AZI2
gene geneOn this page
Also known as NAP1FLJ21939AZ2
Summary
AZI2 (5-azacytidine induced 2, HGNC:24002) is a protein-coding gene on chromosome 3p24.1, encoding 5-azacytidine-induced protein 2 (Q9H6S1). Adapter protein which binds TBK1 and IKBKE playing a role in antiviral innate immunity.
AZI2, or NAP1, contributes to the activation of NFKB (see MIM 164011)-dependent gene expression by activating IKK-related kinases, such as NAK (TBK1; MIM 604834) (Fujita et al., 2003 [PubMed 14560022]).
Source: NCBI Gene 64343 — RefSeq curated summary.
At a glance
- GWAS associations: 1
- Clinical variants (ClinVar): 58 total — 1 pathogenic
- Druggable target: yes
- MANE Select transcript:
NM_022461
Identifiers
Gene identifiers
| Field | Value |
|---|---|
| HGNC ID | HGNC:24002 |
| Approved symbol | AZI2 |
| Name | 5-azacytidine induced 2 |
| Location | 3p24.1 |
| Locus type | gene with protein product |
| Status | Approved |
| Aliases | NAP1, FLJ21939, AZ2 |
| Ensembl gene | ENSG00000163512 |
| Ensembl biotype | protein_coding |
| OMIM | 609916 |
| Entrez | 64343 |
Gene structure
Transcript identifiers
Ensembl transcripts: 26 — 19 protein_coding, 6 retained_intron, 1 protein_coding_CDS_not_defined
ENST00000295748, ENST00000334100, ENST00000414162, ENST00000415852, ENST00000420543, ENST00000429369, ENST00000457172, ENST00000462936, ENST00000463512, ENST00000470234, ENST00000476174, ENST00000479665, ENST00000488978, ENST00000492044, ENST00000889265, ENST00000889266, ENST00000889267, ENST00000889268, ENST00000889269, ENST00000889270, ENST00000912521, ENST00000958175, ENST00000958176, ENST00000958177, ENST00000958178, ENST00000958179
RefSeq mRNA: 4 — MANE Select: NM_022461
NM_001134432, NM_001134433, NM_001271650, NM_022461
CCDS: CCDS2647, CCDS46782, CCDS46783
Canonical transcript exons
ENST00000479665 — 8 exons
| Exon | Start | End |
|---|---|---|
| ENSE00001839362 | 28321047 | 28324454 |
| ENSE00003481784 | 28336737 | 28336885 |
| ENSE00003483722 | 28338493 | 28338615 |
| ENSE00003560852 | 28340402 | 28340622 |
| ENSE00003576368 | 28326832 | 28326950 |
| ENSE00003629457 | 28337937 | 28338036 |
| ENSE00003784409 | 28332369 | 28332427 |
| ENSE00003841512 | 28348601 | 28348824 |
Expression profiles
Bgee: expression breadth ubiquitous, 287 present calls, max score 96.61.
FANTOM5 (CAGE): breadth ubiquitous, TPM avg 34.5980 / max 260.9960, expressed in 1824 samples.
FANTOM5 promoters (9 alternative TSS)
| Promoter ID | TPM avg | Samples expressed |
|---|---|---|
| 41549 | 18.2965 | 1816 |
| 41547 | 12.7444 | 1739 |
| 41544 | 1.0025 | 659 |
| 41546 | 0.9732 | 611 |
| 41541 | 0.3755 | 96 |
| 41543 | 0.3630 | 123 |
| 41542 | 0.3509 | 105 |
| 41548 | 0.2705 | 110 |
| 41545 | 0.2215 | 83 |
Top tissues by expression
294 total, by Bgee expression score (0-100, higher = more expressed):
| Tissue | Anatomy ID | Expression score | Quality |
|---|---|---|---|
| stromal cell of endometrium | CL:0002255 | 96.61 | gold quality |
| monocyte | CL:0000576 | 96.45 | gold quality |
| mucosa of paranasal sinus | UBERON:0005030 | 96.45 | gold quality |
| calcaneal tendon | UBERON:0003701 | 96.32 | gold quality |
| omental fat pad | UBERON:0010414 | 96.22 | gold quality |
| peritoneum | UBERON:0002358 | 96.19 | gold quality |
| buccal mucosa cell | CL:0002336 | 96.17 | gold quality |
| mucosa of stomach | UBERON:0001199 | 96.15 | gold quality |
| right lung | UBERON:0002167 | 96.03 | gold quality |
| lower lobe of lung | UBERON:0008949 | 96.01 | gold quality |
| mononuclear cell | CL:0000842 | 95.89 | gold quality |
| adipose tissue of abdominal region | UBERON:0007808 | 95.89 | gold quality |
| leukocyte | CL:0000738 | 95.73 | gold quality |
| ganglionic eminence | UBERON:0004023 | 95.36 | gold quality |
| ventricular zone | UBERON:0003053 | 95.23 | gold quality |
| adenohypophysis | UBERON:0002196 | 95.12 | gold quality |
| endocervix | UBERON:0000458 | 95.04 | gold quality |
| upper lobe of left lung | UBERON:0008952 | 95.00 | gold quality |
| upper lobe of lung | UBERON:0008948 | 94.98 | gold quality |
| left coronary artery | UBERON:0001626 | 94.97 | gold quality |
| pituitary gland | UBERON:0000007 | 94.91 | gold quality |
| colonic epithelium | UBERON:0000397 | 94.87 | gold quality |
| tibial artery | UBERON:0007610 | 94.86 | gold quality |
| popliteal artery | UBERON:0002250 | 94.85 | gold quality |
| nerve | UBERON:0001021 | 94.82 | gold quality |
| tibial nerve | UBERON:0001323 | 94.82 | gold quality |
| gall bladder | UBERON:0002110 | 94.79 | gold quality |
| adrenal tissue | UBERON:0018303 | 94.76 | gold quality |
| subcutaneous adipose tissue | UBERON:0002190 | 94.73 | gold quality |
| ectocervix | UBERON:0012249 | 94.72 | gold quality |
Single-cell (SCXA)
Detected in 1 experiment(s), a significant marker in 1.
| Experiment | Marker? | Max mean expression |
|---|---|---|
| E-ANND-3 | yes | 12.99 |
Regulation
Is transcription factor: no
Literature-anchored findings (GeneRIF, showing 7)
- These results define NAK-associated protein 1 (NAP1) as an activator of IkappaB kinase-related kinases and suggest that the NAK-NAP1 complex may protect cells from TNF-alpha-induced apoptosis by promoting NF-kappaB activation. (PMID:14560022)
- Both the cytoplasmic and TLR3-mediated dsRNA recognition pathways converge upon NAP1 for the activation of the IRF-3 and IFN-beta promoter. (PMID:17142768)
- the spatiotemporal mobilization of TICAM-1 in response to dsRNA and the formation of the TICAM-1 speckles containing RIP1 and NAP1 are important for the activation of the TLR3-TICAM-1 pathway. (PMID:17982077)
- (AZI2)3’UTR confers variant-dependent transcriptional regulation of SLC6A3, a potential risk factor for substance abuse disorders. (PMID:28983843)
- AZI2 mediates TBK1 activation at unresolved selective autophagy cargo receptor complexes with implications for CD8 T-cell infiltration in breast cancer. (PMID:37733921)
- NAK-associated protein 1/NAP1 activates TBK1 to ensure accurate mitosis and cytokinesis. (PMID:38059900)
- TBK1 adaptor AZI2/NAP1 regulates NDP52-driven mitochondrial autophagy. (PMID:39276928)
Cross-species orthologs
3 orthologs
| Organism | Symbol | Gene ID |
|---|---|---|
| danio_rerio | azi2 | ENSDARG00000102419 |
| mus_musculus | Azi2 | ENSMUSG00000039285 |
| rattus_norvegicus | Azi2 | ENSRNOG00000010096 |
Paralogs (1): TBKBP1 (ENSG00000198933)
Protein
Protein identifiers
5-azacytidine-induced protein 2 — Q9H6S1 (reviewed: Q9H6S1)
Alternative names: NF-kappa-B-activating kinase-associated protein 1, TILP
All UniProt accessions (4): C9JGA2, C9JVK8, Q9H6S1, H7C1Z1
UniProt curated annotations — full annotation on UniProt →
Function. Adapter protein which binds TBK1 and IKBKE playing a role in antiviral innate immunity. Activates serine/threonine-protein kinase TBK1 and facilitates its oligomerization. Enhances the phosphorylation of NF-kappa-B p65 subunit RELA by TBK1. Promotes TBK1-induced as well as TNF or PMA-induced activation of NF-kappa-B. Participates in IFNB promoter activation via TICAM1.
Subunit / interactions. Homodimer. Interacts with IKBKE. Interacts with TBK1. Interacts with TICAM1. Interacts with TAX1BP1. Interacts with CALCOCO2. (Microbial infection) Interacts with vaccinia virus protein C6.
Subcellular location. Cytoplasm.
Tissue specificity. Widely expressed. Abundant expression seen in the pancreas and testis.
Post-translational modifications. Ubiquitinated via ‘Lys-48’-linked polyubiquitination by TRIM38, leading to its degradation.
Isoforms (4)
| UniProt ID | Names | Canonical? |
|---|---|---|
| Q9H6S1-1 | 1, Long | yes |
| Q9H6S1-3 | 2, Short | |
| Q9H6S1-4 | 3 | |
| Q9H6S1-5 | 4 |
RefSeq proteins (4): NP_001127904, NP_001127905, NP_001258579, NP_071906* (*=MANE)
Domains & families (InterPro)
| ID | Name | Type |
|---|---|---|
| IPR024581 | TBD | Domain |
| IPR051891 | TBK1-IKBKE_adapters | Family |
Pfam: PF12845
UniProt features (17 total): splice variant 6, region of interest 2, strand 2, helix 2, coiled-coil region 2, modified residue 2, chain 1
Structure
Experimental structures (PDB)
5 structures.
| PDB | Method | Resolution (Å) |
|---|---|---|
| 5EP6 | X-RAY DIFFRACTION | 1.45 |
| 5Z7L | X-RAY DIFFRACTION | 2.02 |
| 7EA2 | X-RAY DIFFRACTION | 2.14 |
| 5Z7G | X-RAY DIFFRACTION | 2.3 |
| 7EA7 | X-RAY DIFFRACTION | 2.69 |
Predicted structure (AlphaFold)
| Model | pLDDT | Fraction very-high |
|---|---|---|
| AF-Q9H6S1-F1 | 69.50 | 0.38 |
Functional residue map
Curated UniProt residues grouped by drug-discovery relevance — catalytic, ligand-binding, modification, and mutation-validated positions. Source: UniProtKB sequence features.
Post-translational modifications (2): 318, 353
Function
Pathways and Gene Ontology
Reactome pathways
0 pathways
MSigDB gene sets: 229 (showing top):
GOBP_DENDRITIC_CELL_DIFFERENTIATION, GOBP_RESPONSE_TO_PEPTIDE, GOBP_CANONICAL_NF_KAPPAB_SIGNAL_TRANSDUCTION, GOBP_RESPONSE_TO_TYPE_I_INTERFERON, FOXO4_01, LA_MEN1_TARGETS, GOBP_NEGATIVE_REGULATION_OF_INTRACELLULAR_SIGNAL_TRANSDUCTION, EVI1_05, IRF7_01, GOBP_DEFENSE_RESPONSE_TO_OTHER_ORGANISM, GOBP_LEUKOCYTE_PROLIFERATION, AML_Q6, GOBP_MITOTIC_CELL_CYCLE, GOBP_NEGATIVE_REGULATION_OF_CANONICAL_NF_KAPPAB_SIGNAL_TRANSDUCTION, NAKAMURA_TUMOR_ZONE_PERIPHERAL_VS_CENTRAL_DN
GO Biological Process (7): mitotic cell cycle (GO:0000278), T cell activation (GO:0042110), negative regulation of canonical NF-kappaB signal transduction (GO:0043124), dendritic cell proliferation (GO:0044565), defense response to virus (GO:0051607), type I interferon-mediated signaling pathway (GO:0060337), dendritic cell differentiation (GO:0097028)
GO Molecular Function (1): protein binding (GO:0005515)
GO Cellular Component (2): cytoplasm (GO:0005737), serine/threonine protein kinase complex (GO:1902554)
GO top-level categories
Rollup of top GO terms by namespace:
| Category | Terms |
|---|---|
| cell cycle | 1 |
| mitotic nuclear division | 1 |
| lymphocyte activation | 1 |
| canonical NF-kappaB signal transduction | 1 |
| regulation of canonical NF-kappaB signal transduction | 1 |
| negative regulation of intracellular signal transduction | 1 |
| mononuclear cell proliferation | 1 |
| defense response | 1 |
| response to virus | 1 |
| cellular response to type I interferon | 1 |
| interferon-mediated signaling pathway | 1 |
| mononuclear cell differentiation | 1 |
| binding | 1 |
| intracellular anatomical structure | 1 |
| cellular anatomical structure | 1 |
| protein kinase complex | 1 |
Protein interactions and networks
STRING
586 interactions, top by confidence (×1000):
| Protein A | Protein B | Partner UniProt | Score |
|---|---|---|---|
| AZI2 | IKBKE | Q14164 | 966 |
| AZI2 | TBK1 | Q9UHD2 | 955 |
| AZI2 | TANK | Q92844 | 884 |
| AZI2 | TRAF3 | Q13114 | 732 |
| AZI2 | IKBKG | Q9Y6K9 | 682 |
| AZI2 | CALCOCO2 | Q13137 | 643 |
| AZI2 | IRF3 | Q14653 | 619 |
| AZI2 | EXOC2 | Q96KP1 | 599 |
| AZI2 | ZBP1 | Q9H171 | 599 |
| AZI2 | RALB | P11234 | 596 |
| AZI2 | TBKBP1 | A7MCY6 | 595 |
| AZI2 | OTUD5 | Q96G74 | 594 |
| AZI2 | IRF7 | Q92985 | 533 |
| AZI2 | RB1CC1 | Q8TDY2 | 529 |
| AZI2 | CMC1 | Q7Z7K0 | 499 |
IntAct
49 interactions, top by confidence:
| A | B | Type | Score |
|---|---|---|---|
| TBK1 | TBKBP1 | psi-mi:“MI:0914”(association) | 0.860 |
| AZI2 | TBK1 | psi-mi:“MI:0915”(physical association) | 0.810 |
| CALCOCO2 | TBKBP1 | psi-mi:“MI:0914”(association) | 0.640 |
| CALCOCO2 | AZI2 | psi-mi:“MI:0914”(association) | 0.640 |
| TBK1 | TTC4 | psi-mi:“MI:0914”(association) | 0.540 |
| APBA3 | DUSP11 | psi-mi:“MI:0914”(association) | 0.530 |
| BBOX1 | ITPRID2 | psi-mi:“MI:0914”(association) | 0.530 |
| APBA3 | CLSTN1 | psi-mi:“MI:0914”(association) | 0.530 |
| OPG029 | AZI2 | psi-mi:“MI:0915”(physical association) | 0.520 |
| AZI2 | OPG029 | psi-mi:“MI:0915”(physical association) | 0.520 |
| AZI2 | psi-mi:“MI:0915”(physical association) | 0.510 | |
| NAA10 | OFD1 | psi-mi:“MI:0914”(association) | 0.480 |
| GABARAP | AZI2 | psi-mi:“MI:0407”(direct interaction) | 0.440 |
| GABARAPL1 | AZI2 | psi-mi:“MI:0407”(direct interaction) | 0.440 |
| GABARAPL2 | AZI2 | psi-mi:“MI:0407”(direct interaction) | 0.440 |
| TNFAIP3 | LRRIQ3 | psi-mi:“MI:2364”(proximity) | 0.420 |
| AZI2 | IKBKE | psi-mi:“MI:0915”(physical association) | 0.400 |
| AZI2 | psi-mi:“MI:0915”(physical association) | 0.370 | |
| EGLN3 | FAM168B | psi-mi:“MI:0914”(association) | 0.350 |
| TBKBP1 | psi-mi:“MI:0914”(association) | 0.350 | |
| AHRR | psi-mi:“MI:0914”(association) | 0.350 | |
| TBK1 | FMNL1 | psi-mi:“MI:0914”(association) | 0.350 |
BioGRID (87): AZI2 (Affinity Capture-Western), TRIM38 (Affinity Capture-Western), AZI2 (Affinity Capture-MS), AZI2 (Affinity Capture-MS), AZI2 (Affinity Capture-MS), AZI2 (Affinity Capture-MS), AZI2 (Two-hybrid), AZI2 (Affinity Capture-MS), AZI2 (Affinity Capture-MS), AZI2 (Affinity Capture-Western), AZI2 (Affinity Capture-MS), TBK1 (Co-crystal Structure), TBK1 (Reconstituted Complex), AZI2 (Affinity Capture-MS), AZI2 (Co-crystal Structure)
ESM2 similar proteins: A0A088MLT8, A2AQ25, B3KU38, B5DF41, E9PSK7, O15079, O35274, P0DPB3, P0DPB4, P12755, P49140, P85299, Q0D2I5, Q14DQ1, Q1LY51, Q3B7M3, Q3SYW5, Q4KMA0, Q4R3X1, Q50H33, Q5F3L9, Q5FVG6, Q5RD40, Q5XKK7, Q60698, Q6ZNC4, Q6ZUS6, Q6ZWB6, Q80U23, Q80U62, Q80XA6, Q812A5, Q86YI8, Q8BXL9, Q8K2W6, Q8ND83, Q8NFH8, Q8QFX1, Q8TEK3, Q924W7
Diamond homologs: A2A9T0, A7MCY6, Q3SYW5, Q4KMA0, Q4R3X1, Q5RD40, Q6DG50, Q9H6S1, Q9QYP6
SIGNOR signaling
0 interactions.
Enriched among interaction partners
Reactome pathways and GO biological processes over-represented among this gene’s 37 IntAct physical interaction partners (hypergeometric vs the genome-wide background, BH-FDR, gene-set size 15–500, ranked by fold). A functional readout of the neighbourhood — distinct from this gene’s own memberships above, and biased toward well-studied / hub proteins, so read it as themes rather than proof.
Reactome pathways:
| Pathway | Partners | Fold | FDR |
|---|---|---|---|
| TNFR1-induced proapoptotic signaling | 5 | 95.5× | 1e-07 |
| Regulation of TNFR1 signaling | 7 | 68.2× | 1e-09 |
GO biological processes:
| GO term | Partners | Fold | FDR |
|---|---|---|---|
| positive regulation of canonical NF-kappaB signal transduction | 5 | 11.7× | 4e-03 |
Disease & clinical
Clinical variants and AI predictions
ClinVar
58 variants total. Per-class counts are floors (≥ shown; pagination cap):
| Classification | Count (floor) |
|---|---|
| Pathogenic | 1 |
| Likely pathogenic | 0 |
| Uncertain significance | 48 |
| Likely benign | 1 |
| Benign | 0 |
Top pathogenic / likely-pathogenic (1)
| Variant ID | HGVS | Classification |
|---|---|---|
| 57397 | GRCh38/hg38 3p26.3-22.2(chr3:52266-37148076)x3 | Pathogenic |
SpliceAI
2213 predictions. Top by Δscore:
| Variant | Effect | Δscore |
|---|---|---|
| 3:28316419:GCTTA:G | donor_gain | 1.0000 |
| 3:28316420:CTTA:C | donor_gain | 1.0000 |
| 3:28316421:TTA:T | donor_gain | 1.0000 |
| 3:28316422:TA:T | donor_gain | 1.0000 |
| 3:28316423:AG:A | donor_loss | 1.0000 |
| 3:28316424:G:C | donor_loss | 1.0000 |
| 3:28316424:G:GG | donor_gain | 1.0000 |
| 3:28316425:TAA:T | donor_loss | 1.0000 |
| 3:28316426:AA:A | donor_loss | 1.0000 |
| 3:28319622:GCAT:G | donor_gain | 1.0000 |
| 3:28319626:G:GG | donor_gain | 1.0000 |
| 3:28319653:G:GT | donor_gain | 1.0000 |
| 3:28319654:A:T | donor_gain | 1.0000 |
| 3:28319670:G:GT | donor_gain | 1.0000 |
| 3:28319670:G:T | donor_gain | 1.0000 |
| 3:28324451:CAGG:C | acceptor_gain | 1.0000 |
| 3:28324455:C:CC | acceptor_gain | 1.0000 |
| 3:28336784:T:A | donor_gain | 1.0000 |
| 3:28336881:CATCA:C | acceptor_gain | 1.0000 |
| 3:28336883:TCA:T | acceptor_gain | 1.0000 |
| 3:28336884:CA:C | acceptor_gain | 1.0000 |
| 3:28336884:CAC:C | acceptor_gain | 1.0000 |
| 3:28336886:C:CC | acceptor_gain | 1.0000 |
| 3:28337927:A:C | donor_gain | 1.0000 |
| 3:28337935:AC:A | donor_gain | 1.0000 |
| 3:28337936:CC:C | donor_gain | 1.0000 |
| 3:28337936:CCCTG:C | donor_gain | 1.0000 |
| 3:28338486:AACTT:A | donor_loss | 1.0000 |
| 3:28338487:ACTTA:A | donor_loss | 1.0000 |
| 3:28338488:CTT:C | donor_loss | 1.0000 |
AlphaMissense
2583 scored. Top likely-pathogenic:
| Variant | Protein change | am_pathogenicity |
|---|---|---|
| 3:28340463:A:G | L52P | 0.999 |
| 3:28340496:A:G | L41P | 0.999 |
| 3:28340496:A:T | L41H | 0.999 |
| 3:28340471:T:A | K49N | 0.998 |
| 3:28340471:T:G | K49N | 0.998 |
| 3:28340488:C:G | A44P | 0.998 |
| 3:28340499:G:T | A40D | 0.998 |
| 3:28340501:A:C | F39L | 0.998 |
| 3:28340501:A:T | F39L | 0.998 |
| 3:28340503:A:G | F39L | 0.998 |
| 3:28337963:A:G | L138P | 0.997 |
| 3:28338542:C:G | R97P | 0.997 |
| 3:28340466:C:G | R51P | 0.997 |
| 3:28340485:A:C | Y45D | 0.997 |
| 3:28340485:A:G | Y45H | 0.997 |
| 3:28340586:A:G | I11T | 0.997 |
| 3:28337993:A:G | L128P | 0.996 |
| 3:28338546:A:C | Y96D | 0.996 |
| 3:28338555:A:C | Y93D | 0.996 |
| 3:28340487:G:T | A44E | 0.996 |
| 3:28337972:A:G | L135P | 0.995 |
| 3:28338549:C:G | A95P | 0.995 |
| 3:28340472:T:A | K49I | 0.995 |
| 3:28340583:A:G | L12P | 0.995 |
| 3:28340455:A:G | S55P | 0.994 |
| 3:28340479:C:G | D47H | 0.994 |
| 3:28340496:A:C | L41R | 0.994 |
| 3:28340502:A:G | F39S | 0.994 |
| 3:28340504:A:C | H38Q | 0.994 |
| 3:28340504:A:T | H38Q | 0.994 |
dbSNP variants (sampled 300 via entrez): RS1000248644 (3:28331787 T>C), RS1000423212 (3:28325061 GAA>G), RS1000563047 (3:28323104 TTCTC>T), RS1000812479 (3:28343133 A>G), RS1000968253 (3:28335727 T>C), RS1000990811 (3:28330408 C>A,T), RS1001165603 (3:28337060 G>A,C), RS1001177809 (3:28335563 G>A), RS1001215033 (3:28328226 T>G), RS1001379073 (3:28345673 GA>G,GAA), RS1001490990 (3:28349460 G>C), RS1001662363 (3:28320753 A>G), RS1001674300 (3:28328622 T>C), RS1001742773 (3:28342768 A>C), RS1001966026 (3:28323975 T>A)
Disease associations
OMIM: gene MIM:609916 | disease phenotypes:
GenCC curated gene-disease
Mondo (0):
Orphanet (0):
HPO phenotypes
0 total (0 of 0 shown, HPO-id order):
GWAS associations
1 associations (top):
| Study | Trait | p-value |
|---|---|---|
| GCST003901_9 | Cognitive decline (age-related) | 1.000000e-06 |
Drugs & pharmacology
Drug and pharmacology data
Is drug target: yes
ChEMBL targets (1): CHEMBL4523456 (SINGLE PROTEIN)
PharmGKB: 1 entry (VIP=true, CPIC=false)
ChEMBL bioactivities
5 potent at pChembl≥5 of 5 total, top 5 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).
| pChembl | Type | Value | Unit | Molecule |
|---|---|---|---|---|
| 7.57 | Kd | 26.91 | nM | CHEMBL3752910 |
| 7.42 | ED50 | 38.34 | nM | CHEMBL3752910 |
| 5.53 | Kd | 2982 | nM | CHEMBL4462318 |
| 5.34 | Kd | 4543 | nM | CHEMBL5653589 |
| 5.19 | ED50 | 6473 | nM | CHEMBL5653589 |
PubChem BioAssay actives
3 with measured affinity, of 5 total; 3 most potent distinct compounds. Largely complementary to BindingDB; screening values are coarse (µM, 4 dp), so sub-nM hits tie at the floor.
| Compound | Assay | Type | Value | Unit |
|---|---|---|---|---|
| 4-methyl-3-[(1-methyl-6-pyridin-3-ylpyrazolo[3,4-d]pyrimidin-4-yl)amino]-N-[3-(trifluoromethyl)phenyl]benzamide | 2147934: Binding affinity to human AZI2 incubated for 45 mins by Kinobead based pull down assay | kd | 0.0269 | uM |
| 2,6-difluoro-N-[3-fluoro-4-[6-methoxy-7-[3-(4-methylpiperazin-1-yl)propoxy]quinolin-4-yl]oxyphenyl]benzenesulfonamide | 1573326: Binding affinity to AZI2 in SILAC-labeled human MDA-MB-231 cells lysate by mass spectrometry based kinAffinity assay | kd | 2.9820 | uM |
| 4-methyl-3-[(2-methyl-6-pyridin-3-ylpyrazolo[3,4-d]pyrimidin-4-yl)amino]-N-[3-(trifluoromethyl)phenyl]benzamide | 2147934: Binding affinity to human AZI2 incubated for 45 mins by Kinobead based pull down assay | kd | 4.5429 | uM |
CTD chemical–gene interactions
35 total (human), top 30 by PubMed support.
| Chemical | Actions (top 5) | PubMed papers |
|---|---|---|
| Valproic Acid | decreases expression, decreases methylation, increases expression | 5 |
| Cyclosporine | increases expression | 3 |
| sodium arsenite | decreases expression | 2 |
| cobaltous chloride | increases expression | 2 |
| Air Pollutants | decreases expression, increases abundance | 2 |
| methylmercuric chloride | decreases expression | 1 |
| triphenyl phosphate | affects expression | 1 |
| bisphenol A | affects cotreatment, increases methylation | 1 |
| decabromobiphenyl ether | affects expression | 1 |
| trichostatin A | affects cotreatment, decreases expression | 1 |
| beta-lapachone | increases expression | 1 |
| ochratoxin A | increases expression | 1 |
| di-n-butylphosphoric acid | affects expression | 1 |
| ICG 001 | decreases expression | 1 |
| Decitabine | affects cotreatment, decreases expression | 1 |
| Sunitinib | increases expression | 1 |
| Fulvestrant | affects cotreatment, increases methylation | 1 |
| Cannabidiol | increases expression | 1 |
| Clorgyline | increases expression | 1 |
| Coal | decreases expression, increases abundance | 1 |
| Doxorubicin | decreases expression | 1 |
| Ethyl Methanesulfonate | increases expression | 1 |
| Formaldehyde | decreases expression | 1 |
| Hydrogen Peroxide | decreases expression, affects cotreatment | 1 |
| Methyl Methanesulfonate | decreases expression | 1 |
| Smoke | increases abundance, decreases expression | 1 |
| Theophylline | affects cotreatment, decreases expression | 1 |
| Thimerosal | increases expression | 1 |
| Tobacco Smoke Pollution | increases expression | 1 |
| Tretinoin | increases expression | 1 |
ChEMBL screening assays
2 unique, capped per target: 2 binding
Representative assays (with source publication via chembl_document):
| Assay ID | Type | Description | Source paper |
|---|---|---|---|
| CHEMBL4371456 | Binding | Binding affinity to AZI2 in SILAC-labeled human MDA-MB-231 cells lysate by mass spectrometry based kinAffinity assay | Discovery of N-[4-(Quinolin-4-yloxy)phenyl]benzenesulfonamides as Novel AXL Kinase Inhibitors. — J Med Chem |
Cellosaurus cell lines
10 cell lines: 10 cancer cell line
First 10 cell lines (id-ordered, not curated):
| Cellosaurus | Name | Category | Sex |
|---|---|---|---|
| CVCL_B1KU | Abcam HeLa AZI2 KO | Cancer cell line | Female |
| CVCL_C8QB | HeLa S3 penta KO-AZI2/TBKBP1 DKO clone 20 | Cancer cell line | Female |
| CVCL_C9DV | HeLa S3 AZI2/TBKBP1 DKO clone 13 | Cancer cell line | Female |
| CVCL_C9DW | HeLa S3 penta KO-ULK1/ULK2 DKO-AZI2/TBKBP1 DKO | Cancer cell line | Female |
| CVCL_D2Q0 | HeLa S3 AZI2/TBKBP1 DKO clone 14 | Cancer cell line | Female |
| CVCL_D2Q1 | HeLa S3 penta KO-AZI2/TBKBP1 DKO clone 26 | Cancer cell line | Female |
| CVCL_D2YA | HeLa S3 AZI2 KO clone 32 | Cancer cell line | Female |
| CVCL_D2YB | HeLa S3 AZI2 KO clone 62 | Cancer cell line | Female |
| CVCL_SE40 | HAP1 AZI2 (-) 1 | Cancer cell line | Male |
| CVCL_SE41 | HAP1 AZI2 (-) 2 | Cancer cell line | Male |
Clinical trials (associated diseases)
0 trials via MONDO — disease-level, not drug-specific.
Related Atlas pages
No linked Atlas pages yet — the cross-entity mesh grows as the corpus expands.