IL1B
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Also known as IL1F2IL-1BIL1-BETA
Summary
IL1B (interleukin 1 beta, HGNC:5992) is a protein-coding gene on chromosome 2q14.1, encoding Interleukin-1 beta (P01584). Potent pro-inflammatory cytokine.
The protein encoded by this gene is a member of the interleukin 1 cytokine family. This cytokine is produced by activated macrophages as a proprotein, which is proteolytically processed to its active form by caspase 1 (CASP1/ICE). This cytokine is an important mediator of the inflammatory response, and is involved in a variety of cellular activities, including cell proliferation, differentiation, and apoptosis. The induction of cyclooxygenase-2 (PTGS2/COX2) by this cytokine in the central nervous system (CNS) is found to contribute to inflammatory pain hypersensitivity. Similarly, IL-1B has been implicated in human osteoarthritis pathogenesis. Patients with severe Coronavirus Disease 2019 (COVID-19) present elevated levels of pro-inflammatory cytokines such as IL-1B in bronchial alveolar lavage fluid samples. The lung damage induced by the Severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) is to a large extent, a result of the inflammatory response promoted by cytokines such as IL-1B. This gene and eight other interleukin 1 family genes form a cytokine gene cluster on chromosome 2.
Source: NCBI Gene 3553 — RefSeq curated summary.
At a glance
- Gene–disease (curated): hereditary diffuse gastric adenocarcinoma (No Known Disease Relationship, GenCC)
- GWAS associations: 5
- Clinical variants (ClinVar): 41 total
- Phenotypes (HPO): 3
- Druggable target: yes — 4 molecules with ChEMBL bioactivity
- Transcription factor: yes — 21 downstream targets (CollecTRI)
- MANE Select transcript:
NM_000576
Identifiers
Gene identifiers
| Field | Value |
|---|---|
| HGNC ID | HGNC:5992 |
| Approved symbol | IL1B |
| Name | interleukin 1 beta |
| Location | 2q14.1 |
| Locus type | gene with protein product |
| Status | Approved |
| Aliases | IL1F2, IL-1B, IL1-BETA |
| Ensembl gene | ENSG00000125538 |
| Ensembl biotype | protein_coding |
| OMIM | 147720 |
| Entrez | 3553 |
Gene structure
Transcript identifiers
Ensembl transcripts: 8 — 4 protein_coding, 3 retained_intron, 1 protein_coding_CDS_not_defined
ENST00000263341, ENST00000416750, ENST00000418817, ENST00000432018, ENST00000477398, ENST00000487639, ENST00000491056, ENST00000496280
RefSeq mRNA: 1 — MANE Select: NM_000576
NM_000576
CCDS: CCDS2102
Canonical transcript exons
ENST00000263341 — 7 exons
| Exon | Start | End |
|---|---|---|
| ENSE00000856835 | 112829751 | 112830573 |
| ENSE00001000625 | 112836708 | 112836779 |
| ENSE00003506405 | 112833374 | 112833575 |
| ENSE00003508205 | 112836183 | 112836244 |
| ENSE00003582426 | 112832662 | 112832826 |
| ENSE00003615183 | 112831292 | 112831422 |
| ENSE00003647827 | 112835566 | 112835617 |
Expression profiles
Bgee: expression breadth ubiquitous, 228 present calls, max score 99.48.
FANTOM5 (CAGE): breadth ubiquitous, TPM avg 671.8976 / max 92270.6341, expressed in 932 samples.
FANTOM5 promoters (15 alternative TSS)
| Promoter ID | TPM avg | Samples expressed |
|---|---|---|
| 30247 | 661.2614 | 929 |
| 30227 | 3.2827 | 260 |
| 30235 | 2.4374 | 226 |
| 30226 | 1.6328 | 207 |
| 30232 | 1.3000 | 190 |
| 30234 | 0.9422 | 168 |
| 30230 | 0.4533 | 126 |
| 30236 | 0.1685 | 49 |
| 30233 | 0.1108 | 38 |
| 30229 | 0.1050 | 43 |
Top tissues by expression
282 total, by Bgee expression score (0-100, higher = more expressed):
| Tissue | Anatomy ID | Expression score | Quality |
|---|---|---|---|
| periodontal ligament | UBERON:0008266 | 99.48 | gold quality |
| granulocyte | CL:0000094 | 93.93 | gold quality |
| monocyte | CL:0000576 | 93.30 | gold quality |
| leukocyte | CL:0000738 | 92.97 | gold quality |
| mononuclear cell | CL:0000842 | 92.85 | gold quality |
| blood | UBERON:0000178 | 92.04 | gold quality |
| bone marrow cell | CL:0002092 | 91.60 | gold quality |
| bone marrow | UBERON:0002371 | 89.22 | gold quality |
| cartilage tissue | UBERON:0002418 | 87.85 | gold quality |
| pancreatic ductal cell | CL:0002079 | 86.65 | silver quality |
| gall bladder | UBERON:0002110 | 86.14 | gold quality |
| vermiform appendix | UBERON:0001154 | 86.05 | gold quality |
| decidua | UBERON:0002450 | 85.12 | gold quality |
| spleen | UBERON:0002106 | 83.86 | gold quality |
| primordial germ cell in gonad | CL:0000670 ∩ UBERON:0000991 | 83.69 | gold quality |
| mucosa of urinary bladder | UBERON:0001259 | 82.46 | gold quality |
| stromal cell of endometrium | CL:0002255 | 81.80 | gold quality |
| type B pancreatic cell | CL:0000169 | 81.51 | gold quality |
| olfactory bulb | UBERON:0002264 | 81.50 | gold quality |
| parietal pleura | UBERON:0002400 | 81.02 | gold quality |
| buccal mucosa cell | CL:0002336 | 81.01 | gold quality |
| caecum | UBERON:0001153 | 80.81 | gold quality |
| male germ line stem cell (sensu Vertebrata) in testis | CL:0000089 ∩ UBERON:0000473 | 80.51 | gold quality |
| smooth muscle tissue | UBERON:0001135 | 79.99 | gold quality |
| palpebral conjunctiva | UBERON:0001812 | 79.38 | gold quality |
| body of stomach | UBERON:0001161 | 78.47 | gold quality |
| gingival epithelium | UBERON:0001949 | 78.35 | gold quality |
| epithelial cell of pancreas | CL:0000083 | 78.29 | silver quality |
| rectum | UBERON:0001052 | 77.94 | gold quality |
| superficial temporal artery | UBERON:0001614 | 77.92 | gold quality |
Single-cell (SCXA)
Detected in 24 experiment(s), a significant marker in 24.
| Experiment | Marker? | Max mean expression |
|---|---|---|
| E-HCAD-36 | yes | 23985.52 |
| E-GEOD-135922 | yes | 17552.84 |
| E-MTAB-10855 | yes | 14701.50 |
| E-MTAB-6678 | yes | 12010.48 |
| E-MTAB-6075 | yes | 5036.25 |
| E-GEOD-84465 | yes | 4715.47 |
| E-MTAB-7407 | yes | 3556.63 |
| E-GEOD-149689 | yes | 2589.66 |
| E-CURD-55 | yes | 1113.51 |
| E-MTAB-8559 | yes | 868.80 |
| E-ENAD-21 | yes | 822.52 |
| E-CURD-7 | yes | 700.98 |
| E-CURD-112 | yes | 175.28 |
| E-HCAD-1 | yes | 91.66 |
| E-CURD-122 | yes | 52.56 |
Regulation
Is transcription factor: yes
Downstream targets (CollecTRI)
21 targets.
| Target | Regulation |
|---|---|
| ADAM15 | Activation |
| CLDN1 | Activation |
| CTSK | Activation |
| DEPTOR | Activation |
| DIO1 | Repression |
| ENPP1 | Repression |
| GCH1 | Activation |
| GDF5 | Repression |
| HAS2 | Activation |
| IL6 | Activation |
| ITGA2 | Activation |
| ITGA3 | Repression |
| KRT1 | Repression |
| LGALS9 | Activation |
| MC1R | Activation |
| MMP3 | Activation |
| SCNN1A | Repression |
| SELE | Activation |
| SERPINA3 | Activation |
| VCAM1 | Activation |
| YTHDC2 | Activation |
Upstream regulators (CollecTRI, top): AHR, ANXA1, AP1, APP, ATF3, ATF4, ATF5, BCL6, CEBPB, CEBPD, CEBPG, CREB1, DDIT3, E2F1, EGR1, EHF, ELF3, ESR1, FOS, FOXC1, FOXO1, GLI2, HBP1, HES1, HIF1A, HMGA1, HMGB1, HNF1B, HNF4A, HR, HSF1, HTATIP2, IL6, IRF1, IRF2, IRF4, IRF5, IRF6, IRF8, JUN
miRNA regulators (miRDB)
27 targeting IL1B, 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-5692A | 100.00 | 74.40 | 6850 |
| HSA-MIR-190A-3P | 100.00 | 80.35 | 5520 |
| HSA-MIR-495-3P | 99.96 | 72.81 | 4197 |
| HSA-MIR-5688 | 99.96 | 73.23 | 4504 |
| HSA-MIR-205-3P | 99.92 | 69.92 | 3165 |
| HSA-MIR-7-1-3P | 99.91 | 71.53 | 4384 |
| HSA-MIR-7-2-3P | 99.91 | 71.40 | 4394 |
| HSA-MIR-30A-3P | 99.87 | 69.74 | 2928 |
| HSA-MIR-30D-3P | 99.87 | 69.92 | 2917 |
| HSA-MIR-30E-3P | 99.87 | 69.68 | 2942 |
| HSA-MIR-4729 | 99.69 | 72.18 | 4233 |
| HSA-MIR-4743-3P | 99.62 | 68.12 | 2095 |
| HSA-MIR-4276 | 99.56 | 67.66 | 2514 |
| HSA-MIR-3147 | 99.52 | 66.34 | 388 |
| HSA-MIR-888-5P | 99.30 | 70.15 | 1855 |
| HSA-MIR-330-5P | 98.73 | 67.63 | 1788 |
| HSA-MIR-1178-3P | 98.57 | 67.09 | 890 |
| HSA-MIR-326 | 98.25 | 66.44 | 1565 |
| HSA-MIR-4303 | 98.01 | 68.13 | 2304 |
| HSA-MIR-27B-5P | 97.34 | 66.55 | 549 |
| HSA-MIR-4313 | 97.18 | 63.15 | 420 |
| HSA-MIR-549A-5P | 96.35 | 68.08 | 587 |
| HSA-MIR-1291 | 96.28 | 65.89 | 1224 |
| HSA-MIR-6775-3P | 95.76 | 65.91 | 982 |
| HSA-MIR-7976 | 95.75 | 65.67 | 1186 |
| HSA-MIR-328-3P | 92.82 | 64.37 | 521 |
| HSA-MIR-6090 | 91.01 | 62.65 | 222 |
Literature-anchored findings (GeneRIF, showing 40)
- The level of IL-1 beta is significantly higher in sera of cicatricial pemphigoid patients with active disease before intravenous immunoglobulin therapy compared to the post-treatment level. (PMID:11448121)
- There were no significant differences in the distributions of the IL-1RN and IL-1B genotypes, allel frequencies or halotypes. (PMID:11686217)
- These studies demonstrate that PEIPC and PECPC isomers are potent activators of endothelial cells increasing synthesis of IL-8 and MCP-1. (PMID:11751881)
- data fall short of showing significant association between a variant of the promoter of interleukin-1beta, polymorphism of angiotensinogen, and the missense variant of endothelial nitric oxide synthase and occurrence of idiopathic recurrent miscarriage (PMID:11756575)
- Repressed transcription of IL-1beta and rapid decay of IL-1beta mRNA in septic shock neutrophils correlated with reductions in levels of IL-1beta after stimulation with LPS (PMID:11770040)
- Interleukin-1 alpha and beta system in testis–quantitative analysis. Expression of immunomodulatory genes in male gonad. (PMID:11774564)
- IL-1 beta increases CD40 ligand-induced cytokine secretion by monocyte-derived dendritic cells (DC), CD34+-derived DC, and peripheral blood DC independently of T cell-derived cytokines. (PMID:11777965)
- Heat shock factor 1 represses transcription of the IL-1beta gene through physical interaction with the nuclear factor of interleukin 6 (PMID:11801594)
- role in upregulating VEGF in vascular smooth muscle cells via the P38 mitogen-activated protein kinase pathway (PMID:11806247)
- Genotype A2A2 of IL-1beta is associated with severe forms of rheumatoid arthritis. The allelic combination A1 IL-1beta/A2 IL-1Ra is less often present in rheumatoid arthritis patients with severe disease. (PMID:11838837)
- Test found no evidence of an association of mutations with hypertension. (PMID:11840488)
- Up-regulation of prostaglandin E2 synthesis by interleukin-1beta in human orbital fibroblasts (PMID:11847219)
- Carriage of IL1beta2 and IL1RN*2 together with non-carriage of TNF2 is associated with increased susceptibility, but not with a prognosis of IgAN. (PMID:11849463)
- differentiated articular chondrocytes are highly responsive to IL-1beta and that p38 MAPK mediates this response by inducing COX-2 gene expression. (PMID:11853544)
- T helper 1-type immunity to trophoblast antigens in women with a history of recurrent pregnancy loss is associated with polymorphism of the IL1B promoter region (PMID:11857060)
- In dengue shock syndrome pts, IL-1beta was significantly associated with t-PA (p < 0.03). IL1B is involved in the onset and regulation of hemostasis. (PMID:11858187)
- in semsen of normal/infertile men (PMID:11868623)
- Lidocaine inhibits secretion of IL-8 and IL-1beta and stimulates secretion of IL-1 receptor antagonist by epithelial cells. (PMID:11876744)
- Up-regulation of IL1-beta is crucial for the pathogenesis of myeloma (PMID:11896542)
- Il-1beta genotype carries asthma susceptibility only in men (PMID:11898000)
- role in Candida albicans-induced interferon-gamma production in human whole blood cultures (PMID:11920321)
- process of cervical dilatation during parturition at term is associated with an increased expression of interleukin-1 beta, interleukin-6 and interleukin-8 mRNA in the lower uterine segment (PMID:11950481)
- Increased frequency of interleukin-1beta (-511) allele 2 in febrile seizures. polymorphism of interleukin-1beta at position -511 (PMID:11955925)
- Interleukin-1beta processing following Shigella flexneri infection of human monocyte-derived dendritic cells. (PMID:11981835)
- results suggest that NFkappaB is involved in the IL-1beta-induced COX-2 expression in the mesenchymal cells of human amnion (PMID:12021045)
- secretion from acute myelogenous leukemia blasts was up-regulated by leptin (PMID:12031914)
- TNF-alpha, IL1-beta, and immunoglobulin (GM and KM) gene polymorphisms in sarcoidosis. (PMID:12039524)
- Interleukin 1 beta induces overexpression of mucin genes in cultured tumor cells which is inhibitable by a retinoic acid receptor alpha antagonist. (PMID:12042033)
- role in inducing cyclooxygenase-2 and presenilin-1 gene expression potentiated by hypoxia in primary human neural cells (PMID:12050157)
- expressed in human gastric carcinoma with Epstein-Barr virus infection (PMID:12050395)
- Association of an interleukin 1B gene polymorphism with Parkinson’s disease (PMID:12070246)
- Tumors derived from a retroviral vector coding human IL-1BETA gene transduced into Lewis lung carcinoma cells secrete IL-1 beta into the tumor milieu, which promotes tumor growth through hyperneovascularization. (PMID:12077278)
- role in NF-kappa B induction modulated by a novel PAAD-containing protein (PMID:12093792)
- plays a role the pathogenesis of the otitis media with effusion (REVIEW) (PMID:12101072)
- Interleukin 1beta polymorphisms increase risk of hypochlorhydria and atrophic gastritis and reduce risk of duodenal ulcer recurrence in Japan. (PMID:12105837)
- There are associations of spontaneous preterm delivery with the fetal carriage of IL1B+3953*1 and IL1RN*2 alleles in African and Hispanic populations, respectively. (PMID:12114904)
- Association of interleukin-4 and interleukin-1B gene variants with Larsen score progression in rheumatoid arthritis. (PMID:12115161)
- Association of the interleukin-1 gene cluster on chromosome 2q13 with knee osteoarthritis. (PMID:12115182)
- role of p38 map kinase, NF-kappaB, and protein kinase c in IL-1beta mRNA expression by human peripheral blood leukocytes, monocytes, and neutrophils in response to Anaplasma phagocytophila (PMID:12117921)
- Acanthamoeba castellanii by release of ADP and other metabolites lead to human monocytic cell death through apoptosis and stimulate the secretion of IL-1beta (PMID:12117953)
Cross-species orthologs
4 orthologs
| Organism | Symbol | Gene ID |
|---|---|---|
| danio_rerio | il1fma | ENSDARG00000089383 |
| danio_rerio | il1b | ENSDARG00000098700 |
| mus_musculus | Il1b | ENSMUSG00000027398 |
| rattus_norvegicus | Il1b | ENSRNOG00000004649 |
Paralogs (7): IL37 (ENSG00000125571), IL36G (ENSG00000136688), IL1RN (ENSG00000136689), IL36A (ENSG00000136694), IL36RN (ENSG00000136695), IL36B (ENSG00000136696), IL1F10 (ENSG00000136697)
Protein
Protein identifiers
Interleukin-1 beta — P01584 (reviewed: P01584)
Alternative names: Catabolin
All UniProt accessions (4): C9JSC2, C9JVK0, P01584, C9JWV2
UniProt curated annotations — full annotation on UniProt →
Function. Potent pro-inflammatory cytokine. Initially discovered as the major endogenous pyrogen, induces prostaglandin synthesis, neutrophil influx and activation, T-cell activation and cytokine production, B-cell activation and antibody production, and fibroblast proliferation and collagen production. Promotes Th17 differentiation of T-cells. Synergizes with IL12/interleukin-12 to induce IFNG synthesis from T-helper 1 (Th1) cells. Plays a role in angiogenesis by inducing VEGF production synergistically with TNF and IL6. Involved in transduction of inflammation downstream of pyroptosis: its mature form is specifically released in the extracellular milieu by passing through the gasdermin-D (GSDMD) pore. Acts as a sensor of S.pyogenes infection in skin: cleaved and activated by pyogenes SpeB protease, leading to an inflammatory response that prevents bacterial growth during invasive skin infection.
Subunit / interactions. Monomer. In its precursor form, weakly interacts with full-length MEFV; the mature cytokine does not interact at all. Interacts with integrins ITGAV:ITGBV and ITGA5:ITGB1; integrin-binding is required for IL1B signaling. Interacts with cargo receptor TMED10; the interaction is direct and is required for the secretion of IL1B mature form. Interacts with HSP90AB1; the interaction facilitates cargo translocation into the ERGIC. Interacts with HSP90B1; the interaction facilitates cargo translocation into the ERGIC.
Subcellular location. Cytoplasm. Cytosol. Secreted. Lysosome. Extracellular exosome.
Tissue specificity. Expressed in activated monocytes/macrophages (at protein level).
Post-translational modifications. Activation of the IL1B precursor involves a CASP1-catalyzed proteolytic cleavage. Processing and secretion are temporarily associated. (Microbial infection) Cleavage by S.pyogenes cysteine protease SpeB promotes its activation independently of CASP1.
Activity regulation. (Microbial infection) Cleavage by S.pyogenes cysteine protease SpeB promotes its activation independently of CASP1. SpeB-mediated maturation of IL1B plays a dual role depending on infection site: while IL1B inflammatory response prevents bacterial growth during invasive skin infections, it promotes streptococcal infection of the nasopharynx by disrupting colonization resistance mediated by the microbiota.
Induction. By LPS. Transcription and translation induced by M.tuberculosis and a number of different M.tuberculosis components in macrophages; EsxA is the most potent activator tested (at protein level). In pancreatic islets, release is increased by high glucose treatment. In pancreatic islets and macrophages, release is also increased by endocannabinoid anandamide/AEA.
Miscellaneous. The IL1B production occurs in 2 steps, each being controlled by different stimuli. First, inflammatory signals, such as LPS, stimulate the synthesis and promote the accumulation of cytosolic stores of pro-IL1B (priming). Then additional signals are required for inflammasome assembly, leading to CASP1 activation, pro-IL1B processing and eventually secretion of the active cytokine. IL1B processing and secretion are temporarily associated.
Similarity. Belongs to the IL-1 family.
RefSeq proteins (1): NP_000567* (*=MANE)
Domains & families (InterPro)
| ID | Name | Type |
|---|---|---|
| IPR000975 | IL-1_fam | Family |
| IPR003502 | IL-1_propep | Domain |
| IPR008996 | IL1/FGF | Homologous_superfamily |
| IPR020877 | IL-1_CS | Conserved_site |
Pfam: PF00340, PF02394
UniProt features (44 total): strand 14, mutagenesis site 12, site 8, sequence conflict 3, helix 2, propeptide 1, chain 1, sequence variant 1, short sequence motif 1, turn 1
Structure
Experimental structures (PDB)
64 structures, top 30 by resolution.
| PDB | Method | Resolution (Å) |
|---|---|---|
| 8RYS | X-RAY DIFFRACTION | 1.16 |
| 5R8Q | X-RAY DIFFRACTION | 1.23 |
| 5R7W | X-RAY DIFFRACTION | 1.27 |
| 5R8E | X-RAY DIFFRACTION | 1.35 |
| 5R8M | X-RAY DIFFRACTION | 1.39 |
| 5R8F | X-RAY DIFFRACTION | 1.41 |
| 5R8O | X-RAY DIFFRACTION | 1.42 |
| 5R8G | X-RAY DIFFRACTION | 1.43 |
| 5R85 | X-RAY DIFFRACTION | 1.44 |
| 6Y8I | X-RAY DIFFRACTION | 1.46 |
| 5R87 | X-RAY DIFFRACTION | 1.47 |
| 5R8A | X-RAY DIFFRACTION | 1.47 |
| 5R8D | X-RAY DIFFRACTION | 1.47 |
| 5R8I | X-RAY DIFFRACTION | 1.47 |
| 5R8K | X-RAY DIFFRACTION | 1.47 |
| 5R88 | X-RAY DIFFRACTION | 1.48 |
| 5R8N | X-RAY DIFFRACTION | 1.48 |
| 4GAI | X-RAY DIFFRACTION | 1.49 |
| 5R8B | X-RAY DIFFRACTION | 1.49 |
| 5R86 | X-RAY DIFFRACTION | 1.5 |
| 5R8H | X-RAY DIFFRACTION | 1.5 |
| 2NVH | X-RAY DIFFRACTION | 1.53 |
| 5R8P | X-RAY DIFFRACTION | 1.53 |
| 1L2H | X-RAY DIFFRACTION | 1.54 |
| 5R8C | X-RAY DIFFRACTION | 1.54 |
| 5R8L | X-RAY DIFFRACTION | 1.56 |
| 5R8J | X-RAY DIFFRACTION | 1.62 |
| 5R89 | X-RAY DIFFRACTION | 1.65 |
| 3POK | X-RAY DIFFRACTION | 1.7 |
| 8RYK | X-RAY DIFFRACTION | 1.8 |
Predicted structure (AlphaFold)
| Model | pLDDT | Fraction very-high |
|---|---|---|
| AF-P01584-F1 | 76.24 | 0.49 |
Antibody-complex structures (SAbDab): 8 — 2KH2, 4G6J, 4G6M, 5BVP, 5MVZ, 7CHY, 7CHZ, 7Z4T
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 (8): 204 (important for interaction with integrin); 105–106 ((microbial infection) cleavage; s.pyogenes speb); 115–116 ((microbial infection) cleavage; s.pyogenes speb); 120 (involved in receptor binding); 171 (important for interaction with integrin); 179 (important for interaction with integrin); 181 (important for interaction with integrin); 190 (important for interaction with integrin)
Mutagenesis-validated functional residues (12):
| Position | Phenotype |
|---|---|
| 6–27 | promotes release of il1b precursors through the gasdermin-d (gsdmd) ring-shaped pore complex. |
| 27 | loss of activation by casp1; when associated with a-116. |
| 87–111 | promotes release of il1b precursors through the gasdermin-d (gsdmd) ring-shaped pore complex. |
| 116 | loss of activation by casp1; when associated with a-27. |
| 171 | suppression of integrin binding; when associated with k-244. markedly reduced activity; when associated with e-190; e-20 |
| 179 | suppression of integrin binding; when associated with e-181 and k-244. markedly reduced activity; when associated with e |
| 181 | suppression of integrin binding; when associated with e-179 and k-244. markedly reduced activity; when associated with e |
| 190 | suppression of integrin binding; when associated with k-244. markedly reduced activity; when associated with e-171; e-20 |
| 204 | suppression of integrin binding; when associated with k-244. markedly reduced activity; when associated with e-171; e-19 |
| 221 | enhanced integrin binding. |
| 233 | no effect on binding to il1r or on il1b activity. markedly reduced activity; when associated with e-171; e-190 and e-204 |
| 244 | increased affinity for integrin itgav:itgb3. suppression of integrin binding; when associated with e-171; e-190 or e-204 |
Function
Pathways and Gene Ontology
Reactome pathways
9 pathways
| ID | Pathway |
|---|---|
| R-HSA-448706 | Interleukin-1 processing |
| R-HSA-5620971 | Pyroptosis |
| R-HSA-5660668 | CLEC7A/inflammasome pathway |
| R-HSA-6783783 | Interleukin-10 signaling |
| R-HSA-6785807 | Interleukin-4 and Interleukin-13 signaling |
| R-HSA-9020702 | Interleukin-1 signaling |
| R-HSA-9660826 | Purinergic signaling in leishmaniasis infection |
| R-HSA-9960519 | CASP4-mediated substrate cleavage |
| R-HSA-9960525 | CASP5-mediated substrate cleavage |
MSigDB gene sets: 996 (showing top):
GOBP_MYELOID_CELL_DIFFERENTIATION, GSE45365_NK_CELL_VS_CD11B_DC_DN, GOBP_PLATELET_DERIVED_GROWTH_FACTOR_RECEPTOR_SIGNALING_PATHWAY, GOBP_ENDOTHELIAL_CELL_DEVELOPMENT, GOBP_REGULATION_OF_CELL_ACTIVATION, GOBP_POSITIVE_REGULATION_OF_MITOTIC_NUCLEAR_DIVISION, MODULE_92, GOBP_RESPONSE_TO_NITROGEN_COMPOUND, GOBP_NEGATIVE_REGULATION_OF_TRANSMEMBRANE_TRANSPORT, GOBP_REGULATION_OF_LEUKOCYTE_PROLIFERATION, GOBP_CARBOHYDRATE_TRANSPORT, GOBP_REGULATION_OF_CELLULAR_RESPONSE_TO_GROWTH_FACTOR_STIMULUS, GOBP_EPITHELIUM_DEVELOPMENT, GOBP_NEGATIVE_REGULATION_OF_CELL_DEVELOPMENT, REACTOME_INNATE_IMMUNE_SYSTEM
GO Biological Process (94): fever generation (GO:0001660), positive regulation of T cell mediated immunity (GO:0002711), apoptotic process (GO:0006915), inflammatory response (GO:0006954), immune response (GO:0006955), signal transduction (GO:0007165), JNK cascade (GO:0007254), cell-cell signaling (GO:0007267), embryo implantation (GO:0007566), positive regulation of cell population proliferation (GO:0008284), negative regulation of cell population proliferation (GO:0008285), response to carbohydrate (GO:0009743), vascular endothelial growth factor production (GO:0010573), positive regulation of vascular endothelial growth factor production (GO:0010575), positive regulation of gene expression (GO:0010628), positive regulation of platelet-derived growth factor receptor signaling pathway (GO:0010641), positive regulation of epithelial to mesenchymal transition (GO:0010718), positive regulation of macrophage derived foam cell differentiation (GO:0010744), negative regulation of D-glucose transmembrane transport (GO:0010829), smooth muscle adaptation (GO:0014805), cytokine-mediated signaling pathway (GO:0019221), hyaluronan biosynthetic process (GO:0030213), positive regulation of cell migration (GO:0030335), neutrophil chemotaxis (GO:0030593), positive regulation of vascular endothelial growth factor receptor signaling pathway (GO:0030949), positive regulation of prostaglandin biosynthetic process (GO:0031394), positive regulation of fever generation (GO:0031622), positive regulation of prostaglandin secretion (GO:0032308), response to lipopolysaccharide (GO:0032496), positive regulation of granulocyte macrophage colony-stimulating factor production (GO:0032725), positive regulation of type II interferon production (GO:0032729), positive regulation of interleukin-2 production (GO:0032743), positive regulation of interleukin-6 production (GO:0032755), positive regulation of interleukin-8 production (GO:0032757), positive regulation of immature T cell proliferation in thymus (GO:0033092), response to ATP (GO:0033198), positive regulation of heterotypic cell-cell adhesion (GO:0034116), ectopic germ cell programmed cell death (GO:0035234), positive regulation of T cell proliferation (GO:0042102), regulation of canonical NF-kappaB signal transduction (GO:0043122)
GO Molecular Function (6): cytokine activity (GO:0005125), interleukin-1 receptor binding (GO:0005149), integrin binding (GO:0005178), protein domain specific binding (GO:0019904), protein binding (GO:0005515), receptor ligand activity (GO:0048018)
GO Cellular Component (7): extracellular region (GO:0005576), obsolete extracellular space (GO:0005615), lysosome (GO:0005764), cytosol (GO:0005829), secretory granule (GO:0030141), cytoplasm (GO:0005737), vesicle (GO:0031982)
Reactome top-level categories
Rollup of top-6 pathways:
| Category | Pathways |
|---|---|
| Interleukin-1 family signaling | 2 |
| Signaling by Interleukins | 2 |
| Non-canonical inflammasome activation | 2 |
| Regulated Necrosis | 1 |
| CLEC7A (Dectin-1) signaling | 1 |
| Cell recruitment (pro-inflammatory response) | 1 |
GO top-level categories
Rollup of top GO terms by namespace:
| Category | Terms |
|---|---|
| cellular anatomical structure | 3 |
| cell communication | 2 |
| signaling | 2 |
| cell population proliferation | 2 |
| regulation of cell population proliferation | 2 |
| positive regulation of cell differentiation | 2 |
| signaling receptor binding | 2 |
| acute-phase response | 1 |
| heat generation | 1 |
| T cell mediated immunity | 1 |
| positive regulation of lymphocyte mediated immunity | 1 |
| regulation of T cell mediated immunity | 1 |
| positive regulation of adaptive immune response based on somatic recombination of immune receptors built from immunoglobulin superfamily domains | 1 |
| programmed cell death | 1 |
| apoptotic signaling pathway | 1 |
| execution phase of apoptosis | 1 |
| defense response | 1 |
| immune system process | 1 |
| response to stimulus | 1 |
| cellular process | 1 |
| regulation of cellular process | 1 |
| cellular response to stimulus | 1 |
| MAPK cascade | 1 |
| multicellular organism development | 1 |
| female pregnancy | 1 |
| reproductive process | 1 |
| positive regulation of cellular process | 1 |
| negative regulation of cellular process | 1 |
| response to oxygen-containing compound | 1 |
| cytokine production | 1 |
| positive regulation of cytokine production | 1 |
| vascular endothelial growth factor production | 1 |
| regulation of vascular endothelial growth factor production | 1 |
| gene expression | 1 |
| regulation of gene expression | 1 |
| positive regulation of macromolecule biosynthetic process | 1 |
| positive regulation of signal transduction | 1 |
| regulation of platelet-derived growth factor receptor signaling pathway | 1 |
| platelet-derived growth factor receptor signaling pathway | 1 |
| epithelial to mesenchymal transition | 1 |
Protein interactions and networks
STRING
8488 interactions, top by confidence (×1000):
| Protein A | Protein B | Partner UniProt | Score |
|---|---|---|---|
| IL1B | IL2 | P01585 | 999 |
| IL1B | IL1R1 | P14778 | 999 |
| IL1B | IFNG | P01579 | 998 |
| IL1B | IL4 | P05112 | 998 |
| IL1B | IL5 | P05113 | 998 |
| IL1B | MYD88 | P78397 | 998 |
| IL1B | TNFRSF1A | P19438 | 997 |
| IL1B | IL1RAP | Q9NPH3 | 997 |
| IL1B | CSF2 | P04141 | 996 |
| IL1B | IL1R2 | P27930 | 996 |
| IL1B | CSF3 | P09919 | 993 |
| IL1B | TNF | P01375 | 993 |
| IL1B | IL6 | P05231 | 990 |
| IL1B | CASP1 | P29466 | 988 |
| IL1B | TLR4 | O00206 | 984 |
IntAct
16 interactions, top by confidence:
| A | B | Type | Score |
|---|---|---|---|
| IL1RAP | IL1B | psi-mi:“MI:0914”(association) | 0.760 |
| IL1RAP | IL1B | psi-mi:“MI:0915”(physical association) | 0.760 |
| IL1B | IL1R1 | psi-mi:“MI:0407”(direct interaction) | 0.440 |
| CASP1 | IL1B | psi-mi:“MI:0570”(protein cleavage) | 0.440 |
| IL1B | PKM | psi-mi:“MI:0217”(phosphorylation reaction) | 0.440 |
| IKBKG | IL1B | psi-mi:“MI:0915”(physical association) | 0.400 |
| STING1 | ZSWIM8 | psi-mi:“MI:0914”(association) | 0.350 |
| MYC | psi-mi:“MI:0914”(association) | 0.350 | |
| ATG16L1 | psi-mi:“MI:0914”(association) | 0.350 | |
| A2M | IL1B | psi-mi:“MI:2364”(proximity) | 0.270 |
BioGRID (60): A2M (Co-localization), IL1B (Affinity Capture-RNA), IL1B (Biochemical Activity), IL1B (Co-localization), IL1B (Biochemical Activity), IL1B (Affinity Capture-RNA), IL1B (Affinity Capture-RNA), IL1B (Affinity Capture-RNA), IL1B (Affinity Capture-RNA), IL1B (Affinity Capture-RNA), IL1B (Affinity Capture-RNA), IL1B (Affinity Capture-RNA), GSDMD (Affinity Capture-Western), CASP8 (Affinity Capture-Western), NEDD4 (Affinity Capture-Western)
ESM2 similar proteins: A4UYK8, O46612, O46613, P01582, P01583, P01584, P04822, P08831, P09428, P10749, P14628, P16598, P18430, P21621, P26889, P41687, P46648, P48089, P48090, P51493, P51745, P79161, P79162, P79182, P79340, Q14D04, Q28292, Q28385, Q28386, Q28579, Q2HZH0, Q2MH07, Q32NG6, Q3HWU1, Q3UIR3, Q63264, Q6PUD2, Q6R2X3, Q6ZUJ8, Q865X7
Diamond homologs: A4UYK8, P01584, P09428, P10749, P14628, P21621, P26889, P41687, P46648, P48090, P51493, P51745, P79162, P79182, Q28292, Q28386, Q2HZH0, Q2MH07, Q63264, Q6PUD2, Q6R2X3, Q865X8, Q8WNR2, Q9D6Z6, Q9WVG1, Q9XS77, Q9YGD3, Q9QYY1, Q9UBH0, O18999, P18510, P25085, P25086, P26890, Q29056, Q866R8, Q9BEH0, Q9NZH8, Q8WWZ1, Q9GMZ4
SIGNOR signaling
39 interactions.
| A | Effect | B | Mechanism |
|---|---|---|---|
| IL1B | “up-regulates activity” | IL1R1 | binding |
| IL1B | “down-regulates activity” | LPL | |
| IL1B | “down-regulates quantity by repression” | GDF5 | “transcriptional regulation” |
| IL1B | “down-regulates quantity by repression” | KRT1 | “transcriptional regulation” |
| IL1B | “down-regulates quantity by repression” | SCNN1A | “transcriptional regulation” |
| IL1B | “down-regulates quantity by repression” | ENPP1 | “transcriptional regulation” |
| IL1B | “up-regulates quantity by expression” | GCH1 | “transcriptional regulation” |
| “UVB radiation” | up-regulates | IL1B | |
| IL1B | “up-regulates quantity by expression” | MC1R | “transcriptional regulation” |
| “A9/b1 integrin” | “up-regulates quantity by expression” | IL1B | |
| IL1B | “down-regulates quantity by repression” | ITGA3 | “transcriptional regulation” |
| IL1B | “up-regulates quantity by expression” | ITGA2 | “transcriptional regulation” |
| IRF5 | up-regulates | IL1B | “transcriptional regulation” |
| IL1B | “up-regulates quantity by expression” | SERPINA3 | “transcriptional regulation” |
| NfKb-p65/p50 | “up-regulates quantity by expression” | IL1B | “transcriptional regulation” |
| NfKb-p65/p50 | “up-regulates quantity” | IL1B | “transcriptional regulation” |
| RELA | “up-regulates quantity by expression” | IL1B | “transcriptional regulation” |
| IL1B | “up-regulates quantity by expression” | IL6 | “transcriptional regulation” |
| IL1B | up-regulates | Immune_response | |
| IL1B | “up-regulates activity” | STAT3 | |
| M1_polarization | up-regulates | IL1B | |
| IL1B | down-regulates | IL1R2 | binding |
| IL1B | up-regulates | IL1R1 | binding |
| IL1B | up-regulates | IL1RAP | binding |
| HIF1A | “up-regulates quantity by expression” | IL1B | “transcriptional regulation” |
| RELA | “down-regulates activity” | IL1B | “transcriptional regulation” |
| MFGE8 | “down-regulates quantity by repression” | IL1B | “transcriptional regulation” |
Disease & clinical
Clinical variants and AI predictions
ClinVar
41 variants total. Per-class counts are floors (≥ shown; pagination cap):
| Classification | Count (floor) |
|---|---|
| Pathogenic | 0 |
| Likely pathogenic | 0 |
| Uncertain significance | 14 |
| Likely benign | 4 |
| Benign | 2 |
Top pathogenic / likely-pathogenic (0)
SpliceAI
573 predictions. Top by Δscore:
| Variant | Effect | Δscore |
|---|---|---|
| 2:112830570:CACT:C | acceptor_gain | 1.0000 |
| 2:112830572:CT:C | acceptor_gain | 1.0000 |
| 2:112830580:C:CT | acceptor_gain | 1.0000 |
| 2:112831288:TTAC:T | donor_loss | 1.0000 |
| 2:112831289:TACCT:T | donor_loss | 1.0000 |
| 2:112831290:A:AC | donor_gain | 1.0000 |
| 2:112831290:AC:A | donor_gain | 1.0000 |
| 2:112831290:ACCT:A | donor_gain | 1.0000 |
| 2:112831290:ACCTC:A | donor_gain | 1.0000 |
| 2:112831291:C:CA | donor_gain | 1.0000 |
| 2:112831291:CC:C | donor_gain | 1.0000 |
| 2:112831291:CCT:C | donor_gain | 1.0000 |
| 2:112831291:CCTC:C | donor_gain | 1.0000 |
| 2:112831291:CCTCC:C | donor_gain | 1.0000 |
| 2:112831397:T:C | acceptor_gain | 1.0000 |
| 2:112831418:CACCA:C | acceptor_gain | 1.0000 |
| 2:112831419:ACCA:A | acceptor_gain | 1.0000 |
| 2:112831420:CCA:C | acceptor_gain | 1.0000 |
| 2:112831420:CCAC:C | acceptor_gain | 1.0000 |
| 2:112831421:CA:C | acceptor_gain | 1.0000 |
| 2:112831421:CAC:C | acceptor_gain | 1.0000 |
| 2:112831422:AC:A | acceptor_loss | 1.0000 |
| 2:112831423:C:CC | acceptor_gain | 1.0000 |
| 2:112831423:CTGAA:C | acceptor_loss | 1.0000 |
| 2:112832657:TTTAC:T | donor_loss | 1.0000 |
| 2:112832658:TTA:T | donor_loss | 1.0000 |
| 2:112832659:TA:T | donor_loss | 1.0000 |
| 2:112832660:A:C | donor_loss | 1.0000 |
| 2:112833415:T:A | donor_gain | 1.0000 |
| 2:112833449:T:TA | donor_gain | 1.0000 |
AlphaMissense
1816 scored. Top likely-pathogenic:
| Variant | Protein change | am_pathogenicity |
|---|---|---|
| 2:112830488:A:G | F228S | 0.999 |
| 2:112830520:G:C | F217L | 0.999 |
| 2:112830520:G:T | F217L | 0.999 |
| 2:112830521:A:G | F217S | 0.999 |
| 2:112830522:A:G | F217L | 0.999 |
| 2:112830526:A:C | F215L | 0.999 |
| 2:112830526:A:T | F215L | 0.999 |
| 2:112830528:A:G | F215L | 0.999 |
| 2:112830386:A:G | F262S | 0.998 |
| 2:112830527:A:G | F215S | 0.998 |
| 2:112831362:A:G | L176S | 0.998 |
| 2:112830428:A:T | V248D | 0.997 |
| 2:112830458:A:T | I238N | 0.997 |
| 2:112830521:A:C | F217C | 0.997 |
| 2:112831416:A:G | F158S | 0.997 |
| 2:112830385:G:C | F262L | 0.996 |
| 2:112830385:G:T | F262L | 0.996 |
| 2:112830386:A:C | F262C | 0.996 |
| 2:112830387:A:G | F262L | 0.996 |
| 2:112830454:G:C | S239R | 0.996 |
| 2:112830454:G:T | S239R | 0.996 |
| 2:112830456:T:G | S239R | 0.996 |
| 2:112830458:A:C | I238S | 0.996 |
| 2:112830458:A:G | I238T | 0.996 |
| 2:112830484:C:A | E229D | 0.996 |
| 2:112830484:C:G | E229D | 0.996 |
| 2:112830488:A:C | F228C | 0.996 |
| 2:112831339:A:C | Y184D | 0.996 |
| 2:112832703:A:G | L142P | 0.996 |
| 2:112832745:T:G | D128A | 0.996 |
dbSNP variants (sampled 300 via entrez): RS1000050546 (2:112830098 C>A,T), RS1000769125 (2:112831737 A>G), RS1000920623 (2:112838616 AC>A), RS1001096830 (2:112838305 A>C,G), RS1001547340 (2:112833094 T>A), RS1001657797 (2:112837058 A>T), RS1001997232 (2:112834776 G>T), RS1002063576 (2:112833326 T>C), RS1002282836 (2:112834355 T>C), RS1002440259 (2:112829987 AAAAC>A,AAAACAAAC), RS1002926902 (2:112835382 A>C), RS1003267588 (2:112833836 T>C), RS1003764587 (2:112829531 T>C), RS1004229091 (2:112837713 A>C,G), RS1004295535 (2:112837790 C>T)
Disease associations
OMIM: gene MIM:147720 | disease phenotypes: MIM:608316
GenCC curated gene-disease
| Disease | Classification | Inheritance |
|---|---|---|
| hereditary diffuse gastric adenocarcinoma | No Known Disease Relationship | Unknown |
Mondo (5): coronary heart disease, susceptibility to, 2 (MONDO:0012009), endometriosis (MONDO:0005133), cholangiocarcinoma (MONDO:0019087), antisynthetase syndrome (MONDO:0019344), hereditary diffuse gastric adenocarcinoma (MONDO:0007648)
Orphanet (2): Cholangiocarcinoma (Orphanet:70567), Antisynthetase syndrome (Orphanet:81)
HPO phenotypes
3 total (4 of 3 shown, HPO-id order):
| HPO | Term |
|---|---|
| HP:0001442 | Typified by somatic mosaicism |
| HP:0012126 | Stomach cancer |
| HP:0410067 | Increased level of L-fucose in urine |
| HP:0030127 | Endometriosis |
GWAS associations
5 associations (top):
| Study | Trait | p-value |
|---|---|---|
| GCST005038_21 | Allergic disease (asthma, hay fever or eczema) | 2.000000e-10 |
| GCST006656_2 | Dysmenorrheic pain severity | 2.000000e-16 |
| GCST008362_147 | Birth weight | 3.000000e-08 |
| GCST008751_1 | Gestational age at birth (child effect) | 4.000000e-14 |
| GCST008752_1 | Post-term birth | 4.000000e-08 |
EFO canonical traits (4, from GWAS)
| EFO ID | Trait name |
|---|---|
| EFO:0007889 | dysmenorrheic pain measurement |
| EFO:0004344 | birth weight |
| EFO:0005112 | gestational age |
| EFO:0006921 | birth measurement |
MeSH disease descriptors (3)
| Descriptor | Name | Tree numbers |
|---|---|---|
| D018281 | Cholangiocarcinoma | C04.557.470.200.025.450 |
| D004715 | Endometriosis | C12.050.351.500.163; C12.100.250.163 |
| C537778 | Antisynthetase syndrome (supp.) |
Drugs & pharmacology
Drug and pharmacology data
Is drug target: yes
ChEMBL targets (1): CHEMBL1909490 (SINGLE PROTEIN)
Molecules with ChEMBL bioactivity
4 molecules (phase ≥1), by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 21,416 (via chembl_molecule»patent_compound — counts attach to the compound, not the gene–compound relationship, so off-target/promiscuous molecules can dominate).
| Molecule | Name | Phase | Patents |
|---|---|---|---|
| CHEMBL43452 | POMALIDOMIDE | 4 | 13,354 |
| CHEMBL848 | LENALIDOMIDE | 4 | 5,256 |
| CHEMBL3989927 | IBERDOMIDE | 3 | 1,300 |
| CHEMBL3989934 | AVADOMIDE | 2 | 1,506 |
PharmGKB: 1 entry (VIP=true, CPIC=false)
PharmGKB clinical annotations
15 annotations.
| Variant | Type | Level | Drugs | Phenotypes |
|---|---|---|---|---|
| rs1143623 | Toxicity | 3 | Platinum compounds | Non-Small Cell Lung Carcinoma |
| rs1143623 | Efficacy | 3 | Tumor necrosis factor alpha (TNF-alpha) inhibitors;ustekinumab | Psoriasis |
| rs1143627 | Toxicity | 3 | aspirin | |
| rs1143627 | Efficacy | 3 | Tumor necrosis factor alpha (TNF-alpha) inhibitors;ustekinumab | Psoriasis |
| rs1143634 | Toxicity | 3 | antipsychotics | Schizophrenia |
| rs1143634 | Efficacy | 3 | infliximab | Crohn Disease |
| rs1143634 | Dosage,Efficacy | 3 | morphine | Pain;Postoperative |
| rs12621220 | Toxicity | 3 | Platinum compounds | Non-Small Cell Lung Carcinoma |
| rs16944 | Efficacy | 3 | Bisphosphonates;clodronate;etidronic acid;risedronate;tiludronate | Osteitis Deformans |
| rs16944 | Efficacy | 3 | lansoprazole;omeprazole;rabeprazole | Helicobacter Infections |
| rs16944 | Efficacy | 3 | pravastatin | |
| rs16944 | Toxicity | 3 | antipsychotics | Schizophrenia |
| rs4848306 | Efficacy | 3 | Tumor necrosis factor alpha (TNF-alpha) inhibitors | Inflammatory Bowel Diseases;Ulcerative Colitis |
| rs4849127 | Toxicity | 3 | antipsychotics | Schizophrenia |
PharmGKB variants
6 variants.
| Variant | Genes | Level | Score | #Clin annots | Drugs |
|---|---|---|---|---|---|
| rs16944 | IL1B | 3 | 3.00 | 4 | Bisphosphonates;clodronate;etidronic acid;risedronate;tiludronate;lansoprazole;omeprazole;rabeprazole;pravastatin;antipsychotics |
| rs1143623 | IL1B | 3 | 3.75 | 2 | Tumor necrosis factor alpha (TNF-alpha) inhibitors;ustekinumab;Platinum compounds |
| rs1143627 | IL1B | 3 | 3.75 | 2 | Tumor necrosis factor alpha (TNF-alpha) inhibitors;ustekinumab;aspirin |
| rs1143634 | IL1B | 3 | 3.00 | 4 | morphine;antipsychotics;infliximab |
| rs4848306 | IL1B | 3 | 3.00 | 1 | Tumor necrosis factor alpha (TNF-alpha) inhibitors |
| rs4849127 | IL1B | 3 | 3.00 | 1 | antipsychotics |
Binding affinities (BindingDB)
146 measured of 169 human assays (170 total across all organisms); most potent 50 below. Values come from heterogeneous assays and are not directly comparable.
| Ligand | Measure | Value | Patent |
|---|---|---|---|
| 4-chloro-N-[(3,3-difluoro-1-hydroxy-5-methylcyclohexyl)methyl]-1-(2,2,2-trifluoroethyl)indole-3-carboxamide | IC50 | 1.4 nM | US-10322143: Inhibitors of ADAMTS4 or ADAMTS5 for use in preventing or treating cardiac remodeling and chronic heart failure |
| CC-220 (Compound 6) | IC50 | 28 nM | US-9694015: Methods for the treatment of locally advanced breast cancer |
| 4-chloro-N-[[(1S,3S)-1-hydroxy-3-methylcyclohexyl]methyl]-1-(2,2,2-trifluoroethyl)indole-3-carboxamide | IC50 | 55 nM | US-10323000: Indole derivatives and their use in neurodegenerative diseases |
| 1-(2-aminoethyl)-4-chloro-N-[(4,4-difluorocyclohexyl)methyl]indole-3-carboxamide | IC50 | 55 nM | US-10323000: Indole derivatives and their use in neurodegenerative diseases |
| 4-chloro-1-(3,3-difluoropropyl)-N-[[(1S,3S)-1-hydroxy-3-methylcyclohexyl]methyl]indole-3-carboxamide | IC50 | 55 nM | US-10323000: Indole derivatives and their use in neurodegenerative diseases |
| 4-chloro-N-[(4,4-difluorocyclohexyl)methyl]-1-(3,3,3-trifluoropropyl)indole-3-carboxamide | IC50 | 55 nM | US-10323000: Indole derivatives and their use in neurodegenerative diseases |
| 4-chloro-N-[[(1R)-3,3-difluoro-1-hydroxycyclohexyl]methyl]-1-(2-methoxyethyl)indole-3-carboxamide | IC50 | 55 nM | US-10323000: Indole derivatives and their use in neurodegenerative diseases |
| 4-chloro-N-[(3,3-difluoro-1-hydroxycyclohexyl)methyl]-1-(2-methoxyethyl)indole-3-carboxamide | IC50 | 55 nM | US-10323000: Indole derivatives and their use in neurodegenerative diseases |
| 4-chloro-N-[(4,4-difluoro-1-hydroxycyclohexyl)methyl]-1-(2-methoxyethyl)indole-3-carboxamide | IC50 | 55 nM | US-10323000: Indole derivatives and their use in neurodegenerative diseases |
| N-[[(1S,4R)-2-bicyclo[2.2.1]heptanyl]methyl]-4-chloro-1-(oxetan-3-yl)indole-3-carboxamide | IC50 | 55 nM | US-10323000: Indole derivatives and their use in neurodegenerative diseases |
| N-[1-(1-adamantyl)ethyl]-4-chloro-1-(oxetan-3-yl)indole-3-carboxamide | IC50 | 55 nM | US-10323000: Indole derivatives and their use in neurodegenerative diseases |
| 4-chloro-N-[(1-hydroxy-3,3-dimethylcyclohexyl)methyl]-1-(oxetan-3-yl)indole-3-carboxamide | IC50 | 55 nM | US-10323000: Indole derivatives and their use in neurodegenerative diseases |
| 4-chloro-N-[[(1S)-3,3-difluorocyclohexyl]methyl]-1-(oxetan-3-yl)indole-3-carboxamide | IC50 | 55 nM | US-10323000: Indole derivatives and their use in neurodegenerative diseases |
| 4-chloro-1-(oxetan-3-yl)-N-(spiro[2.5]octan-7-ylmethyl)indole-3-carboxamide | IC50 | 55 nM | US-10323000: Indole derivatives and their use in neurodegenerative diseases |
| N-[2-[(1S,2S,4S)-2-bicyclo[2.2.1]hept-5-enyl]ethyl]-4-chloro-1-(oxetan-3-yl)indole-3-carboxamide | IC50 | 55 nM | US-10323000: Indole derivatives and their use in neurodegenerative diseases |
| 4-chloro-N-[(1-hydroxy-3-methylcyclohexyl)methyl]-1-(oxetan-3-yl)indole-3-carboxamide | IC50 | 55 nM | US-10323000: Indole derivatives and their use in neurodegenerative diseases |
| 4-chloro-N-[[(1S)-3,3-difluoro-1-hydroxycyclohexyl]methyl]-1-(oxetan-3-yl)indole-3-carboxamide | IC50 | 55 nM | US-10323000: Indole derivatives and their use in neurodegenerative diseases |
| 4-chloro-N-[(3,3-difluoro-1-hydroxycyclohexyl)methyl]-1-(oxetan-3-yl)indole-3-carboxamide | IC50 | 55 nM | US-10323000: Indole derivatives and their use in neurodegenerative diseases |
| 4-chloro-N-[[(1S,3S)-1-hydroxy-3-methylcyclohexyl]methyl]-1-(oxetan-3-yl)indole-3-carboxamide | IC50 | 55 nM | US-10323000: Indole derivatives and their use in neurodegenerative diseases |
| 4-chloro-N-[[(1R,3R)-1-hydroxy-3-methylcyclohexyl]methyl]-1-(oxetan-3-yl)indole-3-carboxamide | IC50 | 55 nM | US-10323000: Indole derivatives and their use in neurodegenerative diseases |
| 4-chloro-N-[(4,4-difluorocyclohexyl)methyl]-1-(oxetan-3-yl)indole-3-carboxamide | IC50 | 55 nM | US-10323000: Indole derivatives and their use in neurodegenerative diseases |
| 4-chloro-N-[[(1R,3R)-1-hydroxy-3-methylcyclohexyl]methyl]-1-(oxolan-3-yl)indole-3-carboxamide | IC50 | 55 nM | US-10323000: Indole derivatives and their use in neurodegenerative diseases |
| 4-chloro-N-[(4,4-difluorocyclohexyl)methyl]-1-(oxetan-2-ylmethyl)indole-3-carboxamide | IC50 | 55 nM | US-10323000: Indole derivatives and their use in neurodegenerative diseases |
| tert-butyl 3-[4-chloro-3-[(4,4-difluoro-1-hydroxycyclohexyl)methylcarbamoyl]indol-1-yl]azetidine-1-carboxylate | IC50 | 55 nM | US-10323000: Indole derivatives and their use in neurodegenerative diseases |
| 4-chloro-N-[(3,3-difluoro-1-hydroxycyclohexyl)methyl]-1-pyrrolidin-3-ylindole-3-carboxamide | IC50 | 55 nM | US-10323000: Indole derivatives and their use in neurodegenerative diseases |
| tert-butyl 3-[4-chloro-3-[(4,4-difluorocyclohexyl)methylcarbamoyl]indol-1-yl]pyrrolidine-1-carboxylate | IC50 | 55 nM | US-10323000: Indole derivatives and their use in neurodegenerative diseases |
| tert-butyl (2S)-2-[[4-chloro-3-[(4,4-difluorocyclohexyl)methylcarbamoyl]indol-1-yl]methyl]azetidine-1-carboxylate | IC50 | 55 nM | US-10323000: Indole derivatives and their use in neurodegenerative diseases |
| 1-(azetidin-2-ylmethyl)-4-chloro-N-[(3,3-difluoro-1-hydroxycyclohexyl)methyl]indole-3-carboxamide | IC50 | 55 nM | US-10323000: Indole derivatives and their use in neurodegenerative diseases |
| 1-(azetidin-3-ylmethyl)-4-chloro-N-[(3,3-difluoro-1-hydroxycyclohexyl)methyl]indole-3-carboxamide | IC50 | 55 nM | US-10323000: Indole derivatives and their use in neurodegenerative diseases |
| 4-chloro-N-[(4,4-difluorocyclohexyl)methyl]-1-[[(5R)-2-oxo-1,3-oxazolidin-5-yl]methyl]indole-3-carboxamide | IC50 | 55 nM | US-10323000: Indole derivatives and their use in neurodegenerative diseases |
| 4-chloro-N-[[(1S)-3,3-difluoro-1-hydroxycyclohexyl]methyl]-1-[[(2S)-oxolan-2-yl]methyl]indole-3-carboxamide | IC50 | 55 nM | US-10323000: Indole derivatives and their use in neurodegenerative diseases |
| 4-chloro-N-[(4,4-difluoro-1-hydroxycyclohexyl)methyl]-1-[[(2R)-oxolan-2-yl]methyl]indole-3-carboxamide | IC50 | 55 nM | US-10323000: Indole derivatives and their use in neurodegenerative diseases |
| 4-chloro-N-[(4,4-difluorocyclohexyl)methyl]-1-[[(2R)-oxolan-2-yl]methyl]indole-3-carboxamide | IC50 | 55 nM | US-10323000: Indole derivatives and their use in neurodegenerative diseases |
| 4-chloro-N-[(3,3-difluoro-1-hydroxycyclohexyl)methyl]-1-[[(2R)-oxolan-2-yl]methyl]indole-3-carboxamide | IC50 | 55 nM | US-10323000: Indole derivatives and their use in neurodegenerative diseases |
| 4-chloro-N-[(4,4-difluorocyclohexyl)methyl]-1-[[(2S)-oxolan-2-yl]methyl]indole-3-carboxamide | IC50 | 55 nM | US-10323000: Indole derivatives and their use in neurodegenerative diseases |
| 4-chloro-N-[(3,3-difluoro-1-hydroxycyclohexyl)methyl]-1-(oxolan-2-ylmethyl)indole-3-carboxamide | IC50 | 55 nM | US-10323000: Indole derivatives and their use in neurodegenerative diseases |
| 4-chloro-N-[[(1S,3S)-1-hydroxy-3-methylcyclohexyl]methyl]-1-(oxolan-2-ylmethyl)indole-3-carboxamide | IC50 | 55 nM | US-10323000: Indole derivatives and their use in neurodegenerative diseases |
| 4-chloro-N-[[3,3-difluoro-5-(trifluoromethyl)cyclohexyl]methyl]-1-(oxolan-2-ylmethyl)indole-3-carboxamide | IC50 | 55 nM | US-10323000: Indole derivatives and their use in neurodegenerative diseases |
| 4-chloro-N-[(3,3-difluoro-1-hydroxycyclohexyl)methyl]-1-(oxolan-3-ylmethyl)indole-3-carboxamide | IC50 | 55 nM | US-10323000: Indole derivatives and their use in neurodegenerative diseases |
| 4-chloro-N-[(4,4-difluoro-1-hydroxycyclohexyl)methyl]-1-(oxolan-3-ylmethyl)indole-3-carboxamide | IC50 | 55 nM | US-10323000: Indole derivatives and their use in neurodegenerative diseases |
| 4-chloro-N-[(4,4-difluorocyclohexyl)methyl]-1-(1,4-dioxan-2-ylmethyl)indole-3-carboxamide | IC50 | 55 nM | US-10323000: Indole derivatives and their use in neurodegenerative diseases |
| 4-chloro-N-[(4,4-difluorocyclohexyl)methyl]-1-[[(2S)-1-methylazetidin-2-yl]methyl]indole-3-carboxamide | IC50 | 55 nM | US-10323000: Indole derivatives and their use in neurodegenerative diseases |
| tert-butyl (2S)-2-[[4-chloro-3-[(4,4-difluorocyclohexyl)methylcarbamoyl]indol-1-yl]methyl]pyrrolidine-1-carboxylate | IC50 | 55 nM | US-10323000: Indole derivatives and their use in neurodegenerative diseases |
| 4-chloro-N-[(4,4-difluorocyclohexyl)methyl]-1-[[(2R)-pyrrolidin-2-yl]methyl]indole-3-carboxamide | IC50 | 55 nM | US-10323000: Indole derivatives and their use in neurodegenerative diseases |
| 4-chloro-N-[(4,4-difluorocyclohexyl)methyl]-1-[[(2R)-5-oxopyrrolidin-2-yl]methyl]indole-3-carboxamide | IC50 | 55 nM | US-10323000: Indole derivatives and their use in neurodegenerative diseases |
| 4-chloro-N-[(4,4-difluorocyclohexyl)methyl]-1-[2-[ethyl(methyl)amino]-2-oxoethyl]indole-3-carboxamide | IC50 | 55 nM | US-10323000: Indole derivatives and their use in neurodegenerative diseases |
| tert-butyl 3-[[4-chloro-3-[(4,4-difluorocyclohexyl)methylcarbamoyl]indol-1-yl]methyl]morpholine-4-carboxylate | IC50 | 55 nM | US-10323000: Indole derivatives and their use in neurodegenerative diseases |
| 4-chloro-N-[(4,4-difluoro-1-hydroxycyclohexyl)methyl]-1-(oxan-2-ylmethyl)indole-3-carboxamide | IC50 | 55 nM | US-10323000: Indole derivatives and their use in neurodegenerative diseases |
| 4-chloro-N-[(4,4-difluorocyclohexyl)methyl]-1-(oxan-2-ylmethyl)indole-3-carboxamide | IC50 | 55 nM | US-10323000: Indole derivatives and their use in neurodegenerative diseases |
| tert-butyl (2S)-2-[[4-chloro-3-[(4,4-difluoro-1-hydroxycyclohexyl)methylcarbamoyl]indol-1-yl]methyl]pyrrolidine-1-carboxylate | IC50 | 55 nM | US-10323000: Indole derivatives and their use in neurodegenerative diseases |
ChEMBL bioactivities
413 potent at pChembl≥5 of 422 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).
| pChembl | Type | Value | Unit | Molecule |
|---|---|---|---|---|
| 9.40 | IC50 | 0.4 | nM | CHEMBL5426651 |
| 9.40 | IC50 | 0.4 | nM | CHEMBL5414596 |
| 9.34 | IC50 | 0.46 | nM | IBERDOMIDE |
| 9.22 | IC50 | 0.6 | nM | CHEMBL5992744 |
| 9.15 | IC50 | 0.7 | nM | CHEMBL5774519 |
| 9.10 | IC50 | 0.8 | nM | CHEMBL5433380 |
| 9.10 | IC50 | 0.8 | nM | CHEMBL5991941 |
| 9.10 | IC50 | 0.8 | nM | CHEMBL5906571 |
| 9.10 | IC50 | 0.8 | nM | CHEMBL5797061 |
| 9.10 | IC50 | 0.8 | nM | CHEMBL5910216 |
| 9.07 | IC50 | 0.85 | nM | CHEMBL5949264 |
| 9.05 | IC50 | 0.9 | nM | CHEMBL5881090 |
| 9.00 | Ki | 1 | nM | CHEMBL293979 |
| 9.00 | Ki | 1 | nM | CHEMBL299288 |
| 8.92 | IC50 | 1.2 | nM | CHEMBL6036597 |
| 8.89 | IC50 | 1.3 | nM | CHEMBL5970809 |
| 8.89 | IC50 | 1.3 | nM | CHEMBL5752218 |
| 8.80 | IC50 | 1.6 | nM | CHEMBL5808276 |
| 8.80 | IC50 | 1.6 | nM | CHEMBL5763108 |
| 8.74 | IC50 | 1.8 | nM | CHEMBL5782617 |
| 8.72 | IC50 | 1.9 | nM | CHEMBL5928082 |
| 8.72 | IC50 | 1.9 | nM | CHEMBL5971979 |
| 8.64 | IC50 | 2.3 | nM | CHEMBL6011033 |
| 8.59 | IC50 | 2.6 | nM | CHEMBL6029082 |
| 8.59 | IC50 | 2.6 | nM | CHEMBL5812129 |
| 8.52 | IC50 | 3 | nM | CHEMBL5852308 |
| 8.52 | IC50 | 3 | nM | CHEMBL5960754 |
| 8.49 | IC50 | 3.2 | nM | CHEMBL5761984 |
| 8.49 | IC50 | 3.2 | nM | CHEMBL5801636 |
| 8.48 | IC50 | 3.3 | nM | CHEMBL6049792 |
| 8.46 | IC50 | 3.5 | nM | CHEMBL6015148 |
| 8.44 | IC50 | 3.6 | nM | CHEMBL5758980 |
| 8.33 | IC50 | 4.7 | nM | CHEMBL6001622 |
| 8.23 | IC50 | 5.9 | nM | CHEMBL5782662 |
| 8.22 | IC50 | 6 | nM | CHEMBL5840970 |
| 8.21 | IC50 | 6.2 | nM | CHEMBL5922366 |
| 8.20 | IC50 | 6.3 | nM | CHEMBL5847930 |
| 8.18 | IC50 | 6.6 | nM | CHEMBL5973713 |
| 8.17 | IC50 | 6.8 | nM | CHEMBL5834410 |
| 8.13 | IC50 | 7.4 | nM | CHEMBL5963394 |
| 8.12 | IC50 | 7.6 | nM | CHEMBL5763742 |
| 8.08 | IC50 | 8.3 | nM | CHEMBL5882443 |
| 7.99 | IC50 | 10.2 | nM | CHEMBL5790303 |
| 7.93 | IC50 | 11.8 | nM | CHEMBL5984350 |
| 7.89 | IC50 | 13 | nM | CHEMBL5874946 |
| 7.74 | IC50 | 18.3 | nM | CHEMBL5808248 |
| 7.64 | IC50 | 22.7 | nM | CHEMBL5836561 |
| 7.62 | IC50 | 24.1 | nM | CHEMBL6015125 |
| 7.60 | IC50 | 25.3 | nM | CHEMBL6035509 |
| 7.59 | IC50 | 25.5 | nM | CHEMBL6009102 |
PubChem BioAssay actives
19 with measured affinity, of 439 total; 15 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 |
|---|---|---|---|---|
| (3S)-3-[[(4S,7S)-7-[[4-(carboxymethoxy)benzoyl]amino]-6,10-dioxo-2,3,4,7,8,9-hexahydro-1H-pyridazino[1,2-a]diazepine-4-carbonyl]amino]-4-oxobutanoic acid | 2100630: Binding affinity to Interleukin-1beta (unknown origin) assessed as inhibition constant | ki | 0.0010 | uM |
| (3S)-3-[[(4S,7S)-7-[(2-fluorobenzoyl)amino]-6,10-dioxo-2,3,4,7,8,9-hexahydro-1H-pyridazino[1,2-a]diazepine-4-carbonyl]amino]-4-oxobutanoic acid | 2100630: Binding affinity to Interleukin-1beta (unknown origin) assessed as inhibition constant | ki | 0.0010 | uM |
| 3-[[2-[2-[2-[2-[2-[(3-carboxy-5-quinolin-4-ylanilino)methyl]phenoxy]ethoxy]ethoxy]ethoxy]phenyl]methylamino]-5-quinolin-4-ylbenzoic acid | 2088628: Binding affinity to Interleukin-1beta (unknown origin) assessed as dissociation constant | kd | 0.0400 | uM |
| (3S)-4-oxo-3-[2-[2-oxo-3-(3-phenylpropanoylamino)-1-pyridinyl]propanoylamino]butanoic acid | 2100630: Binding affinity to Interleukin-1beta (unknown origin) assessed as inhibition constant | ki | 0.1500 | uM |
| (3R)-3-[[2-[6-benzyl-2-oxo-3-(3-phenylpropanoylamino)-1-pyridinyl]acetyl]amino]-4-oxobutanoic acid | 2100630: Binding affinity to Interleukin-1beta (unknown origin) assessed as inhibition constant | ki | 0.1500 | uM |
| (3S)-4-oxo-3-[[2-[2-oxo-6-phenyl-3-(3-phenylpropanoylamino)-1-pyridinyl]acetyl]amino]butanoic acid | 2100630: Binding affinity to Interleukin-1beta (unknown origin) assessed as inhibition constant | ki | 0.9000 | uM |
| (3R)-3-[2-[6-benzyl-2-oxo-3-(3-phenylpropanoylamino)-1-pyridinyl]propanoylamino]-4-oxobutanoic acid | 2100630: Binding affinity to Interleukin-1beta (unknown origin) assessed as inhibition constant | ki | 0.9700 | uM |
| 4-[4-hydroxy-3-[(3S)-6-methyl-2-oxo-3-(1H-pyrazol-4-yl)-1H-indol-3-yl]phenyl]benzene-1,3-dicarboxylic acid | 2071788: Binding affinity to C-terminally avi-tagged human IL-1 beta assessed as dissociation constant by surface plasmon resonance analysis | kd | 1.1000 | uM |
| 2-[(7S)-4-(benzenesulfonyl)-7-(2-morpholin-4-ylethylcarbamoyl)-1,4-diazepane-1-carbonyl]-8-[4-formyl-3-(trifluoromethyl)phenyl]imidazo[1,2-a]pyridine-6-carboxylic acid | 2071791: Antagonist activity at human recombinant His-tagged wild type IL-1 beta assessed as inhibition of IL-1 beta/Alexa 647 labeled human IL-1R1 (1 to 332) interaction preincubated with IL-1 beta for 1 hr followed by IL-1R1 addition and measured after 1 hr by TR-FRET assay | ic50 | 1.2000 | uM |
| (3S)-3-[[(2S)-2-[[(2S)-2-[[(2S)-2-acetamido-3-(4-hydroxyphenyl)propanoyl]amino]-3-methylbutanoyl]amino]propanoyl]amino]-4-oxobutanoic acid | 627038: Induction of IL-1 beta production in LPS-induced human THP-1 cells by ELISA | ic50 | 2.0000 | uM |
| methyl (1R,2S,5S,7R,10S,11S,13R,15S)-7,15-dihydroxy-2,6,6,10,13,15-hexamethyl-17-methylidene-14,16-dioxotetracyclo[11.3.1.02,11.05,10]heptadecane-1-carboxylate | 627038: Induction of IL-1 beta production in LPS-induced human THP-1 cells by ELISA | ic50 | 2.7000 | uM |
| methyl (1R,2S,11S,12S,14R,16S)-16-hydroxy-2,6,6,11,14,16-hexamethyl-18-methylidene-8,15,17-trioxo-7-oxatetracyclo[12.3.1.02,12.05,11]octadec-4-ene-1-carboxylate | 627038: Induction of IL-1 beta production in LPS-induced human THP-1 cells by ELISA | ic50 | 3.7000 | uM |
| methyl (1R,2S,12S,14R,16S)-16-hydroxy-2,6,6,11,14,16-hexamethyl-18-methylidene-8,15,17-trioxo-7-oxatetracyclo[12.3.1.02,12.05,10]octadeca-4,10-diene-1-carboxylate | 627038: Induction of IL-1 beta production in LPS-induced human THP-1 cells by ELISA | ic50 | 4.4000 | uM |
| [(1S,3R,4S,5R,6S,7S,10R,14R,15S)-5-acetyloxy-14-(furan-3-yl)-3-hydroxy-10,15-dimethyl-9-oxo-7-propan-2-yl-2-oxapentacyclo[8.6.1.13,6.06,17.011,15]octadec-11-en-4-yl] (E)-2-methylbut-2-enoate | 1607901: Inhibition of IL1-beta (unknown origin) | ic50 | 7.8000 | uM |
| 2-[(7S)-4-(benzenesulfonyl)-7-(2-morpholin-4-ylethylcarbamoyl)-1,4-diazepane-1-carbonyl]-8-(4-formyl-3-propan-2-ylphenyl)imidazo[1,2-a]pyridine-6-carboxylic acid | 2071791: Antagonist activity at human recombinant His-tagged wild type IL-1 beta assessed as inhibition of IL-1 beta/Alexa 647 labeled human IL-1R1 (1 to 332) interaction preincubated with IL-1 beta for 1 hr followed by IL-1R1 addition and measured after 1 hr by TR-FRET assay | ic50 | 8.3000 | uM |
CTD chemical–gene interactions
1155 total (human), top 30 by PubMed support.
| Chemical | Actions (top 5) | PubMed papers |
|---|---|---|
| Lipopolysaccharides | decreases reaction, increases expression, affects expression, increases reaction, increases abundance (+11 more) | 174 |
| Particulate Matter | affects response to substance, increases cleavage, affects reaction, affects cotreatment, increases abundance (+5 more) | 64 |
| Acetylcysteine | decreases expression, decreases reaction, increases reaction, increases abundance, affects binding (+5 more) | 43 |
| Resveratrol | increases reaction, increases secretion, increases abundance, decreases activity, decreases reaction (+10 more) | 42 |
| Dinoprostone | increases chemical synthesis, increases secretion, affects expression, increases activity, decreases reaction (+4 more) | 40 |
| Dexamethasone | affects expression, affects reaction, decreases reaction, increases expression, increases reaction (+9 more) | 32 |
| Tetrachlorodibenzodioxin | increases expression, affects reaction, increases reaction, affects binding, affects cotreatment (+5 more) | 27 |
| Tetradecanoylphorbol Acetate | decreases reaction, increases secretion, affects cotreatment, increases expression, affects expression (+3 more) | 26 |
| Quercetin | increases phosphorylation, decreases secretion, decreases response to substance, increases secretion, increases reaction (+8 more) | 25 |
| Air Pollutants | affects cotreatment, increases abundance, increases expression, increases response to substance, affects response to substance (+4 more) | 24 |
| sodium arsenite | increases activity, increases degradation, increases secretion, decreases response to substance, affects reaction (+7 more) | 22 |
| Adenosine Triphosphate | increases secretion, increases cleavage, increases expression, increases reaction, affects reaction (+2 more) | 21 |
| SB 203580 | increases reaction, decreases reaction, decreases response to substance, increases cleavage, decreases expression (+7 more) | 20 |
| 2-(2-amino-3-methoxyphenyl)-4H-1-benzopyran-4-one | affects reaction, affects cotreatment, decreases reaction, increases chemical synthesis, increases expression (+5 more) | 20 |
| lipopolysaccharide, Escherichia coli O111 B4 | decreases reaction, increases expression, increases cleavage, increases abundance, increases acylation (+6 more) | 20 |
| Glucose | increases expression, increases secretion, affects cotreatment, affects reaction, decreases expression (+3 more) | 20 |
| Nitric Oxide | decreases reaction, increases abundance, increases reaction, affects cotreatment, affects reaction (+3 more) | 19 |
| Cadmium Chloride | decreases expression, increases reaction, affects reaction, decreases reaction, affects cotreatment (+5 more) | 19 |
| Silicon Dioxide | affects cotreatment, affects reaction, increases cleavage, increases expression, decreases reaction (+3 more) | 18 |
| pyrazolanthrone | affects cotreatment, decreases reaction, increases expression, increases activity, decreases expression (+4 more) | 17 |
| Glucosamine | decreases expression, increases phosphorylation, increases expression, affects cotreatment, increases activity (+8 more) | 17 |
| Tobacco Smoke Pollution | decreases secretion, affects cotreatment, decreases reaction, increases expression, increases reaction (+2 more) | 17 |
| Vehicle Emissions | affects cotreatment, decreases reaction, increases secretion, increases abundance, decreases expression (+4 more) | 15 |
| Benzo(a)pyrene | decreases reaction, affects expression, affects reaction, increases expression, increases reaction (+3 more) | 15 |
| 1-Methyl-4-phenylpyridinium | increases reaction, increases cleavage, increases secretion, increases expression, decreases reaction (+1 more) | 15 |
| bisphenol A | increases abundance, decreases reaction, increases expression, increases reaction, affects expression (+5 more) | 14 |
| 3-(4-methylphenylsulfonyl)-2-propenenitrile | affects binding, increases cleavage, affects localization, increases phosphorylation, decreases secretion (+8 more) | 14 |
| Cadmium | increases reaction, decreases reaction, increases expression, increases abundance, increases secretion (+3 more) | 13 |
| Indomethacin | increases abundance, affects cotreatment, increases secretion, increases activity, increases chemical synthesis (+5 more) | 12 |
| nickel sulfate | increases expression, increases secretion, affects cotreatment, decreases reaction, decreases expression | 11 |
ChEMBL screening assays
26 unique, capped per target: 26 binding
Representative assays (with source publication via chembl_document):
| Assay ID | Type | Description | Source paper |
|---|---|---|---|
| CHEMBL1913641 | Binding | Induction of IL-1 beta production in LPS-induced human THP-1 cells by ELISA | Berkeleyones and related meroterpenes from a deep water acid mine waste fungus that inhibit the production of interleukin 1-β from induced inflammasomes. — J Nat Prod |
Cellosaurus cell lines
5 cell lines: 5 cancer cell line
First 10 cell lines (id-ordered, not curated):
| Cellosaurus | Name | Category | Sex |
|---|---|---|---|
| CVCL_B1AE | Abcam THP-1 IL1B KO | Cancer cell line | Male |
| CVCL_B8IB | Abcam HCT 116 IL1B KO | Cancer cell line | Male |
| CVCL_B8XB | Abcam MCF-7 IL1B KO | Cancer cell line | Female |
| CVCL_B9KK | Abcam A-549 IL1B KO | Cancer cell line | Male |
| CVCL_E0EZ | Ubigene HeLa IL1B KO | Cancer cell line | Female |
Clinical trials (associated diseases)
305 trials via MONDO — disease-level, not drug-specific.
| Trial | Phase | Status | Title |
|---|---|---|---|
| NCT00286351 | PHASE4 | COMPLETED | Use of Arimidex and Zoladex as Pretreatment to IVF in Women With Ovarian Endometriosis |
| NCT00621179 | PHASE4 | COMPLETED | Endometrial Markers and Response of Endometriosis Patients to Prolonged GnRH Agonist Prior to IVF |
| NCT00625950 | PHASE4 | COMPLETED | Endometriosis Patients Undergoing Quinagolide Treatment |
| NCT00654524 | PHASE4 | UNKNOWN | Randomized Study of Gonadotropin-releasing-hormone Agonist (GnRH-a) or Expectant Management for Endometriosis |
| NCT00735852 | PHASE4 | COMPLETED | Decapeptyl SR With Livial Add Back Therapy in the Management of Chronic Cyclical Pelvic Pain in Pre Menopausal Women |
| NCT00844012 | PHASE4 | UNKNOWN | Continuous Postoperative Use of Low-Dose Combined Oral Contraceptivesfor for Endometriosis-Related Chronic Pelvic Pain |
| NCT01056042 | PHASE4 | COMPLETED | Efficacy of Injectable Contraceptive and Oral Contraceptive Administered After Surgical Treatment of Endometriosis With Pain |
| NCT01581359 | PHASE4 | COMPLETED | The Effect of Pre-treatment With GnRH Analogues Prior in Vitro Fertilization in Patients With Endometriosis |
| NCT01682642 | PHASE4 | COMPLETED | The Influence of Adjuvant Medical Treatment of Peritoneal Endometriosis on the Outcome of IVF. A Prospective Randomized Analysis. |
| NCT01769781 | PHASE4 | COMPLETED | Anastrazole Plus GnRH-agonist in the Treatment of Endometriosis Recurrence |
| NCT01779232 | PHASE4 | COMPLETED | Danazol Treatment in Endometriosis Women Before IVF |
| NCT02158845 | PHASE4 | COMPLETED | Levonorgestrel-releasing Intrauterine System in Patients With Endometriosis |
| NCT02165917 | PHASE4 | UNKNOWN | Study to Compare Peritoneal Ablation by Excision Only and Excision With the Use of an Adhesion Barrier |
| NCT02213081 | PHASE4 | COMPLETED | Ulipristal for Endometriosis-related Pelvic Pain |
| NCT02214550 | PHASE4 | COMPLETED | Chronic Pain Risk Associated With Menstrual Period Pain |
| NCT02385448 | PHASE4 | UNKNOWN | Comparing the Use of Dienogest and Combined Oral Contraceptive Pills (Microgynon) to Reduce the Risk of Recurrence of Endometriotic Cyst After Conservative Surgery |
| NCT02387931 | PHASE4 | COMPLETED | Supplementation in Adolescent Girls With Endometriosis |
| NCT02393482 | PHASE4 | UNKNOWN | Psychological Impact of Amenorrhea in Women With Endometriosis |
| NCT02427386 | PHASE4 | COMPLETED | Homeopathic Treatment of Chronic Pelvic Pain in Women With Endometriosis |
| NCT02475564 | PHASE4 | COMPLETED | Resveratrol for Pain Due to Endometriosis |
| NCT02480647 | PHASE4 | COMPLETED | Clinical Trial the Use of Levonorgestrel-releasing Intrauterine System Versus Etonogestrel Implant in Endometriosis |
| NCT02534688 | PHASE4 | COMPLETED | Effectiveness of Levonorgestrel-intrauterine System (LNG-IUS) Versus Depot Medroxyprogesterone Acetate (DMPA) in Treatment of Pelvic Pain in Clinically Diagnosed Endometriotic Patients |
| NCT02812186 | PHASE4 | COMPLETED | Deep Versus Moderate Neuromuscular Blockade During Laparoscopic Surgery |
| NCT04218487 | PHASE4 | UNKNOWN | Xuefu-Zhuyu Capsule for the Treatment of Qizhi Xueyu Zheng (Qi Stagnation and Blood Stasis Syndrome) |
| NCT04554693 | PHASE4 | ACTIVE_NOT_RECRUITING | The Use of Low Dose Metronidazole to Decrease Postoperative Pain After Endometriosis Surgery |
| NCT04942015 | PHASE4 | UNKNOWN | Honghuaruyi Wan for Endometriosis Dysmenorrhea |
| NCT05013242 | PHASE4 | UNKNOWN | Goserline Acetate VS Dienogest in Endometriosi |
| NCT05059626 | PHASE4 | RECRUITING | Endometriosis and Microvascular Dysfunction; Simvastatin and Duavee |
| NCT05331053 | PHASE4 | TERMINATED | MicroRNA Activation of LOX-1 Mechanisms in Endometriosis |
| NCT05560230 | PHASE4 | COMPLETED | Intraoperative Clonidine for Postoperative Pain Management in Patients Undergoing Surgical Treatment for Endometriosis |
| NCT05962034 | PHASE4 | RECRUITING | Thromboxane Function in Women With Endometriosis |
| NCT06523530 | PHASE4 | RECRUITING | Effect of a GnRH Analog on Hepatic Steatosis |
| NCT06543550 | PHASE4 | RECRUITING | Comparison Between the Effects of Implantable Gestrinone and Oral Dienogest in the Treatment of Endometriosis |
| NCT06577233 | PHASE4 | RECRUITING | Superior Hypogastric Nerve Plexus Block With Bupivacaine After Robotic Resection of Endometriosis |
| NCT06951802 | PHASE4 | RECRUITING | Endometriosis and Pain Treatment by Intraoperative Administration of Low-dose Ketamine |
| NCT07144904 | PHASE4 | NOT_YET_RECRUITING | Assessing the Efficacy of Indocyanine Green for Ureter Identification During Robot-Assisted Surgery in Advanced-Stage Endometriosis |
| NCT07182032 | PHASE4 | WITHDRAWN | Ketamine in Central Sensitization |
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Related Atlas pages
- Associated diseases: hereditary diffuse gastric adenocarcinoma
- Disease cohort memberships (association, not causation — diseases whose associated-gene cohort lists this gene; a subset are also under Associated diseases): antisynthetase syndrome, cholangiocarcinoma, coronary heart disease, susceptibility to, 2, endometriosis, hereditary diffuse gastric adenocarcinoma