RER1

Summary

RER1 (retention in endoplasmic reticulum sorting receptor 1, HGNC:30309) is a protein-coding gene on chromosome 1p36.32, encoding Protein RER1 (O15258). Involved in the retrieval of endoplasmic reticulum membrane proteins from the early Golgi compartment. It is a selective cancer dependency (DepMap: 10.4% of cell lines).

The protein encoded by this gene is a multi-pass membrane protein that is localized to the golgi apparatus. It is involved in the retention of endoplasmic reticulum (ER) membrane proteins in the ER and retrieval of ER membrane proteins from the early Golgi compartment to facilitate gamma-secretase complex assembly.

Source: NCBI Gene 11079 — RefSeq curated summary.

At a glance

• GWAS associations: 5
• Clinical variants (ClinVar): 24 total
• Druggable target: yes
• Cancer dependency (DepMap): dependent in 10.4% of screened cell lines
• MANE Select transcript: NM_007033

Identifiers

Gene identifiers

Field	Value
HGNC ID	HGNC:30309
Approved symbol	RER1
Name	retention in endoplasmic reticulum sorting receptor 1
Location	1p36.32
Locus type	gene with protein product
Status	Approved
Ensembl gene	ENSG00000157916
Ensembl biotype	protein_coding
OMIM	620048
Entrez	11079

Gene structure

Transcript identifiers

Ensembl transcripts: 48 — 46 protein_coding, 2 retained_intron

ENST00000306256, ENST00000378512, ENST00000378513, ENST00000378518, ENST00000443438, ENST00000462129, ENST00000488353, ENST00000493207, ENST00000605895, ENST00000874469, ENST00000874470, ENST00000874471, ENST00000874472, ENST00000874473, ENST00000874474, ENST00000874475, ENST00000874476, ENST00000874477, ENST00000874478, ENST00000874479, ENST00000874480, ENST00000874481, ENST00000874482, ENST00000874483, ENST00000874484, ENST00000874485, ENST00000874486, ENST00000920616, ENST00000920617, ENST00000920618, ENST00000920619, ENST00000920620, ENST00000920621, ENST00000920622, ENST00000920623, ENST00000920624, ENST00000920625, ENST00000920626, ENST00000920627, ENST00000920628, ENST00000920629, ENST00000920630, ENST00000954665, ENST00000954666, ENST00000954667, ENST00000954668, ENST00000954669, ENST00000954670

RefSeq mRNA: 1 — MANE Select: NM_007033 NM_007033

CCDS: CCDS41232

Canonical transcript exons

ENST00000605895 — 7 exons

Exon	Start	End
ENSE00001035864	2395784	2395871
ENSE00001035866	2399415	2399514
ENSE00001035875	2397116	2397220
ENSE00001412658	2391841	2391958
ENSE00003467094	2403035	2405436
ENSE00003591377	2400857	2400935
ENSE00003727037	2402207	2402342

Expression profiles

Bgee: expression breadth ubiquitous, 294 present calls, max score 98.88.

FANTOM5 (CAGE): breadth ubiquitous, TPM avg 98.8561 / max 310.3740, expressed in 1828 samples.

FANTOM5 promoters (1 alternative TSS)

Promoter ID	TPM avg	Samples expressed
216	98.8561	1828

Top tissues by expression

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

Tissue	Anatomy ID	Expression score	Quality
lower esophagus mucosa	UBERON:0035834	98.88	gold quality
right adrenal gland	UBERON:0001233	98.61	gold quality
left adrenal gland	UBERON:0001234	98.61	gold quality
left adrenal gland cortex	UBERON:0035825	98.60	gold quality
right adrenal gland cortex	UBERON:0035827	98.60	gold quality
left testis	UBERON:0004533	98.59	gold quality
right testis	UBERON:0004534	98.55	gold quality
rectum	UBERON:0001052	98.53	gold quality
esophagus mucosa	UBERON:0002469	98.46	gold quality
body of pancreas	UBERON:0001150	98.37	gold quality
adrenal cortex	UBERON:0001235	98.30	gold quality
skin of leg	UBERON:0001511	98.18	gold quality
adrenal gland	UBERON:0002369	98.15	gold quality
skin of abdomen	UBERON:0001416	98.11	gold quality
metanephros cortex	UBERON:0010533	98.10	gold quality
small intestine Peyer’s patch	UBERON:0003454	98.09	gold quality
stromal cell of endometrium	CL:0002255	98.07	gold quality
right lobe of liver	UBERON:0001114	98.05	gold quality
granulocyte	CL:0000094	98.04	gold quality
minor salivary gland	UBERON:0001830	98.03	gold quality
body of stomach	UBERON:0001161	97.98	gold quality
transverse colon	UBERON:0001157	97.94	gold quality
right ovary	UBERON:0002118	97.90	gold quality
adrenal tissue	UBERON:0018303	97.90	gold quality
mucosa of transverse colon	UBERON:0004991	97.89	gold quality
esophagus	UBERON:0001043	97.86	gold quality
gall bladder	UBERON:0002110	97.86	gold quality
left ovary	UBERON:0002119	97.85	gold quality
right lobe of thyroid gland	UBERON:0001119	97.81	gold quality
mouth mucosa	UBERON:0003729	97.79	gold quality

Single-cell (SCXA)

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

Experiment	Marker?	Max mean expression
E-HCAD-5	yes	33.71
E-GEOD-93593	yes	7.85
E-ANND-3	no	0.00

Regulation

Is transcription factor: no

miRNA regulators (miRDB)

93 targeting RER1, 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-1277-5P	100.00	73.95	5056
HSA-MIR-5692B	100.00	71.32	2622
HSA-MIR-5692C	100.00	71.32	2622
HSA-MIR-5011-5P	100.00	83.46	5820
HSA-MIR-190A-3P	100.00	80.35	5520
HSA-MIR-4668-3P	100.00	68.74	2635
HSA-MIR-3185	99.99	68.12	1959
HSA-MIR-371B-5P	99.99	75.34	4759
HSA-MIR-373-5P	99.98	75.36	4753
HSA-MIR-616-5P	99.98	75.58	4775
HSA-MIR-12136	99.98	72.81	5713
HSA-MIR-548AN	99.97	70.91	2817
HSA-MIR-3658	99.96	73.87	4379
HSA-MIR-3910	99.95	71.13	2227
HSA-MIR-96-5P	99.95	72.80	2140
HSA-MIR-205-3P	99.92	69.92	3165
HSA-MIR-145-5P	99.92	71.13	1836
HSA-MIR-5195-3P	99.92	70.92	1877
HSA-MIR-374A-5P	99.90	71.34	2923
HSA-MIR-374B-5P	99.90	69.98	2734
HSA-MIR-6783-3P	99.89	67.92	2059
HSA-MIR-1343-3P	99.89	66.78	1815
HSA-MIR-4731-5P	99.89	67.23	2537
HSA-MIR-369-3P	99.85	70.52	2264
HSA-MIR-1323	99.83	69.89	2471
HSA-MIR-4420	99.82	70.08	1624
HSA-MIR-6756-5P	99.82	67.97	2466
HSA-MIR-181B-2-3P	99.81	70.06	1646
HSA-MIR-181B-3P	99.81	70.06	1646
HSA-MIR-4659A-3P	99.80	72.62	4248

Functional genomics

DepMap (CRISPR cell-line fitness): dependent in 10.4% of screened cell lines.

Literature-anchored findings (GeneRIF, showing 9)

• Downregulation of Rer1 leads to increased surface localization of Pen2, whereas overexpression of Rer1 stabilizes unassembled Pen2. Rer1 is the first identified interaction partner of mammalian transmembrane-based retention/retrieval signals. (PMID:17668005)
• RER1 modulates amyloid-beta production by altering trafficking of gamma-secretase and amyloid precursor protein. (PMID:23043097)
• Synoviolin up-regulates amyloid beta production by targeting a negative regulator of gamma-secretase, Rer1, for degradation. (PMID:23129766)
• Rer1p depletion reduced ciliary length and function by increasing gamma-secretase complex assembly and activity and, consequently, enhancing Notch signaling as well as reducing Foxj1a expression. (PMID:23479743)
• Rer1p regulates the ER retention of immature or misfolded rhodopsin and modulates its intracellular trafficking through the early secretory pathway. (PMID:25096327)
• Charcot-Marie-Tooth disease-related PMP22 is trapped in the endoplasmic reticulum by calnexin-dependent retention and Rer1-mediated early Golgi retrieval systems and partly degraded by the Hrd1-mediated endoplasmic reticulum-associated degradation system. (PMID:25385046)
• RER1 is a novel and potential important mediator of elevated alphaSyn levels (PMID:28877262)
• Study in knockout mice and genetically modified human HAP1 cell line suggests that Rer1 maintains Notch signaling by maintaining sufficient expression of the gamma-secretase complex on the cell surface and regulating neural stem cell maintenance during cerebral cortex development. (PMID:30260951)
• The present study has demonstrated that RER1 enhances the progression of PC through promoting cell proliferation, migration and aggressiveness. (PMID:30630537)

Cross-species orthologs

5 orthologs

Organism	Symbol	Gene ID
danio_rerio	rer1	ENSDARG00000012747
mus_musculus	Rer1	ENSMUSG00000029048
rattus_norvegicus	Rer1	ENSRNOG00000014270
drosophila_melanogaster	CG11857	FBGN0039303
caenorhabditis_elegans		WBGENE00009783

Protein

Protein identifiers

Protein RER1 — O15258 (reviewed: O15258)

All UniProt accessions (6): A0A0A0MR06, O15258, Q5T091, Q5T092, Q5T093, Q5T094

UniProt curated annotations — full annotation on UniProt →

Function. Involved in the retrieval of endoplasmic reticulum membrane proteins from the early Golgi compartment.

Subcellular location. Golgi apparatus membrane.

Similarity. Belongs to the RER1 family.

RefSeq proteins (1): NP_008964* (*=MANE)

Domains & families (InterPro)

ID	Name	Type
IPR004932	Rer1	Family

Pfam: PF03248

UniProt features (11 total): modified residue 5, transmembrane region 3, initiator methionine 1, chain 1, sequence conflict 1

Structure

Experimental structures (PDB)

0 structures.

Predicted structure (AlphaFold)

Model	pLDDT	Fraction very-high
AF-O15258-F1	79.25	0.40

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 (5): 2, 2, 6, 10, 95

Function

Pathways and Gene Ontology

Reactome pathways

0 pathways

MSigDB gene sets: 184 (showing top): BROWNE_HCMV_INFECTION_30MIN_DN, GOBP_NEUROMUSCULAR_JUNCTION_DEVELOPMENT, MULLIGHAN_NPM1_SIGNATURE_3_UP, YAGI_AML_WITH_INV_16_TRANSLOCATION, MORF_RAB5A, ENK_UV_RESPONSE_KERATINOCYTE_UP, GOBP_POSITIVE_REGULATION_OF_PROTEIN_LOCALIZATION, GOCC_CELL_SURFACE, HSIAO_HOUSEKEEPING_GENES, TATTATA_MIR374, GOBP_VESICLE_MEDIATED_TRANSPORT, MORF_PSMC2, GOBP_PROTEIN_LOCALIZATION_TO_CELL_PERIPHERY, PATIL_LIVER_CANCER, GOBP_POSITIVE_REGULATION_OF_PROTEIN_LOCALIZATION_TO_CELL_PERIPHERY

GO Biological Process (5): protein retention in ER lumen (GO:0006621), retrograde vesicle-mediated transport, Golgi to endoplasmic reticulum (GO:0006890), skeletal muscle acetylcholine-gated channel clustering (GO:0071340), positive regulation of protein localization to plasma membrane (GO:1903078), neuromuscular junction development (GO:0007528)

GO Molecular Function (2): acetylcholine receptor binding (GO:0033130), protein binding (GO:0005515)

GO Cellular Component (8): Golgi membrane (GO:0000139), endoplasmic reticulum (GO:0005783), endoplasmic reticulum-Golgi intermediate compartment (GO:0005793), Golgi apparatus (GO:0005794), plasma membrane (GO:0005886), cell surface (GO:0009986), cytoplasm (GO:0005737), membrane (GO:0016020)

GO top-level categories

Rollup of top GO terms by namespace:

Category	Terms
cytoplasm	3
intracellular membrane-bounded organelle	3
cellular anatomical structure	3
endomembrane system	2
maintenance of protein localization in endoplasmic reticulum	1
Golgi vesicle transport	1
postsynaptic membrane organization	1
neuromuscular junction development	1
receptor clustering	1
protein localization to plasma membrane	1
regulation of protein localization to plasma membrane	1
positive regulation of protein localization to cell periphery	1
positive regulation of protein localization to membrane	1
synapse organization	1
signaling receptor binding	1
binding	1
Golgi apparatus	1
bounding membrane of organelle	1
membrane	1
cell periphery	1
intracellular anatomical structure	1

Protein interactions and networks

STRING

1444 interactions, top by confidence (×1000):

Protein A	Protein B	Partner UniProt	Score
RER1	PREB	Q9HCU5	833
RER1	PSENEN	Q9NZ42	775
RER1	KDELR1	P24390	692
RER1	MNS1	Q8NEH6	631
RER1	GOLPH3	Q9H4A6	621
RER1	SURF4	O15260	617
RER1	TTYH1	Q9H313	617
RER1	SEC63	Q9UGP8	595
RER1	LMAN1	P49257	591
RER1	ERGIC3	Q9Y282	590
RER1	MAN1B1	Q9UKM7	572
RER1	STX5	Q13190	566
RER1	COPE	O14579	566
RER1	ERGIC2	Q96RQ1	544
RER1	NCSTN	Q92542	543

IntAct

117 interactions, top by confidence:

A	B	Type	Score
NIPAL1	ESYT2	psi-mi:“MI:0914”(association)	0.640
ASPH	STXBP3	psi-mi:“MI:0914”(association)	0.640
RER1	WIPF1	psi-mi:“MI:0915”(physical association)	0.560
RER1	SCAND1	psi-mi:“MI:0915”(physical association)	0.560
RER1	SYT16	psi-mi:“MI:0915”(physical association)	0.560
SLC2A12	METTL15	psi-mi:“MI:0914”(association)	0.530
DPEP1	ILVBL	psi-mi:“MI:0914”(association)	0.530
SLC30A2	RER1	psi-mi:“MI:0914”(association)	0.530
TMEM184A	SLC33A1	psi-mi:“MI:0914”(association)	0.530
CCR6	PODXL	psi-mi:“MI:0914”(association)	0.530
SYCE3	RER1	psi-mi:“MI:0914”(association)	0.530
ATP1A3	AGPAT2	psi-mi:“MI:0914”(association)	0.530
SLC30A2	ESYT2	psi-mi:“MI:0914”(association)	0.530
NRAS	ESYT2	psi-mi:“MI:2364”(proximity)	0.480
env	PGRMC1	psi-mi:“MI:0914”(association)	0.460
SDC1	ILVBL	psi-mi:“MI:0915”(physical association)	0.400
	ESYT2	psi-mi:“MI:0914”(association)	0.350
E5	ESYT2	psi-mi:“MI:0914”(association)	0.350
HSCB	RBP5	psi-mi:“MI:0914”(association)	0.350
APP	MGST3	psi-mi:“MI:0914”(association)	0.350
UPK1A	TMEM223	psi-mi:“MI:0914”(association)	0.350
DPEP1	TMEM120B	psi-mi:“MI:0914”(association)	0.350
SYCE3	TRIM24	psi-mi:“MI:0914”(association)	0.350
	AP3D1	psi-mi:“MI:0914”(association)	0.350
CNR2	ILVBL	psi-mi:“MI:0914”(association)	0.350
Npc1	ESYT2	psi-mi:“MI:0914”(association)	0.350
COPB2	ESYT2	psi-mi:“MI:0914”(association)	0.350

BioGRID (226): RER1 (Affinity Capture-Western), PMP22 (Affinity Capture-Western), RER1 (Affinity Capture-Western), RER1 (Affinity Capture-MS), RER1 (Affinity Capture-MS), RER1 (Affinity Capture-MS), RER1 (Affinity Capture-MS), RER1 (Affinity Capture-MS), RER1 (Affinity Capture-MS), RER1 (Affinity Capture-MS), RER1 (Affinity Capture-MS), RER1 (Affinity Capture-RNA), RER1 (Co-fractionation), RER1 (Co-fractionation), RER1 (Co-fractionation)

ESM2 similar proteins: A0A1B4XBI5, A0MD35, A2BP21, A2BUK1, A2C057, A3PAU3, A4QKA0, A5PJ65, A8G5N5, E9PQX1, F5HDD0, O15258, O36388, O48670, O48671, O87787, P04135, P09175, P09298, P0C655, P24412, P28948, P28959, P33464, P36299, P46895, P51765, P52371, P68334, P84400, P9WEK8, Q00138, Q01017, Q04507, Q04565, Q197D8, Q1KZ54, Q31A92, Q3M5L6, Q46JV2

Diamond homologs: A5PJ65, O15258, O48670, O48671, P25560, P52879, P79003, Q10358, Q498C8, Q54D10, Q5R5U4, Q5ZHM5, Q9CQU3, Q9ZPV7, Q9ZWI7

SIGNOR signaling

0 interactions.

Enriched among interaction partners

Reactome pathways and GO biological processes over-represented among this gene’s 128 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
R-HSA-425366	5	11.3×	2e-03
Signaling by BRAF and RAF1 fusions	5	10.7×	2e-03
Class A/1 (Rhodopsin-like receptors)	9	8.3×	1e-04
SLC-mediated transmembrane transport	10	7.4×	1e-04
GPCR ligand binding	8	6.4×	1e-03
Peptide ligand-binding receptors	6	5.6×	5e-03
Transport of small molecules	13	4.1×	7e-04
Signaling by GPCR	8	4.0×	6e-03

GO biological processes:

GO term	Partners	Fold	FDR
amino acid transport	5	14.4×	8e-03
positive regulation of cytosolic calcium ion concentration	7	7.6×	8e-03

Disease & clinical

Clinical variants and AI predictions

ClinVar

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

Classification	Count (floor)
Pathogenic	0
Likely pathogenic	0
Uncertain significance	10
Likely benign	0
Benign	0

Top pathogenic / likely-pathogenic (0)

SpliceAI

1684 predictions. Top by Δscore:

Variant	Effect	Δscore
1:2391966:G:GT	donor_gain	1.0000
1:2391967:A:T	donor_gain	1.0000
1:2391970:GGC:G	donor_gain	1.0000
1:2397216:TGCAG:T	donor_loss	1.0000
1:2397217:GCAGG:G	donor_loss	1.0000
1:2397220:GGTA:G	donor_loss	1.0000
1:2397222:T:G	donor_loss	1.0000
1:2402338:TCAAG:T	donor_loss	1.0000
1:2402339:CAAG:C	donor_loss	1.0000
1:2402340:AAGGT:A	donor_loss	1.0000
1:2402341:AGGTA:A	donor_loss	1.0000
1:2402343:GTAA:G	donor_loss	1.0000
1:2402344:T:G	donor_loss	1.0000
1:2403033:A:AG	acceptor_gain	1.0000
1:2403034:G:GG	acceptor_gain	1.0000
1:2391360:T:A	donor_gain	0.9900
1:2391925:G:GT	donor_gain	0.9900
1:2392029:G:GT	donor_gain	0.9900
1:2395841:G:GA	donor_gain	0.9900
1:2397112:CTA:C	acceptor_loss	0.9900
1:2397113:TAGAT:T	acceptor_loss	0.9900
1:2397114:A:AG	acceptor_gain	0.9900
1:2397114:A:AT	acceptor_loss	0.9900
1:2397115:G:GG	acceptor_gain	0.9900
1:2397115:GATTT:G	acceptor_gain	0.9900
1:2398278:G:T	donor_gain	0.9900
1:2399409:TTTCA:T	acceptor_loss	0.9900
1:2399410:TTCA:T	acceptor_loss	0.9900
1:2399411:TCAGG:T	acceptor_loss	0.9900
1:2399412:CAG:C	acceptor_loss	0.9900

AlphaMissense

1288 scored. Top likely-pathogenic:

Variant	Protein change	am_pathogenicity
1:2397164:T:A	W44R	1.000
1:2397164:T:C	W44R	1.000
1:2399433:T:C	Y69H	1.000
1:2399455:T:C	L76P	1.000
1:2399461:T:C	L78P	1.000
1:2399472:T:C	F82L	1.000
1:2399474:T:A	F82L	1.000
1:2399474:T:G	F82L	1.000
1:2399476:T:C	L83P	1.000
1:2399482:C:A	P85H	1.000
1:2400895:T:C	F109L	1.000
1:2400897:C:A	F109L	1.000
1:2400897:C:G	F109L	1.000
1:2400904:T:C	F112L	1.000
1:2400905:T:G	F112C	1.000
1:2400906:C:A	F112L	1.000
1:2400906:C:G	F112L	1.000
1:2402277:T:C	F146L	1.000
1:2402279:C:A	F146L	1.000
1:2402279:C:G	F146L	1.000
1:2402280:T:A	W147R	1.000
1:2402280:T:C	W147R	1.000
1:2402287:T:A	I149N	1.000
1:2402290:T:A	L150Q	1.000
1:2402298:T:C	Y153H	1.000
1:2402311:T:A	L157H	1.000
1:2402311:T:C	L157P	1.000
1:2403040:G:A	M169I	1.000
1:2403040:G:C	M169I	1.000
1:2403040:G:T	M169I	1.000

dbSNP variants (sampled 300 via entrez): RS1000072187 (1:2399827 C>G,T), RS1000133224 (1:2394926 C>T), RS1000140309 (1:2400575 G>A), RS1000295618 (1:2397611 G>A), RS1000366264 (1:2399678 C>A,G,T), RS1000438809 (1:2392973 C>A,T), RS1000865154 (1:2405093 T>TGA), RS1000987998 (1:2390989 A>C,G), RS1001169594 (1:2394246 G>C), RS1001252551 (1:2396075 A>G), RS1001419117 (1:2391224 C>T), RS1001425317 (1:2401017 T>G), RS1001478555 (1:2392239 C>T), RS1002005641 (1:2397680 G>A), RS1002208599 (1:2395035 C>T)

Disease associations

OMIM: gene MIM:620048 | disease phenotypes: MIM:614870

GenCC curated gene-disease

Mondo (1): peroxisome biogenesis disorder 6A (Zellweger) (MONDO:0013936)

Orphanet (1): Zellweger syndrome (Orphanet:912)

HPO phenotypes

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

GWAS associations

5 associations (top):

Study	Trait	p-value
GCST005951_34	Body mass index	3.000000e-08
GCST005951_35	Body mass index	4.000000e-08
GCST009391_1801	Metabolite levels	4.000000e-06
GCST011816_1	Vitamin C levels	6.000000e-10
GCST90011900_34	Serum alkaline phosphatase levels	8.000000e-16

EFO canonical traits (4, from GWAS)

EFO ID	Trait name
EFO:0004340	body mass index
EFO:0010403	triacylglycerol 48:0 measurement
EFO:0600003	vitamin C measurement
EFO:0004533	alkaline phosphatase measurement

MeSH disease descriptors (1)

Descriptor	Name	Tree numbers
C566422	Peroxisome Biogenesis Disorder, Complementation Group 7 (supp.)

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (1): CHEMBL6066396 (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
5.40	Kd	3972	nM	CHEMBL5653589
5.40	ED50	3972	nM	CHEMBL5653589

PubChem BioAssay actives

1 with measured affinity, of 4 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-[(2-methyl-6-pyridin-3-ylpyrazolo[3,4-d]pyrimidin-4-yl)amino]-N-[3-(trifluoromethyl)phenyl]benzamide	2149217: Binding affinity to human RER1 incubated for 45 mins by Kinobead based pull down assay	kd	3.9724	uM

CTD chemical–gene interactions

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

Chemical	Actions (top 5)	PubMed papers
Valproic Acid	increases expression, affects expression, affects cotreatment	4
bisphenol A	decreases methylation, increases expression	3
Benzo(a)pyrene	affects methylation	2
FR900359	affects phosphorylation	1
triphenyl phosphate	affects expression	1
methylparaben	increases expression	1
isobutyl alcohol	increases abundance, increases expression, affects cotreatment	1
CGP 52608	affects binding, increases reaction	1
bisphenol B	increases expression	1
Grape Seed Proanthocyanidins	increases expression, affects cotreatment	1
bisphenol AF	increases expression	1
Acetaminophen	increases expression	1
Air Pollutants	affects expression, increases abundance	1
Atrazine	decreases expression	1
Cadmium	increases abundance, increases expression	1
Caffeine	affects phosphorylation	1
Carbamazepine	affects expression	1
Catechin	affects cotreatment, increases expression	1
Diethylhexyl Phthalate	increases expression	1
Doxorubicin	decreases expression	1
Gasoline	affects cotreatment, increases abundance, increases expression	1
Hydralazine	affects cotreatment, increases expression	1
Ivermectin	decreases expression	1
Ozone	affects expression, increases abundance	1
Polycyclic Aromatic Hydrocarbons	affects cotreatment, increases abundance, increases expression	1
Quercetin	decreases phosphorylation	1
Smoke	decreases expression	1
Testosterone	decreases expression	1
7,8-Dihydro-7,8-dihydroxybenzo(a)pyrene 9,10-oxide	increases expression	1
Sodium Selenite	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
CHEMBL5652259	Binding	Binding affinity to human RER1 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

Cellosaurus cell lines

2 cell lines: 2 cancer cell line

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

Cellosaurus	Name	Category	Sex
CVCL_TI80	HAP1 RER1 (-) 1	Cancer cell line	Male
CVCL_TI81	HAP1 RER1 (-) 2	Cancer cell line	Male

Clinical trials (associated diseases)

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