	2148230: Binding affinity to human DERA incubated for 45 mins by Kinobead based pull down assay	kd	3.0922	uM

CTD chemical–gene interactions

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

Chemical	Actions (top 5)	PubMed papers
bisphenol A	affects cotreatment, increases methylation, increases expression	2
Resveratrol	affects cotreatment, increases expression	2
Cisplatin	increases expression	2
Valproic Acid	affects expression, decreases methylation	2
Cyclosporine	decreases expression	2
aristolochic acid I	decreases expression	1
GSK-J4	decreases expression	1
bisphenol F	affects cotreatment, increases methylation	1
dicrotophos	decreases expression	1
biochanin A	decreases expression	1
triphenyl phosphate	affects expression	1
arsenite	affects binding, increases reaction	1
sodium arsenite	affects expression	1
cobaltous chloride	decreases expression	1
2,3-bis(3’-hydroxybenzyl)butyrolactone	increases expression, affects cotreatment	1
di-n-butylphosphoric acid	affects expression	1
4-(5-benzo(1,3)dioxol-5-yl-4-pyridin-2-yl-1H-imidazol-2-yl)benzamide	affects cotreatment, increases expression	1
erucylphospho-N,N,N-trimethylpropylammonium	decreases expression	1
LDN 193189	increases expression, affects cotreatment	1
Temozolomide	decreases expression	1
Sunitinib	decreases expression	1
Fulvestrant	affects cotreatment, increases methylation	1
Leflunomide	decreases expression	1
Acetaminophen	decreases expression	1
Air Pollutants	decreases expression, increases abundance	1
Benzo(a)pyrene	affects methylation	1
Coumestrol	affects cotreatment, increases expression	1
Dexamethasone	increases expression	1
Estradiol	increases expression	1
Ethyl Methanesulfonate	increases expression	1

ChEMBL screening assays

4 unique, capped per target: 4 binding

Representative assays (with source publication via chembl_document):

Assay ID	Type	Description	Source paper
CHEMBL4118651	Binding	Binding affinity to DERA in human NCI-H23 cells at 1 uM by mass spectrometry based pull down assay	Studies of TAK1-centered polypharmacology with novel covalent TAK1 inhibitors. — Bioorg Med Chem

Clinical trials (associated diseases)

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