CA6
gene geneOn this page
Summary
CA6 (carbonic anhydrase 6, HGNC:1380) is a protein-coding gene on chromosome 1p36.23, encoding Carbonic anhydrase 6 (P23280). Reversible hydration of carbon dioxide.
The protein encoded by this gene is one of several isozymes of carbonic anhydrase. This protein is found only in salivary glands and saliva and protein may play a role in the reversible hydratation of carbon dioxide though its function in saliva is unknown.
Source: NCBI Gene 765 — RefSeq curated summary.
At a glance
- GWAS associations: 3
- Clinical variants (ClinVar): 66 total — 2 pathogenic, 1 likely-pathogenic
- Druggable target: yes — 47 molecules with ChEMBL bioactivity
- MANE Select transcript:
NM_001215
Identifiers
Gene identifiers
| Field | Value |
|---|---|
| HGNC ID | HGNC:1380 |
| Approved symbol | CA6 |
| Name | carbonic anhydrase 6 |
| Location | 1p36.23 |
| Locus type | gene with protein product |
| Status | Approved |
| Ensembl gene | ENSG00000131686 |
| Ensembl biotype | protein_coding |
| OMIM | 114780 |
| Entrez | 765 |
Gene structure
Transcript identifiers
Ensembl transcripts: 6 — 5 protein_coding, 1 protein_coding_CDS_not_defined
ENST00000377436, ENST00000377442, ENST00000377443, ENST00000476083, ENST00000480186, ENST00000549778
RefSeq mRNA: 4 — MANE Select: NM_001215
NM_001215, NM_001270500, NM_001270501, NM_001270502
CCDS: CCDS30578, CCDS57970, CCDS57971
Canonical transcript exons
ENST00000377443 — 8 exons
| Exon | Start | End |
|---|---|---|
| ENSE00000739889 | 8957137 | 8957285 |
| ENSE00001842797 | 8945868 | 8945965 |
| ENSE00001948966 | 8974622 | 8975092 |
| ENSE00002846718 | 8949263 | 8949442 |
| ENSE00003531235 | 8962587 | 8962656 |
| ENSE00003642291 | 8958910 | 8959002 |
| ENSE00003650334 | 8970867 | 8970981 |
| ENSE00003693295 | 8967659 | 8967816 |
Expression profiles
Bgee: expression breadth ubiquitous, 108 present calls, max score 100.00.
FANTOM5 (CAGE): breadth tissue_specific, TPM avg 49.3086 / max 48869.9940, expressed in 37 samples.
FANTOM5 promoters (1 alternative TSS)
| Promoter ID | TPM avg | Samples expressed |
|---|---|---|
| 475 | 49.3086 | 37 |
Top tissues by expression
255 total, by Bgee expression score (0-100, higher = more expressed):
| Tissue | Anatomy ID | Expression score | Quality |
|---|---|---|---|
| parotid gland | UBERON:0001831 | 100.00 | gold quality |
| upper arm skin | UBERON:0004263 | 95.71 | gold quality |
| upper leg skin | UBERON:0004262 | 94.07 | gold quality |
| skin of leg | UBERON:0001511 | 87.15 | gold quality |
| zone of skin | UBERON:0000014 | 85.11 | gold quality |
| skin of hip | UBERON:0001554 | 82.94 | gold quality |
| skin of abdomen | UBERON:0001416 | 81.51 | gold quality |
| diaphragm | UBERON:0001103 | 81.23 | gold quality |
| primordial germ cell in gonad | CL:0000670 ∩ UBERON:0000991 | 76.87 | gold quality |
| mammalian vulva | UBERON:0000997 | 76.53 | gold quality |
| cauda epididymis | UBERON:0004360 | 69.39 | gold quality |
| tongue squamous epithelium | UBERON:0006919 | 69.37 | gold quality |
| hair follicle | UBERON:0002073 | 67.35 | gold quality |
| tongue | UBERON:0001723 | 66.81 | gold quality |
| superior surface of tongue | UBERON:0007371 | 65.41 | gold quality |
| buccal mucosa cell | CL:0002336 | 64.65 | gold quality |
| tonsil | UBERON:0002372 | 64.58 | gold quality |
| vastus lateralis | UBERON:0001379 | 63.78 | gold quality |
| granulocyte | CL:0000094 | 63.25 | gold quality |
| quadriceps femoris | UBERON:0001377 | 62.80 | gold quality |
| nipple | UBERON:0002030 | 62.35 | gold quality |
| epithelium of nasopharynx | UBERON:0001951 | 61.50 | gold quality |
| olfactory bulb | UBERON:0002264 | 61.26 | gold quality |
| type B pancreatic cell | CL:0000169 | 61.12 | gold quality |
| blood | UBERON:0000178 | 60.98 | gold quality |
| body of tongue | UBERON:0011876 | 59.99 | gold quality |
| lymph node | UBERON:0000029 | 59.53 | gold quality |
| periodontal ligament | UBERON:0008266 | 59.50 | gold quality |
| secondary oocyte | CL:0000655 | 59.39 | gold quality |
| oocyte | CL:0000023 | 59.32 | gold quality |
Single-cell (SCXA)
Detected in 4 experiment(s), a significant marker in 2.
| Experiment | Marker? | Max mean expression |
|---|---|---|
| E-MTAB-9841 | yes | 553.93 |
| E-MTAB-10855 | yes | 446.74 |
| E-MTAB-7303 | no | 94.25 |
| E-ANND-3 | no | 4.35 |
Regulation
Is transcription factor: no
Upstream regulators (CollecTRI, top): CEBPB, DDIT3
miRNA regulators (miRDB)
18 targeting CA6, 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-498-5P | 99.76 | 69.64 | 1807 |
| HSA-MIR-556-3P | 99.74 | 68.75 | 1203 |
| HSA-MIR-1252-3P | 99.55 | 67.71 | 2862 |
| HSA-MIR-155-5P | 99.35 | 70.16 | 1509 |
| HSA-MIR-6731-5P | 99.28 | 67.42 | 2375 |
| HSA-MIR-10399-5P | 99.17 | 69.87 | 2610 |
| HSA-MIR-6504-3P | 99.17 | 69.31 | 2891 |
| HSA-MIR-6871-5P | 98.90 | 66.67 | 671 |
| HSA-MIR-29B-1-5P | 98.86 | 68.35 | 1364 |
| HSA-MIR-6731-3P | 98.61 | 67.86 | 749 |
| HSA-MIR-6878-5P | 98.49 | 67.91 | 2142 |
| HSA-MIR-6509-3P | 98.32 | 67.33 | 1343 |
| HSA-MIR-6826-3P | 98.19 | 66.32 | 1153 |
| HSA-MIR-30C-1-3P | 97.80 | 66.36 | 1499 |
| HSA-MIR-30C-2-3P | 97.80 | 66.45 | 1499 |
| HSA-MIR-6788-5P | 97.80 | 66.41 | 1532 |
| HSA-MIR-6748-3P | 97.20 | 65.66 | 836 |
| HSA-MIR-675-5P | 92.97 | 60.95 | 66 |
Literature-anchored findings (GeneRIF, showing 29)
- The cloning, expression and purification of this isozyme are reported. (PMID:17499996)
- analysis of allele & genotype distribution of 3 polymorphisms in CA6 gene; no association between polymorphisms in exons 2 & 3 & caries experience; positive association between salivary buffer capacity & rs2274327 (PMID:19721466)
- The gustin gene dimorphism rs2274333 observed in supertaster and nontaster subjects may influence the protein conformation and, thereby, affect zinc ion binding. (PMID:20631203)
- The polymerase chain reaction followed by restriction fragment length polymorphism assay described here can be used as an alternative to sequencing in bitter taster status research, and could be employed as a survey tool in nutrigenomic studies. (PMID:21631296)
- The data of this study showed how the combination of the TAS2R38 and gustin gene genotypes modulate PROP phenotype. (PMID:21712049)
- The aim of this study was to investigate carbonic anhydrase (CA) VI Exon 2 single nucleotide polymorphism (SNP) and its possible association with salivary parameters in type 2 diabetic patients compared to healthy adults. (PMID:22198626)
- The 1.9A crystal structure of the human CA VI catalytic domain reveals a prototypical mammalian CA fold, and a novel dimeric arrangement as compared to previously-reported CA structures. (PMID:22366092)
- results suggest that polymorphisms in the CA6 gene are associated with the concentrations of secreted CA VI. (PMID:23652931)
- The rs2274333 polymorphism of the gustin gene affects PROP sensitivity. (PMID:24040192)
- SNPs associated with taste perception and taste bud anatomy (PMID:24534176)
- Study showed that PROP (6-n-propylthiouracil) bitterness was due to TAS2R38 diplotypes, whereas the density of fungiform papillae was more closely associated with gustin genotypes (PMID:25447475)
- We also found that the haplotype (ACA) (rs2274328, rs17032907 and rs11576766)of the carbonic anhydrase VI was associated with a low number of decayed, missing, and filled teeth index with an odds ratio (95% confidence interval) of 0.635 (0.440-0.918). (PMID:26125798)
- CA6 is a specific marker for serous acinar cells of salivary glands and acinic cell carcinoma (AciCC). (PMID:26212680)
- dental plaque amount, lactobacilli count, age, and saliva buffer capacity, as well as CA6 (T55M) gene polymorphism, explained total of 87.8% of variations in DMFT scores. (PMID:26377569)
- Results found that the CA VI gene polymorphism rs2274327 showed no correlation between salivary parameters and dental-oral health status in Eastern Anatolian Turkish children. (PMID:27100223)
- genetic association studies in population of elderly women in Poland: Data suggest that SNPs in TAS2R38 (rs713598, rs1726866, rs10246939) and an SNP in CA6 (rs2274333) are associated with intake of and preferences for some foods (coffee and white cabbage) among the population studied. (TAS2R38 = taste receptor type 2 member 38; CA6 = carbonic anhydrase VI) (PMID:28455260)
- The current study suggests that genetic variation in TAS2R38 and CA6 influences picky eating in preschoolers. (PMID:28858874)
- Anti-CA6 was the most prevalent novel autoantibody in patients with dry eye, and was associated with younger age and more severe disease. Longitudinal studies are needed to determine whether anti-CA6 is a marker for early Sjogren’s syndrome. (PMID:29504954)
- Results indicate that carbonic anhydrase VI (CA6) gene polymorphisms influence Streptococcus mutans colonization, tooth biofilm microbiota composition and risk of dental caries in Swedish adolescents. (PMID:30679524)
- Polymorphism in the CAVI gene can affect salivary properties but there is no direct connection with dental caries. (PMID:32013665)
- Taste Changes in Patients with Inflammatory Bowel Disease: Associations with PROP Phenotypes and polymorphisms in the salivary protein, Gustin and CD36 Receptor Genes. (PMID:32033224)
- Investigation of carbonic anhydrase 6 gene polymorphism rs2274327 in relation to the oral health status and salivary composition in type 2 diabetic patients. (PMID:32319846)
- Combined effect of starch and sucrose on carbonic anhydrase VI activity in saliva and biofilm of children with early childhood caries. Exposure to starch and sucrose alters carbonic anhydrase VI activity in saliva and biofilm. (PMID:32918121)
- Associations of the activity and concentration of carbonic anhydrase VI with susceptibility to dental caries: A systematic review and meta-analysis. (PMID:36815304)
- Association between Carbonic Anhydrase VI Gene Copy Number Variations and Dental Caries Experience. (PMID:37011600)
- The gustin gene variation at rs2274333 and PROP taster status affect dietary fat perception: a stepwise multiple regression model study. (PMID:38467201)
- Association of the bitter taste genes TAS2R38 and CA6 and breast cancer risk; a case-control study of Polish women in Poland and Polish immigrants in USA. (PMID:38687739)
- Gene Methylation Affects Salivary Levels of the Taste Buds’ Trophic Factor, Gustin Protein. (PMID:38732551)
- Association between LTF/MMP20/CA6/TAS1R2 polymorphisms and susceptibility to dental caries. (PMID:39212776)
Cross-species orthologs
17 orthologs
| Organism | Symbol | Gene ID |
|---|---|---|
| danio_rerio | ca6 | ENSDARG00000056499 |
| mus_musculus | Car6 | ENSMUSG00000028972 |
| rattus_norvegicus | Car6 | ENSRNOG00000021355 |
| drosophila_melanogaster | CAH13 | FBGN0033542 |
| drosophila_melanogaster | CAH14 | FBGN0034554 |
| drosophila_melanogaster | CAH15 | FBGN0034560 |
| drosophila_melanogaster | CAH7 | FBGN0037788 |
| drosophila_melanogaster | CAH8 | FBGN0038956 |
| drosophila_melanogaster | CAH4 | FBGN0039235 |
| drosophila_melanogaster | CAH9 | FBGN0039486 |
| drosophila_melanogaster | CAH6 | FBGN0039838 |
| drosophila_melanogaster | CAH16 | FBGN0040628 |
| drosophila_melanogaster | CAH5 | FBGN0040629 |
| drosophila_melanogaster | CARPB | FBGN0052698 |
| caenorhabditis_elegans | WBGENE00000279 | |
| caenorhabditis_elegans | WBGENE00000283 | |
| caenorhabditis_elegans | cah-6 | WBGENE00000284 |
Paralogs (14): CA11 (ENSG00000063180), CA12 (ENSG00000074410), CA2 (ENSG00000104267), CA9 (ENSG00000107159), CA14 (ENSG00000118298), CA1 (ENSG00000133742), CA10 (ENSG00000154975), CA3 (ENSG00000164879), CA4 (ENSG00000167434), CA7 (ENSG00000168748), CA5B (ENSG00000169239), CA5A (ENSG00000174990), CA8 (ENSG00000178538), CA13 (ENSG00000185015)
Protein
Protein identifiers
Carbonic anhydrase 6 — P23280 (reviewed: P23280)
Alternative names: Carbonate dehydratase VI, Carbonic anhydrase VI, Salivary carbonic anhydrase, Secreted carbonic anhydrase
All UniProt accessions (3): P23280, F8W148, Q8N4G4
UniProt curated annotations — full annotation on UniProt →
Function. Reversible hydration of carbon dioxide. Its role in saliva is unknown.
Subcellular location. Secreted.
Tissue specificity. Major constituent of saliva.
Activity regulation. Inhibited by coumarins, sulfonamide derivatives such as acetazolamide (AZA), saccharin and Foscarnet (phosphonoformate trisodium salt).
Similarity. Belongs to the alpha-carbonic anhydrase family.
Isoforms (3)
| UniProt ID | Names | Canonical? |
|---|---|---|
| P23280-1 | 1 | yes |
| P23280-2 | 2 | |
| P23280-3 | 3 |
RefSeq proteins (4): NP_001206, NP_001257429, NP_001257430, NP_001257431 (=MANE)
Domains & families (InterPro)
| ID | Name | Type |
|---|---|---|
| IPR001148 | CA_dom | Domain |
| IPR018338 | Carbonic_anhydrase_a-class_CS | Conserved_site |
| IPR023561 | Carbonic_anhydrase_a-class | Family |
| IPR036398 | CA_dom_sf | Homologous_superfamily |
Pfam: PF00194
Enzyme classification (BRENDA):
- EC 4.2.1.1 — carbonic anhydrase (BRENDA: 178 organisms, 196 substrates, 2137 inhibitors, 263 Km, 291 kcat entries)
Substrate kinetics (BRENDA)
9 substrates with measured Km, best-characterized 9. Km ranges are aggregated across organisms/conditions.
| Substrate | Km (mM) | Measurements |
|---|---|---|
| CO2 | 0.012–4700 | 194 |
| 4-NITROPHENYL ACETATE | 0.0024–30.53 | 16 |
| H2CO3 | 0.434–112.7 | 16 |
| HCO3- | 9.3–37 | 4 |
| P-NITROPHENYL ACETATE | 3.86–6.8 | 4 |
| 4-NITROPHENYL PHOSPHATE | 0.935–2.195 | 2 |
| COS | 1.86 | 1 |
| HISTAMINE | 7.9 | 1 |
| CS2 | — | 0 |
Catalyzed reactions (Rhea), 1 shown:
- hydrogencarbonate + H(+) = CO2 + H2O (RHEA:10748)
UniProt features (46 total): strand 15, helix 9, sequence variant 6, binding site 4, sequence conflict 3, splice variant 2, glycosylation site 2, signal peptide 1, chain 1, disulfide bond 1, domain 1, active site 1
Structure
Experimental structures (PDB)
1 structures.
| PDB | Method | Resolution (Å) |
|---|---|---|
| 3FE4 | X-RAY DIFFRACTION | 1.9 |
Predicted structure (AlphaFold)
| Model | pLDDT | Fraction very-high |
|---|---|---|
| AF-P23280-F1 | 89.49 | 0.78 |
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 (1): 85 (proton donor/acceptor)
Ligand- & substrate-binding residues (4): 111; 113; 138; 220–221
Disulfide bonds (1): 42–224
Glycosylation sites (2): 67, 256
Function
Pathways and Gene Ontology
Reactome pathways
2 pathways
| ID | Pathway |
|---|---|
| R-HSA-1475029 | Reversible hydration of carbon dioxide |
| R-HSA-1430728 | Metabolism |
MSigDB gene sets: 97 (showing top):
GOMF_CARBONATE_DEHYDRATASE_ACTIVITY, GOBP_SENSORY_PERCEPTION_OF_CHEMICAL_STIMULUS, GOBP_DETECTION_OF_CHEMICAL_STIMULUS_INVOLVED_IN_SENSORY_PERCEPTION_OF_TASTE, MARTINEZ_RB1_TARGETS_DN, GOBP_SENSORY_PERCEPTION_OF_TASTE, MODULE_294, TGIF_01, MODULE_99, GOBP_DETECTION_OF_STIMULUS, GOBP_SENSORY_PERCEPTION, MARCINIAK_ER_STRESS_RESPONSE_VIA_CHOP, MODULE_295, GOMF_HYDRO_LYASE_ACTIVITY, XU_GH1_EXOGENOUS_TARGETS_DN, MODULE_343
GO Biological Process (1): detection of chemical stimulus involved in sensory perception of bitter taste (GO:0001580)
GO Molecular Function (5): carbonate dehydratase activity (GO:0004089), zinc ion binding (GO:0008270), protein binding (GO:0005515), lyase activity (GO:0016829), metal ion binding (GO:0046872)
GO Cellular Component (5): extracellular region (GO:0005576), obsolete extracellular space (GO:0005615), cytosol (GO:0005829), extracellular exosome (GO:0070062), cytoplasm (GO:0005737)
Reactome top-level categories
Rollup of top-1 pathways:
| Category | Pathways |
|---|---|
| Metabolism | 1 |
GO top-level categories
Rollup of top GO terms by namespace:
| Category | Terms |
|---|---|
| cellular anatomical structure | 3 |
| detection of chemical stimulus involved in sensory perception of taste | 1 |
| sensory perception of bitter taste | 1 |
| hydro-lyase activity | 1 |
| transition metal ion binding | 1 |
| binding | 1 |
| catalytic activity | 1 |
| cation binding | 1 |
| cytoplasm | 1 |
| extracellular vesicle | 1 |
| intracellular anatomical structure | 1 |
Protein interactions and networks
STRING
1362 interactions, top by confidence (×1000):
| Protein A | Protein B | Partner UniProt | Score |
|---|---|---|---|
| CA6 | CHST8 | Q9H2A9 | 875 |
| CA6 | SLC2A5 | P22732 | 863 |
| CA6 | CHST9 | Q7L1S5 | 858 |
| CA6 | CYP24A1 | Q07973 | 806 |
| CA6 | BPIFA2 | Q96DR5 | 770 |
| CA6 | ENO1 | P06733 | 766 |
| CA6 | CST4 | P01036 | 681 |
| CA6 | PIGR | P01833 | 679 |
| CA6 | TAS2R38 | P59533 | 664 |
| CA6 | CHST10 | O43529 | 660 |
| CA6 | MUC7 | Q8TAX7 | 656 |
| CA6 | ALB | P02768 | 591 |
| CA6 | SLC4A4 | Q9Y6R1 | 578 |
| CA6 | AZGP1 | P25311 | 574 |
| CA6 | NKX2-5 | P52952 | 562 |
IntAct
11 interactions, top by confidence:
| A | B | Type | Score |
|---|---|---|---|
| FRMD1 | A2ML1 | psi-mi:“MI:0914”(association) | 0.530 |
| STK11 | A2ML1 | psi-mi:“MI:0914”(association) | 0.350 |
| HBQ1 | IGLL5 | psi-mi:“MI:0914”(association) | 0.350 |
| CA6 | PLXNA2 | psi-mi:“MI:0914”(association) | 0.350 |
| CORO1C | A2ML1 | psi-mi:“MI:0914”(association) | 0.350 |
| TIMM10 | IGLL5 | psi-mi:“MI:0914”(association) | 0.350 |
| CA6 | QSOX1 | psi-mi:“MI:0914”(association) | 0.350 |
| C10orf53 | CST4 | psi-mi:“MI:0914”(association) | 0.350 |
| RSRP1 | A2ML1 | psi-mi:“MI:0914”(association) | 0.350 |
BioGRID (70): KRT31 (Two-hybrid), KRT40 (Two-hybrid), NOTCH2NL (Two-hybrid), CA6 (Affinity Capture-MS), CA6 (Affinity Capture-MS), RHOBTB3 (Affinity Capture-MS), PLXNA3 (Affinity Capture-MS), NPC2 (Affinity Capture-MS), CA6 (Affinity Capture-MS), DDX19B (Affinity Capture-MS), CA6 (Affinity Capture-MS), IMMP1L (Affinity Capture-MS), CA6 (Affinity Capture-MS), PLXNA2 (Affinity Capture-MS), PTCD2 (Affinity Capture-MS)
ESM2 similar proteins: A0A7H0DN92, A0JN41, A7MAQ2, F4HUC4, F4IHR4, F4JIK2, O04846, O43570, O57211, P04195, P08060, P0DO50, P0DSY1, P0DSY2, P10731, P12890, P18761, P18915, P19021, P20508, P23280, P28651, P35219, P48284, P61215, P97467, Q10462, Q18932, Q20781, Q5PPN4, Q5R4U0, Q5TZ24, Q64444, Q68CI2, Q6RZI9, Q75N34, Q75N35, Q84UV8, Q865C0, Q866X6
Diamond homologs: A0ZSF2, A0ZSF3, A0ZSF4, A0ZSF5, A0ZSF6, A0ZSF7, B3A0P2, B3A0Q6, B8V7P3, F4HUC4, O43570, P08060, P18761, P22748, P23280, P23471, P23589, P35218, P43165, P48284, P83299, P84537, Q10462, Q16790, Q27504, Q27908, Q62656, Q84UV8, Q865C0, Q8CI85, Q8UWA5, Q8VHB5, Q92051, Q9ERQ8, Q9FM99, Q9MZ30, Q9NL38, Q9QZA0, Q9Y2D0, P07630
SIGNOR signaling
0 interactions.
Disease & clinical
Clinical variants and AI predictions
ClinVar
66 variants total. Per-class counts are floors (≥ shown; pagination cap):
| Classification | Count (floor) |
|---|---|
| Pathogenic | 2 |
| Likely pathogenic | 1 |
| Uncertain significance | 52 |
| Likely benign | 6 |
| Benign | 2 |
Top pathogenic / likely-pathogenic (3)
| Variant ID | HGVS | Classification |
|---|---|---|
| 565070 | GRCh37/hg19 1p36.23-36.22(chr1:7331314-9427796)x1 | Pathogenic |
| 565071 | GRCh37/hg19 1p36.23-36.22(chr1:7391956-9775929)x1 | Pathogenic |
| 1807831 | GRCh37/hg19 1p36.23-36.22(chr1:8473813-9852687)x1 | Likely pathogenic |
SpliceAI
1222 predictions. Top by Δscore:
| Variant | Effect | Δscore |
|---|---|---|
| 1:8949261:AGAAG:A | acceptor_gain | 1.0000 |
| 1:8949262:GAA:G | acceptor_gain | 1.0000 |
| 1:8949262:GAAGG:G | acceptor_gain | 1.0000 |
| 1:8958904:TTACA:T | acceptor_loss | 1.0000 |
| 1:8958905:TACA:T | acceptor_loss | 1.0000 |
| 1:8958906:ACAGA:A | acceptor_loss | 1.0000 |
| 1:8958907:CA:C | acceptor_loss | 1.0000 |
| 1:8958908:A:AC | acceptor_loss | 1.0000 |
| 1:8958908:A:AG | acceptor_gain | 1.0000 |
| 1:8958909:G:GG | acceptor_gain | 1.0000 |
| 1:8958909:G:GT | acceptor_loss | 1.0000 |
| 1:8959001:AGGT:A | donor_loss | 1.0000 |
| 1:8959002:GGTA:G | donor_loss | 1.0000 |
| 1:8959003:G:GG | donor_gain | 1.0000 |
| 1:8959003:G:T | donor_loss | 1.0000 |
| 1:8959004:T:G | donor_loss | 1.0000 |
| 1:8962581:CTGCA:C | acceptor_loss | 1.0000 |
| 1:8962582:TGCA:T | acceptor_loss | 1.0000 |
| 1:8962583:GCAG:G | acceptor_loss | 1.0000 |
| 1:8962584:CA:C | acceptor_loss | 1.0000 |
| 1:8962585:A:AG | acceptor_gain | 1.0000 |
| 1:8962585:AGG:A | acceptor_loss | 1.0000 |
| 1:8962586:G:GT | acceptor_gain | 1.0000 |
| 1:8962586:GGT:G | acceptor_gain | 1.0000 |
| 1:8962655:AGG:A | donor_loss | 1.0000 |
| 1:8962656:GGTA:G | donor_loss | 1.0000 |
| 1:8962657:G:GA | donor_loss | 1.0000 |
| 1:8962657:G:GG | donor_gain | 1.0000 |
| 1:8962658:T:G | donor_loss | 1.0000 |
| 1:8967652:T:TA | acceptor_gain | 1.0000 |
AlphaMissense
2028 scored. Top likely-pathogenic:
| Variant | Protein change | am_pathogenicity |
|---|---|---|
| 1:8949288:G:C | W35C | 0.998 |
| 1:8949288:G:T | W35C | 0.998 |
| 1:8967759:C:G | C224W | 0.997 |
| 1:8970927:C:A | R264S | 0.997 |
| 1:8957214:C:G | H113D | 0.996 |
| 1:8957219:G:C | W114C | 0.996 |
| 1:8957219:G:T | W114C | 0.996 |
| 1:8967758:G:A | C224Y | 0.996 |
| 1:8949308:G:A | C42Y | 0.995 |
| 1:8949309:T:G | C42W | 0.995 |
| 1:8949329:C:A | P49H | 0.995 |
| 1:8949429:C:A | N82K | 0.995 |
| 1:8949429:C:G | N82K | 0.995 |
| 1:8967737:G:T | G217V | 0.995 |
| 1:8967757:T:A | C224S | 0.995 |
| 1:8967757:T:C | C224R | 0.995 |
| 1:8967758:G:C | C224S | 0.995 |
| 1:8967775:T:A | W230R | 0.995 |
| 1:8967775:T:C | W230R | 0.995 |
| 1:8970953:A:C | R272S | 0.995 |
| 1:8970953:A:T | R272S | 0.995 |
| 1:8949286:T:A | W35R | 0.994 |
| 1:8949286:T:C | W35R | 0.994 |
| 1:8957217:T:A | W114R | 0.994 |
| 1:8957217:T:C | W114R | 0.994 |
| 1:8957251:A:T | E125V | 0.994 |
| 1:8967739:T:C | S218P | 0.994 |
| 1:8967743:T:C | L219P | 0.994 |
| 1:8957252:G:C | E125D | 0.993 |
| 1:8957252:G:T | E125D | 0.993 |
dbSNP variants (sampled 300 via entrez): RS1000049368 (1:8973268 C>T), RS1000082108 (1:8956902 C>T), RS1000176600 (1:8972208 C>T), RS1000271047 (1:8963128 G>A), RS1000305566 (1:8951310 G>A), RS1000448919 (1:8969870 A>C), RS1000460832 (1:8961977 C>T), RS1000585051 (1:8956026 C>T), RS1000659538 (1:8974787 A>G,T), RS1000702559 (1:8945590 C>T), RS1000708157 (1:8962827 T>C), RS1000777549 (1:8974944 T>C), RS1001296897 (1:8956597 C>T), RS1001328638 (1:8947350 C>T), RS1001369006 (1:8947987 G>A)
Disease associations
OMIM: gene MIM:114780 | disease phenotypes:
GenCC curated gene-disease
Mondo (0):
Orphanet (0):
HPO phenotypes
0 total (0 of 0 shown, HPO-id order):
GWAS associations
3 associations (top):
| Study | Trait | p-value |
|---|---|---|
| GCST003262_875 | Post bronchodilator FEV1 | 4.000000e-06 |
| GCST006585_1479 | Blood protein levels | 2.000000e-106 |
| GCST006585_30 | Blood protein levels | 9.000000e-113 |
EFO canonical traits (1, from GWAS)
| EFO ID | Trait name |
|---|---|
| EFO:0004314 | forced expiratory volume |
Drugs & pharmacology
Drug and pharmacology data
Is drug target: yes
ChEMBL targets (2): CHEMBL2095180 (PROTEIN FAMILY), CHEMBL3025 (SINGLE PROTEIN)
Molecules with ChEMBL bioactivity
47 molecules (phase ≥1), by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 788,151 (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 |
|---|---|---|---|
| CHEMBL19 | METHAZOLAMIDE | 4 | 65 |
| CHEMBL20 | ACETAZOLAMIDE | 4 | 28,768 |
| CHEMBL750 | ZONISAMIDE | 4 | 16,649 |
| CHEMBL1054 | TRICHLORMETHIAZIDE | 4 | 11,619 |
| CHEMBL1055 | CHLORTHALIDONE | 4 | 20,442 |
| CHEMBL118 | CELECOXIB | 4 | 112,844 |
| CHEMBL1200471 | PYRITHIONE ZINC | 4 | 24,834 |
| CHEMBL1286 | LEVETIRACETAM | 4 | 13,997 |
| CHEMBL17 | DICHLORPHENAMIDE | 4 | 9,022 |
| CHEMBL18 | ETHOXZOLAMIDE | 4 | 3,042 |
| CHEMBL21 | SULFANILAMIDE | 4 | 153,075 |
| CHEMBL2105581 | VERALIPRIDE | 4 | 1,165 |
| CHEMBL218490 | DORZOLAMIDE | 4 | 10,216 |
| CHEMBL220491 | BRINZOLAMIDE | 4 | 8,355 |
| CHEMBL220492 | TOPIRAMATE | 4 | 35,160 |
| CHEMBL255863 | NILOTINIB | 4 | 38,627 |
| CHEMBL26 | SULPIRIDE | 4 | 58,543 |
| CHEMBL325041 | BORTEZOMIB | 4 | 13,120 |
| CHEMBL328560 | SULTHIAME | 4 | 4,563 |
| CHEMBL35 | FUROSEMIDE | 4 | 224,045 |
| CHEMBL406 | INDAPAMIDE | 4 | |
| CHEMBL419 | MAFENIDE | 4 | |
| CHEMBL424 | SALICYLIC ACID | 4 | |
| CHEMBL506247 | TANNIC ACID | 4 | |
| CHEMBL58323 | LACOSAMIDE | 4 | |
| CHEMBL609 | TRIENTINE | 4 | |
| CHEMBL6466 | COUMARIN | 4 | |
| CHEMBL865 | VALDECOXIB | 4 | |
| CHEMBL902 | FAMOTIDINE | 4 | |
| CHEMBL926 | DOBUTAMINE | 4 |
PharmGKB: 1 entry (VIP=true, CPIC=false)
Binding affinities (BindingDB)
71 measured of 109 human assays (156 total across all organisms); most potent 50 below. Values come from heterogeneous assays and are not directly comparable.
| Ligand | Measure | Value |
|---|---|---|
| 3-(butylamino)-4-phenoxy-5-sulfamoylbenzoic acid | EC50 | 0.0469 nM |
| aliphatic sulfamate, 1 | KI | 3.7 nM |
| 2-(hydrazinecarbonyl)-3-(2-methylphenyl)-1H-indole-5-sulfonamide | KI | 107 nM |
| 3-(2-bromophenyl)-2-(hydrazinecarbonyl)-1H-indole-5-sulfonamide | KI | 110 nM |
| Topiramate, 3 | KI | 250 nM |
| 6-oxo-6,7,8,9,10,11-hexahydrocyclohepta[c]chromen-3-yl sulfamate | IC50 | 300 nM |
| JFD00715 | KI | 328 nM |
| trichloromethiazide, 6 | KI | 345 nM |
| bis-sulfamate, 3 | KI | 378 nM |
| N-(p-sulfamoylphenyl)-alpha-glycopyranosylamine, 7 | KI | 510 nM |
| aliphatic sulfamate, 2 | KI | 530 nM |
| 3-(2-fluorophenyl)-2-(hydrazinecarbonyl)-1H-indole-5-sulfonamide | KI | 621 nM |
| N-(p-sulfamoylphenyl)-alpha-glycopyranosylamine, 6 | KI | 630 nM |
| Investigational agent, 5 | KI | 810 nM |
| Investigational agent, 4 | KI | 850 nM |
| bis-sulfamate, 4 | KI | 890 nM |
| N-(p-sulfamoylphenyl)-alpha-glycopyranosylamine, 2 | KI | 1000 nM |
| 4-Methyl-N-(4-nitrophenyl) benzenesulfonamide (11) | IC50 | 1130 nM |
| N-(4-cyanophenyl)-4-methylbenzenesulfonamide (10) | IC50 | 1480 nM |
| 1,3,4-Thiadiazole-2-sulfonamide, 6 | IC50 | 2700 nM |
| BMCL182567 Compound 6b | KI | 2840 nM |
| [2-(cycloheptylmethyl)-1,1-dioxo–benzothiophen-6-yl] sulfamate | KI | 3600 nM |
| 4-Methyl-N-(2-nitrophenyl) benzenesulfonamide (7) | IC50 | 5380 nM |
| Carbonic anhydrase inhibitors (CAIs), 5 | KI | 5480 nM |
| Carbonic anhydrase inhibitors (CAIs), 6 | KI | 9340 nM |
| salicylic acid | KI | 9900 nM |
| 4-chloro-N-(2-methyl-2,3-dihydro-1H-indol-1-yl)-3-sulfamoylbenzamide | KD | 10000 nM |
| phenol | KI | 10200 nM |
| hCA inhibitor, 1 | KI | 13700 nM |
| Bis(3,4-dihydroxyphenyl)methanone | KI | 18000 nM |
| N-(2-cyanophenyl)-4-methylbenzenesulfonamide (6) | IC50 | 18200 nM |
| hCA inhibitor, 5 | KI | 18400 nM |
| Carbonic anhydrase inhibitors (CAIs), 7 | KI | 21700 nM |
| 4-methylbenzene-1-sulfonamide | IC50 | 22100 nM |
| hCA inhibitor, 5 | KI | 24300 nM |
| hCA inhibitor, 6 | KI | 25300 nM |
| 2-sulfanilamidopyrimidine | IC50 | 26200 nM |
| 4-Amino-N-(pyrimidin-2-yl) benzenesulfonamide (Sulfadiazine) (14) | IC50 | 28400 nM |
| TETRABROMOCATECHOL | KI | 32100 nM |
| 9(R(S))-Hydroxy-1,2,3,4-tetrahydro-1,4-methanonaphthalen-2(R(S))-yl sulfate (8) | KI | 32700 nM |
| hCA inhibitor, 2 | KI | 37200 nM |
| 3,5-difluorophenol | KI | 38800 nM |
| trans-(1R(S),6R(S))-6-Hydroxycyclohex-3-enyl hydrogen sulfate (4) | KI | 41300 nM |
| Brinzolamide, BRZ | KI | 45000 nM |
| hCA inhibitor, 3 | KI | 48100 nM |
| Dorzolamide, DZA | KI | 50000 nM |
| Carbonic anhydrase inhibitors (CAIs), 1 | IC50 | 50000 nM |
| 7-chloro-2-methyl-3-(2-methylphenyl)-4-oxo-1,2,3,4-tetrahydroquinazoline-6-sulfonamide | KI | 54000 nM |
| Carbonic anhydrase inhibitors (CAIs), 3 | KI | 70200 nM |
| hCA inhibitor, 4 | KI | 71200 nM |
ChEMBL bioactivities
720 potent at pChembl≥5 of 792 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).
PubChem BioAssay actives
844 with measured affinity, of 1307 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 |
|---|---|---|---|---|
| 1-(4-chlorosulfonyl-3,5-dimethylphenyl)-5-oxopyrrolidine-3-carboxylic acid | 1763398: Inhibition of human recombinant CA6 assessed as intrinsic dissociation constant by thermal shift assay | kd | <0.0001 | uM |
| methyl 5-oxo-1-(4-sulfamoylphenyl)pyrrolidine-3-carboxylate | 1515320: Binding affinity to recombinant human CA6 assessed as intrinsic dissociation constant by DSF-based fluorescence thermal shift assay | kd | <0.0001 | uM |
| 1-(2-chloro-3,5-dimethyl-4-sulfamoylphenyl)-N-[(E)-(4-methoxyphenyl)methylideneamino]-5-oxopyrrolidine-3-carboxamide | 1515320: Binding affinity to recombinant human CA6 assessed as intrinsic dissociation constant by DSF-based fluorescence thermal shift assay | kd | 0.0001 | uM |
| N-[(E)-benzylideneamino]-5-oxo-1-(4-sulfamoylphenyl)pyrrolidine-3-carboxamide | 1515320: Binding affinity to recombinant human CA6 assessed as intrinsic dissociation constant by DSF-based fluorescence thermal shift assay | kd | 0.0001 | uM |
| N-[(E)-(4-bromophenyl)methylideneamino]-1-(2-chloro-3,5-dimethyl-4-sulfamoylphenyl)-5-oxopyrrolidine-3-carboxamide | 1515320: Binding affinity to recombinant human CA6 assessed as intrinsic dissociation constant by DSF-based fluorescence thermal shift assay | kd | 0.0001 | uM |
| 4-(2-chloro-3,5-dimethyl-4-sulfamoylanilino)-3-(4-phenyl-5-sulfanylidene-1H-1,2,4-triazol-3-yl)butanoic acid | 1515320: Binding affinity to recombinant human CA6 assessed as intrinsic dissociation constant by DSF-based fluorescence thermal shift assay | kd | 0.0001 | uM |
| 1-(2-chloro-3,5-dimethyl-4-sulfamoylphenyl)-N-[(E)-(4-nitrophenyl)methylideneamino]-5-oxopyrrolidine-3-carboxamide | 1515320: Binding affinity to recombinant human CA6 assessed as intrinsic dissociation constant by DSF-based fluorescence thermal shift assay | kd | 0.0001 | uM |
| 1-(3,5-dimethyl-4-sulfamoylphenyl)-N-[(E)-(4-nitrophenyl)methylideneamino]-5-oxopyrrolidine-3-carboxamide | 1515320: Binding affinity to recombinant human CA6 assessed as intrinsic dissociation constant by DSF-based fluorescence thermal shift assay | kd | 0.0001 | uM |
| 1-(2-chloro-3,5-dimethyl-4-sulfamoylphenyl)-N-[(E)-(4-chlorophenyl)methylideneamino]-5-oxopyrrolidine-3-carboxamide | 1515320: Binding affinity to recombinant human CA6 assessed as intrinsic dissociation constant by DSF-based fluorescence thermal shift assay | kd | 0.0001 | uM |
| sulfamic acid | 552129: Inhibition of human recombinant CA6 by stopped-flow CO2 hydration assay | ki | 0.0001 | uM |
| sulfamide | 552129: Inhibition of human recombinant CA6 by stopped-flow CO2 hydration assay | ki | 0.0001 | uM |
| N-benzyl-2,4-dichloro-5-sulfamoylbenzamide | 1361387: Binding affinity to recombinant N-terminal His6-tagged human carbonic anhydrase 6 (21 to 290 residues) expressed in Escherichia coli Rosetta 2 (DE3) strain assessed as intrinsic Kd in presence of ANS by fluorescent thermal shift assay | kd | 0.0002 | uM |
| N-benzyl-2-(benzylamino)-4-chloro-5-sulfamoylbenzamide | 1361387: Binding affinity to recombinant N-terminal His6-tagged human carbonic anhydrase 6 (21 to 290 residues) expressed in Escherichia coli Rosetta 2 (DE3) strain assessed as intrinsic Kd in presence of ANS by fluorescent thermal shift assay | kd | 0.0002 | uM |
| N-benzyl-4-chloro-2-phenylsulfanyl-5-sulfamoylbenzamide | 1520085: Binding affinity to recombinant human carbonic anhydrase 6 expressed in Escherichia coli expression system assessed as kinetic dissociation constant fluorescent thermal shift assay | kd | 0.0002 | uM |
| N-benzyl-4-chloro-2-cyclohexylsulfanyl-5-sulfamoylbenzamide | 1520085: Binding affinity to recombinant human carbonic anhydrase 6 expressed in Escherichia coli expression system assessed as kinetic dissociation constant fluorescent thermal shift assay | kd | 0.0002 | uM |
| 4-[1-[(2R)-1-(3-azabicyclo[3.2.2]nonan-3-yl)-3-methyl-1-oxobutan-2-yl]triazol-4-yl]benzenesulfonamide | 1557414: Inhibition of carbonic anhydrase (unknown origin) | ki | 0.0002 | uM |
| 1-(3-bromophenyl)-5-oxo-N-(4-sulfamoylphenyl)pyrrolidine-3-carboxamide | 1515320: Binding affinity to recombinant human CA6 assessed as intrinsic dissociation constant by DSF-based fluorescence thermal shift assay | kd | 0.0002 | uM |
| N-[(E)-benzylideneamino]-1-(2-chloro-3,5-dimethyl-4-sulfamoylphenyl)-5-oxopyrrolidine-3-carboxamide | 1515320: Binding affinity to recombinant human CA6 assessed as intrinsic dissociation constant by DSF-based fluorescence thermal shift assay | kd | 0.0002 | uM |
| (2R)-3-phenyl-2-[4-(4-sulfamoylphenyl)triazol-1-yl]-N-(2-thiophen-3-ylethyl)propanamide | 1557414: Inhibition of carbonic anhydrase (unknown origin) | ki | 0.0002 | uM |
| 1-(3,5-dimethyl-4-sulfamoylphenyl)-N-[(E)-(4-methoxyphenyl)methylideneamino]-5-oxopyrrolidine-3-carboxamide | 1515320: Binding affinity to recombinant human CA6 assessed as intrinsic dissociation constant by DSF-based fluorescence thermal shift assay | kd | 0.0002 | uM |
| N-[(E)-(4-chlorophenyl)methylideneamino]-1-(3,5-dimethyl-4-sulfamoylphenyl)-5-oxopyrrolidine-3-carboxamide | 1515320: Binding affinity to recombinant human CA6 assessed as intrinsic dissociation constant by DSF-based fluorescence thermal shift assay | kd | 0.0002 | uM |
| 4-nitrobenzenesulfonamide | 50173: Compound was evaluated for the inhibition of Carbonic anhydrase | ki | 0.0002 | uM |
| N-butyl-2,4-dichloro-5-sulfamoylbenzamide | 1520085: Binding affinity to recombinant human carbonic anhydrase 6 expressed in Escherichia coli expression system assessed as kinetic dissociation constant fluorescent thermal shift assay | kd | 0.0002 | uM |
| (2R)-N-benzyl-3-methyl-2-[4-(4-sulfamoylphenyl)triazol-1-yl]butanamide | 1557414: Inhibition of carbonic anhydrase (unknown origin) | ki | 0.0002 | uM |
| 2-benzylsulfanyl-N-butyl-4-chloro-5-sulfamoylbenzamide | 1520085: Binding affinity to recombinant human carbonic anhydrase 6 expressed in Escherichia coli expression system assessed as kinetic dissociation constant fluorescent thermal shift assay | kd | 0.0003 | uM |
| N-butyl-4-chloro-2-phenylsulfanyl-5-sulfamoylbenzamide | 1520085: Binding affinity to recombinant human carbonic anhydrase 6 expressed in Escherichia coli expression system assessed as kinetic dissociation constant fluorescent thermal shift assay | kd | 0.0003 | uM |
| N-butyl-4-chloro-2-(2-phenylethylsulfanyl)-5-sulfamoylbenzamide | 1520085: Binding affinity to recombinant human carbonic anhydrase 6 expressed in Escherichia coli expression system assessed as kinetic dissociation constant fluorescent thermal shift assay | kd | 0.0003 | uM |
| 2,4-dibromo-N-butyl-5-sulfamoylbenzamide | 1361387: Binding affinity to recombinant N-terminal His6-tagged human carbonic anhydrase 6 (21 to 290 residues) expressed in Escherichia coli Rosetta 2 (DE3) strain assessed as intrinsic Kd in presence of ANS by fluorescent thermal shift assay | kd | 0.0003 | uM |
| N-[(E)-(4-bromophenyl)methylideneamino]-1-(3,5-dimethyl-4-sulfamoylphenyl)-5-oxopyrrolidine-3-carboxamide | 1515320: Binding affinity to recombinant human CA6 assessed as intrinsic dissociation constant by DSF-based fluorescence thermal shift assay | kd | 0.0003 | uM |
| 1-[[1-(2-chloro-3,5-dimethyl-4-sulfamoylphenyl)-5-oxopyrrolidine-3-carbonyl]amino]-3-phenylthiourea | 1515320: Binding affinity to recombinant human CA6 assessed as intrinsic dissociation constant by DSF-based fluorescence thermal shift assay | kd | 0.0003 | uM |
| 3-chloro-2,6-dimethyl-4-[2-oxo-4-(4-phenyl-5-sulfanylidene-1H-1,2,4-triazol-3-yl)pyrrolidin-1-yl]benzenesulfonamide | 1515320: Binding affinity to recombinant human CA6 assessed as intrinsic dissociation constant by DSF-based fluorescence thermal shift assay | kd | 0.0003 | uM |
| 1-(2-bromophenyl)-5-oxo-N-(4-sulfamoylphenyl)pyrrolidine-3-carboxamide | 1515320: Binding affinity to recombinant human CA6 assessed as intrinsic dissociation constant by DSF-based fluorescence thermal shift assay | kd | 0.0003 | uM |
| 5-oxo-1-phenyl-N-(4-sulfamoylphenyl)pyrrolidine-3-carboxamide | 1515320: Binding affinity to recombinant human CA6 assessed as intrinsic dissociation constant by DSF-based fluorescence thermal shift assay | kd | 0.0003 | uM |
| 4-chlorobenzenesulfonamide | 50173: Compound was evaluated for the inhibition of Carbonic anhydrase | ki | 0.0003 | uM |
| 2-benzylsulfanyl-4-bromo-N-butyl-5-sulfamoylbenzamide | 1520085: Binding affinity to recombinant human carbonic anhydrase 6 expressed in Escherichia coli expression system assessed as kinetic dissociation constant fluorescent thermal shift assay | kd | 0.0004 | uM |
| 2-(benzenesulfonyl)-N-benzyl-4-chloro-5-sulfamoylbenzamide | 1520085: Binding affinity to recombinant human carbonic anhydrase 6 expressed in Escherichia coli expression system assessed as kinetic dissociation constant fluorescent thermal shift assay | kd | 0.0004 | uM |
| 2-(benzylamino)-4-chloro-N-(2-methoxyethyl)-5-sulfamoylbenzamide | 1361387: Binding affinity to recombinant N-terminal His6-tagged human carbonic anhydrase 6 (21 to 290 residues) expressed in Escherichia coli Rosetta 2 (DE3) strain assessed as intrinsic Kd in presence of ANS by fluorescent thermal shift assay | kd | 0.0004 | uM |
| 2-(benzylamino)-4-chloro-N-(2-hydroxyethyl)-5-sulfamoylbenzamide | 1361387: Binding affinity to recombinant N-terminal His6-tagged human carbonic anhydrase 6 (21 to 290 residues) expressed in Escherichia coli Rosetta 2 (DE3) strain assessed as intrinsic Kd in presence of ANS by fluorescent thermal shift assay | kd | 0.0004 | uM |
| N-butyl-4-chloro-2-cyclohexylsulfanyl-5-sulfamoylbenzamide | 1520085: Binding affinity to recombinant human carbonic anhydrase 6 expressed in Escherichia coli expression system assessed as kinetic dissociation constant fluorescent thermal shift assay | kd | 0.0004 | uM |
| 1-(3,5-dimethyl-4-sulfamoylphenyl)-5-oxopyrrolidine-3-carboxylic acid | 1515320: Binding affinity to recombinant human CA6 assessed as intrinsic dissociation constant by DSF-based fluorescence thermal shift assay | kd | 0.0004 | uM |
| N-(3,5-dimethylpyrazol-1-yl)-1-(3,5-dimethyl-4-sulfamoylphenyl)-5-oxopyrrolidine-3-carboxamide | 1515320: Binding affinity to recombinant human CA6 assessed as intrinsic dissociation constant by DSF-based fluorescence thermal shift assay | kd | 0.0004 | uM |
| 3-chloro-2,6-dimethyl-4-[2-oxo-4-(2-sulfanylidene-3H-1,3,4-oxadiazol-5-yl)pyrrolidin-1-yl]benzenesulfonamide | 1515320: Binding affinity to recombinant human CA6 assessed as intrinsic dissociation constant by DSF-based fluorescence thermal shift assay | kd | 0.0004 | uM |
| 1-(2-chloro-3,5-dimethyl-4-sulfamoylphenyl)-N-(3,5-dimethylpyrazol-1-yl)-5-oxopyrrolidine-3-carboxamide | 1515320: Binding affinity to recombinant human CA6 assessed as intrinsic dissociation constant by DSF-based fluorescence thermal shift assay | kd | 0.0004 | uM |
| N-[(E)-benzylideneamino]-1-(3,5-dimethyl-4-sulfamoylphenyl)-5-oxopyrrolidine-3-carboxamide | 1515320: Binding affinity to recombinant human CA6 assessed as intrinsic dissociation constant by DSF-based fluorescence thermal shift assay | kd | 0.0004 | uM |
| 3-chloro-4-[4-(3,5-dimethylpyrazole-1-carbonyl)-2-oxopyrrolidin-1-yl]-2,6-dimethylbenzenesulfonamide | 1515320: Binding affinity to recombinant human CA6 assessed as intrinsic dissociation constant by DSF-based fluorescence thermal shift assay | kd | 0.0004 | uM |
| 4-[4-(3,5-dimethylpyrazole-1-carbonyl)-2-oxopyrrolidin-1-yl]-2,6-dimethylbenzenesulfonamide | 1515320: Binding affinity to recombinant human CA6 assessed as intrinsic dissociation constant by DSF-based fluorescence thermal shift assay | kd | 0.0004 | uM |
| 5-oxo-1-(4-sulfamoylphenyl)pyrrolidine-3-carboxylic acid | 1515320: Binding affinity to recombinant human CA6 assessed as intrinsic dissociation constant by DSF-based fluorescence thermal shift assay | kd | 0.0004 | uM |
| N-benzyl-4-chloro-2-cyclohexylsulfonyl-5-sulfamoylbenzamide | 1520085: Binding affinity to recombinant human carbonic anhydrase 6 expressed in Escherichia coli expression system assessed as kinetic dissociation constant fluorescent thermal shift assay | kd | 0.0005 | uM |
| 3-chloro-4-[4-(hydrazinecarbonyl)-2-oxopyrrolidin-1-yl]-2,6-dimethylbenzenesulfonamide | 1515320: Binding affinity to recombinant human CA6 assessed as intrinsic dissociation constant by DSF-based fluorescence thermal shift assay | kd | 0.0005 | uM |
| methyl 1-(2-chloro-3,5-dimethyl-4-sulfamoylphenyl)-5-oxopyrrolidine-3-carboxylate | 1515320: Binding affinity to recombinant human CA6 assessed as intrinsic dissociation constant by DSF-based fluorescence thermal shift assay | kd | 0.0005 | uM |
CTD chemical–gene interactions
15 total (human), top 15 by PubMed support.
| Chemical | Actions (top 5) | PubMed papers |
|---|---|---|
| oryzalin | affects binding, decreases activity | 1 |
| perfluorooctanoic acid | increases expression | 1 |
| 1-nitropyrene | decreases expression | 1 |
| perfluorooctane sulfonic acid | increases expression | 1 |
| 2-palmitoylglycerol | increases expression | 1 |
| perfluorohexanesulfonic acid | increases expression | 1 |
| (+)-JQ1 compound | decreases expression | 1 |
| Acetazolamide | affects binding, decreases activity | 1 |
| Arsenic | affects expression | 1 |
| Carmustine | decreases expression | 1 |
| Nickel | decreases expression | 1 |
| Propylthiouracil | affects response to substance | 1 |
| Tretinoin | increases expression | 1 |
| Famotidine | affects binding, decreases activity | 1 |
| Aflatoxin B1 | increases methylation | 1 |
ChEMBL screening assays
107 unique, capped per target: 105 binding, 2 admet
Representative assays (with source publication via chembl_document):
| Assay ID | Type | Description | Source paper |
|---|---|---|---|
| CHEMBL3386760 | Binding | Inhibition of carbonic anhydrase (unknown origin) | Substituted thieno[2,3-b]thiophenes and related congeners: Synthesis, β-glucuronidase inhibition activity, crystal structure, and POM analyses. — Bioorg Med Chem |
| CHEMBL4187337 | ADMET | Binding affinity to recombinant human N-terminal His6-tagged carbonic anhydrase 6 expressed in Escherichia coli BL21 (DE3) in presence of ANS by fluorescent thermal shift assay | Benzimidazole design, synthesis, and docking to build selective carbonic anhydrase VA inhibitors. — Bioorg Med Chem |
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.