CECR2
gene geneOn this page
Also known as KIAA1740
Summary
CECR2 (CECR2 histone acetyl-lysine reader, HGNC:1840) is a protein-coding gene on chromosome 22q11.1-q11.21, encoding Chromatin remodeling regulator CECR2 (Q9BXF3). Regulatory subunit of the ATP-dependent CERF-1 and CERF-5 ISWI chromatin remodeling complexes, which form ordered nucleosome arrays on chromatin and facilitate access to DNA during DNA-templated processes such as DNA replication, transcription, and repair. It is a selective cancer dependency (DepMap: 36.4% of cell lines).
This gene encodes a bromodomain-containing protein that is involved in chromatin remodeling, and may additionally play a role in DNA damage response. The encoded protein functions as part of an ATP-dependent complex that is involved in neurulation. This gene is a candidate gene for Cat Eye Syndrome. Alternative splicing results in multiple transcript variants.
Source: NCBI Gene 27443 — RefSeq curated summary.
At a glance
- GWAS associations: 1
- Clinical variants (ClinVar): 48 total — 2 pathogenic, 3 likely-pathogenic
- Druggable target: yes
- Cancer dependency (DepMap): dependent in 36.4% of screened cell lines
- MANE Select transcript:
NM_001290047
Identifiers
Gene identifiers
| Field | Value |
|---|---|
| HGNC ID | HGNC:1840 |
| Approved symbol | CECR2 |
| Name | CECR2 histone acetyl-lysine reader |
| Location | 22q11.1-q11.21 |
| Locus type | gene with protein product |
| Status | Approved |
| Aliases | KIAA1740 |
| Ensembl gene | ENSG00000099954 |
| Ensembl biotype | protein_coding |
| OMIM | 607576 |
| Entrez | 27443 |
Gene structure
Transcript identifiers
Ensembl transcripts: 7 — 5 protein_coding, 1 nonsense_mediated_decay, 1 protein_coding_CDS_not_defined
ENST00000262608, ENST00000342247, ENST00000355219, ENST00000400585, ENST00000497534, ENST00000612582, ENST00000925336
RefSeq mRNA: 2 — MANE Select: NM_001290047
NM_001290046, NM_001290047
CCDS: CCDS77646, CCDS93111
Canonical transcript exons
ENST00000262608 — 19 exons
| Exon | Start | End |
|---|---|---|
| ENSE00001426606 | 17552835 | 17558151 |
| ENSE00001543635 | 17524118 | 17524271 |
| ENSE00001592054 | 17538993 | 17539119 |
| ENSE00001598036 | 17511813 | 17511896 |
| ENSE00001606307 | 17548148 | 17549564 |
| ENSE00001653782 | 17541839 | 17541967 |
| ENSE00001677027 | 17538520 | 17538557 |
| ENSE00001684496 | 17504847 | 17505016 |
| ENSE00001704267 | 17537103 | 17537232 |
| ENSE00001713996 | 17542157 | 17543003 |
| ENSE00001720235 | 17538640 | 17538731 |
| ENSE00001756874 | 17503082 | 17503131 |
| ENSE00001775438 | 17500631 | 17500735 |
| ENSE00001805660 | 17540412 | 17540800 |
| ENSE00003505471 | 17499410 | 17499549 |
| ENSE00003616125 | 17497403 | 17497586 |
| ENSE00003674122 | 17477588 | 17477682 |
| ENSE00003678912 | 17552031 | 17552142 |
| ENSE00003719738 | 17369460 | 17369909 |
Expression profiles
Bgee: expression breadth ubiquitous, 199 present calls, max score 89.77.
FANTOM5 (CAGE): breadth broad, TPM avg 4.5308 / max 156.1556, expressed in 483 samples.
FANTOM5 promoters (8 alternative TSS)
| Promoter ID | TPM avg | Samples expressed |
|---|---|---|
| 209372 | 2.5402 | 413 |
| 209374 | 1.0533 | 338 |
| 209373 | 0.5351 | 180 |
| 209375 | 0.1034 | 41 |
| 190975 | 0.0901 | 54 |
| 190971 | 0.0884 | 43 |
| 190973 | 0.0724 | 37 |
| 209376 | 0.0478 | 17 |
Top tissues by expression
249 total, by Bgee expression score (0-100, higher = more expressed):
| Tissue | Anatomy ID | Expression score | Quality |
|---|---|---|---|
| tibialis anterior | UBERON:0001385 | 89.77 | gold quality |
| biceps brachii | UBERON:0001507 | 87.57 | gold quality |
| deltoid | UBERON:0001476 | 87.54 | silver quality |
| vastus lateralis | UBERON:0001379 | 86.91 | silver quality |
| skeletal muscle tissue of biceps brachii | UBERON:0004502 | 86.39 | gold quality |
| quadriceps femoris | UBERON:0001377 | 86.19 | silver quality |
| skeletal muscle tissue | UBERON:0001134 | 86.16 | gold quality |
| secondary oocyte | CL:0000655 | 85.85 | gold quality |
| cerebellar hemisphere | UBERON:0002245 | 84.28 | gold quality |
| cerebellum | UBERON:0002037 | 84.16 | gold quality |
| cerebellar cortex | UBERON:0002129 | 84.16 | gold quality |
| skeletal muscle tissue of rectus abdominis | UBERON:0004511 | 84.13 | gold quality |
| right hemisphere of cerebellum | UBERON:0014890 | 83.93 | gold quality |
| gastrocnemius | UBERON:0001388 | 83.43 | gold quality |
| muscle of leg | UBERON:0001383 | 82.72 | gold quality |
| ganglionic eminence | UBERON:0004023 | 82.45 | gold quality |
| hindlimb stylopod muscle | UBERON:0004252 | 82.35 | gold quality |
| muscle tissue | UBERON:0002385 | 82.20 | gold quality |
| oocyte | CL:0000023 | 81.85 | gold quality |
| primordial germ cell in gonad | CL:0000670 ∩ UBERON:0000991 | 81.82 | gold quality |
| male germ line stem cell (sensu Vertebrata) in testis | CL:0000089 ∩ UBERON:0000473 | 80.83 | gold quality |
| medial globus pallidus | UBERON:0002477 | 78.55 | gold quality |
| ventricular zone | UBERON:0003053 | 78.30 | gold quality |
| liver | UBERON:0002107 | 78.02 | gold quality |
| right lobe of liver | UBERON:0001114 | 77.95 | gold quality |
| corpus callosum | UBERON:0002336 | 76.93 | gold quality |
| pancreatic ductal cell | CL:0002079 | 76.39 | silver quality |
| sural nerve | UBERON:0015488 | 75.93 | gold quality |
| globus pallidus | UBERON:0001875 | 75.59 | gold quality |
| pituitary gland | UBERON:0000007 | 75.34 | gold quality |
Single-cell (SCXA)
Detected in 1 experiment(s), a significant marker in 1.
| Experiment | Marker? | Max mean expression |
|---|---|---|
| E-ANND-3 | yes | 6.42 |
Regulation
Is transcription factor: no
Upstream regulators (CollecTRI, top): SALL4, SMARCA1, SMARCA5
Functional genomics
DepMap (CRISPR cell-line fitness): dependent in 36.4% of screened cell lines.
Literature-anchored findings (GeneRIF, showing 7)
- The genes CECR2, SLC25A18 and ATP6V1E1, mapping within the critical region for cat eye syndrome (CES), may be responsible for anorectal, renal and preauricular anomalies in patients with CES. (PMID:22395867)
- Cecr2 is important for gamma-H2AX formation and DNA double strand break repair, Cecr2 is a novel DNA damage response protein. (PMID:22699752)
- The bromodomains of BRD9, CECR2, and the second bromodomain of TAF1 recognize the longer butyryl mark on histones. In addition, the TAF1 second bromodomain is capable of binding crotonyl marks. (PMID:26365797)
- NMR Analyses of Acetylated H2A.Z Isoforms Identify Differential Binding Interactions with the Bromodomain of the NURF Nucleosome Remodeling Complex. (PMID:32356653)
- Discovery of a hidden transient state in all bromodomain families. (PMID:33468647)
- A novel tumor suppressor CECR2 down regulation links glutamine metabolism contributes tumor growth in laryngeal squamous cell carcinoma. (PMID:33826083)
- CECR2 drives breast cancer metastasis by promoting NF-kappaB signaling and macrophage-mediated immune suppression. (PMID:35108062)
Cross-species orthologs
5 orthologs
| Organism | Symbol | Gene ID |
|---|---|---|
| danio_rerio | cecr2 | ENSDARG00000078310 |
| mus_musculus | Cecr2 | ENSMUSG00000071226 |
| rattus_norvegicus | Cecr2 | ENSRNOG00000011566 |
| drosophila_melanogaster | Acf | FBGN0027620 |
| caenorhabditis_elegans | WBGENE00001470 |
Paralogs (11): BAZ1B (ENSG00000009954), BAZ2A (ENSG00000076108), KAT2A (ENSG00000108773), KAT2B (ENSG00000114166), BAZ2B (ENSG00000123636), BRDT (ENSG00000137948), BRD4 (ENSG00000141867), BRD3 (ENSG00000169925), BPTF (ENSG00000171634), BAZ1A (ENSG00000198604), BRD2 (ENSG00000204256)
Protein
Protein identifiers
Chromatin remodeling regulator CECR2 — Q9BXF3 (reviewed: Q9BXF3)
Alternative names: Cat eye syndrome critical region protein 2
All UniProt accessions (5): Q9BXF3, A0A087WT21, A0A0R4J2E1, B7WPH3, H0Y2Z1
UniProt curated annotations — full annotation on UniProt →
Function. Regulatory subunit of the ATP-dependent CERF-1 and CERF-5 ISWI chromatin remodeling complexes, which form ordered nucleosome arrays on chromatin and facilitate access to DNA during DNA-templated processes such as DNA replication, transcription, and repair. The complexes do not have the ability to slide mononucleosomes to the center of a DNA template. The CERF-1 ISWI chromatin remodeling complex has a lower ATP hydrolysis rate than the CERF-5 ISWI chromatin remodeling complex. Plays a role in various processes during development: required during embryogenesis for neural tube closure and inner ear development. In adults, required for spermatogenesis, via the formation of ISWI-type chromatin complexes. In histone-modifying complexes, CECR2 recognizes and binds acylated histones: binds histones that are acetylated and/or butyrylated. May also be involved through its interaction with LRPPRC in the integration of cytoskeletal network with vesicular trafficking, nucleocytosolic shuttling, transcription, chromosome remodeling and cytokinesis.
Subunit / interactions. Component of the CERF-1 ISWI chromatin remodeling complex (also called the CECR2-containing remodeling factor (CERF) complex) at least composed of CECR2 and SMARCA1. Component of the CERF-5 ISWI chromatin remodeling complex at least composed of SMARCA5/SNF2H and CECR2. LUZP1 is detected as part of the CERF-1 and CERF-5 complexes in embryonic stem (ES) cells where it is involved in complex stabilization but is not detected in the complexes in the testis. Interacts with CCAR2; CCAR2 may form part of the CERF-1 and/or CEF-5 ISWI chromatin remodeling complexes in ES cells. Interacts with acetylated lysine residues on histone H2A and H3 (in vitro). Interacts with LRPPRC.
Subcellular location. Nucleus.
Tissue specificity. Highly expressed in skeletal muscle, thymus, placenta and lung. Expressed at lower level in brain, heart, colon, spleen, kidney.
Domain organisation. The Bromo domain recognizes and binds acetylated histones. Also recognizes and binds histones that are butyrylated.
Miscellaneous. Candidate gene for the Cat Eye Syndrome (CES), a developmental disorder associated with the duplication of a 2 Mb region of 22q11.2. Duplication usually takes in the form of a surpernumerary bisatellited isodicentric chromosome, resulting in four copies of the region (represents an inv dup(22)(q11)). CES is characterized clinically by the combination of coloboma of the iris and anal atresia with fistula, downslanting palpebral fissures, preauricular tags and/or pits, frequent occurrence of heart and renal malformations, and normal or near-normal mental development.
Isoforms (3)
| UniProt ID | Names | Canonical? |
|---|---|---|
| Q9BXF3-1 | A | yes |
| Q9BXF3-2 | B, CECR2B | |
| Q9BXF3-3 | C |
RefSeq proteins (2): NP_001276975, NP_001276976* (*=MANE)
Domains & families (InterPro)
| ID | Name | Type |
|---|---|---|
| IPR001487 | Bromodomain | Domain |
| IPR018359 | Bromodomain_CS | Conserved_site |
| IPR029614 | CECR2 | Family |
| IPR036427 | Bromodomain-like_sf | Homologous_superfamily |
Pfam: PF00439
UniProt features (42 total): compositionally biased region 8, modified residue 7, region of interest 7, helix 7, splice variant 4, sequence conflict 4, sequence variant 2, chain 1, domain 1, strand 1
Structure
Experimental structures (PDB)
3 structures.
| PDB | Method | Resolution (Å) |
|---|---|---|
| 8RU1 | X-RAY DIFFRACTION | 1.66 |
| 3NXB | X-RAY DIFFRACTION | 1.83 |
| 5V84 | X-RAY DIFFRACTION | 2.7 |
Predicted structure (AlphaFold)
| Model | pLDDT | Fraction very-high |
|---|---|---|
| AF-Q9BXF3-F1 | 50.01 | 0.14 |
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 (7): 422, 546, 571, 1014, 1197, 1203, 1312
Function
Pathways and Gene Ontology
Reactome pathways
0 pathways
MSigDB gene sets: 186 (showing top):
GOBP_MORPHOGENESIS_OF_AN_EPITHELIUM, GOBP_SINGLE_FERTILIZATION, GOBP_EMBRYO_DEVELOPMENT_ENDING_IN_BIRTH_OR_EGG_HATCHING, GOBP_EPITHELIUM_DEVELOPMENT, GOBP_MACROMOLECULE_CATABOLIC_PROCESS, GOBP_NEUROGENESIS, GOBP_NEURAL_TUBE_DEVELOPMENT, GOBP_VESICLE_MEDIATED_TRANSPORT, GOBP_MORPHOGENESIS_OF_EMBRYONIC_EPITHELIUM, GOBP_DNA_CATABOLIC_PROCESS, GOBP_MORPHOGENESIS_OF_AN_EPITHELIAL_FOLD, GOBP_EAR_DEVELOPMENT, GOBP_CYTOKINESIS, LIAO_METASTASIS, RICKMAN_HEAD_AND_NECK_CANCER_A
GO Biological Process (13): neural fold formation (GO:0001842), neural tube closure (GO:0001843), apoptotic DNA fragmentation (GO:0006309), chromatin remodeling (GO:0006338), cytoskeleton organization (GO:0007010), single fertilization (GO:0007338), vesicle-mediated transport (GO:0016192), inner ear receptor cell stereocilium organization (GO:0060122), cytoskeleton-dependent cytokinesis (GO:0061640), cochlea development (GO:0090102), execution phase of apoptosis (GO:0097194), chromatin organization (GO:0006325), neural tube development (GO:0021915)
GO Molecular Function (2): ATP-dependent chromatin remodeler activity (GO:0140658), protein binding (GO:0005515)
GO Cellular Component (4): euchromatin (GO:0000791), nucleus (GO:0005634), CERF complex (GO:0090537), ISWI-type complex (GO:0031010)
GO top-level categories
Rollup of top GO terms by namespace:
| Category | Terms |
|---|---|
| primary neural tube formation | 2 |
| cellular process | 2 |
| morphogenesis of embryonic epithelium | 1 |
| anatomical structure formation involved in morphogenesis | 1 |
| morphogenesis of an epithelial fold | 1 |
| tube closure | 1 |
| DNA catabolic process | 1 |
| apoptotic nuclear changes | 1 |
| chromatin organization | 1 |
| organelle organization | 1 |
| fertilization | 1 |
| transport | 1 |
| neuron projection development | 1 |
| inner ear receptor cell development | 1 |
| cytokinesis | 1 |
| inner ear development | 1 |
| anatomical structure development | 1 |
| apoptotic process | 1 |
| bleb assembly | 1 |
| cellular component organization | 1 |
| nervous system development | 1 |
| tube development | 1 |
| chordate embryonic development | 1 |
| epithelium development | 1 |
| DNA binding | 1 |
| chromatin remodeling | 1 |
| ATP-dependent activity, acting on DNA | 1 |
| binding | 1 |
| chromatin | 1 |
| intracellular membrane-bounded organelle | 1 |
| ISWI-type complex | 1 |
| SWI/SNF superfamily-type complex | 1 |
Protein interactions and networks
STRING
1718 interactions, top by confidence (×1000):
| Protein A | Protein B | Partner UniProt | Score |
|---|---|---|---|
| CECR2 | SMARCA1 | P28370 | 972 |
| CECR2 | HEBP2 | Q9Y5Z4 | 914 |
| CECR2 | SMARCA5 | O60264 | 850 |
| CECR2 | UXT | Q9UBK9 | 845 |
| CECR2 | MAP1S | Q66K74 | 834 |
| CECR2 | LRPPRC | P42704 | 799 |
| CECR2 | BAZ2A | Q9UIF9 | 562 |
| CECR2 | BAZ1B | Q9UIG0 | 549 |
| CECR2 | BAZ2B | Q9UIF8 | 541 |
| CECR2 | HDHD5 | Q9BXW7 | 538 |
| CECR2 | BRD1 | O95696 | 533 |
| CECR2 | BRD7 | Q9NPI1 | 523 |
| CECR2 | BRD9 | Q9H8M2 | 516 |
| CECR2 | ATAD2 | Q6PL18 | 469 |
| CECR2 | SLC25A18 | Q9H1K4 | 462 |
IntAct
11 interactions, top by confidence:
| A | B | Type | Score |
|---|---|---|---|
| SMARCA1 | RBBP4 | psi-mi:“MI:0914”(association) | 0.770 |
| KPNA1 | TCERG1 | psi-mi:“MI:0914”(association) | 0.640 |
| CECR2 | SMARCA1 | psi-mi:“MI:0915”(physical association) | 0.620 |
| SMARCA5 | RBBP4 | psi-mi:“MI:0914”(association) | 0.530 |
| CECR2 | NEXN | psi-mi:“MI:0915”(physical association) | 0.400 |
| SLC16A11 | ESYT2 | psi-mi:“MI:0914”(association) | 0.350 |
| NUCKS1 | SMARCA5 | psi-mi:“MI:0914”(association) | 0.350 |
| PARP1 | KPNA3 | psi-mi:“MI:0914”(association) | 0.350 |
| SMARCA1 | CBX1 | psi-mi:“MI:0914”(association) | 0.350 |
| SOX7 | NFIB | psi-mi:“MI:2364”(proximity) | 0.270 |
BioGRID (59): CECR2 (Proximity Label-MS), CECR2 (Affinity Capture-MS), CECR2 (Affinity Capture-MS), CECR2 (Affinity Capture-MS), CECR2 (Proximity Label-MS), SMARCA5 (Affinity Capture-MS), SMARCA1 (Affinity Capture-MS), DBT (Affinity Capture-MS), TP53 (Affinity Capture-MS), CUL7 (Affinity Capture-MS), AKAP8 (Affinity Capture-MS), FXR2 (Affinity Capture-MS), TRIP6 (Affinity Capture-MS), TRAF7 (Affinity Capture-MS), FMR1 (Affinity Capture-MS)
ESM2 similar proteins: A0JPN4, A2A288, A2ARK0, A6ND36, A6QQJ8, A7E316, E9Q0S6, E9Q2Z1, O15037, O54714, O54967, O70260, O70405, O75385, O94983, P42335, P48778, Q07912, Q0P4K8, Q17R13, Q1LVK9, Q32PJ7, Q4V8I3, Q5D1E7, Q5D1E8, Q5DTV4, Q5HYM0, Q5JV73, Q5SWY7, Q5SXM2, Q5U2X5, Q5XIS1, Q68CZ2, Q6A037, Q6IRU7, Q6P1H6, Q6S5L8, Q7TP65, Q7TSG2, Q80U38
Diamond homologs: A0A0R4IXF6, A0A7U2QYM2, A2AHJ4, A2AUY4, A2BIL7, B2RRD7, B7ZS37, D4A7T3, E9Q2Z1, F1QW93, F1R5H6, F7DRV9, G5E8P1, O15164, O60885, O74350, O88379, O88665, O95696, P13709, P21675, P25440, P35817, P51123, P53236, P54816, P55201, P87152, Q02206, Q03330, Q07442, Q08D75, Q09948, Q12830, Q15059, Q1LUC3, Q23590, Q32S26, Q338B9, Q4R8Y1
SIGNOR signaling
2 interactions.
| A | Effect | B | Mechanism |
|---|---|---|---|
| CECR2 | “form complex” | CERF | binding |
| SALL4 | “up-regulates quantity by expression” | CECR2 | “transcriptional regulation” |
Disease & clinical
Clinical variants and AI predictions
ClinVar
48 variants total. Per-class counts are floors (≥ shown; pagination cap):
| Classification | Count (floor) |
|---|---|
| Pathogenic | 2 |
| Likely pathogenic | 3 |
| Uncertain significance | 4 |
| Likely benign | 4 |
| Benign | 11 |
Top pathogenic / likely-pathogenic (5)
| Variant ID | HGVS | Classification |
|---|---|---|
| 1807686 | GRCh37/hg19 22q11.1-11.21(chr22:16888900-18649190)x4 | Pathogenic |
| 443578 | GRCh37/hg19 22q11.1-11.21(chr22:16888899-18648856)x4 | Pathogenic |
| 4073549 | NM_001290047.2(CECR2):c.1737dup (p.Thr580fs) | Likely pathogenic |
| 4073551 | NM_001290047.2(CECR2):c.1819C>T (p.Arg607Ter) | Likely pathogenic |
| 4073552 | NM_001290047.2(CECR2):c.4153C>G (p.Gln1385Glu) | Likely pathogenic |
SpliceAI
4836 predictions. Top by Δscore:
| Variant | Effect | Δscore |
|---|---|---|
| 22:17477584:TCA:T | acceptor_loss | 1.0000 |
| 22:17477585:CAG:C | acceptor_loss | 1.0000 |
| 22:17477586:A:AG | acceptor_gain | 1.0000 |
| 22:17477586:A:G | acceptor_loss | 1.0000 |
| 22:17477586:AG:A | acceptor_gain | 1.0000 |
| 22:17477587:G:GT | acceptor_gain | 1.0000 |
| 22:17477587:GG:G | acceptor_gain | 1.0000 |
| 22:17477587:GGA:G | acceptor_gain | 1.0000 |
| 22:17477678:ATCAC:A | donor_gain | 1.0000 |
| 22:17477679:TCAC:T | donor_gain | 1.0000 |
| 22:17477680:CAC:C | donor_gain | 1.0000 |
| 22:17477681:AC:A | donor_gain | 1.0000 |
| 22:17477682:CG:C | donor_loss | 1.0000 |
| 22:17477683:GTGA:G | donor_gain | 1.0000 |
| 22:17477684:T:A | donor_loss | 1.0000 |
| 22:17477685:G:GT | donor_loss | 1.0000 |
| 22:17477686:A:AG | donor_gain | 1.0000 |
| 22:17477687:G:GG | donor_gain | 1.0000 |
| 22:17497383:T:TA | acceptor_gain | 1.0000 |
| 22:17497387:T:A | acceptor_gain | 1.0000 |
| 22:17497388:G:A | acceptor_gain | 1.0000 |
| 22:17497395:T:TA | acceptor_gain | 1.0000 |
| 22:17497396:G:A | acceptor_gain | 1.0000 |
| 22:17497397:GTCTA:G | acceptor_gain | 1.0000 |
| 22:17497399:CTAG:C | acceptor_loss | 1.0000 |
| 22:17497399:CTAGG:C | acceptor_gain | 1.0000 |
| 22:17497400:TA:T | acceptor_loss | 1.0000 |
| 22:17497400:TAG:T | acceptor_gain | 1.0000 |
| 22:17497401:A:AG | acceptor_gain | 1.0000 |
| 22:17497401:AG:A | acceptor_gain | 1.0000 |
AlphaMissense
9569 scored. Top likely-pathogenic:
| Variant | Protein change | am_pathogenicity |
|---|---|---|
| 22:17369835:T:A | W18R | 1.000 |
| 22:17369835:T:C | W18R | 1.000 |
| 22:17369837:G:C | W18C | 1.000 |
| 22:17369837:G:T | W18C | 1.000 |
| 22:17369845:C:A | P21Q | 1.000 |
| 22:17369851:T:A | I23N | 1.000 |
| 22:17369859:T:C | F26L | 1.000 |
| 22:17369861:C:A | F26L | 1.000 |
| 22:17369861:C:G | F26L | 1.000 |
| 22:17369871:T:C | F30L | 1.000 |
| 22:17369873:T:A | F30L | 1.000 |
| 22:17369873:T:G | F30L | 1.000 |
| 22:17369883:T:C | F34L | 1.000 |
| 22:17369885:C:A | F34L | 1.000 |
| 22:17369885:C:G | F34L | 1.000 |
| 22:17369890:T:C | L36P | 1.000 |
| 22:17477592:T:C | L44S | 1.000 |
| 22:17477637:T:C | L59P | 1.000 |
| 22:17477649:T:C | L63P | 1.000 |
| 22:17477652:T:A | L64H | 1.000 |
| 22:17477652:T:C | L64P | 1.000 |
| 22:17497426:T:C | L82P | 1.000 |
| 22:17497447:G:C | R89P | 1.000 |
| 22:17497449:T:A | W90R | 1.000 |
| 22:17497449:T:C | W90R | 1.000 |
| 22:17497531:T:C | L117P | 1.000 |
| 22:17497540:T:C | L120P | 1.000 |
| 22:17497542:T:C | C121R | 1.000 |
| 22:17497543:G:A | C121Y | 1.000 |
| 22:17497544:T:G | C121W | 1.000 |
dbSNP variants (sampled 300 via entrez): RS1000002778 (22:17454260 C>G), RS1000014133 (22:17427025 G>A,C), RS1000027772 (22:17555567 C>G,T), RS1000051609 (22:17454066 AC>A), RS1000072717 (22:17539672 A>G), RS1000079412 (22:17432304 C>T), RS1000098995 (22:17502536 G>C,T), RS1000102038 (22:17466154 G>A), RS1000109157 (22:17525509 G>C), RS1000116644 (22:17358062 A>G), RS1000134676 (22:17465907 C>T), RS1000144723 (22:17391627 A>G), RS1000149045 (22:17483479 C>T), RS1000163660 (22:17516090 C>T), RS1000176815 (22:17549977 C>A,T)
Disease associations
OMIM: gene MIM:607576 | 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 |
|---|---|---|
| GCST005959_7 | Waist-to-hip ratio adjusted for BMI x sex interaction | 1.000000e-06 |
EFO canonical traits (2, from GWAS)
| EFO ID | Trait name |
|---|---|
| EFO:0007788 | BMI-adjusted waist-hip ratio |
| EFO:0008343 | sex interaction measurement |
Drugs & pharmacology
Drug and pharmacology data
Is drug target: yes
ChEMBL targets (2): CHEMBL3108639 (SINGLE PROTEIN), CHEMBL6195542 (PROTEIN-PROTEIN INTERACTION)
PharmGKB: 1 entry (VIP=true, CPIC=false)
GtoPdb / IUPHAR curated pharmacology
(IUPHAR/BPS Guide to Pharmacology — expert-curated)
Target class: other protein — Non-enzymatic BRD containing proteins
Most potent curated ligand interactions (2 total), top 2:
| Ligand | Action | Affinity | Parameter |
|---|---|---|---|
| NVS-1 | Inhibition | 7.33 | pIC50 |
| compound 50 [PMID: 24313754] | Inhibition | 6.8 | pIC50 |
Binding affinities (BindingDB)
38 measured of 38 human assays (38 total across all organisms); most potent 38 below. Values come from heterogeneous assays and are not directly comparable.
| Ligand | Measure | Value | Patent |
|---|---|---|---|
| 6-(but-3-en-1-yl)-4-(3-(difluoromethoxy)-5-(morpholine-4-carbonyl)phenyl)-1H-pyrrolo[2,3-c]pyridin-7(6H)-one | IC50 | 10 nM | US-10183009: Therapeutic compounds and uses thereof |
| 6-but-3-enyl-4-[4-fluoro-3-(morpholine-4-carbonyl)phenyl]-1H-pyrrolo[2,3-c]pyridin-7-one | IC50 | 11 nM | US-10183009: Therapeutic compounds and uses thereof |
| 6-but-3-enyl-4-[3-methyl-7-(morpholine-4-carbonyl)benzimidazol-5-yl]-1H-pyrrolo[2,3-e]pyridin-7-one and 6-but-3-enyl-4-[1-methyl-7-(morpholine-4-carbonyl)benzimidazol-5-yl]-1H-pyrrolo[2,3-c]pyridin-7-one | IC50 | 11 nM | US-10183009: Therapeutic compounds and uses thereof |
| 6-but-3-enyl-4-[1-methyl-6-(morpholine-4-carbonyl)benzimidazol-4-yl]-1H-pyrrolo[2,3-e]pyridin-7-one | IC50 | 11 nM | US-10183009: Therapeutic compounds and uses thereof |
| 6-but-3-enyl-4-[4-fluoro-3-(morpholine-4-carbonyl)phenyl]-2-methyl-1H-pyrrolo[2,3-c]pyridin-7-one | IC50 | 11 nM | US-10183009: Therapeutic compounds and uses thereof |
| 6-but-3-enyl-4-[6-(morpholine-4-carbonyl)-1H-benzimidazol-4-yl]-1H-pyrrolo[2,3-c]pyridin-7-one | IC50 | 12 nM | US-10183009: Therapeutic compounds and uses thereof |
| 6-but-3-enyl-4-[4-chloro-3-(morpholine-4-carbonyl)phenyl]-2-methyl-1H-pyrrolo[2,3-c]pyridin-7-one | IC50 | 12 nM | US-10183009: Therapeutic compounds and uses thereof |
| 6-but-3-enyl-4-[3-ethyl-7-(morpholine-4-carbonyl)benzimidazol-5-yl]-1H-pyrrolo[2,3-c]pyridin-7-one | IC50 | 14 nM | US-10183009: Therapeutic compounds and uses thereof |
| 6-but-3-enyl-4-[3-fluoro-5-(morpholine-4-carbonyl)phenyl]-2-methyl-1H-pyrrolo[2,3-c]pyridin-7-one | IC50 | 14 nM | US-10183009: Therapeutic compounds and uses thereof |
| 6-but-3-enyl-4-[3,4-difluoro-5-(morpholine-4-carbonyl)phenyl]-1H-pyrrolo[2,3-c]pyridin-7-one | IC50 | 17 nM | US-10183009: Therapeutic compounds and uses thereof |
| 6-but-3-enyl-4-[3-fluoro-5-(3-methylmorpholine-4-carbonyl)phenyl]-1H-pyrrolo[2,3-c]pyridin-7-one | IC50 | 19 nM | US-10183009: Therapeutic compounds and uses thereof |
| 6-but-3-enyl-4-[3-fluoro-5-(morpholine-4-carbonyl)phenyl]-1H-pyrrolo[2,3-c]pyridin-7-one | IC50 | 20 nM | US-10183009: Therapeutic compounds and uses thereof |
| 4-(6-(but-3-en-1-yl)-7-oxo-6,7-dihydro-1H-pyrrolo[2,3-c]pyridin-4-yl)-N,N-dimethyl-1H-benzo[d]imidazole-6-carboxamide | IC50 | 20 nM | US-10183009: Therapeutic compounds and uses thereof |
| 3-(6-but-3-enyl-7-oxo-1H-pyrrolo[2,3-c]pyridin-4-yl)-5-(morpholine-4-carbonyl)benzonitrile | IC50 | 21 nM | US-10183009: Therapeutic compounds and uses thereof |
| 6-but-3-enyl-4-[7-(morpholine-4-carbonyl)-3H-benzimidazol-5-yl]-1H-pyrrolo[2,3-c]pyridin-7-one | IC50 | 21 nM | US-10183009: Therapeutic compounds and uses thereof |
| 2-methyl-7-(6-methyl-7-oxo-3aH-pyrrolo[2,3-c]pyridin-4-yl)-4H-1,4-benzoxazin-3-one | IC50 | 36 nM | US-10150767: Therapeutic compounds and uses thereof |
| 6-methyl-4-(1,2,3,4-tetrahydroisoquinolin-6-yl)-3aH-pyrrolo[2,3-c]pyridin-7-one | IC50 | 54 nM | US-10150767: Therapeutic compounds and uses thereof |
| 4-(6-methyl-7-oxo-2,3,3a,4,5,7a-hexahydro-1H-pyrrolo[2,3-c]pyridin-4-yl)-N-phenylbenzamide | IC50 | 75 nM | US-10150767: Therapeutic compounds and uses thereof |
| 6-but-3-enyl-4-[3-(5-methyl-1,3,4-oxadiazol-2-yl)phenyl]-1H-pyrrolo[2,3-c]pyridin-7-one | IC50 | 95 nM | US-10183009: Therapeutic compounds and uses thereof |
| 3-(6-but-3-enyl-7-oxo-1H-pyrrolo[2,3-c]pyridin-4-yl)-N,N-dimethyl-benzamide | IC50 | 110 nM | US-10183009: Therapeutic compounds and uses thereof |
| 4-[4-(3,3-difluoroazetidine-1-carbonyl)phenyl]-6-methyl-3aH-pyrrolo[2,3-c]pyridin-7-one | IC50 | 130 nM | US-10150767: Therapeutic compounds and uses thereof |
| 3-(2,6-dimethyl-7-oxo-2,3,3a,4,5,7a-hexahydro-1H-pyrrolo[2,3-c]pyridin-4-yl)-N,N-dimethylbenzamide | IC50 | 130 nM | US-10150767: Therapeutic compounds and uses thereof |
| 3-methoxy-N-[4-(6-methyl-7-oxo-3aH-pyrrolo[2,3-c]pyridin-4-yl)phenyl]propanamide | IC50 | 170 nM | US-10150767: Therapeutic compounds and uses thereof |
| 6-methyl-4-[4-(4-methyl-3-oxopiperazine-1-carbonyl)phenyl]-3aH-pyrrolo[2,3-c]pyridin-7-one | IC50 | 240 nM | US-10150767: Therapeutic compounds and uses thereof |
| 3-(6-(2-cyclopropylethyl)-2-methyl-7-oxo-6,7-dihydro-1H-pyrrolo[2,3-c]pyridin-4-yl)-N,N-dimethylbenzamide | IC50 | 480 nM | US-10183009: Therapeutic compounds and uses thereof |
| 3-(6-but-2-enyl-7-oxo-1H-pyrrolo[2,3-c]pyridin-4-yl)-N-methyl-benzamide | IC50 | 640 nM | US-10183009: Therapeutic compounds and uses thereof |
| N,N-dimethyl-4-(6-methyl-7-oxo-2,3,3a,4,5,7a-hexahydro-1H-pyrrolo[2,3-c]pyridin-4-yl)benzamide | IC50 | 730 nM | US-10150767: Therapeutic compounds and uses thereof |
| 4-[5-(6-acetyl-2,6-diazaspiro[3.3]heptane-2-carbonyl)-2-methoxy-phenyl]-6-[(E)-but-2-enyl]-1H-pyrrolo[2,3-c]pyridin-7-one | IC50 | 900 nM | US-10183009: Therapeutic compounds and uses thereof |
| 3-(6-ethyl-7-oxo-3aH-pyrrolo[2,3-c]pyridin-4-yl)-N,N-dimethylbenzamide | IC50 | 1300 nM | US-10150767: Therapeutic compounds and uses thereof |
| 4-[6-[(E)-but-2-enyl]-7-oxo-1H-pyrrolo[2,3-c]pyridin-4-yl]-2-chloro-benzamide | IC50 | 1600 nM | US-10183009: Therapeutic compounds and uses thereof |
| 4-[5-(azetidine-1-carbonyl)-2-methoxy-phenyl]-6-[(E)-but-2-enyl]-1H-pyrrolo[2,3-c]pyridin-7-one | IC50 | 1800 nM | US-10183009: Therapeutic compounds and uses thereof |
| 3-[6-(2-methoxyethyl)-7-oxo-1H-pyrrolo[2,3-c]pyridin-4-yl]-N,N-dimethyl-benzamide | IC50 | 2000 nM | US-10183009: Therapeutic compounds and uses thereof |
| 4-[6-[(E)-but-2-enyl]-7-oxo-1H-pyrrolo[2,3-c]pyridin-4-yl]-2-chloro-N,N-dimethyl-benzamide | IC50 | 2000 nM | US-10183009: Therapeutic compounds and uses thereof |
| 3-[6-(2-cyclopropylethyl)-7-oxo-1H-pyrrolo[2,3-c]pyridin-4-yl]-4-methoxy-benzonitrile | IC50 | 3400 nM | US-10183009: Therapeutic compounds and uses thereof |
| 6-but-2-enyl-4-[4-(hydroxymethyl)phenyl]-1H-pyrrolo[2,3-c]pyridin-7-one | IC50 | 4500 nM | US-10183009: Therapeutic compounds and uses thereof |
| N,N-dimethyl-3-[6-(3-methylbut-2-enyl)-7-oxo-1H-pyrrolo[2,3-c]pyridin-4-yl]benzamide | IC50 | 5200 nM | US-10183009: Therapeutic compounds and uses thereof |
| 3-[6-(cyclopropylmethyl)-7-oxo-1H-pyrrolo[2,3-c]pyridin-4-yl]-N,N-dimethyl-benzamide | IC50 | 5600 nM | US-10183009: Therapeutic compounds and uses thereof |
| 3-[6-(3-methoxypropyl)-7-oxo-1H-pyrrolo[2,3-c]pyridin-4-yl]-N,N-dimethyl-benzamide | IC50 | 9300 nM | US-10183009: Therapeutic compounds and uses thereof |
ChEMBL bioactivities
212 potent at pChembl≥5 of 228 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).
PubChem BioAssay actives
147 with measured affinity, of 297 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 |
|---|---|---|---|---|
| 4-[4-[(dimethylamino)methyl]-3,5-dimethoxyphenyl]-2-methyl-2,7-naphthyridin-1-one | 2191062: Binding affinity to CECR2 (unknown origin) assessed as dissociation constant by bromoKdselect analysis | kd | 0.0010 | uM |
| N-[4-bromo-3-[(3R)-3-cyclopropylpyrrolidin-1-yl]sulfonylphenyl]-2-(5-methyl-6,7-dihydro-4H-triazolo[4,5-c]pyridin-1-yl)acetamide | 1561896: Displacement of Alexa Fluor 647-labeled GSK tracer from FLAG-6His-Tev-fused CECR2 (424 to 543 residue) (unknown origin) measured after 15 mins by TR-FRET assay | ic50 | 0.0063 | uM |
| N-[4-chloro-3-[(3R)-3-cyclopropylpyrrolidin-1-yl]sulfonylphenyl]-2-(5-methyl-6,7-dihydro-4H-triazolo[4,5-c]pyridin-1-yl)acetamide | 1561910: Binding affinity to human partial length CECR2 (P423 to D543 residues) expressed in bacterial expression system by BROMOscan assay | kd | 0.0079 | uM |
| ethyl N-[6-[3-(methanesulfonamido)-4-methylphenyl]-3-methyl-[1,2,4]triazolo[4,3-b]pyridazin-8-yl]carbamate | 1995398: Binding affinity to CECR2 (unknown origin) assessed as dissociation constant by site-directed competition binding assay | kd | 0.0080 | uM |
| 6-[4-[3-(dimethylamino)propoxy]phenyl]-2-methylsulfonyl-N-(3-pyrazol-1-ylpropyl)pyrimidin-4-amine | 1561964: Binding affinity to CECR2 (unknown origin) by ITC analysis | kd | 0.0100 | uM |
| 5-[4-(2-aminoethyl)anilino]-4-chloro-2-methylpyridazin-3-one | 1769026: Binding affinity to CECR2 (unknown origin) by BROMOscan method | kd | 0.0110 | uM |
| N-[1-[6-(3-methoxyphenyl)pyrimidin-4-yl]piperidin-4-yl]-N-methyl-7-oxo-6-prop-2-enyl-1H-pyrrolo[2,3-c]pyridine-4-carboxamide | 1488887: Inhibition of recombinant human N-terminal His6-FLAG-tagged CECR2 expressed in Rosetta2 (DE3) pLysS cells after 60 mins by TR-FRET assay | ic50 | 0.0160 | uM |
| N-[4-bromo-3-[(3S)-3-methylpyrrolidin-1-yl]sulfonylphenyl]-2-[(4S)-4-cyclopropyl-4-methyl-2,5-dioxoimidazolidin-1-yl]acetamide | 1561910: Binding affinity to human partial length CECR2 (P423 to D543 residues) expressed in bacterial expression system by BROMOscan assay | kd | 0.0251 | uM |
| N-[4-bromo-3-[(3S)-3-methylpyrrolidin-1-yl]sulfonylphenyl]-2-(5-propan-2-yl-6,7-dihydro-4H-triazolo[4,5-c]pyridin-1-yl)acetamide | 1561896: Displacement of Alexa Fluor 647-labeled GSK tracer from FLAG-6His-Tev-fused CECR2 (424 to 543 residue) (unknown origin) measured after 15 mins by TR-FRET assay | ic50 | 0.0316 | uM |
| N-[4-bromo-3-[(3S)-3-cyclopropylpyrrolidin-1-yl]sulfonylphenyl]-2-(5-methyl-6,7-dihydro-4H-triazolo[4,5-c]pyridin-1-yl)acetamide | 1561896: Displacement of Alexa Fluor 647-labeled GSK tracer from FLAG-6His-Tev-fused CECR2 (424 to 543 residue) (unknown origin) measured after 15 mins by TR-FRET assay | ic50 | 0.0398 | uM |
| N-[1-[6-(2-fluorophenyl)pyrimidin-4-yl]piperidin-4-yl]-N-methyl-7-oxo-6-prop-2-enyl-1H-pyrrolo[2,3-c]pyridine-4-carboxamide | 1488887: Inhibition of recombinant human N-terminal His6-FLAG-tagged CECR2 expressed in Rosetta2 (DE3) pLysS cells after 60 mins by TR-FRET assay | ic50 | 0.0440 | uM |
| N-[1-[6-(2-methoxyphenyl)pyrimidin-4-yl]piperidin-4-yl]-N-methyl-7-oxo-6-prop-2-enyl-1H-pyrrolo[2,3-c]pyridine-4-carboxamide | 1488887: Inhibition of recombinant human N-terminal His6-FLAG-tagged CECR2 expressed in Rosetta2 (DE3) pLysS cells after 60 mins by TR-FRET assay | ic50 | 0.0450 | uM |
| N-[1-[6-(furan-2-yl)pyrimidin-4-yl]piperidin-4-yl]-N-methyl-7-oxo-6-prop-2-enyl-1H-pyrrolo[2,3-c]pyridine-4-carboxamide | 1488887: Inhibition of recombinant human N-terminal His6-FLAG-tagged CECR2 expressed in Rosetta2 (DE3) pLysS cells after 60 mins by TR-FRET assay | ic50 | 0.0450 | uM |
| N-methyl-N-[1-[6-(2-methylphenyl)pyrimidin-4-yl]piperidin-4-yl]-7-oxo-6-prop-2-enyl-1H-pyrrolo[2,3-c]pyridine-4-carboxamide | 1488887: Inhibition of recombinant human N-terminal His6-FLAG-tagged CECR2 expressed in Rosetta2 (DE3) pLysS cells after 60 mins by TR-FRET assay | ic50 | 0.0460 | uM |
| N-cyclopropyl-2-propylsulfonyl-6-[1-(2,2,6,6-tetramethylpiperidin-4-yl)indol-5-yl]pyrimidin-4-amine | 1289187: Binding affinity to CERC2 (unknown origin) by alphascreen assay | ic50 | 0.0470 | uM |
| N-[4-bromo-3-[(3S)-3-methylpyrrolidin-1-yl]sulfonylphenyl]-2-(5-methyl-6,7-dihydro-4H-triazolo[4,5-c]pyridin-1-yl)acetamide | 1561896: Displacement of Alexa Fluor 647-labeled GSK tracer from FLAG-6His-Tev-fused CECR2 (424 to 543 residue) (unknown origin) measured after 15 mins by TR-FRET assay | ic50 | 0.0501 | uM |
| N-[4-bromo-3-[(3S)-3-methylpyrrolidin-1-yl]sulfonylphenyl]-2-(5-ethyl-6,7-dihydro-4H-triazolo[4,5-c]pyridin-1-yl)acetamide | 1561896: Displacement of Alexa Fluor 647-labeled GSK tracer from FLAG-6His-Tev-fused CECR2 (424 to 543 residue) (unknown origin) measured after 15 mins by TR-FRET assay | ic50 | 0.0501 | uM |
| N-[1-(6-cyclopropyl-2-methylpyrimidin-4-yl)piperidin-4-yl]-N-methyl-7-oxo-6-prop-2-enyl-1H-pyrrolo[2,3-c]pyridine-4-carboxamide | 1488887: Inhibition of recombinant human N-terminal His6-FLAG-tagged CECR2 expressed in Rosetta2 (DE3) pLysS cells after 60 mins by TR-FRET assay | ic50 | 0.0520 | uM |
| N-[1-(6-tert-butylpyrimidin-4-yl)piperidin-4-yl]-N-methyl-7-oxo-6-prop-2-enyl-1H-pyrrolo[2,3-c]pyridine-4-carboxamide | 1488887: Inhibition of recombinant human N-terminal His6-FLAG-tagged CECR2 expressed in Rosetta2 (DE3) pLysS cells after 60 mins by TR-FRET assay | ic50 | 0.0550 | uM |
| N-methyl-7-oxo-6-prop-2-enyl-N-[1-(6-pyrazol-1-ylpyrimidin-4-yl)piperidin-4-yl]-1H-pyrrolo[2,3-c]pyridine-4-carboxamide | 1488887: Inhibition of recombinant human N-terminal His6-FLAG-tagged CECR2 expressed in Rosetta2 (DE3) pLysS cells after 60 mins by TR-FRET assay | ic50 | 0.0590 | uM |
| N-[4-bromo-3-[(3S)-3-methylpyrrolidin-1-yl]sulfonylphenyl]-2-(2-oxo-1,3-benzoxazol-3-yl)acetamide | 1561896: Displacement of Alexa Fluor 647-labeled GSK tracer from FLAG-6His-Tev-fused CECR2 (424 to 543 residue) (unknown origin) measured after 15 mins by TR-FRET assay | ic50 | 0.0631 | uM |
| N-[1-(6-methoxy-2-methylpyrimidin-4-yl)piperidin-4-yl]-N-methyl-7-oxo-6-prop-2-enyl-1H-pyrrolo[2,3-c]pyridine-4-carboxamide | 1488887: Inhibition of recombinant human N-terminal His6-FLAG-tagged CECR2 expressed in Rosetta2 (DE3) pLysS cells after 60 mins by TR-FRET assay | ic50 | 0.0710 | uM |
| 4-[4-[(dimethylamino)methyl]-2,5-dimethoxyphenyl]-2-methyl-2,7-naphthyridin-1-one | 1309655: Binding affinity to human CECR2 expressed in Escherichia coli L21(DE3)-R3-pRARE2 cells by BROMOScan analysis | kd | 0.0770 | uM |
| N-[4-bromo-3-[(3S)-3-methylpyrrolidin-1-yl]sulfonylphenyl]-2-(5-propyltriazol-1-yl)acetamide | 1561896: Displacement of Alexa Fluor 647-labeled GSK tracer from FLAG-6His-Tev-fused CECR2 (424 to 543 residue) (unknown origin) measured after 15 mins by TR-FRET assay | ic50 | 0.0794 | uM |
| N-[4-bromo-3-[(3S)-3-methylpyrrolidin-1-yl]sulfonylphenyl]-2-[5-[(dimethylamino)methyl]triazol-1-yl]acetamide | 1561896: Displacement of Alexa Fluor 647-labeled GSK tracer from FLAG-6His-Tev-fused CECR2 (424 to 543 residue) (unknown origin) measured after 15 mins by TR-FRET assay | ic50 | 0.0794 | uM |
| N-[1-(6-cyclopropylpyrimidin-4-yl)piperidin-4-yl]-N-methyl-7-oxo-6-prop-2-enyl-1H-pyrrolo[2,3-c]pyridine-4-carboxamide | 1488887: Inhibition of recombinant human N-terminal His6-FLAG-tagged CECR2 expressed in Rosetta2 (DE3) pLysS cells after 60 mins by TR-FRET assay | ic50 | 0.0830 | uM |
| N-[1-(2,6-dimethylpyrimidin-4-yl)piperidin-4-yl]-N-methyl-7-oxo-6-prop-2-enyl-1H-pyrrolo[2,3-c]pyridine-4-carboxamide | 1488887: Inhibition of recombinant human N-terminal His6-FLAG-tagged CECR2 expressed in Rosetta2 (DE3) pLysS cells after 60 mins by TR-FRET assay | ic50 | 0.0930 | uM |
| 2-(5-acetyl-6,7-dihydro-4H-triazolo[4,5-c]pyridin-1-yl)-N-[4-bromo-3-[(3S)-3-methylpyrrolidin-1-yl]sulfonylphenyl]acetamide | 1561896: Displacement of Alexa Fluor 647-labeled GSK tracer from FLAG-6His-Tev-fused CECR2 (424 to 543 residue) (unknown origin) measured after 15 mins by TR-FRET assay | ic50 | 0.1000 | uM |
| N-[4-bromo-3-[(3S)-3-methylpyrrolidin-1-yl]sulfonylphenyl]-2-[(4R)-4-cyclopropyl-4-methyl-2,5-dioxoimidazolidin-1-yl]acetamide | 1561896: Displacement of Alexa Fluor 647-labeled GSK tracer from FLAG-6His-Tev-fused CECR2 (424 to 543 residue) (unknown origin) measured after 15 mins by TR-FRET assay | ic50 | 0.1259 | uM |
| N-[4-bromo-3-[(3S,4S)-3,4-dimethylpyrrolidin-1-yl]sulfonylphenyl]-2-(4-cyclopropyl-4-methyl-2,5-dioxoimidazolidin-1-yl)acetamide | 1561896: Displacement of Alexa Fluor 647-labeled GSK tracer from FLAG-6His-Tev-fused CECR2 (424 to 543 residue) (unknown origin) measured after 15 mins by TR-FRET assay | ic50 | 0.1259 | uM |
| N-[4-chloro-3-[(3S)-3-cyclopropylpyrrolidin-1-yl]sulfonylphenyl]-2-(5-methyl-6,7-dihydro-4H-triazolo[4,5-c]pyridin-1-yl)acetamide | 1561896: Displacement of Alexa Fluor 647-labeled GSK tracer from FLAG-6His-Tev-fused CECR2 (424 to 543 residue) (unknown origin) measured after 15 mins by TR-FRET assay | ic50 | 0.1259 | uM |
| N-[1-(6-methoxypyrimidin-4-yl)piperidin-4-yl]-N-methyl-7-oxo-6-prop-2-enyl-1H-pyrrolo[2,3-c]pyridine-4-carboxamide | 1488887: Inhibition of recombinant human N-terminal His6-FLAG-tagged CECR2 expressed in Rosetta2 (DE3) pLysS cells after 60 mins by TR-FRET assay | ic50 | 0.1300 | uM |
| N-[4-bromo-3-[(3S)-3-methylpyrrolidin-1-yl]sulfonylphenyl]-2-[5-(2,2,2-trifluoroethyl)-6,7-dihydro-4H-triazolo[4,5-c]pyridin-1-yl]acetamide | 1561896: Displacement of Alexa Fluor 647-labeled GSK tracer from FLAG-6His-Tev-fused CECR2 (424 to 543 residue) (unknown origin) measured after 15 mins by TR-FRET assay | ic50 | 0.1585 | uM |
| N-[5-(3-methyl-[1,2,4]triazolo[3,4-a]phthalazin-6-yl)-2-morpholin-4-ylphenyl]methanesulfonamide | 1066065: Displacement of H4Ac4 peptide from CECR2 bromodomain (unknown origin) by AlphaScreen assay | ic50 | 0.1585 | uM |
| N,N-dimethyl-3-(7-oxo-6-prop-2-enyl-1H-pyrrolo[2,3-c]pyridin-4-yl)benzamide | 1625911: Inhibition of recombinant His-tagged CECR2 (unknown origin) using biotinylated ligand incubated for 10 mins by TR-FRET assay | ic50 | 0.1700 | uM |
| N,2-dimethyl-7-oxo-N-[1-[(1S)-1-phenylethyl]piperidin-4-yl]-6-prop-2-enyl-1H-pyrrolo[2,3-c]pyridine-4-carboxamide | 1488887: Inhibition of recombinant human N-terminal His6-FLAG-tagged CECR2 expressed in Rosetta2 (DE3) pLysS cells after 60 mins by TR-FRET assay | ic50 | 0.1900 | uM |
| 2-(benzotriazol-1-yl)-N-[4-bromo-3-[(3S)-3-methylpyrrolidin-1-yl]sulfonylphenyl]acetamide | 1561896: Displacement of Alexa Fluor 647-labeled GSK tracer from FLAG-6His-Tev-fused CECR2 (424 to 543 residue) (unknown origin) measured after 15 mins by TR-FRET assay | ic50 | 0.1995 | uM |
| N-methyl-7-oxo-6-prop-2-enyl-N-[1-[6-(trifluoromethyl)pyrimidin-4-yl]piperidin-4-yl]-1H-pyrrolo[2,3-c]pyridine-4-carboxamide | 1488887: Inhibition of recombinant human N-terminal His6-FLAG-tagged CECR2 expressed in Rosetta2 (DE3) pLysS cells after 60 mins by TR-FRET assay | ic50 | 0.2000 | uM |
| N,2-dimethyl-7-oxo-N-[1-[(1R)-1-phenylethyl]piperidin-4-yl]-6-prop-2-enyl-1H-pyrrolo[2,3-c]pyridine-4-carboxamide | 1488887: Inhibition of recombinant human N-terminal His6-FLAG-tagged CECR2 expressed in Rosetta2 (DE3) pLysS cells after 60 mins by TR-FRET assay | ic50 | 0.2000 | uM |
| 6-but-3-enyl-4-[1-methyl-7-(morpholine-4-carbonyl)benzimidazol-5-yl]-1H-pyrrolo[2,3-c]pyridin-7-one | 1513935: Inhibition of recombinant His-tagged CECR2 (unknown origin) after 10 mins by TR-FRET assay | ic50 | 0.2300 | uM |
| N,N-dimethyl-3-(6-methyl-7-oxo-1H-pyrrolo[2,3-c]pyridin-4-yl)benzamide | 1513935: Inhibition of recombinant His-tagged CECR2 (unknown origin) after 10 mins by TR-FRET assay | ic50 | 0.2400 | uM |
| N-methyl-7-oxo-6-prop-2-enyl-N-(1-pyrimidin-4-ylpiperidin-4-yl)-1H-pyrrolo[2,3-c]pyridine-4-carboxamide | 1488887: Inhibition of recombinant human N-terminal His6-FLAG-tagged CECR2 expressed in Rosetta2 (DE3) pLysS cells after 60 mins by TR-FRET assay | ic50 | 0.2400 | uM |
| N,N,2-trimethyl-5-(3-methyl-[1,2,4]triazolo[3,4-a]phthalazin-6-yl)benzenesulfonamide | 1066065: Displacement of H4Ac4 peptide from CECR2 bromodomain (unknown origin) by AlphaScreen assay | ic50 | 0.2512 | uM |
| N-[4-bromo-3-[(3S)-3-methylpyrrolidin-1-yl]sulfonylphenyl]-2-[5-(methoxymethyl)triazol-1-yl]acetamide | 1561896: Displacement of Alexa Fluor 647-labeled GSK tracer from FLAG-6His-Tev-fused CECR2 (424 to 543 residue) (unknown origin) measured after 15 mins by TR-FRET assay | ic50 | 0.2512 | uM |
| N-[4-bromo-3-[(3S)-3-methylpyrrolidin-1-yl]sulfonylphenyl]-2-(5-methyl-6,7-dihydro-4H-triazolo[4,5-c]pyridin-3-yl)acetamide | 1561896: Displacement of Alexa Fluor 647-labeled GSK tracer from FLAG-6His-Tev-fused CECR2 (424 to 543 residue) (unknown origin) measured after 15 mins by TR-FRET assay | ic50 | 0.2512 | uM |
| 2-(1,2-benzoxazol-3-yl)-N-[4-bromo-3-[(3S)-3-methylpyrrolidin-1-yl]sulfonylphenyl]acetamide | 1561896: Displacement of Alexa Fluor 647-labeled GSK tracer from FLAG-6His-Tev-fused CECR2 (424 to 543 residue) (unknown origin) measured after 15 mins by TR-FRET assay | ic50 | 0.2512 | uM |
| N-[4-bromo-3-[(3S)-3-methylpyrrolidin-1-yl]sulfonylphenyl]-2-[4-[(dimethylamino)methyl]triazol-1-yl]acetamide | 1561896: Displacement of Alexa Fluor 647-labeled GSK tracer from FLAG-6His-Tev-fused CECR2 (424 to 543 residue) (unknown origin) measured after 15 mins by TR-FRET assay | ic50 | 0.2512 | uM |
| N-[4-bromo-3-[(3S)-3-methylpyrrolidin-1-yl]sulfonylphenyl]-2-(4,5,6,7-tetrahydrotriazolo[4,5-c]pyridin-1-yl)acetamide | 1561896: Displacement of Alexa Fluor 647-labeled GSK tracer from FLAG-6His-Tev-fused CECR2 (424 to 543 residue) (unknown origin) measured after 15 mins by TR-FRET assay | ic50 | 0.2512 | uM |
| N,6-dimethyl-7-oxo-N-[1-(1-phenylethyl)piperidin-4-yl]-1H-pyrrolo[2,3-c]pyridine-4-carboxamide | 1488887: Inhibition of recombinant human N-terminal His6-FLAG-tagged CECR2 expressed in Rosetta2 (DE3) pLysS cells after 60 mins by TR-FRET assay | ic50 | 0.3300 | uM |
| 3-(6-but-3-enyl-7-oxo-1H-pyrrolo[2,3-c]pyridin-4-yl)-5-(morpholine-4-carbonyl)benzonitrile | 1513935: Inhibition of recombinant His-tagged CECR2 (unknown origin) after 10 mins by TR-FRET assay | ic50 | 0.3500 | uM |
CTD chemical–gene interactions
22 total (human), top 22 by PubMed support.
| Chemical | Actions (top 5) | PubMed papers |
|---|---|---|
| bisphenol A | affects cotreatment, increases methylation, decreases methylation, increases expression | 3 |
| trichostatin A | affects cotreatment, decreases expression | 2 |
| sodium arsenite | decreases expression, increases expression | 2 |
| Benzo(a)pyrene | affects methylation | 2 |
| FR900359 | increases phosphorylation | 1 |
| propionaldehyde | decreases expression | 1 |
| benzo(e)pyrene | increases methylation | 1 |
| potassium chromate(VI) | increases expression | 1 |
| aflatoxin B2 | increases methylation | 1 |
| 4-(5-benzo(1,3)dioxol-5-yl-4-pyridin-2-yl-1H-imidazol-2-yl)benzamide | affects cotreatment, decreases expression | 1 |
| dorsomorphin | affects cotreatment, decreases expression | 1 |
| Fulvestrant | affects cotreatment, increases methylation | 1 |
| Diethylhexyl Phthalate | increases expression | 1 |
| Doxorubicin | decreases expression | 1 |
| Methapyrilene | increases methylation | 1 |
| Phenylmercuric Acetate | affects cotreatment, decreases expression | 1 |
| Silicon Dioxide | decreases expression | 1 |
| Dronabinol | increases expression | 1 |
| Tobacco Smoke Pollution | decreases expression | 1 |
| Tretinoin | decreases expression | 1 |
| Valproic Acid | decreases expression | 1 |
| Aflatoxin B1 | increases methylation | 1 |
ChEMBL screening assays
135 unique, capped per target: 134 binding, 1 functional
Representative assays (with source publication via chembl_document):
| Assay ID | Type | Description | Source paper |
|---|---|---|---|
| CHEMBL3111334 | Binding | Displacement of H4Ac4 peptide from CECR2 bromodomain (unknown origin) by AlphaScreen assay | [1,2,4]triazolo[4,3-a]phthalazines: inhibitors of diverse bromodomains. — J Med Chem |
| CHEMBL5723057 | Functional | Affinity Biochemical interaction: (AlphaScreen) EUB0000233b CECR2 | Affinity Biochemical Literature for EUbOPEN Chemogenomic Library |
Cellosaurus cell lines
2 cell lines: 2 cancer cell line
First 10 cell lines (id-ordered, not curated):
| Cellosaurus | Name | Category | Sex |
|---|---|---|---|
| CVCL_SI67 | HAP1 CECR2 (-) 1 | Cancer cell line | Male |
| CVCL_SI68 | HAP1 CECR2 (-) 2 | Cancer cell line | Male |
Clinical trials (associated diseases)
0 trials via MONDO — disease-level, not drug-specific.
Related Atlas pages
No linked Atlas pages yet — the cross-entity mesh grows as the corpus expands.