CA3
gene geneOn this page
Also known as Car3CAIII
Summary
CA3 (carbonic anhydrase 3, HGNC:1374) is a protein-coding gene on chromosome 8q21.2, encoding Carbonic anhydrase 3 (P07451). Reversible hydration of carbon dioxide.
Carbonic anhydrase III (CAIII) is a member of a multigene family (at least six separate genes are known) that encodes carbonic anhydrase isozymes. These carbonic anhydrases are a class of metalloenzymes that catalyze the reversible hydration of carbon dioxide and are differentially expressed in a number of cell types. The expression of the CA3 gene is strictly tissue specific and present at high levels in skeletal muscle and much lower levels in cardiac and smooth muscle. A proportion of carriers of Duchenne muscle dystrophy have a higher CA3 level than normal. The gene spans 10.3 kb and contains seven exons and six introns.
Source: NCBI Gene 761 — RefSeq curated summary.
At a glance
- GWAS associations: 5
- Clinical variants (ClinVar): 25 total
- Druggable target: yes — 34 molecules with ChEMBL bioactivity
- MANE Select transcript:
NM_005181
Identifiers
Gene identifiers
| Field | Value |
|---|---|
| HGNC ID | HGNC:1374 |
| Approved symbol | CA3 |
| Name | carbonic anhydrase 3 |
| Location | 8q21.2 |
| Locus type | gene with protein product |
| Status | Approved |
| Aliases | Car3, CAIII |
| Ensembl gene | ENSG00000164879 |
| Ensembl biotype | protein_coding |
| OMIM | 114750 |
| Entrez | 761 |
Gene structure
Transcript identifiers
Ensembl transcripts: 5 — 4 protein_coding, 1 retained_intron
ENST00000285381, ENST00000520921, ENST00000522207, ENST00000967721, ENST00000967722
RefSeq mRNA: 1 — MANE Select: NM_005181
NM_005181
CCDS: CCDS6238
Canonical transcript exons
ENST00000285381 — 7 exons
| Exon | Start | End |
|---|---|---|
| ENSE00001018977 | 85444034 | 85444126 |
| ENSE00001018985 | 85448034 | 85449040 |
| ENSE00001018987 | 85442073 | 85442191 |
| ENSE00001018988 | 85446142 | 85446297 |
| ENSE00001018993 | 85445156 | 85445218 |
| ENSE00001725111 | 85438859 | 85438943 |
| ENSE00003507901 | 85439712 | 85439909 |
Expression profiles
Bgee: expression breadth ubiquitous, 216 present calls, max score 99.89.
FANTOM5 (CAGE): breadth broad, TPM avg 11.0631 / max 2928.8440, expressed in 244 samples.
FANTOM5 promoters (1 alternative TSS)
| Promoter ID | TPM avg | Samples expressed |
|---|---|---|
| 89613 | 11.0631 | 244 |
Top tissues by expression
291 total, by Bgee expression score (0-100, higher = more expressed):
| Tissue | Anatomy ID | Expression score | Quality |
|---|---|---|---|
| skeletal muscle tissue of rectus abdominis | UBERON:0004511 | 99.89 | gold quality |
| hindlimb stylopod muscle | UBERON:0004252 | 99.83 | gold quality |
| vastus lateralis | UBERON:0001379 | 99.69 | gold quality |
| biceps brachii | UBERON:0001507 | 99.64 | gold quality |
| skeletal muscle tissue of biceps brachii | UBERON:0004502 | 99.59 | gold quality |
| quadriceps femoris | UBERON:0001377 | 99.55 | gold quality |
| diaphragm | UBERON:0001103 | 99.40 | gold quality |
| skeletal muscle tissue | UBERON:0001134 | 99.35 | gold quality |
| gastrocnemius | UBERON:0001388 | 99.34 | gold quality |
| gluteal muscle | UBERON:0002000 | 99.31 | gold quality |
| triceps brachii | UBERON:0001509 | 99.24 | gold quality |
| muscle organ | UBERON:0001630 | 98.59 | gold quality |
| skeletal muscle organ | UBERON:0014892 | 98.59 | gold quality |
| body of tongue | UBERON:0011876 | 98.33 | gold quality |
| muscle of leg | UBERON:0001383 | 98.23 | gold quality |
| deltoid | UBERON:0001476 | 98.18 | gold quality |
| tibialis anterior | UBERON:0001385 | 96.40 | gold quality |
| right lung | UBERON:0002167 | 95.46 | gold quality |
| muscle tissue | UBERON:0002385 | 93.52 | gold quality |
| tongue | UBERON:0001723 | 90.13 | gold quality |
| mucosa of stomach | UBERON:0001199 | 86.33 | gold quality |
| upper lobe of left lung | UBERON:0008952 | 86.09 | gold quality |
| upper lobe of lung | UBERON:0008948 | 85.70 | gold quality |
| trabecular bone tissue | UBERON:0002483 | 85.69 | gold quality |
| superior surface of tongue | UBERON:0007371 | 82.62 | gold quality |
| primordial germ cell in gonad | CL:0000670 ∩ UBERON:0000991 | 82.11 | gold quality |
| left uterine tube | UBERON:0001303 | 81.92 | gold quality |
| lower lobe of lung | UBERON:0008949 | 81.74 | gold quality |
| minor salivary gland | UBERON:0001830 | 80.65 | gold quality |
| adipose tissue of abdominal region | UBERON:0007808 | 78.65 | gold quality |
Single-cell (SCXA)
Detected in 1 experiment(s), a significant marker in 1.
| Experiment | Marker? | Max mean expression |
|---|---|---|
| E-ANND-3 | no | 0.00 |
Regulation
Is transcription factor: no
Upstream regulators (CollecTRI, top): AHR, AR, MECOM
miRNA regulators (miRDB)
59 targeting CA3, 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-3646 | 100.00 | 73.56 | 5283 |
| HSA-MIR-29A-3P | 100.00 | 73.11 | 1835 |
| HSA-MIR-29B-3P | 100.00 | 73.18 | 1833 |
| HSA-MIR-29C-3P | 100.00 | 73.15 | 1833 |
| HSA-MIR-200B-3P | 100.00 | 73.31 | 2693 |
| HSA-MIR-200C-3P | 100.00 | 73.35 | 2685 |
| HSA-MIR-429 | 100.00 | 73.44 | 2698 |
| HSA-MIR-3185 | 99.99 | 68.12 | 1959 |
| HSA-MIR-4778-3P | 99.93 | 70.40 | 1818 |
| HSA-MIR-7978 | 99.86 | 66.90 | 856 |
| HSA-MIR-3663-3P | 99.84 | 70.39 | 798 |
| HSA-MIR-5010-3P | 99.83 | 70.60 | 2357 |
| HSA-MIR-4307 | 99.82 | 70.45 | 3374 |
| HSA-MIR-4659A-3P | 99.80 | 72.62 | 4248 |
| HSA-MIR-4659B-3P | 99.80 | 72.62 | 4248 |
| HSA-MIR-8084 | 99.73 | 69.57 | 1760 |
| HSA-MIR-1200 | 99.71 | 70.42 | 1838 |
| HSA-MIR-518A-5P | 99.70 | 69.01 | 2209 |
| HSA-MIR-527 | 99.70 | 69.01 | 2209 |
| HSA-MIR-4729 | 99.69 | 72.18 | 4233 |
| HSA-MIR-378A-5P | 99.65 | 66.33 | 1311 |
| HSA-MIR-6512-3P | 99.65 | 66.07 | 1468 |
| HSA-MIR-6720-5P | 99.65 | 66.22 | 1459 |
| HSA-MIR-6073 | 99.60 | 70.36 | 793 |
| HSA-MIR-510-3P | 99.54 | 70.06 | 2965 |
| HSA-MIR-7159-5P | 99.53 | 72.12 | 2472 |
| HSA-MIR-6833-5P | 99.50 | 68.93 | 1161 |
| HSA-MIR-3140-5P | 99.39 | 69.04 | 1136 |
| HSA-MIR-3911 | 99.38 | 66.95 | 1087 |
| HSA-MIR-6505-3P | 99.34 | 67.39 | 1071 |
Literature-anchored findings (GeneRIF, showing 16)
- Crystallization and preliminary X-ray analysis of human carbonic anhydrase III (PMID:11976500)
- Data show that inserting histidine residues into the active site cavity of carbonic anhydrase II or III results in rates of proton transfer to the zinc-bound hydroxide that are antagonistic or suppressive with respect to the corresponding single mutants. (PMID:12171926)
- Proton transfer within the active-site cavity of carbonic anhydrase III (PMID:12484342)
- myoglobin/carbonic anhydrase III ratio in the blood proved to be a more specific indicator for myocardial damage than myoglobin alone after myocardial infarction. (PMID:12745799)
- CAIII expression is upregulated in kidney cortex samples from the end-stage kidney of a patient with Dent’s disease owing to the G506E mutation of CLCN5 (PMID:18322545)
- CAIII promotes transformation and invasion capability in hepatoma cells through FAK signaling pathway. (PMID:18444244)
- The level of CAIII is specifically insufficient in the skeletal muscle of myasthenia gravis patients. (PMID:19301202)
- The carbonic anhydrase CA3 isoform displayed an increased abundance during muscle aging, which was independently verified by immunoblotting of differently aged human skeletal muscle samples. (PMID:22797148)
- The generation of CA III and IV autoantibodies, antioxidant enzymes, and cytokines might influence each other. (PMID:23049597)
- Report that anti-CAIII antibodies may be useful for diagnosing microscopic polyangiitis. (PMID:23981757)
- this study detected the formation and colocalization of 6-nitrotryptophan-containing proteins and CAIII in the skin of atopic dermatitis patients, not only in the lesional part but also in the nonlesional part, through histochemical analyses (PMID:24838180)
- CAIII and Hsp70 expressions were higher in LPRD patients that in non-LPRD patients, suggesting the possibility as one of biomomarker in LPRD diagnosis. (PMID:26847302)
- these data clearly suggests that CAIII serves as an important antioxidant critical in protecting NP cells against oxidative stress-induced injury. (PMID:29559661)
- Carbonic Anhydrase III Promotes Cell Migration and Epithelial-Mesenchymal Transition in Oral Squamous Cell Carcinoma. (PMID:32183030)
- Carbonic anhydrase III is a new target of HIF1alpha in prostate cancer model. (PMID:32777521)
- Carbonic anhydrase 2 and 3 as risk biomarkers for dilated cardiomyopathy associated heart failure. (PMID:35016406)
Cross-species orthologs
18 orthologs
| Organism | Symbol | Gene ID |
|---|---|---|
| danio_rerio | cahz | ENSDARG00000011166 |
| danio_rerio | ca2 | ENSDARG00000014488 |
| mus_musculus | Car3 | ENSMUSG00000027559 |
| rattus_norvegicus | Car3 | ENSRNOG00000010079 |
| 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), CA6 (ENSG00000131686), CA1 (ENSG00000133742), CA10 (ENSG00000154975), CA4 (ENSG00000167434), CA7 (ENSG00000168748), CA5B (ENSG00000169239), CA5A (ENSG00000174990), CA8 (ENSG00000178538), CA13 (ENSG00000185015)
Protein
Protein identifiers
Carbonic anhydrase 3 — P07451 (reviewed: P07451)
Alternative names: Carbonate dehydratase III, Carbonic anhydrase III
All UniProt accessions (3): E5RHI4, P07451, V9HWA3
UniProt curated annotations — full annotation on UniProt →
Function. Reversible hydration of carbon dioxide.
Subcellular location. Cytoplasm.
Tissue specificity. Muscle specific.
Post-translational modifications. S-thiolated both by thiol-disulfide exchange with glutathione disulfide and by oxyradical-initiated S-thiolation with reduced glutathione. S-glutathionylated in hepatocytes under oxidative stress.
Activity regulation. Activated by proton donors such as imidazole and the dipeptide histidylhistidine. Inhibited by coumarins and sulfonamide derivatives such as acetazolamide.
Similarity. Belongs to the alpha-carbonic anhydrase family.
RefSeq proteins (1): NP_005172* (*=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 (55 total): strand 17, modified residue 14, helix 10, binding site 4, mutagenesis site 3, turn 2, initiator methionine 1, chain 1, domain 1, sequence variant 1, region of interest 1
Structure
Experimental structures (PDB)
5 structures.
| PDB | Method | Resolution (Å) |
|---|---|---|
| 3UYQ | X-RAY DIFFRACTION | 1.7 |
| 1Z93 | X-RAY DIFFRACTION | 2.1 |
| 1Z97 | X-RAY DIFFRACTION | 2.1 |
| 2HFW | X-RAY DIFFRACTION | 2.5 |
| 3UYN | X-RAY DIFFRACTION | 2.6 |
Predicted structure (AlphaFold)
| Model | pLDDT | Fraction very-high |
|---|---|---|
| AF-P07451-F1 | 97.99 | 0.99 |
Functional residue map
Curated UniProt residues grouped by drug-discovery relevance — catalytic, ligand-binding, modification, and mutation-validated positions. Source: UniProtKB sequence features.
Ligand- & substrate-binding residues (4): 94; 96; 119; 198–199
Post-translational modifications (14): 43, 48, 50, 55, 73, 127, 129, 176, 182, 187, 216, 219, 2, 29
Mutagenesis-validated functional residues (3):
| Position | Phenotype |
|---|---|
| 64 | enhanced proton transfer in catalysis. |
| 67 | enhanced proton transfer in catalysis. |
| 197 | enhanced activity by at least 10-fold. |
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: 196 (showing top):
TGGTGCT_MIR29A_MIR29B_MIR29C, GOBP_RESPONSE_TO_NITROGEN_COMPOUND, GOBP_RESPONSE_TO_ETHANOL, GOBP_HEPATICOBILIARY_SYSTEM_DEVELOPMENT, GOMF_CARBONATE_DEHYDRATASE_ACTIVITY, YAO_HOXA10_TARGETS_VIA_PROGESTERONE_UP, GOBP_NEGATIVE_REGULATION_OF_REACTIVE_OXYGEN_SPECIES_METABOLIC_PROCESS, HUMMERICH_MALIGNANT_SKIN_TUMOR_DN, DARWICHE_SKIN_TUMOR_PROMOTER_UP, GOBP_REGENERATION, DARWICHE_PAPILLOMA_RISK_LOW_UP, DARWICHE_PAPILLOMA_RISK_HIGH_DN, GOBP_MULTICELLULAR_ORGANISMAL_MOVEMENT, DARWICHE_SQUAMOUS_CELL_CARCINOMA_DN, RIZKI_TUMOR_INVASIVENESS_3D_DN
GO Biological Process (14): skeletal muscle contraction (GO:0003009), response to oxidative stress (GO:0006979), positive regulation of cell population proliferation (GO:0008284), response to bacterium (GO:0009617), cellular response to insulin stimulus (GO:0032869), response to lipid (GO:0033993), cellular response to leptin stimulus (GO:0044320), response to ethanol (GO:0045471), cellular response to hypoxia (GO:0071456), liver regeneration (GO:0097421), negative regulation of reactive oxygen species biosynthetic process (GO:1903427), negative regulation of intrinsic apoptotic signaling pathway in response to hydrogen peroxide (GO:1903751), negative regulation of apoptotic process (GO:0043066), response to alcohol (GO:0097305)
GO Molecular Function (7): carbonate dehydratase activity (GO:0004089), zinc ion binding (GO:0008270), nickel cation binding (GO:0016151), phosphatase activity (GO:0016791), protein binding (GO:0005515), lyase activity (GO:0016829), metal ion binding (GO:0046872)
GO Cellular Component (4): nucleus (GO:0005634), cytoplasm (GO:0005737), cytosol (GO:0005829), sarcomere (GO:0030017)
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 |
| transition metal ion binding | 2 |
| striated muscle contraction | 1 |
| musculoskeletal movement | 1 |
| response to stress | 1 |
| cell population proliferation | 1 |
| regulation of cell population proliferation | 1 |
| positive regulation of cellular process | 1 |
| response to other organism | 1 |
| response to insulin | 1 |
| cellular response to peptide hormone stimulus | 1 |
| response to chemical | 1 |
| cellular response to hormone stimulus | 1 |
| response to leptin | 1 |
| response to alcohol | 1 |
| response to hypoxia | 1 |
| cellular response to stress | 1 |
| cellular response to decreased oxygen levels | 1 |
| liver development | 1 |
| animal organ regeneration | 1 |
| negative regulation of biosynthetic process | 1 |
| reactive oxygen species biosynthetic process | 1 |
| regulation of reactive oxygen species biosynthetic process | 1 |
| negative regulation of reactive oxygen species metabolic process | 1 |
| intrinsic apoptotic signaling pathway in response to hydrogen peroxide | 1 |
| negative regulation of hydrogen peroxide-mediated programmed cell death | 1 |
| negative regulation of oxidative stress-induced intrinsic apoptotic signaling pathway | 1 |
| regulation of intrinsic apoptotic signaling pathway in response to hydrogen peroxide | 1 |
| apoptotic process | 1 |
| regulation of apoptotic process | 1 |
| negative regulation of programmed cell death | 1 |
| response to oxygen-containing compound | 1 |
| hydro-lyase activity | 1 |
| phosphoric ester hydrolase activity | 1 |
| binding | 1 |
| catalytic activity | 1 |
| cation binding | 1 |
| intracellular membrane-bounded organelle | 1 |
| intracellular anatomical structure | 1 |
| cytoplasm | 1 |
Protein interactions and networks
STRING
1284 interactions, top by confidence (×1000):
| Protein A | Protein B | Partner UniProt | Score |
|---|---|---|---|
| CA3 | CA4 | P22748 | 822 |
| CA3 | CYP24A1 | Q07973 | 779 |
| CA3 | SLC2A5 | P22732 | 764 |
| CA3 | ENO1 | P06733 | 656 |
| CA3 | ALB | P02768 | 590 |
| CA3 | MB | P02144 | 586 |
| CA3 | SPARC | P09486 | 494 |
| CA3 | TG | P01266 | 492 |
| CA3 | FTH1 | P02794 | 482 |
| CA3 | RNASE1 | P07998 | 468 |
| CA3 | CASP8 | Q14790 | 455 |
| CA3 | ENO3 | P13929 | 439 |
| CA3 | CALM1 | P02593 | 433 |
| CA3 | CKM | P06732 | 431 |
| CA3 | SLC4A4 | Q9Y6R1 | 416 |
IntAct
10 interactions, top by confidence:
| A | B | Type | Score |
|---|---|---|---|
| CA3 | LXN | psi-mi:“MI:0915”(physical association) | 0.560 |
| CA3 | HPCAL1 | psi-mi:“MI:0915”(physical association) | 0.560 |
| HSD17B10 | SSB | psi-mi:“MI:0914”(association) | 0.530 |
| TMEM120A | CA3 | psi-mi:“MI:0915”(physical association) | 0.400 |
| MECOM | ATP2A1 | psi-mi:“MI:0914”(association) | 0.350 |
| LXN | CA3 | psi-mi:“MI:0915”(physical association) | 0.000 |
| CA3 | HPCAL1 | psi-mi:“MI:0915”(physical association) | 0.000 |
BioGRID (9): CA3 (Two-hybrid), CA3 (Two-hybrid), CA3 (Two-hybrid), CA3 (Affinity Capture-MS), CA3 (Affinity Capture-MS), CA3 (Affinity Capture-MS), CA3 (Affinity Capture-MS), CA3 (Affinity Capture-MS), CA3 (Affinity Capture-Luminescence)
ESM2 similar proteins: B0BNN3, O76206, P00441, P00445, P00915, P00916, P00917, P00918, P00919, P00920, P00921, P00922, P07450, P07451, P07452, P07630, P13634, P14141, P16015, P27139, P28755, P35217, P43166, P48282, P48284, P60052, P82205, P83299, Q0IIW3, Q1LZA1, Q27504, Q3SZX4, Q42961, Q5S1S4, Q6C662, Q7M316, Q7M317, Q8HXQ0, Q8HXQ1, Q8HXQ2
Diamond homologs: A0A7H0DN92, A0JN41, B0BNN3, O57211, P00915, P00916, P00917, P00918, P00919, P00920, P00921, P04195, P07450, P07451, P07452, P07630, P0DSY1, P0DSY2, P13634, P14141, P16015, P20508, P23470, P23471, P23589, P27139, P35217, P35218, P43165, P43166, P48282, P48283, P61215, P83299, Q05909, Q1LZA1, Q3SZX4, Q5R4U0, Q5S1S4, Q66HG6
SIGNOR signaling
0 interactions.
Disease & clinical
Clinical variants and AI predictions
ClinVar
25 variants total. Per-class counts are floors (≥ shown; pagination cap):
| Classification | Count (floor) |
|---|---|
| Pathogenic | 0 |
| Likely pathogenic | 0 |
| Uncertain significance | 20 |
| Likely benign | 0 |
| Benign | 0 |
Top pathogenic / likely-pathogenic (0)
SpliceAI
850 predictions. Top by Δscore:
| Variant | Effect | Δscore |
|---|---|---|
| 8:85438941:ACGGT:A | donor_loss | 1.0000 |
| 8:85438942:CGG:C | donor_loss | 1.0000 |
| 8:85438944:G:GG | donor_gain | 1.0000 |
| 8:85438945:T:A | donor_loss | 1.0000 |
| 8:85439709:TA:T | acceptor_loss | 1.0000 |
| 8:85439710:A:AG | acceptor_gain | 1.0000 |
| 8:85439710:A:AT | acceptor_loss | 1.0000 |
| 8:85439711:G:GG | acceptor_gain | 1.0000 |
| 8:85439711:G:GT | acceptor_loss | 1.0000 |
| 8:85439866:G:GT | donor_gain | 1.0000 |
| 8:85439866:G:T | donor_gain | 1.0000 |
| 8:85439905:GTCAA:G | donor_gain | 1.0000 |
| 8:85439906:TC:T | donor_gain | 1.0000 |
| 8:85439910:G:GG | donor_gain | 1.0000 |
| 8:85442071:A:AG | acceptor_gain | 1.0000 |
| 8:85442072:G:GG | acceptor_gain | 1.0000 |
| 8:85443593:A:T | donor_gain | 1.0000 |
| 8:85443597:T:G | donor_gain | 1.0000 |
| 8:85444024:A:AG | acceptor_gain | 1.0000 |
| 8:85444024:AT:A | acceptor_gain | 1.0000 |
| 8:85444024:ATG:A | acceptor_gain | 1.0000 |
| 8:85444025:T:A | acceptor_gain | 1.0000 |
| 8:85444025:T:G | acceptor_gain | 1.0000 |
| 8:85444025:T:TA | acceptor_loss | 1.0000 |
| 8:85444026:G:A | acceptor_gain | 1.0000 |
| 8:85444029:TTCAG:T | acceptor_loss | 1.0000 |
| 8:85444030:TCAGC:T | acceptor_loss | 1.0000 |
| 8:85444031:CA:C | acceptor_loss | 1.0000 |
| 8:85444032:A:AG | acceptor_gain | 1.0000 |
| 8:85444032:AG:A | acceptor_loss | 1.0000 |
AlphaMissense
1716 scored. Top likely-pathogenic:
| Variant | Protein change | am_pathogenicity |
|---|---|---|
| 8:85439723:T:A | W16R | 0.992 |
| 8:85439723:T:C | W16R | 0.992 |
| 8:85439725:G:C | W16C | 0.992 |
| 8:85439725:G:T | W16C | 0.992 |
| 8:85442129:T:A | W97R | 0.992 |
| 8:85442129:T:C | W97R | 0.992 |
| 8:85439766:C:A | P30H | 0.991 |
| 8:85446256:T:A | W208R | 0.991 |
| 8:85446256:T:C | W208R | 0.991 |
| 8:85442126:C:G | H96D | 0.989 |
| 8:85438922:T:A | W5R | 0.988 |
| 8:85438922:T:C | W5R | 0.988 |
| 8:85438924:G:C | W5C | 0.988 |
| 8:85438924:G:T | W5C | 0.988 |
| 8:85442157:A:T | E106V | 0.988 |
| 8:85442158:G:C | E106D | 0.988 |
| 8:85442158:G:T | E106D | 0.988 |
| 8:85448145:T:C | F259L | 0.988 |
| 8:85448147:C:A | F259L | 0.988 |
| 8:85448147:C:G | F259L | 0.988 |
| 8:85442131:G:C | W97C | 0.987 |
| 8:85442131:G:T | W97C | 0.987 |
| 8:85446217:G:C | G195R | 0.987 |
| 8:85448129:G:C | R253S | 0.987 |
| 8:85448129:G:T | R253S | 0.987 |
| 8:85439865:G:T | G63V | 0.986 |
| 8:85442186:G:C | A116P | 0.986 |
| 8:85444035:T:C | L118P | 0.985 |
| 8:85448104:G:C | R245P | 0.985 |
| 8:85439769:T:A | V31D | 0.984 |
dbSNP variants (sampled 300 via entrez): RS1000139317 (8:85448617 C>A,T), RS1000184320 (8:85440520 C>A,T), RS1000346313 (8:85441299 A>G), RS1000411101 (8:85448048 G>A,C), RS1000590530 (8:85439200 A>G), RS1000706967 (8:85442927 T>C,G), RS1000744616 (8:85446588 G>T), RS1000818472 (8:85446794 C>G), RS1000919432 (8:85438829 A>C,G), RS1001161152 (8:85438455 T>A,C), RS1001275624 (8:85438198 C>G,T), RS1002349080 (8:85444968 A>C), RS1002489418 (8:85445342 A>G), RS1002712201 (8:85446239 G>A), RS1002769042 (8:85443052 T>C)
Disease associations
OMIM: gene MIM:114750 | disease phenotypes:
GenCC curated gene-disease
Mondo (0):
Orphanet (0):
HPO phenotypes
0 total (0 of 0 shown, HPO-id order):
GWAS associations
5 associations (top):
| Study | Trait | p-value |
|---|---|---|
| GCST002040_1 | Blood trace element (Zn levels) | 6.000000e-12 |
| GCST004605_42 | Mean corpuscular hemoglobin concentration | 4.000000e-09 |
| GCST006585_2776 | Blood protein levels | 2.000000e-08 |
| GCST008059_149 | Estimated glomerular filtration rate | 1.000000e-11 |
| GCST90002387_323 | Immature fraction of reticulocytes | 6.000000e-19 |
EFO canonical traits (1, from GWAS)
| EFO ID | Trait name |
|---|---|
| EFO:0004528 | mean corpuscular hemoglobin concentration |
Drugs & pharmacology
Drug and pharmacology data
Is drug target: yes
ChEMBL targets (2): CHEMBL2095180 (PROTEIN FAMILY), CHEMBL2885 (SINGLE PROTEIN)
Molecules with ChEMBL bioactivity
34 molecules (phase ≥1), by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 3,052,761 (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 |
| CHEMBL1055 | CHLORTHALIDONE | 4 | 20,442 |
| CHEMBL112 | ACETAMINOPHEN | 4 | 157,242 |
| CHEMBL118 | CELECOXIB | 4 | 112,844 |
| CHEMBL1200471 | PYRITHIONE ZINC | 4 | 24,834 |
| CHEMBL1286 | LEVETIRACETAM | 4 | 13,997 |
| CHEMBL14060 | PHENOL | 4 | 1,871,332 |
| CHEMBL18 | ETHOXZOLAMIDE | 4 | 3,042 |
| CHEMBL218490 | DORZOLAMIDE | 4 | 10,216 |
| CHEMBL255863 | NILOTINIB | 4 | 38,627 |
| CHEMBL26 | SULPIRIDE | 4 | 58,543 |
| CHEMBL325041 | BORTEZOMIB | 4 | 13,120 |
| CHEMBL406 | INDAPAMIDE | 4 | 16,097 |
| CHEMBL537 | HYDROQUINONE | 4 | 296,240 |
| CHEMBL58323 | LACOSAMIDE | 4 | 5,692 |
| CHEMBL609 | TRIENTINE | 4 | 120,457 |
| CHEMBL6466 | COUMARIN | 4 | 202,873 |
| CHEMBL865 | VALDECOXIB | 4 | 41,681 |
| CHEMBL926 | DOBUTAMINE | 4 | |
| CHEMBL941 | IMATINIB | 4 | |
| CHEMBL140 | CURCUMIN | 3 | |
| CHEMBL145 | CAFFEIC ACID | 3 | |
| CHEMBL165 | RESVERATROL | 3 | |
| CHEMBL19612 | SPERMIDINE | 3 | |
| CHEMBL50 | QUERCETIN | 3 | |
| CHEMBL508338 | THIMEROSAL | 3 | |
| CHEMBL574 | P-TOLUENESULFONAMIDE | 3 | |
| CHEMBL251680 | COUMAPHOS | 2 |
PharmGKB: 1 entry (VIP=true, CPIC=false)
Binding affinities (BindingDB)
27 measured of 33 human assays (53 total across all organisms); most potent 27 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 |
| aliphatic sulfamate, 2 | KI | 530 nM |
| 3-(2-fluorophenyl)-2-(hydrazinecarbonyl)-1H-indole-5-sulfonamide | KI | 621 nM |
| Investigational agent, 5 | KI | 810 nM |
| Investigational agent, 4 | KI | 850 nM |
| bis-sulfamate, 4 | KI | 890 nM |
| BMCL182567 Compound 6b | KI | 2840 nM |
| [2-(cycloheptylmethyl)-1,1-dioxo–benzothiophen-6-yl] sulfamate | KI | 3600 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 |
| 3,5-difluorophenol | KI | 38800 nM |
| 7-chloro-2-methyl-3-(2-methylphenyl)-4-oxo-1,2,3,4-tetrahydroquinazoline-6-sulfonamide | KI | 54000 nM |
| 4-chloro-2-[(furan-2-ylmethyl)amino]-5-sulfamoylbenzoic acid | IC50 | 125000 nM |
| 4-cyanophenol | KI | 131000 nM |
| 2,5-difluorophenol | KI | 134000 nM |
| 4-aminophenol | KI | 159000 nM |
| benzene-1,3-diol | KI | 795000 nM |
| 1,2-Dihydroxybenzene, XI | KI | 4e+06 nM |
ChEMBL bioactivities
254 potent at pChembl≥5 of 376 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).
PubChem BioAssay actives
266 with measured affinity, of 975 total; 50 most potent distinct compounds. Largely complementary to BindingDB; screening values are coarse (µM, 4 dp), so sub-nM hits tie at the floor.
| Compound | Assay | Type | Value | Unit |
|---|---|---|---|---|
| 4-[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 |
| (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 |
| 4-nitrobenzenesulfonamide | 50173: Compound was evaluated for the inhibition of Carbonic anhydrase | ki | 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 |
| 4-chlorobenzenesulfonamide | 50173: Compound was evaluated for the inhibition of Carbonic anhydrase | ki | 0.0003 | uM |
| Acetazolamide | 50175: Compound was evaluated for the inhibition of Carbonic anhydrase (Non competitive) | ki | 0.0008 | uM |
| N-(3-methyl-5-sulfamoyl-1,3,4-thiadiazol-2-ylidene)acetamide | 311025: Inhibition of human carbonic anhydrase 3 | ki | 0.0011 | uM |
| N-benzyl-4-chloro-2-phenylsulfanyl-5-sulfamoylbenzamide | 1520081: Binding affinity to recombinant human carbonic anhydrase 3 expressed in Escherichia coli expression system assessed as kinetic dissociation constant fluorescent thermal shift assay | kd | 0.0067 | uM |
| N-benzyl-2,4-dichloro-5-sulfamoylbenzamide | 1361383: Binding affinity to recombinant human carbonic anhydrase 3 (4 to 260 residues) expressed in Escherichia coli BL21 (DE3) strain assessed as intrinsic Kd in presence of ANS by fluorescent thermal shift assay | kd | 0.0075 | uM |
| 2-(benzylamino)-4-chloro-N-(3-hydroxypropyl)-5-sulfamoylbenzamide | 1361383: Binding affinity to recombinant human carbonic anhydrase 3 (4 to 260 residues) expressed in Escherichia coli BL21 (DE3) strain assessed as intrinsic Kd in presence of ANS by fluorescent thermal shift assay | kd | 0.0076 | uM |
| 2,4-dichloro-5-sulfamoylbenzoic acid | 1361383: Binding affinity to recombinant human carbonic anhydrase 3 (4 to 260 residues) expressed in Escherichia coli BL21 (DE3) strain assessed as intrinsic Kd in presence of ANS by fluorescent thermal shift assay | kd | 0.0084 | uM |
| 4-chloro-2-(cyclooctylamino)-5-sulfamoylbenzamide | 1361383: Binding affinity to recombinant human carbonic anhydrase 3 (4 to 260 residues) expressed in Escherichia coli BL21 (DE3) strain assessed as intrinsic Kd in presence of ANS by fluorescent thermal shift assay | kd | 0.0096 | uM |
| N-benzyl-4-chloro-2-cyclohexylsulfanyl-5-sulfamoylbenzamide | 1520081: Binding affinity to recombinant human carbonic anhydrase 3 expressed in Escherichia coli expression system assessed as kinetic dissociation constant fluorescent thermal shift assay | kd | 0.0100 | uM |
| 4-chloro-2-(2-phenylethylsulfanyl)-5-sulfamoylbenzoic acid | 1520081: Binding affinity to recombinant human carbonic anhydrase 3 expressed in Escherichia coli expression system assessed as kinetic dissociation constant fluorescent thermal shift assay | kd | 0.0120 | uM |
| 4-bromo-N-butyl-2-phenylsulfanyl-5-sulfamoylbenzamide | 1520081: Binding affinity to recombinant human carbonic anhydrase 3 expressed in Escherichia coli expression system assessed as kinetic dissociation constant fluorescent thermal shift assay | kd | 0.0130 | uM |
| 2,2-dioxo-3,4-dihydro-[1,3,4]thiadiazolo[2,3-c][1,2,4]thiadiazine-7-sulfonamide | 50185: Evaluated for its activity against carbonic anhydrase (CA) in anesthetized rabbits | ic50 | 0.0140 | uM |
| N-butyl-4-chloro-2-phenylsulfanyl-5-sulfamoylbenzamide | 1520081: Binding affinity to recombinant human carbonic anhydrase 3 expressed in Escherichia coli expression system assessed as kinetic dissociation constant fluorescent thermal shift assay | kd | 0.0160 | uM |
| 2,4-dibromo-5-sulfamoylbenzoic acid | 1361383: Binding affinity to recombinant human carbonic anhydrase 3 (4 to 260 residues) expressed in Escherichia coli BL21 (DE3) strain assessed as intrinsic Kd in presence of ANS by fluorescent thermal shift assay | kd | 0.0170 | uM |
| 6-(2-chloroethyl)-5,7-dioxo-[1,3,4]thiadiazolo[3,2-a][1,3,5]triazine-2-sulfonamide | 50185: Evaluated for its activity against carbonic anhydrase (CA) in anesthetized rabbits | ic50 | 0.0180 | uM |
| 4-chloro-2-(cyclooctylamino)-5-sulfamoylbenzoic acid | 1361383: Binding affinity to recombinant human carbonic anhydrase 3 (4 to 260 residues) expressed in Escherichia coli BL21 (DE3) strain assessed as intrinsic Kd in presence of ANS by fluorescent thermal shift assay | kd | 0.0190 | uM |
| 2-(benzenesulfonyl)-N-benzyl-4-chloro-5-sulfamoylbenzamide | 1520081: Binding affinity to recombinant human carbonic anhydrase 3 expressed in Escherichia coli expression system assessed as kinetic dissociation constant fluorescent thermal shift assay | kd | 0.0200 | uM |
| 2,2,2-trifluoro-N-(3-methyl-5-sulfamoyl-1,3,4-thiadiazol-2-ylidene)acetamide | 50185: Evaluated for its activity against carbonic anhydrase (CA) in anesthetized rabbits | ic50 | 0.0200 | uM |
| 6-ethyl-5,7-dioxo-[1,3,4]thiadiazolo[3,2-a][1,3,5]triazine-2-sulfonamide | 50185: Evaluated for its activity against carbonic anhydrase (CA) in anesthetized rabbits | ic50 | 0.0200 | uM |
| 6-methyl-5,7-dioxo-[1,3,4]thiadiazolo[3,2-a][1,3,5]triazine-2-sulfonamide | 50185: Evaluated for its activity against carbonic anhydrase (CA) in anesthetized rabbits | ic50 | 0.0200 | uM |
| 5,7-dioxo-[1,3,4]thiadiazolo[3,2-a][1,3,5]triazine-2-sulfonamide | 50185: Evaluated for its activity against carbonic anhydrase (CA) in anesthetized rabbits | ic50 | 0.0200 | uM |
| 4-bromo-N-butyl-2-(2-hydroxyethylsulfanyl)-5-sulfamoylbenzamide | 1520081: Binding affinity to recombinant human carbonic anhydrase 3 expressed in Escherichia coli expression system assessed as kinetic dissociation constant fluorescent thermal shift assay | kd | 0.0220 | uM |
| 4-chloro-N-(2-methoxyethyl)-2-phenylsulfanyl-5-sulfamoylbenzamide | 1520081: Binding affinity to recombinant human carbonic anhydrase 3 expressed in Escherichia coli expression system assessed as kinetic dissociation constant fluorescent thermal shift assay | kd | 0.0240 | uM |
| N-butyl-4-chloro-2-(2-phenylethylsulfanyl)-5-sulfamoylbenzamide | 1520081: Binding affinity to recombinant human carbonic anhydrase 3 expressed in Escherichia coli expression system assessed as kinetic dissociation constant fluorescent thermal shift assay | kd | 0.0240 | uM |
| N-butyl-4-chloro-2-cyclohexylsulfanyl-5-sulfamoylbenzamide | 1520081: Binding affinity to recombinant human carbonic anhydrase 3 expressed in Escherichia coli expression system assessed as kinetic dissociation constant fluorescent thermal shift assay | kd | 0.0240 | uM |
| N-butyl-2,4-dichloro-5-sulfamoylbenzamide | 1520081: Binding affinity to recombinant human carbonic anhydrase 3 expressed in Escherichia coli expression system assessed as kinetic dissociation constant fluorescent thermal shift assay | kd | 0.0270 | uM |
| 2-(benzenesulfinyl)-4-bromo-N-(2-hydroxyethyl)-5-sulfamoylbenzamide | 1520081: Binding affinity to recombinant human carbonic anhydrase 3 expressed in Escherichia coli expression system assessed as kinetic dissociation constant fluorescent thermal shift assay | kd | 0.0280 | uM |
| 1-(2,5-dimethyl-4-sulfamoylphenyl)-5-oxopyrrolidine-3-carboxylic acid | 1515316: Binding affinity to recombinant N-terminal His6x-tagged human CA3 (4 to 260 residues) expressed in Escherichia coli BL21(DE3) assessed as intrinsic dissociation constant by DSF-based fluorescence thermal shift assay | kd | 0.0290 | uM |
| 2-(benzylamino)-N-butyl-4-chloro-5-sulfamoylbenzamide | 1361383: Binding affinity to recombinant human carbonic anhydrase 3 (4 to 260 residues) expressed in Escherichia coli BL21 (DE3) strain assessed as intrinsic Kd in presence of ANS by fluorescent thermal shift assay | kd | 0.0300 | uM |
| 4-chloro-2-cyclohexylsulfanyl-N-(2-hydroxyethyl)-5-sulfamoylbenzamide | 1520081: Binding affinity to recombinant human carbonic anhydrase 3 expressed in Escherichia coli expression system assessed as kinetic dissociation constant fluorescent thermal shift assay | kd | 0.0300 | uM |
| 2-(benzylamino)-4-chloro-N-(2-hydroxyethyl)-5-sulfamoylbenzamide | 1361383: Binding affinity to recombinant human carbonic anhydrase 3 (4 to 260 residues) expressed in Escherichia coli BL21 (DE3) strain assessed as intrinsic Kd in presence of ANS by fluorescent thermal shift assay | kd | 0.0300 | uM |
| N-benzyl-2-(benzylamino)-4-chloro-5-sulfamoylbenzamide | 1361383: Binding affinity to recombinant human carbonic anhydrase 3 (4 to 260 residues) expressed in Escherichia coli BL21 (DE3) strain assessed as intrinsic Kd in presence of ANS by fluorescent thermal shift assay | kd | 0.0303 | uM |
| 2,4-dichloro-N-(2-hydroxyethyl)-5-sulfamoylbenzamide | 1361383: Binding affinity to recombinant human carbonic anhydrase 3 (4 to 260 residues) expressed in Escherichia coli BL21 (DE3) strain assessed as intrinsic Kd in presence of ANS by fluorescent thermal shift assay | kd | 0.0310 | uM |
| 4-bromo-N-butyl-2-(2-phenylethylsulfanyl)-5-sulfamoylbenzamide | 1520081: Binding affinity to recombinant human carbonic anhydrase 3 expressed in Escherichia coli expression system assessed as kinetic dissociation constant fluorescent thermal shift assay | kd | 0.0330 | uM |
| 1-(2-chloro-3,5-dimethyl-4-sulfamoylphenyl)-5-oxopyrrolidine-3-carboxylic acid | 1515316: Binding affinity to recombinant N-terminal His6x-tagged human CA3 (4 to 260 residues) expressed in Escherichia coli BL21(DE3) assessed as intrinsic dissociation constant by DSF-based fluorescence thermal shift assay | kd | 0.0330 | uM |
| 2,3,5,6-tetrafluoro-4-(2-hydroxyethylsulfonyl)benzenesulfonamide | 1170166: Inhibition of human carbonic anhydrase 3 at pH7 and 37 degC by fluorescent thermal shift assay | kd | 0.0330 | uM |
| 4-chloro-N-(2-hydroxyethyl)-2-phenylsulfanyl-5-sulfamoylbenzamide | 1520081: Binding affinity to recombinant human carbonic anhydrase 3 expressed in Escherichia coli expression system assessed as kinetic dissociation constant fluorescent thermal shift assay | kd | 0.0370 | uM |
| 2,4-dibromo-N-butyl-5-sulfamoylbenzamide | 1361383: Binding affinity to recombinant human carbonic anhydrase 3 (4 to 260 residues) expressed in Escherichia coli BL21 (DE3) strain assessed as intrinsic Kd in presence of ANS by fluorescent thermal shift assay | kd | 0.0370 | uM |
| 7-hydroxy-5-oxo-[1,3,4]thiadiazolo[3,2-a]pyrimidine-2-sulfonamide | 50185: Evaluated for its activity against carbonic anhydrase (CA) in anesthetized rabbits | ic50 | 0.0370 | uM |
| 2-(benzylamino)-4-chloro-N-(2-methoxyethyl)-5-sulfamoylbenzamide | 1361383: Binding affinity to recombinant human carbonic anhydrase 3 (4 to 260 residues) expressed in Escherichia coli BL21 (DE3) strain assessed as intrinsic Kd in presence of ANS by fluorescent thermal shift assay | kd | 0.0380 | uM |
| 2,4-dibromo-N-(2-hydroxyethyl)-5-sulfamoylbenzamide | 1361383: Binding affinity to recombinant human carbonic anhydrase 3 (4 to 260 residues) expressed in Escherichia coli BL21 (DE3) strain assessed as intrinsic Kd in presence of ANS by fluorescent thermal shift assay | kd | 0.0400 | uM |
| 2-(benzenesulfonyl)-N-butyl-4-chloro-5-sulfamoylbenzamide | 1520081: Binding affinity to recombinant human carbonic anhydrase 3 expressed in Escherichia coli expression system assessed as kinetic dissociation constant fluorescent thermal shift assay | kd | 0.0420 | uM |
| 2,4-dichloro-5-sulfamoylbenzamide | 1361383: Binding affinity to recombinant human carbonic anhydrase 3 (4 to 260 residues) expressed in Escherichia coli BL21 (DE3) strain assessed as intrinsic Kd in presence of ANS by fluorescent thermal shift assay | kd | 0.0440 | uM |
| N-hydroxy-N-methyl-4-nitrobenzenesulfonamide | 50173: Compound was evaluated for the inhibition of Carbonic anhydrase | ki | 0.0440 | uM |
| 2,4-dichloro-N-(2-methoxyethyl)-5-sulfamoylbenzamide | 1520081: Binding affinity to recombinant human carbonic anhydrase 3 expressed in Escherichia coli expression system assessed as kinetic dissociation constant fluorescent thermal shift assay | kd | 0.0460 | uM |
| 4-chloro-2-(cyclohexylamino)-N-(2-methoxyethyl)-5-sulfamoylbenzamide | 1361383: Binding affinity to recombinant human carbonic anhydrase 3 (4 to 260 residues) expressed in Escherichia coli BL21 (DE3) strain assessed as intrinsic Kd in presence of ANS by fluorescent thermal shift assay | kd | 0.0480 | uM |
CTD chemical–gene interactions
51 total (human), top 30 by PubMed support.
| Chemical | Actions (top 5) | PubMed papers |
|---|---|---|
| Valproic Acid | affects cotreatment, increases expression, affects expression | 7 |
| Benzo(a)pyrene | affects methylation, affects cotreatment, affects expression, decreases expression, increases expression | 5 |
| trichostatin A | affects cotreatment, increases expression | 3 |
| Cadmium Chloride | decreases expression, increases abundance, increases expression | 3 |
| Vorinostat | increases expression, affects cotreatment | 2 |
| sulfamidochrysoidine | affects binding, decreases activity | 1 |
| methyleugenol | decreases expression | 1 |
| benzo(b)fluoranthene | affects cotreatment, affects expression | 1 |
| bisphenol A | decreases expression | 1 |
| terbufos | increases methylation | 1 |
| decamethrin | increases expression | 1 |
| sodium arsenite | affects expression | 1 |
| 1,2,5,6-dibenzanthracene | affects cotreatment, affects expression | 1 |
| hydroquinone | decreases expression | 1 |
| 4-aminophenylarsenoxide | affects binding, decreases reaction | 1 |
| dibenzo(a,l)pyrene | affects cotreatment, affects expression | 1 |
| dorzolamide | affects binding, decreases activity | 1 |
| brinzolamide | affects binding, decreases activity | 1 |
| valdecoxib | affects binding, decreases activity | 1 |
| N-(3-chloro-7-indolyl)-1,4-benzenedisulphonamide | affects binding, decreases activity | 1 |
| 4-(5-benzo(1,3)dioxol-5-yl-4-pyridin-2-yl-1H-imidazol-2-yl)benzamide | affects cotreatment, increases expression | 1 |
| clothianidin | increases expression | 1 |
| dorsomorphin | affects cotreatment, increases expression | 1 |
| 5-hydroxythalidomide | affects binding | 1 |
| Celecoxib | affects binding, decreases activity | 1 |
| Topiramate | affects binding, decreases activity | 1 |
| Arsenic Trioxide | affects binding, decreases reaction | 1 |
| Zonisamide | affects binding, decreases activity | 1 |
| Acetazolamide | affects binding, decreases activity | 1 |
| Benzolamide | affects binding, decreases activity | 1 |
ChEMBL screening assays
119 unique, capped per target: 117 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 |
| CHEMBL4187333 | ADMET | Binding affinity to recombinant human N-terminal His6-tagged carbonic anhydrase 3 (4 to 260 residues) 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.