VCAM1
gene geneOn this page
Also known as CD106
Summary
VCAM1 (vascular cell adhesion molecule 1, HGNC:12663) is a protein-coding gene on chromosome 1p21.2, encoding Vascular cell adhesion protein 1 (P19320). Cell adhesion glycoprotein predominantly expressed on the surface of endothelial cells that plays an important role in immune surveillance and inflammation.
This gene is a member of the Ig superfamily and encodes a cell surface sialoglycoprotein expressed by cytokine-activated endothelium. This type I membrane protein mediates leukocyte-endothelial cell adhesion and signal transduction, and may play a role in the development of artherosclerosis and rheumatoid arthritis. Three alternatively spliced transcripts encoding different isoforms have been described for this gene.
Source: NCBI Gene 7412 — RefSeq curated summary.
At a glance
- GWAS associations: 8
- Clinical variants (ClinVar): 101 total
- GTEx eGene: eQTL in 23 tissues, sQTL in 1 (q < 0.05)
- ChEMBL bioactivity: 1 clinical-phase molecule tested; no curated mechanism-of-action drug
- Constraint (gnomAD): pLI 0.00 (LoF-tolerant), LOEUF 0.84 (unconstrained)
- MANE Select transcript:
NM_001078 - Interaction hub: 4,000 STRING partners (top 1% of genes corpus-wide)
- Notable: 101 clinical variants but no curated precision-oncology (CIViC) evidence yet
Identifiers
Gene identifiers
| Field | Value |
|---|---|
| HGNC ID | HGNC:12663 |
| Approved symbol | VCAM1 |
| Name | vascular cell adhesion molecule 1 |
| Location | 1p21.2 |
| Locus type | gene with protein product |
| Status | Approved |
| Aliases | CD106 |
| Ensembl gene | ENSG00000162692 |
| Ensembl biotype | protein_coding |
| OMIM | 192225 |
| Entrez | 7412 |
Gene structure
Transcript identifiers
Ensembl transcripts: 16 — 10 protein_coding, 5 nonsense_mediated_decay, 1 retained_intron
MANE Select: ENST00000294728
Transcript support level (Ensembl TSL; 1 = fully mRNA-supported): TSL 1: 2, TSL 2: 1, TSL 5: 1
ENST00000294728, ENST00000347652, ENST00000370115, ENST00000370119, ENST00000603679, ENST00000650339, ENST00000855907, ENST00000949395, ENST00000949396, ENST00000988852, ENST00001011558, ENST00001011559, ENST00001112640, ENST00001120419, ENST00001125052, ENST00001143533
RefSeq mRNA: 3 — MANE Select: NM_001078
NM_001078, NM_001199834, NM_080682
CCDS: CCDS55617, CCDS773, CCDS774
Canonical transcript exons
ENST00000294728 — 9 exons
| Exon | Start | End |
|---|---|---|
| ENSE00001067751 | 100734502 | 100734768 |
| ENSE00001067753 | 100731198 | 100731518 |
| ENSE00001067755 | 100723020 | 100723340 |
| ENSE00001067756 | 100729107 | 100729382 |
| ENSE00001067757 | 100720476 | 100720751 |
| ENSE00001067758 | 100724624 | 100724890 |
| ENSE00001067759 | 100732418 | 100732684 |
| ENSE00001167786 | 100719742 | 100719924 |
| ENSE00004803124 | 100738123 | 100739045 |
Expression profiles
Bgee: expression breadth ubiquitous, 257 present calls, max score 99.13.
FANTOM5 (CAGE): breadth ubiquitous, TPM avg 14.7029 / max 910.3466, expressed in 928 samples.
Highest expression (Bgee): cartilage tissue, trabecular bone tissue, parietal pleura, vena cava, tendon of biceps brachii.
Genetic regulation across tissues (GTEx eQTL / sQTL)
VCAM1 is an eGene in GTEx v10 — its expression is genetically regulated (eQTL) in 23 tissues and its splicing (sQTL) in 1 (q < 0.05). Strongest associations first; slope = normalized effect of the lead variant’s alternative allele.
showing 20 of 24 significant tissue × QTL associations:
| Tissue | QTL | q-value | Slope | Lead variant |
|---|---|---|---|---|
| Cells Cultured fibroblasts | eqtl | 6.9e-42 | -0.68 | 1:100725310:A:C |
| Skin Sun Exposed Lower leg | eqtl | 7.7e-15 | -0.28 | 1:100725310:A:C |
| Skin Not Sun Exposed Suprapubic | eqtl | 8.7e-10 | -0.24 | 1:100721765:C:T |
| Breast Mammary Tissue | eqtl | 1.6e-07 | +0.25 | 1:100695695:G:A |
| Esophagus Mucosa | eqtl | 1.9e-07 | -0.19 | 1:100725310:A:C |
| Thyroid | eqtl | 2.5e-07 | -0.23 | 1:100721765:C:T |
| Nerve Tibial | eqtl | 6.7e-07 | -0.28 | 1:100691849:C:T |
| Whole Blood | eqtl | 1.2e-05 | -0.19 | 1:100698224:G:A |
| Adipose Subcutaneous | eqtl | 1.3e-05 | -0.23 | 1:100721765:C:T |
| Colon Transverse | eqtl | 9.5e-05 | +0.16 | 1:100589446:G:A |
| Pituitary | eqtl | 2.2e-04 | -0.27 | 1:100725310:A:C |
| Minor Salivary Gland | eqtl | 4.7e-04 | -0.40 | 1:100603549:C:T |
| Pancreas | eqtl | 7.3e-04 | +0.18 | 1:100669621:A:G |
| Esophagus Muscularis | eqtl | 3.3e-03 | -0.16 | 1:100525823:C:T |
| Brain Putamen basal ganglia | eqtl | 3.7e-03 | +0.27 | 1:100571457:G:GTGGTA |
| Colon Sigmoid | eqtl | 7.9e-03 | -0.15 | 1:100623936:A:C |
| Heart Left Ventricle | eqtl | 9.8e-03 | +0.20 | 1:100300140:T:C |
| Spleen | eqtl | 1.3e-02 | -0.17 | 1:101224714:A:G |
| Brain Caudate basal ganglia | eqtl | 1.3e-02 | -0.26 | 1:100605485:A:C |
| Prostate | eqtl | 1.8e-02 | -0.23 | 1:100703651:A:G |
FANTOM5 promoters
1 alternative TSS:
| Promoter ID | TPM avg | Samples expressed |
|---|---|---|
| 4248 | 14.7029 | 928 |
Top tissues by expression
showing 100 of 287 tissues by Bgee expression score (0-100, higher = more expressed):
| Tissue | Anatomy ID | Expression score | Quality |
|---|---|---|---|
| cartilage tissue | UBERON:0002418 | 99.13 | gold quality |
| trabecular bone tissue | UBERON:0002483 | 98.99 | gold quality |
| parietal pleura | UBERON:0002400 | 98.23 | gold quality |
| vena cava | UBERON:0004087 | 98.08 | gold quality |
| tendon of biceps brachii | UBERON:0008188 | 98.08 | gold quality |
| spleen | UBERON:0002106 | 97.98 | gold quality |
| adrenal tissue | UBERON:0018303 | 97.94 | gold quality |
| renal glomerulus | UBERON:0000074 | 97.91 | gold quality |
| metanephric glomerulus | UBERON:0004736 | 97.80 | gold quality |
| synovial joint | UBERON:0002217 | 97.38 | gold quality |
| nephron tubule | UBERON:0001231 | 97.34 | gold quality |
| pleura | UBERON:0000977 | 97.21 | gold quality |
| kidney epithelium | UBERON:0004819 | 97.14 | gold quality |
| lymph node | UBERON:0000029 | 96.63 | gold quality |
| decidua | UBERON:0002450 | 96.19 | gold quality |
| layer of synovial tissue | UBERON:0007616 | 95.41 | gold quality |
| visceral pleura | UBERON:0002401 | 95.40 | gold quality |
| epithelium of nasopharynx | UBERON:0001951 | 95.16 | gold quality |
| nasopharynx | UBERON:0001728 | 95.15 | gold quality |
| germinal epithelium of ovary | UBERON:0001304 | 95.05 | gold quality |
| choroid plexus epithelium | UBERON:0003911 | 94.62 | gold quality |
| kidney | UBERON:0002113 | 93.36 | gold quality |
| metanephros | UBERON:0000081 | 93.25 | gold quality |
| adult mammalian kidney | UBERON:0000082 | 93.20 | gold quality |
| vermiform appendix | UBERON:0001154 | 93.11 | gold quality |
| adrenal gland | UBERON:0002369 | 92.76 | gold quality |
| mucosa of urinary bladder | UBERON:0001259 | 92.64 | gold quality |
| cortex of kidney | UBERON:0001225 | 92.43 | gold quality |
| colonic epithelium | UBERON:0000397 | 92.33 | gold quality |
| ventricular zone | UBERON:0003053 | 92.26 | gold quality |
| left adrenal gland | UBERON:0001234 | 91.97 | gold quality |
| right adrenal gland | UBERON:0001233 | 91.96 | gold quality |
| gall bladder | UBERON:0002110 | 91.60 | gold quality |
| pericardium | UBERON:0002407 | 91.52 | gold quality |
| adrenal cortex | UBERON:0001235 | 91.22 | gold quality |
| right adrenal gland cortex | UBERON:0035827 | 91.11 | gold quality |
| caecum | UBERON:0001153 | 91.06 | gold quality |
| tibia | UBERON:0000979 | 91.00 | gold quality |
| left adrenal gland cortex | UBERON:0035825 | 90.74 | gold quality |
| tonsil | UBERON:0002372 | 90.62 | gold quality |
| epithelial cell of pancreas | CL:0000083 | 90.52 | gold quality |
| placenta | UBERON:0001987 | 90.11 | gold quality |
| tendon | UBERON:0000043 | 89.62 | gold quality |
| rectum | UBERON:0001052 | 89.59 | gold quality |
| metanephros cortex | UBERON:0010533 | 88.93 | gold quality |
| mucosa of sigmoid colon | UBERON:0004993 | 88.84 | gold quality |
| islet of Langerhans | UBERON:0000006 | 88.69 | gold quality |
| omental fat pad | UBERON:0010414 | 88.53 | gold quality |
| peritoneum | UBERON:0002358 | 88.48 | gold quality |
| right ovary | UBERON:0002118 | 88.39 | gold quality |
| calcaneal tendon | UBERON:0003701 | 88.33 | gold quality |
| adipose tissue of abdominal region | UBERON:0007808 | 87.90 | gold quality |
| superficial temporal artery | UBERON:0001614 | 87.70 | gold quality |
| left ovary | UBERON:0002119 | 87.29 | gold quality |
| ovary | UBERON:0000992 | 87.13 | gold quality |
| urethra | UBERON:0000057 | 86.37 | gold quality |
| thoracic mammary gland | UBERON:0005200 | 86.36 | gold quality |
| mammary gland | UBERON:0001911 | 86.18 | gold quality |
| urinary bladder | UBERON:0001255 | 85.67 | gold quality |
| thymus | UBERON:0002370 | 85.59 | gold quality |
| ileal mucosa | UBERON:0000331 | 85.49 | gold quality |
| epithelium of mammary gland | UBERON:0003244 | 85.42 | gold quality |
| periodontal ligament | UBERON:0008266 | 85.41 | gold quality |
| mammary duct | UBERON:0001765 | 85.31 | gold quality |
| mucosa of paranasal sinus | UBERON:0005030 | 85.00 | gold quality |
| colonic mucosa | UBERON:0000317 | 84.87 | gold quality |
| trigeminal ganglion | UBERON:0001675 | 84.68 | gold quality |
| right coronary artery | UBERON:0001625 | 84.59 | gold quality |
| liver | UBERON:0002107 | 84.36 | gold quality |
| connective tissue | UBERON:0002384 | 84.18 | gold quality |
| adipose tissue | UBERON:0001013 | 83.81 | gold quality |
| pylorus | UBERON:0001166 | 83.55 | gold quality |
| endothelial cell | CL:0000115 | 83.52 | silver quality |
| cranial nerve II | UBERON:0000941 | 83.26 | gold quality |
| bone element | UBERON:0001474 | 83.13 | gold quality |
| pancreas | UBERON:0001264 | 83.12 | gold quality |
| renal medulla | UBERON:0000362 | 83.08 | gold quality |
| coronary artery | UBERON:0001621 | 82.98 | gold quality |
| descending thoracic aorta | UBERON:0002345 | 82.86 | gold quality |
| saphenous vein | UBERON:0007318 | 82.82 | gold quality |
| ascending aorta | UBERON:0001496 | 82.81 | gold quality |
| male germ line stem cell (sensu Vertebrata) in testis | CL:0000089 ∩ UBERON:0000473 | 82.62 | gold quality |
| thoracic aorta | UBERON:0001515 | 82.51 | gold quality |
| skin of hip | UBERON:0001554 | 82.51 | gold quality |
| left coronary artery | UBERON:0001626 | 82.44 | gold quality |
| cauda epididymis | UBERON:0004360 | 82.26 | gold quality |
| subcutaneous adipose tissue | UBERON:0002190 | 82.22 | gold quality |
| jejunal mucosa | UBERON:0000399 | 82.07 | gold quality |
| ganglionic eminence | UBERON:0004023 | 81.51 | gold quality |
| dorsal motor nucleus of vagus nerve | UBERON:0002870 | 81.41 | gold quality |
| olfactory segment of nasal mucosa | UBERON:0005386 | 81.23 | gold quality |
| duodenum | UBERON:0002114 | 81.09 | gold quality |
| sigmoid colon | UBERON:0001159 | 80.47 | gold quality |
| aorta | UBERON:0000947 | 80.34 | gold quality |
| type B pancreatic cell | CL:0000169 | 80.15 | silver quality |
| left uterine tube | UBERON:0001303 | 79.93 | gold quality |
| tibial nerve | UBERON:0001323 | 79.60 | gold quality |
| oral cavity | UBERON:0000167 | 79.56 | gold quality |
| seminal vesicle | UBERON:0000998 | 79.43 | gold quality |
| artery | UBERON:0001637 | 79.24 | gold quality |
Single-cell (SCXA)
Detected in 12 experiment(s), a significant marker in 11.
| Experiment | Marker? | Max mean expression |
|---|---|---|
| E-MTAB-8322 | yes | 1536.75 |
| E-MTAB-7407 | yes | 597.59 |
| E-ANND-5 | yes | 582.58 |
| E-GEOD-135922 | yes | 33.99 |
| E-HCAD-4 | yes | 24.46 |
| E-MTAB-10553 | yes | 23.55 |
| E-ANND-3 | yes | 23.25 |
| E-HCAD-9 | yes | 19.88 |
| E-GEOD-93593 | yes | 14.84 |
| E-GEOD-83139 | yes | 13.16 |
| E-CURD-112 | yes | 11.19 |
| E-GEOD-124858 | no | 807.76 |
HPA expression
RNA tissue specificity: Tissue enriched
showing 60 of 76 HPA tissues / cells by nTPM:
| Tissue / cell | Axis | nTPM | Protein (IHC) |
|---|---|---|---|
| Spleen | tissue | 366.8 | medium |
| Lymph node | tissue | 90.1 | low |
| Spinal cord | tissue | 84.0 | |
| Tonsil | tissue | 71.2 | medium |
| Substantia nigra | tissue | 69.4 | |
| Urinary bladder | tissue | 67.7 | not detected |
| Thalamus | tissue | 63.7 | |
| Medulla oblongata | tissue | 59.9 | |
| Midbrain | tissue | 58.0 | |
| Pons | tissue | 57.8 | |
| Periaqueductal gray | tissue | 55.9 | |
| Superior colliculi | tissue | 55.8 | |
| Kidney | tissue | 55.4 | high |
| Hypothalamus | tissue | 55.1 | |
| Septum | tissue | 52.9 | |
| Ovary | tissue | 50.4 | not detected |
| Corpus callosum | tissue | 46.3 | |
| Hippocampal formation | tissue | 42.4 | |
| Liver | tissue | 40.8 | not detected |
| Adrenal gland | tissue | 40.8 | not detected |
| Placenta | tissue | 40.6 | not detected |
| Putamen | tissue | 39.3 | |
| Ventral forebrain | tissue | 35.7 | |
| Amygdala | tissue | 35.0 | |
| Prefrontal cortex | tissue | 33.2 | |
| Cerebral cortex | tissue | 33.2 | not detected |
| Entorhinal cortex | tissue | 33.1 | |
| Appendix | tissue | 32.8 | low |
| Caudate putamen | tissue | 32.6 | |
| Motor cortex | tissue | 32.5 | |
| Retrosplenial cortex | tissue | 31.5 | |
| Basal ganglia | tissue | 29.7 | not detected |
| Retrosplenial and cingulate cortex | tissue | 29.7 | |
| Temporal cortex | tissue | 29.5 | |
| Insular cortex | tissue | 29.0 | |
| Gallbladder | tissue | 27.7 | not detected |
| Frontal cortex | tissue | 27.4 | |
| Occipital cortex | tissue | 27.0 | |
| Somatosensory cortex | tissue | 26.3 | |
| Thymus | tissue | 22.9 | |
| Rectum | tissue | 22.1 | not detected |
| Olfactory bulb | tissue | 20.7 | |
| Adipose tissue | tissue | 20.4 | not detected |
| Parathyroid gland | tissue | 17.3 | not detected |
| Duodenum | tissue | 14.5 | not detected |
| Breast | tissue | 14.1 | not detected |
| Colon | tissue | 14.0 | not detected |
| Stomach 1 | tissue | 13.6 | not detected |
| Small intestine | tissue | 13.5 | not detected |
| Pancreas | tissue | 12.5 | not detected |
| Cerebellum | tissue | 11.7 | not detected |
| Lung | tissue | 10.7 | not detected |
| Smooth muscle | tissue | 10.3 | not detected |
| Choroid plexus | tissue | 10.3 | |
| Locus coeruleus | tissue | 9.2 | |
| Prostate | tissue | 9.1 | not detected |
| Endometrium 1 | tissue | 8.8 | not detected |
| Salivary gland | tissue | 8.2 | not detected |
| Bone marrow | tissue | 7.9 | not detected |
| Esophagus | tissue | 7.2 | not detected |
Brain sub-regions (HPA Brain Atlas): detected in 189; highest nTPM — Ventral spinal cord (84.0), Dorsal spinal cord (74.1), White matter (46.3), Dorsal hippocampus (42.4), Subiculum (38.6).
Regulation
Is transcription factor: no
Upstream regulators (CollecTRI, top): AP1, APLNR, AR, CLOCK, CREB1, EP300, EPAS1, FLCN, FOS, FOXC1, FOXO1, GATA2, GATA3, GATA4, GATA6, HDAC4, HOXA9, ID3, IKBKB, IL1B, IRF1, IRF2, IRF6, JUN, KLF4, MYC, NFATC1, NFE2L2, NFKB1, NFKB2, NFKB, NFKBIA, NFKBID, NR4A3, PARP1, PGR, POU2F1, PPARA, PPARD, PPARG
miRNA regulators (miRDB)
Targeting VCAM1 by miRDB confidence (max_score; target_count = how many genes the miRNA targets in total — lower means more specific).
showing 30 of 49 miRNAs:
| miRNA | Max score | Avg score | miRNA target_count |
|---|---|---|---|
| HSA-MIR-3163 | 100.00 | 77.23 | 8605 |
| HSA-MIR-4692 | 100.00 | 67.32 | 2066 |
| HSA-MIR-3925-3P | 100.00 | 69.95 | 1237 |
| HSA-MIR-4262 | 100.00 | 73.26 | 3931 |
| HSA-MIR-4282 | 99.99 | 75.36 | 6408 |
| HSA-MIR-4514 | 99.99 | 67.10 | 1870 |
| HSA-MIR-1185-1-3P | 99.98 | 71.04 | 2593 |
| HSA-MIR-1185-2-3P | 99.98 | 71.04 | 2593 |
| HSA-LET-7F-2-3P | 99.98 | 70.98 | 2588 |
| HSA-MIR-4775 | 99.98 | 75.00 | 6394 |
| HSA-MIR-507 | 99.97 | 70.11 | 1915 |
| HSA-MIR-590-3P | 99.96 | 74.34 | 6478 |
| HSA-MIR-557 | 99.96 | 70.01 | 1640 |
| HSA-MIR-545-3P | 99.95 | 70.74 | 2783 |
| HSA-LET-7C-3P | 99.95 | 73.42 | 2862 |
| HSA-MIR-9902 | 99.89 | 69.15 | 2250 |
| HSA-MIR-95-5P | 99.89 | 72.17 | 3973 |
| HSA-MIR-7845-5P | 99.88 | 64.88 | 771 |
| HSA-MIR-4503 | 99.85 | 71.45 | 1869 |
| HSA-MIR-202-3P | 99.84 | 71.41 | 1290 |
| HSA-MIR-3180-5P | 99.82 | 69.12 | 2422 |
| HSA-MIR-4799-5P | 99.82 | 70.60 | 2663 |
| HSA-MIR-3121-3P | 99.82 | 71.96 | 3630 |
| HSA-MIR-6739-5P | 99.80 | 67.87 | 2806 |
| HSA-MIR-4766-5P | 99.75 | 69.23 | 2662 |
| HSA-MIR-6733-5P | 99.74 | 67.94 | 2759 |
| HSA-MIR-12129 | 99.72 | 67.45 | 1311 |
| HSA-MIR-5580-3P | 99.70 | 69.41 | 2052 |
| HSA-MIR-548AU-3P | 99.70 | 68.22 | 1373 |
| HSA-MIR-1284 | 99.67 | 73.56 | 1353 |
Functional genomics
gnomAD constraint: pLI 4.18e-09, LOEUF 0.837, missense Z 1.45 — population loss-of-function intolerance (pLI ≥ 0.9 = LoF-intolerant; lower LOEUF = more constrained). gnomAD
Regional missense constraint (gnomAD RMC): no regional variation along ENST00000294728 — one region, missense o/e 0.91.
Literature-anchored findings (GeneRIF, showing 40)
- Premature labor is associated with up-regulation of adhesion molecules in the lower uterine segment (PMID:11776680)
- Soluble VCAM-1 is a very early marker of endothelial cell activation in cardiopulmonary bypass. (PMID:11817523)
- significant increase in plasma levels between day 1 and day 5 of G-CSF-induced stem cell mobilization; possible effect on leukocyte-endothelial cell interactions (PMID:11847011)
- Testosterone attenuates expression of vascular cell adhesion molecule-1 by conversion to estradiol by aromatase in endothelial cells: implications in atherosclerosis (PMID:11904449)
- Elevated soluble CD40 ligand is related to the endothelial adhesion molecules in patients with acute coronary syndrome. (PMID:11922919)
- Human mast cell progenitors use alpha4-integrin, VCAM-1, and PSGL-1, E-selectin for adhesive interactions with human vascular endothelium under flow conditions (PMID:11929779)
- relation between glycemic control, hyperinsulinism and plasma concentration in patients with glucosse intolerance or NIDDM (PMID:11935152)
- Results suggest that exogenous NO inhibits VCAM-1 expression via suppression of NF-kappaB through a cGMP-independent pathway. (PMID:11961404)
- women with stage III and IV endometriosis had higher serum concentrations of soluble VCAM-1, lower serum concentration of soluble ICAM-1 (PMID:11963839)
- The tumor necrosis factor-alpha-stimulated redox-sensitive vascular cell adhesion molecule-1 selective signaling pathway in endothelial cells depends upon isoprenylcysteine carboxyl methyltransferase as a critical component. (PMID:12006387)
- During leukocyte adhesion VCAM-1, ICAM-1, and activated moesin and ezrin clustered in an endothelial actin-rich docking structure that anchored and partially embraced the leukocyte containing other cytoskeletal components (PMID:12082081)
- the preferential expression of VCAM-1 on the endothelium of femoral and iliac arteries in thromboangiitis obliterans (PMID:12086338)
- VCAM-1/alpha4 integrin interactions mediate monocyte adhesion to human saphenous vein (PMID:12097820)
- signal transduction pathways involved in rheumatoid arthritis synovial fibroblast interleukin-18-induced vascular cell adhesion molecule-1 expression (PMID:12105209)
- VCAM-1 expression via effects on interferon regulatory factor-1 expression and activity (PMID:12115600)
- E-selectin, intercellular adhesion molecule-1 (ICAM-1), and vascular adhesion molecule-1 (VCAM-1) were measured in serum from hypertensive patients with LV hypertrophy (PMID:12172318)
- Downregulation of vcam-1 is associated with nodal metastasis in breast cancer (PMID:12172576)
- Synchronized human hematopoietic progenitor cell adhesion fluctuates reversibly during cell cycle transit in ex vivo culture (PMID:12351381)
- induction by tumor necrosis factor alpha (PMID:12387879)
- Of the 10 candidate SNPs analyzed in this pilot study, the variant allele of the nonsynonymous SNP, VCAM1 G1238C, may be associated with protection from stroke. (PMID:12393616)
- Relationship between pathological changes and the expression of vascular cell adhesion molecule-1 in the placenta of patients with pregnancy-induced hypertension complicated by intrauterine growth retardation (PMID:12433638)
- VCAM1 stimulation by thrombin in endothelial cells is mediated by protein kinase C-delta-NF-kappa B and PKC-zeta-GATA signaling pathways (PMID:12493764)
- VCAM1 expression is induced by p38-mediated TNFalpha and suppressed by JNK in human cells (PMID:12587980)
- In adults with sickle cell disease, steady-state serum sVCAM-1 levels do not seem to reflect clinical disease severity, but may reflect bone marrow activity in SCD, underlying the pleiotropic nature of adhesion molecules in vivo. (PMID:12601490)
- Strongly expressed in histological type II of rheumatoid arthritis. (PMID:12643440)
- Crosslinking of CD44 on osteoblastic cells with specific antibodies augmented the expression of intercellular adhesion molecule (ICAM)-1 and vascular cell adhesion molecule (VCAM)-1 (PMID:12650924)
- Endothelial cells have increased expression of VCAM-1, E-selectin, and ICAM-1 when exposed to sickle blood cells. (PMID:12673844)
- VCAM-1-induced, Rac-dependent signaling plays a key role in the modulation of vascular-endothelial cadherin-mediated endothelial cell-cell adhesion and leukocyte extravasation. (PMID:12700137)
- regulation of expression in osteoblasts by interleukin 13 (PMID:12704784)
- a novel role for the P2Y2 receptor in the p38- and Rho kinase-dependent expression of VCAM-1 that mediates the recruitment of monocytes by vascular endothelium associated with the development of atherosclerosis (PMID:12714597)
- Soluble VCAM-1 markedly enhances phosphorylation of both p38 and focal adhesion kinase, but not ERK1/2, in endothelial cells, endothelial cell migration activity in vitro, and neovascularization in Matrigel in vivo. (PMID:12759453)
- Extravasated and oxidized LDL in xanthoma adds to foam cell recruitment by activating tyrosine kinase and inducing adhesion of monocytes to dermal microvascular endothelial cells through VCAM-1 and E-selectin. (PMID:12788528)
- Blood levels do not differ in normal and coronary artery disease patients. (PMID:12940514)
- During infusion of triacylglycerol, PAI-1 increased to approximately 2.6 fold higher levels while tPA and adipsin were unaffected; changes in sVCAM-1 were significantly correlated with those seen for PAI-1. (PMID:12958610)
- presence of vascular cell adhesion molecule (VCAM-1) in placental villi is specific to developmental stage, and it is decreased in fetal growth restriction which could be attributed to the uteroplacental deficiency (PMID:12969778)
- Adrenomedullin and ACTH induce cell surface expression of adhesion molecules E-selectin, VCAM-1, and ICAM-1 on human umbilical vein endothelial cells. (PMID:14534081)
- 11,12-EET analogues were synthesized and compared using a human endothelial cell based TNF-alpha-induced VCAM-1 expression assay. (PMID:14592496)
- Novel androgen receptor/NF-kappaB mediated mechanism for VCAM-1 expression and monocyte adhesion operating in male endothelial cells that may represent an important unrecognized mechanism for the male predisposition to atherosclerosis. (PMID:14684616)
- study demonstrates that overexpression of RORalpha1 and RORalpha4 inhibits TNF-alpha induced expression of VCAM-1 and ICAM-1 in human umbilical vein endothelial cells by inhibiting the NF-B signaling pathway (PMID:14741380)
- sVCAM-1 was associated with dengue disease severity and the time post infection; a significant difference was found in the plasma levels of sVCAM-1 between dengue shock syndrome and dengue fever patients (PMID:14748068)
Cross-species orthologs
5 orthologs
| Organism | Symbol | Gene ID |
|---|---|---|
| danio_rerio | vcam1b | ENSDARG00000062479 |
| mus_musculus | Vcam1 | ENSMUSG00000027962 |
| rattus_norvegicus | Vcam1 | ENSRNOG00000014333 |
| caenorhabditis_elegans | WBGENE00007736 | |
| caenorhabditis_elegans | WBGENE00011418 |
Paralogs (36): CNTN1 (ENSG00000018236), CDON (ENSG00000064309), NEO1 (ENSG00000067141), SDK2 (ENSG00000069188), IGSF9B (ENSG00000080854), IGSF9 (ENSG00000085552), NRCAM (ENSG00000091129), MXRA5 (ENSG00000101825), IGDCC4 (ENSG00000103742), CNTN3 (ENSG00000113805), IGSF21 (ENSG00000117154), CNTN6 (ENSG00000134115), CHL1 (ENSG00000134121), PTPRQ (ENSG00000139304), CNTN4 (ENSG00000144619), BOC (ENSG00000144857), SDK1 (ENSG00000146555), HMCN2 (ENSG00000148357), NCAM1 (ENSG00000149294), CNTN5 (ENSG00000149972), IGSF10 (ENSG00000152580), ROBO4 (ENSG00000154133), ROBO3 (ENSG00000154134), NCAM2 (ENSG00000154654), NFASC (ENSG00000163531), PRTG (ENSG00000166450), ROBO1 (ENSG00000169855), DSCAM (ENSG00000171587), IGDCC3 (ENSG00000174498), VSIG10 (ENSG00000176834), DSCAML1 (ENSG00000177103), CNTN2 (ENSG00000184144), ROBO2 (ENSG00000185008), VSIG10L (ENSG00000186806), DCC (ENSG00000187323), L1CAM (ENSG00000198910)
Mouse-model phenotypes
Observed phenotypes of the mouse ortholog (MGI:98926) from MGI (Alliance of Genome Resources) — knockout/mutant phenotypes, ranked by annotation count. 44 distinct phenotype terms.
| Mouse phenotype (MP) | Records |
|---|---|
| increased leukocyte cell number | 3 |
| decreased bone marrow cell number | 3 |
| abnormal interventricular septum morphology | 2 |
| decreased embryo size | 2 |
| disorganized myocardium | 2 |
| abnormal bone marrow cell morphology/development | 2 |
| abnormal blood cell morphology/development | 2 |
| abnormal chorioallantoic fusion | 2 |
| increased B cell number | 2 |
| decreased B cell number | 2 |
| pericardial effusion | 2 |
| increased immature B cell number | 2 |
| thin ventricle myocardium compact layer | 2 |
| embryonic lethality during organogenesis, complete penetrance | 2 |
| increased monocyte cell number | 1 |
| spleen hyperplasia | 1 |
| decreased body weight | 1 |
| abnormal allantois morphology | 1 |
| abnormal humoral immune response | 1 |
| postnatal lethality | 1 |
| abnormal extraembryonic tissue morphology | 1 |
| abnormal cardiovascular system morphology | 1 |
| abnormal epicardium morphology | 1 |
| abnormal lymphocyte physiology | 1 |
| abnormal CD8-positive, alpha-beta T cell physiology | 1 |
+19 more (showing top 25).
Additional cross-species homologs
Sequence homologs in species beyond Ensembl Compara’s model organisms, by Diamond local protein alignment (% sequence identity; best hit per species). Lower-identity rows are more distant homologs. The matched accessions’ gene symbols aren’t in biobtree yet, so each row shows the UniProt accession.
| Organism | UniProt | Identity | Method |
|---|---|---|---|
| Canis lupus familiaris | Q28260 | 81.1% | Diamond |
| Bos taurus | Q29RR6 | 75.2% | Diamond |
| Gallus gallus | Q03696 | 50.0% | Diamond |
| Drosophila melanogaster | Q9I7U4 | 37.4% | Diamond |
Genomic neighbors (locus context)
Genes flanking this one on the chromosome (NCBI/Entrez gene neighborhood). Positional context only — some neighbors share regulatory elements (bidirectional promoters, antisense/overlapping transcripts), but chromosomal adjacency is not itself a functional relationship (see Interactions for that).
| Symbol | Type | Entrez |
|---|---|---|
| LINC01349 | ncRNA | 100128787 |
| DPH5-DT | ncRNA | 102606465 |
| SLC30A7 | protein-coding | 148867 |
| EXTL2 | protein-coding | 2135 |
| DPH5 | protein-coding | 51611 |
Protein
Protein identifiers
Vascular cell adhesion protein 1 — P19320 (reviewed: P19320)
Alternative names: INCAM-100
All UniProt accessions (3): P19320, A0A3B3ISS8, E9PDD2
UniProt curated annotations — full annotation on UniProt →
Function. Cell adhesion glycoprotein predominantly expressed on the surface of endothelial cells that plays an important role in immune surveillance and inflammation. Acts as a major regulator of leukocyte adhesion to the endothelium through interaction with different types of integrins. During inflammatory responses, binds ligands on the surface of activated endothelial cells to initiate the activation of calcium channels and the plasma membrane-associated small GTPase RAC1 leading to leukocyte transendothelial migration. Also serves as a quality-control checkpoint for entry into bone marrow by providing a ‘don’t-eat-me’ stamping in the context of major histocompatibility complex (MHC) class-I presentation.
Subcellular location. Cell membrane Secreted.
Tissue specificity. Expressed on inflamed vascular endothelium, as well as on macrophage-like and dendritic cell types in both normal and inflamed tissue.
Post-translational modifications. Cleaved by the metalloproteinase ADAM17 to generate the soluble form. Sialoglycoprotein. Ubiquitinated by TRIM65 via ‘Lys-48’-linked ubiquitination; leading to proteasomal degradation.
Domain organisation. Either the first or the fourth Ig-like C2-type domain is required for VLA4-dependent cell adhesion.
Induction. By pro-inflammatory cytokines, including TNFalpha, and also by ROS, oxidized low density lipoprotein, high glucose concentration, toll-like receptor agonists, and shear stress.
Miscellaneous. Major isoform.
Isoforms (3)
| UniProt ID | Names | Canonical? |
|---|---|---|
| P19320-1 | 1, Long, VCAM-7D | yes |
| P19320-2 | 2, Short, VCAM-6D | |
| P19320-3 | 3 |
RefSeq proteins (3): NP_001069, NP_001186763, NP_542413 (=MANE)
Domains & families (InterPro)
| ID | Name | Type |
|---|---|---|
| IPR003598 | Ig_sub2 | Domain |
| IPR003599 | Ig_sub | Domain |
| IPR003987 | ICAM_VCAM_N | Domain |
| IPR003989 | VCAM-1 | Family |
| IPR007110 | Ig-like_dom | Domain |
| IPR008424 | Ig_C2-set | Domain |
| IPR013098 | Ig_I-set | Domain |
| IPR013106 | Ig_V-set | Domain |
| IPR013151 | Immunoglobulin_dom | Domain |
| IPR013783 | Ig-like_fold | Homologous_superfamily |
| IPR036179 | Ig-like_dom_sf | Homologous_superfamily |
| IPR047012 | ICAM_VCAM | Family |
Pfam: PF00047, PF05790, PF07679, PF13927
UniProt features (57 total): strand 15, domain 7, sequence variant 7, glycosylation site 6, disulfide bond 6, sequence conflict 3, helix 3, chain 2, splice variant 2, topological domain 2, mutagenesis site 2, signal peptide 1, transmembrane region 1
Structure
Experimental structures (PDB)
3 structures by resolution:
| PDB | Title | Method | Resolution (Å) |
|---|---|---|---|
| 1VCA | CRYSTAL STRUCTURE OF AN INTEGRIN-BINDING FRAGMENT OF VASCULAR CELL ADHESION MOLECULE-1 AT … | X-RAY DIFFRACTION | 1.8 |
| 1VSC | VCAM-1 | X-RAY DIFFRACTION | 1.9 |
| 1IJ9 | Highly Hydrated Human VCAM-1 Fragment | X-RAY DIFFRACTION | 3 |
Predicted structure (AlphaFold)
| Model | pLDDT | Fraction very-high |
|---|---|---|
| AF-P19320-F1 | 84.24 | 0.50 |
Human Protein Atlas
Protein class: CD markers, Predicted membrane proteins, Predicted secreted proteins, Plasma proteins, Cancer-related genes, Candidate cancer biomarkers
Protein evidence: Evidence at protein level
Subcellular location (HPA, imaging): cell junctions
Antibody reliability (HPA): IH enhanced · IF approved
Functional residue map
Curated UniProt residues grouped by drug-discovery relevance — catalytic, ligand-binding, modification, and mutation-validated positions. Source: UniProtKB sequence features.
Disulfide bonds (6)
| Type | Positions |
|---|---|
| Disulfide bond | 47–95, 52–99, 137–195, 246–291, 335–383, 534–579 |
Glycosylation sites (6)
| Type | Positions |
|---|---|
| N-linked (glcnac…) asparagine | 273, 365, 417, 463, 531, 561 |
Mutagenesis-validated functional residues (2)
| Position | Phenotype |
|---|---|
| 730 | loss of rac1 activation and subsequent leukocyte transmigration. |
| 737 | loss of rac1 activation and subsequent leukocyte transmigration. |
Function
Pathways and Gene Ontology
Reactome pathways
4 curated (TAS) of 11; 0 disease pathways. Curated-first; evidence = TAS (manually curated) vs IEA (electronic inference).
11 pathways:
| ID | Pathway | Evidence |
|---|---|---|
| R-HSA-198933 | Immunoregulatory interactions between a Lymphoid and a non-Lymphoid cell | curated |
| R-HSA-216083 | Integrin cell surface interactions | curated |
| R-HSA-877300 | Interferon gamma signaling | curated |
| R-HSA-6785807 | Interleukin-4 and Interleukin-13 signaling | curated |
| R-HSA-1280218 | Adaptive Immune System | — |
| R-HSA-9938027 | Affinity selection of immunoglobulins | electronic |
| R-HSA-1280215 | Cytokine Signaling in Immune system | — |
| R-HSA-1474244 | Extracellular matrix organization | — |
| R-HSA-168256 | Immune System | — |
| R-HSA-913531 | Interferon Signaling | — |
| R-HSA-449147 | Signaling by Interleukins | — |
MSigDB gene sets: 416 (showing top):
GSE45365_NK_CELL_VS_BCELL_UP, GOBP_REGULATION_OF_CELL_ACTIVATION, GOBP_RESPONSE_TO_NITROGEN_COMPOUND, GOBP_REGULATION_OF_LEUKOCYTE_PROLIFERATION, GOBP_RESPONSE_TO_ETHANOL, BERENJENO_ROCK_SIGNALING_NOT_VIA_RHOA_DN, GOBP_RESPONSE_TO_IONIZING_RADIATION, GOBP_RESPONSE_TO_ZINC_ION, GOBP_HETEROPHILIC_CELL_CELL_ADHESION, MCLACHLAN_DENTAL_CARIES_UP, GOBP_CELL_CHEMOTAXIS, REACTOME_ADAPTIVE_IMMUNE_SYSTEM, REACTOME_CYTOKINE_SIGNALING_IN_IMMUNE_SYSTEM, GOBP_INFLAMMATORY_RESPONSE, GOBP_RESPONSE_TO_PEPTIDE
GO Biological Process (27): response to hypoxia (GO:0001666), chronic inflammatory response (GO:0002544), inflammatory response (GO:0006954), cell adhesion (GO:0007155), heterophilic cell-cell adhesion (GO:0007157), leukocyte cell-cell adhesion (GO:0007159), cell-matrix adhesion (GO:0007160), response to nutrient (GO:0007584), amine metabolic process (GO:0009308), response to zinc ion (GO:0010043), response to ionizing radiation (GO:0010212), membrane to membrane docking (GO:0022614), B cell differentiation (GO:0030183), response to lipopolysaccharide (GO:0032496), cell-cell adhesion mediated by integrin (GO:0033631), heterotypic cell-cell adhesion (GO:0034113), response to nicotine (GO:0035094), cellular response to vascular endothelial growth factor stimulus (GO:0035924), positive regulation of T cell proliferation (GO:0042102), response to ethanol (GO:0045471), leukocyte tethering or rolling (GO:0050901), cell chemotaxis (GO:0060326), innervation (GO:0060384), cardiac neuron differentiation (GO:0060945), cellular response to tumor necrosis factor (GO:0071356), cellular response to amyloid-beta (GO:1904646), cell-cell adhesion (GO:0098609)
GO Molecular Function (4): integrin binding (GO:0005178), primary methylamine oxidase activity (GO:0008131), cell adhesion molecule binding (GO:0050839), cell adhesion mediator activity (GO:0098631)
GO Cellular Component (15): podosome (GO:0002102), early endosome (GO:0005769), endoplasmic reticulum (GO:0005783), Golgi apparatus (GO:0005794), plasma membrane (GO:0005886), microvillus (GO:0005902), external side of plasma membrane (GO:0009897), cell surface (GO:0009986), filopodium (GO:0030175), sarcolemma (GO:0042383), apical part of cell (GO:0045177), extracellular exosome (GO:0070062), alpha9-beta1 integrin-vascular cell adhesion molecule-1 complex (GO:0071065), extracellular region (GO:0005576), membrane (GO:0016020)
Reactome top-level categories
7 top-level categories:
| Category | Pathways |
|---|---|
| Immune System | 2 |
| Cytokine Signaling in Immune system | 2 |
| Adaptive Immune System | 1 |
| Extracellular matrix organization | 1 |
| Signaling by Interleukins | 1 |
| Interferon Signaling | 1 |
| Immunoglobulin maturation | 1 |
GO top-level categories
45 GO namespaces:
| Category | Terms |
|---|---|
| cell-cell adhesion | 4 |
| cellular anatomical structure | 4 |
| actin-based cell projection | 3 |
| response to chemical | 2 |
| cell adhesion molecule binding | 2 |
| cytoplasm | 2 |
| endomembrane system | 2 |
| intracellular membrane-bounded organelle | 2 |
| plasma membrane | 2 |
| response to stress | 1 |
| response to decreased oxygen levels | 1 |
| inflammatory response | 1 |
| defense response | 1 |
| cellular process | 1 |
| cell-substrate adhesion | 1 |
| response to nutrient levels | 1 |
| metabolic process | 1 |
| response to metal ion | 1 |
| response to radiation | 1 |
| membrane docking | 1 |
| lymphocyte differentiation | 1 |
| B cell activation | 1 |
| response to molecule of bacterial origin | 1 |
| response to lipid | 1 |
| response to oxygen-containing compound | 1 |
| cell adhesion mediated by integrin | 1 |
| cellular response to growth factor stimulus | 1 |
| T cell proliferation | 1 |
| regulation of T cell proliferation | 1 |
| positive regulation of lymphocyte proliferation | 1 |
| positive regulation of T cell activation | 1 |
| response to alcohol | 1 |
| signaling receptor binding | 1 |
| protein-containing complex binding | 1 |
| monoamine oxidase activity | 1 |
| protein binding | 1 |
| cell adhesion | 1 |
| endosome | 1 |
| membrane | 1 |
| cell periphery | 1 |
| actin filament bundle | 1 |
| cell surface | 1 |
| side of membrane | 1 |
| extracellular vesicle | 1 |
| plasma membrane protein complex | 1 |
Experimentally-supported GO annotations
GO terms backed by direct experimental evidence (ECO experimental codes) — 27 of 47 annotations. The rest are phylogenetic / computational / electronic (IEA).
27 experimentally-supported GO terms:
Protein interactions and networks
STRING
showing 15 of 4,000 interactions by confidence (×1000):
| Protein A | Protein B | Partner UniProt | Score |
|---|---|---|---|
| VCAM1 | ICAM1 | P05362 | 978 |
| VCAM1 | SELE | P16111 | 946 |
| VCAM1 | SELP | P16109 | 914 |
| VCAM1 | TNF | P01375 | 909 |
| VCAM1 | IL6 | P05231 | 898 |
| VCAM1 | CCL2 | P13500 | 867 |
| VCAM1 | IL1B | P01584 | 867 |
| VCAM1 | IFNG | P01579 | 832 |
| VCAM1 | IL1A | P01583 | 829 |
| VCAM1 | ITGA4 | P13612 | 820 |
| VCAM1 | ITGB2 | P05107 | 819 |
| VCAM1 | ITGB1 | P05556 | 806 |
| VCAM1 | VWF | P04275 | 801 |
| VCAM1 | NFKB1 | P19838 | 791 |
| VCAM1 | IL4 | P05112 | 790 |
IntAct
Human interaction partners of VCAM1 in IntAct, one row per partner (best MIscore; records = supporting IntAct interaction records).
5 partners by confidence:
| Partner | Interaction type | MIscore | Records |
|---|---|---|---|
| ITGB1 | association | 0.660 | 3 |
| PSMD11 | association | 0.530 | 1 |
| APOA1 | association | 0.350 | 1 |
| ATP1A3 | association | 0.350 | 1 |
| ATP2A1 | association | 0.350 | 1 |
BioGRID (494 interactions; top human partners by supporting records): MSN (Affinity Capture-Western; 4 records), TRIM65 (Affinity Capture-Western; 3 records), ACTB (Affinity Capture-MS; 2 records), BCS1L (Affinity Capture-MS; 2 records), EZR (Affinity Capture-Western; 2 records), ITGA4 (Affinity Capture-MS; 2 records), LGALS1 (Affinity Capture-MS; 2 records), NCL (Affinity Capture-MS; 2 records), PARP1 (Proximity Label-MS; 2 records), PODXL2 (Affinity Capture-MS; 2 records), PRKDC (Affinity Capture-MS; 2 records), SEMA4D (Affinity Capture-MS; 2 records), TUBA4A (Affinity Capture-MS; 2 records), VCP (Affinity Capture-Western; 2 records), VDAC1 (Affinity Capture-MS; 2 records)
SIGNOR signaling
3 signaling interactions:
| A | Effect | B | Mechanism |
|---|---|---|---|
| VCAM1 | “up-regulates activity” | “A4/b1 integrin” | binding |
| “AD/b2 integrin” | “up-regulates activity” | VCAM1 | binding |
| hsa-mir-126-5p | “down-regulates quantity by repression” | VCAM1 | “post transcriptional regulation” |
Protein complexes (CORUM) (3)
Experimentally-characterized complexes this protein is a subunit of (★ = the complex contains a known drug target).
3 complexes by size:
| Complex | Subunits | Members |
|---|---|---|
| ★ ITGA4-ITGB1-VCAM1 complex | 3 | ITGA4, ITGB1, VCAM1 |
| ★ ITGA9-ITGB1-VCAM1 complex | 3 | ITGB1, VCAM1, ITGA9 |
| ★ ITGA4-ITGAB7-VCAM1 complex | 3 | ITGB7, VCAM1, ITGA4 |
Ligand–receptor pairs (CellPhoneDB) (4)
Curated ligand–receptor partners (cell-cell communication), distinct from the protein–protein interactions above.
4 ligand–receptor pairs:
| Partner | This gene’s role | Signaling class |
|---|---|---|
| ITGB2;ITGAD | ligand | Adhesion by VCAM |
| ITGB1;ITGA9 | ligand | Adhesion by VCAM |
| ITGB7;ITGA4 | ligand | Adhesion by VCAM |
| ITGB1;ITGA4 | ligand | Adhesion by VCAM |
Disease & clinical
Genetic variants
Variant evidence for VCAM1: 101 ClinVar records (0 pathogenic / likely pathogenic); 8 GWAS associations.
ClinVar
101 variants total. Per-class counts are floors (≥ shown; pagination cap):
| Classification | Count (floor) |
|---|---|
| Pathogenic | 0 |
| Likely pathogenic | 0 |
| Uncertain significance | 81 |
| Likely benign | 13 |
| Benign | 1 |
SpliceAI
Top 10 splice-impact sites by Δscore (adjacent positions with the same effect merged into one range; 41 predictions of 687):
| Position(s) | Effect | Δscore | Sites |
|---|---|---|---|
| 1:100734769–100734770 | donor_loss | 1.0000 | 5 |
| 1:100720474–100720475 | acceptor_loss | 0.9900 | 4 |
| 1:100723214 | donor_gain | 0.9900 | |
| 1:100723341–100723342 | donor_loss | 0.9900 | 6 |
| 1:100723345 | donor_loss | 0.9900 | |
| 1:100724622–100724623 | acceptor_loss | 0.9900 | 6 |
| 1:100729095 | acceptor_gain | 0.9900 | |
| 1:100731196–100731197 | acceptor_loss | 0.9900 | 6 |
| 1:100731519–100731520 | donor_loss | 0.9900 | 5 |
| 1:100734500–100734501 | acceptor_loss | 0.9900 | 6 |
AlphaMissense
577 missense substitutions predicted likely pathogenic (of 4,860 scored), across 200 residues. Top 20 hotspot residues, ranked by the number of likely-pathogenic substitutions (of those reachable by a single-nucleotide change), then by mean score:
| Residue | Likely-pathogenic substitutions | Mean am_pathogenicity | Max am_pathogenicity |
|---|---|---|---|
| C95 | 7 | 0.969 | 0.990 |
| W59 | 7 | 0.961 | 0.994 |
| C291 | 7 | 0.956 | 0.981 |
| C47 | 7 | 0.954 | 0.979 |
| W347 | 7 | 0.945 | 0.989 |
| C483 | 7 | 0.942 | 0.977 |
| C579 | 7 | 0.941 | 0.972 |
| C195 | 7 | 0.938 | 0.979 |
| C425 | 7 | 0.938 | 0.968 |
| C246 | 7 | 0.933 | 0.979 |
| C668 | 7 | 0.931 | 0.977 |
| C137 | 7 | 0.930 | 0.986 |
| C623 | 7 | 0.929 | 0.970 |
| W258 | 7 | 0.914 | 0.982 |
| C534 | 7 | 0.904 | 0.967 |
| C383 | 7 | 0.897 | 0.960 |
| C335 | 7 | 0.891 | 0.964 |
| C52 | 7 | 0.872 | 0.924 |
| C99 | 7 | 0.820 | 0.888 |
| C340 | 7 | 0.796 | 0.863 |
HPA cancer prognostics
RNA cancer specificity: Group enriched (Kidney Renal Clear Cell Carcinoma, Kidney Renal Papillary Cell Carcinoma)
Human Protein Atlas survival analysis — favorable = higher expression predicts better survival.
2 prognostic cancer types:
| Cancer | Prognostic | p-value |
|---|---|---|
| Kidney Renal Clear Cell Carcinoma (TCGA) | favorable | 0.000186 |
| Head and Neck Squamous Cell Carcinoma (TCGA) | favorable | 0.000257 |
Disease associations
OMIM: gene MIM:192225 | disease phenotypes:
GWAS associations
8 associations:
| Study | Trait | p-value |
|---|---|---|
| GCST009597_229 | Multiple sclerosis | 1e-22 |
| GCST005531_104 | Multiple sclerosis | 2e-16 |
| GCST90002388_492 | Lymphocyte count | 3e-13 |
| GCST001198_27 | Multiple sclerosis | 3e-10 |
| GCST90002389_341 | Lymphocyte percentage of white cells | 1e-9 |
| GCST90002399_94 | Neutrophil percentage of white cells | 6e-9 |
| GCST001198_77 | Multiple sclerosis | 4e-8 |
| GCST005532_3 | Sjögren’s syndrome | 4e-6 |
EFO canonical traits (from GWAS)
3 canonical traits:
| EFO ID | Trait name |
|---|---|
| EFO:0004587 | lymphocyte count |
| EFO:0007993 | lymphocyte percentage of leukocytes |
| EFO:0007990 | neutrophil percentage of leukocytes |
Drugs & pharmacology
Drug and pharmacology data
Is drug target: yes
ChEMBL targets (1): CHEMBL3735 (SINGLE PROTEIN)
Molecules with ChEMBL bioactivity
Phase ≥1, by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 251 (via chembl_molecule»patent_compound — counts attach to the compound, not the gene–compound relationship, so off-target/promiscuous molecules can dominate).
1 molecules by phase:
| Molecule | Name | Phase | Patents |
|---|---|---|---|
| CHEMBL83626 | SUCCINOBUCOL | 3 | 251 |
PharmGKB: 1 entry (CPIC guideline: no)
Binding affinities (BindingDB)
206 measured of 228 human assays (229 total across all organisms); most potent 50 below. Values come from heterogeneous assays and are not directly comparable.
| Ligand | Measure | Value | Patent |
|---|---|---|---|
| 4-(4-Trifluoromethyl-phenoxy)-thieno[2,3-c]pyridine-2-carboxylic acid methylamide | IC50 | 0.7 nM | |
| 4-(4-Vinyl-phenoxy)-thieno[2,3-c]pyridine-2-carboxylic acid amide | IC50 | 1 nM | |
| 4-(4-Imidazol-1-yl-phenoxy)-thieno[2,3-c]pyridine-2-carboxylic acid methylamide | IC50 | 2 nM | |
| 4-[4-(Tetrahydro-pyran-2-yloxymethyl)-phenoxy]-thieno[2,3-c]pyridine-2-carboxylic acid amide | IC50 | 2 nM | |
| 4-(4-Cyano-phenoxy)-thieno[2,3-c]pyridine-2-carboxylic acid methylamide | IC50 | 2.8 nM | |
| 4-{4-[2-(2-Methoxy-ethoxy)-ethoxymethyl]-phenoxy}-thieno[2,3-c]pyridine-2-carboxylic acid methylamide | IC50 | 4 nM | |
| 4-(4-Bromo-phenoxy)-thieno[2,3-c]pyridine-2-carboxylic acid amide | IC50 | 4 nM | |
| 4-(4-Pyrazol-1-yl-phenoxy)-thieno[2,3-c]pyridine-2-carboxylic acid methylamide | IC50 | 4 nM | |
| 4-(4-Bromo-phenylsulfanyl)-thieno[2,3-c]pyridine-2-carboxylic acid amide | IC50 | 5 nM | |
| 4-(4-Thiophen-2-yl-phenoxy)-thieno[2,3-c]pyridine-2-carboxylic acid methylamide | IC50 | 5 nM | |
| 4-[4-(2-Methoxy-ethoxymethyl)-phenoxy]-thieno[2,3-c]pyridine-2-carboxylic acid amide | IC50 | 5 nM | |
| 4-(4-Furan-2-yl-phenoxy)-thieno[2,3-c]pyridine-2-carboxylic acid methylamide | IC50 | 5 nM | |
| 4-{4-[2-(2-Methoxy-ethoxy)-ethoxymethyl]-phenoxy}-thieno[2,3-c]pyridine-2-carboxylic acid amide | IC50 | 5 nM | |
| 4-(4-Cyano-phenoxy)-thieno[2,3-c]pyridine-2-carboxylic acid amide | IC50 | 5.1 nM | |
| 4-p-Tolyloxy-thieno[2,3-c]pyridine-2-carboxylic acid amide | IC50 | 6 nM | |
| 4-(4-Iodo-phenoxy)-thieno[2,3-c]pyridine-2-carboxylic acid amide | IC50 | 6 nM | |
| 4-(4-Imidazol-1-yl-phenoxy)-thieno[2,3-c]pyridine-2-carboxylic acid amide | IC50 | 6 nM | |
| 4-(4-Chloro-phenoxy)-thieno[2,3-c]pyridine-2-carboxylic acid amide | IC50 | 6.2 nM | |
| 4-(4-Bromo-phenoxy)-thieno[2,3-c]pyridine-2-carboxylic acid methylamide | IC50 | 7 nM | |
| 4-[4-(2-Methoxy-ethoxymethyl)-phenoxy]-thieno[2,3-c]pyridine-2-carboxylic acid methylamide | IC50 | 7 nM | |
| 4-(4-Chloro-3-fluoro-phenoxy)-thieno[2,3-c]pyridine-2-carboxylic acid amide | IC50 | 8 nM | |
| 4-(4-Chloro-phenoxy)-thieno[2,3-c]pyridine-2-carboxylic acid methylamide | IC50 | 8.2 nM | |
| 4-(Biphenyl-4-yloxy)-thieno[2,3-c]pyridine-2-carboxylic acid methylamide | IC50 | 9 nM | |
| 4-(4-Chloro-phenylsulfanyl)-thieno[2,3-c]pyridine-2-carboxylic acid amide | IC50 | 12 nM | |
| (2S)-2-[[2,6-difluoro-4-[[5-(1,2,4-triazol-1-yl)-2-pyridinyl]sulfonylamino]benzoyl]amino]-3-[4-(1-methyl-2,4-dioxo-4aH-pyrido[3,4-d]pyrimidin-1-ium-3-yl)phenyl]propanoic acid | IC50 | 13 nM | US-9533985: Sulfonamide derivative and medicinal use thereof |
| 4-(3,4-Dimethyl-phenylsulfanyl)-thieno[2,3-c]pyridine-2-carboxylic acid amide | IC50 | 13 nM | |
| 4-[4-(N-Hydroxycarbamimidoyl)-phenoxy]-thieno[2,3-c]pyridine-2-carboxylic acid methylamide | IC50 | 13 nM | |
| 4-(4-Methoxymethyl-phenoxy)-thieno[2,3-c]pyridine-2-carboxylic acid methylamide | IC50 | 13 nM | |
| 4-(4-Chloro-phenoxy)-thieno[2,3-c]pyridine-2-carboxylic acid ethylamide | IC50 | 16 nM | |
| 4-(4-Methoxymethyl-phenoxy)-thieno[2,3-c]pyridine-2-carboxylic acid amide | IC50 | 16 nM | |
| (2S)-2-[[2,6-difluoro-4-[(5-pyrimidin-5-yl-2-pyridinyl)sulfonylamino]benzoyl]amino]-3-[4-(1-methyl-2,4-dioxo-4a,5,6,7,8,8a-hexahydropyrido[3,4-d]pyrimidin-3-yl)phenyl]propanoic acid | IC50 | 18 nM | US-9533985: Sulfonamide derivative and medicinal use thereof |
| 4-(4-Cyano-phenoxy)-thieno[2,3-c]pyridine-2-carboxylic acid methylamide | IC50 | 18 nM | |
| 4-(4-Trifluoromethyl-phenoxy)-thieno[2,3-c]pyridine-2-carboxylic acid amide | IC50 | 19 nM | |
| 4-Phenylsulfanyl-thieno[2,3-c]pyridine-2-carboxylic acid amide | IC50 | 20 nM | |
| 4-(2-Carbamoyl-thieno[2,3-c]pyridin-4-yloxy)-benzoic acid ethyl ester | IC50 | 20 nM | |
| 4-(4-Acetyl-phenoxy)-thieno[2,3-c]pyridine-2-carboxylic acid methylamide | IC50 | 21 nM | |
| (2S)-2-[[2,6-difluoro-4-[[5-(1,3-thiazol-2-yl)-2-pyridinyl]sulfonylamino]benzoyl]amino]-3-[4-(1-methyl-2,4-dioxo-4aH-pyrido[3,4-d]pyrimidin-1-ium-3-yl)phenyl]propanoic acid | IC50 | 22 nM | US-9533985: Sulfonamide derivative and medicinal use thereof |
| (2S)-2-[[2,6-difluoro-4-[[5-(triazol-1-yl)-2-pyridinyl]sulfonylamino]benzoyl]amino]-3-[4-(1-methyl-2,4-dioxo-4a,5,6,7,8,8a-hexahydropyrido[3,4-d]pyrimidin-3-yl)phenyl]propanoic acid | IC50 | 22 nM | US-9533985: Sulfonamide derivative and medicinal use thereof |
| 4-(4-Hydroxymethyl-phenoxy)-thieno[2,3-c]pyridine-2-carboxylic acid methylamide | IC50 | 25 nM | |
| 4-[4-(3-Morpholin-4-yl-3-oxo-propenyl)-phenoxy]-thieno[2,3-c]pyridine-2-carboxylic acid amide | IC50 | 25 nM | |
| 4-(4-Methoxy-phenoxy)-thieno[2,3-c]pyridine-2-carboxylic acid amide | IC50 | 25 nM | |
| 4-(4-Hydroxymethyl-phenoxy)-thieno[2,3-c]pyridine-2-carboxylic acid amide | IC50 | 28 nM | |
| 4-[4-(5-Trifluoromethyl-[1,2,4]oxadiazol-3-yl)-phenoxy]-thieno[2,3-c]pyridine-2-carboxylic acid methylamide | IC50 | 28 nM | |
| 4-(4-Acetylamino-phenoxy)-thieno[2,3-c]pyridine-2-carboxylic acid amide | IC50 | 29 nM | |
| 4-(4-Ethyl-phenoxy)-thieno[2,3-c]pyridine-2-carboxylic acid amide | IC50 | 30 nM | |
| (2S)-2-[[2,6-difluoro-4-[[4-(1,2,3,6-tetrahydropyridin-4-yl)phenyl]sulfonylamino]benzoyl]amino]-3-[4-(1-methyl-2,4-dioxo-4aH-pyrido[3,4-d]pyrimidin-1-ium-3-yl)phenyl]propanoic acid | IC50 | 31 nM | US-9533985: Sulfonamide derivative and medicinal use thereof |
| 4-[4-(1-Hydroxymethyl-cyclopropyl)-phenoxy]-thieno[2,3-c]pyridine-2-carboxylic acid methylamide | IC50 | 31 nM | |
| 4-p-Tolylsulfanyl-thieno[2,3-c]pyridine-2-carboxylic acid hydrazide | IC50 | 32 nM | |
| 4-{4-[2-(2-Morpholin-4-yl-ethylcarbamoyl)-vinyl]-phenoxy}-thieno[2,3-c]pyridine-2-carboxylic acid amide | IC50 | 34 nM | |
| 4-(4-Morpholin-4-yl-phenoxy)-thieno[2,3-c]pyridine-2-carboxylic acid methylamide | IC50 | 35 nM |
ChEMBL bioactivities
68 potent at pChembl≥5 of 107 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).
| pChembl | Type | Value | Unit | Molecule |
|---|---|---|---|---|
| 8.30 | IC50 | 5 | nM | CHEMBL119039 |
| 8.22 | IC50 | 6 | nM | CHEMBL117894 |
| 8.15 | IC50 | 7 | nM | CHEMBL116070 |
| 8.10 | IC50 | 8 | nM | CHEMBL116070 |
| 7.77 | IC50 | 17 | nM | CHEMBL326120 |
| 7.72 | IC50 | 19 | nM | CHEMBL325184 |
| 7.70 | IC50 | 20 | nM | CHEMBL117279 |
| 7.70 | IC50 | 20 | nM | CHEMBL116070 |
| 7.64 | IC50 | 23 | nM | CHEMBL119183 |
| 7.52 | IC50 | 30 | nM | CHEMBL117279 |
| 7.32 | IC50 | 48 | nM | CHEMBL116070 |
| 7.19 | IC50 | 64 | nM | CHEMBL117936 |
| 7.16 | IC50 | 70 | nM | CHEMBL118074 |
| 7.13 | IC50 | 74 | nM | CHEMBL118089 |
| 7.10 | IC50 | 79 | nM | CHEMBL115637 |
| 7.07 | IC50 | 85 | nM | CHEMBL117198 |
| 7.04 | IC50 | 91 | nM | CHEMBL115971 |
| 6.92 | IC50 | 120 | nM | CHEMBL117279 |
| 6.89 | IC50 | 130 | nM | CHEMBL324133 |
| 6.85 | IC50 | 140 | nM | CHEMBL119732 |
| 6.77 | IC50 | 170 | nM | CHEMBL115431 |
| 6.76 | IC50 | 175 | nM | CHEMBL6248 |
| 6.72 | IC50 | 191 | nM | CHEMBL118022 |
| 6.70 | IC50 | 200 | nM | CHEMBL118074 |
| 6.62 | IC50 | 240 | nM | CHEMBL119705 |
| 6.48 | IC50 | 330 | nM | CHEMBL119599 |
| 6.43 | IC50 | 370 | nM | CHEMBL118300 |
| 6.38 | IC50 | 420 | nM | CHEMBL115960 |
| 6.33 | IC50 | 470 | nM | CHEMBL324824 |
| 6.11 | IC50 | 770 | nM | CHEMBL6830 |
| 6.11 | IC50 | 780 | nM | CHEMBL325286 |
| 6.07 | IC50 | 850 | nM | CHEMBL325893 |
| 6.06 | IC50 | 880 | nM | CHEMBL119523 |
| 6.03 | IC50 | 930 | nM | CHEMBL115462 |
| 5.89 | IC50 | 1300 | nM | CHEMBL6257 |
| 5.68 | IC50 | 2100 | nM | CHEMBL266572 |
| 5.64 | IC50 | 2300 | nM | CHEMBL266197 |
| 5.60 | IC50 | 2500 | nM | CHEMBL4166467 |
| 5.60 | IC50 | 2500 | nM | CHEMBL6229 |
| 5.57 | IC50 | 2700 | nM | CHEMBL6371 |
| 5.52 | IC50 | 3000 | nM | CHEMBL53269 |
| 5.46 | IC50 | 3500 | nM | CHEMBL267127 |
| 5.46 | IC50 | 3500 | nM | CHEMBL6249 |
| 5.41 | IC50 | 3900 | nM | CHEMBL118518 |
| 5.40 | IC50 | 4000 | nM | CHEMBL298775 |
| 5.35 | IC50 | 4500 | nM | CHEMBL4166036 |
| 5.30 | IC50 | 5000 | nM | CHEMBL53082 |
| 5.30 | IC50 | 5000 | nM | CHEMBL52799 |
| 5.30 | IC50 | 5000 | nM | CHEMBL51654 |
| 5.30 | IC50 | 5000 | nM | CHEMBL53475 |
PubChem BioAssay actives
68 with measured affinity, of 212 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 |
|---|---|---|---|---|
| N-methyl-4-(4-pyrazol-1-ylphenoxy)thieno[2,3-c]pyridine-2-carboxamide | 216483: Inhibition of VCAM-1 in human endothelial cells | ic50 | 0.0050 | uM |
| N-methyl-4-(4-thiophen-2-ylphenoxy)thieno[2,3-c]pyridine-2-carboxamide | 216483: Inhibition of VCAM-1 in human endothelial cells | ic50 | 0.0060 | uM |
| 4-(4-bromophenoxy)thieno[2,3-c]pyridine-2-carboxamide | 216486: In vitro inhibitory potency compared to IL1-beta induced VCAM-1 in human endothelial cells (ELISA assay) | ic50 | 0.0070 | uM |
| 4-(4-imidazol-1-ylphenoxy)thieno[2,3-c]pyridine-2-carboxamide | 216483: Inhibition of VCAM-1 in human endothelial cells | ic50 | 0.0170 | uM |
| 4-(4-imidazol-1-ylphenoxy)-N-methylthieno[2,3-c]pyridine-2-carboxamide | 216483: Inhibition of VCAM-1 in human endothelial cells | ic50 | 0.0190 | uM |
| 4-[4-[2-(2-methoxyethoxy)ethoxymethyl]phenoxy]-N-methylthieno[2,3-c]pyridine-2-carboxamide | 216486: In vitro inhibitory potency compared to IL1-beta induced VCAM-1 in human endothelial cells (ELISA assay) | ic50 | 0.0200 | uM |
| 4-[4-(methoxymethyl)phenoxy]thieno[2,3-c]pyridine-2-carboxamide | 216483: Inhibition of VCAM-1 in human endothelial cells | ic50 | 0.0230 | uM |
| 4-(4-aminophenoxy)thieno[2,3-c]pyridine-2-carboxamide | 216483: Inhibition of VCAM-1 in human endothelial cells | ic50 | 0.0640 | uM |
| 4-(4-chlorophenoxy)-N-methylthieno[2,3-c]pyridine-2-carboxamide | 216485: In vitro inhibitory potency compared to IL1-beta induced VCAM-1 expression in human endothelial cells (ELISA assay) | ic50 | 0.0700 | uM |
| 4-[4-[1-(hydroxymethyl)cyclopropyl]phenoxy]-N-methylthieno[2,3-c]pyridine-2-carboxamide | 216483: Inhibition of VCAM-1 in human endothelial cells | ic50 | 0.0740 | uM |
| N-methyl-4-(4-phenylphenoxy)thieno[2,3-c]pyridine-2-carboxamide | 216483: Inhibition of VCAM-1 in human endothelial cells | ic50 | 0.0790 | uM |
| 4-(4-cyanophenoxy)thieno[2,3-c]pyridine-2-carboxamide | 216483: Inhibition of VCAM-1 in human endothelial cells | ic50 | 0.0850 | uM |
| 4-(4-cyanophenoxy)-N-methylthieno[2,3-c]pyridine-2-carboxamide | 216483: Inhibition of VCAM-1 in human endothelial cells | ic50 | 0.0910 | uM |
| 4-(4-chlorophenoxy)-N,N-dimethylthieno[2,3-c]pyridine-2-carboxamide | 216483: Inhibition of VCAM-1 in human endothelial cells | ic50 | 0.1300 | uM |
| 4-(4-ethylphenoxy)thieno[2,3-c]pyridine-2-carboxamide | 216483: Inhibition of VCAM-1 in human endothelial cells | ic50 | 0.1400 | uM |
| 4-[4-[2-[2-(2-ethoxyethoxy)ethoxy]-1,1-difluoroethyl]phenoxy]-N-methylthieno[2,3-c]pyridine-2-carboxamide | 216483: Inhibition of VCAM-1 in human endothelial cells | ic50 | 0.1700 | uM |
| 5-methoxy-3-propan-2-yloxy-1-benzothiophene-2-carboxamide | 216491: In vitro potency against TNF alpha induced expression of VCAM-1 on human vascular endothelial cells using CAM ELISA assay | ic50 | 0.1750 | uM |
| 4-[4-(hydroxymethyl)phenoxy]thieno[2,3-c]pyridine-2-carboxamide | 216483: Inhibition of VCAM-1 in human endothelial cells | ic50 | 0.1910 | uM |
| N-methyl-4-[4-(1,2,4-triazol-1-yl)phenoxy]thieno[2,3-c]pyridine-2-carboxamide | 216483: Inhibition of VCAM-1 in human endothelial cells | ic50 | 0.2400 | uM |
| 4-(2-bromo-4-chlorophenoxy)thieno[2,3-c]pyridine-2-carboxamide | 216483: Inhibition of VCAM-1 in human endothelial cells | ic50 | 0.3300 | uM |
| N-methyl-4-[4-(trifluoromethoxy)phenoxy]thieno[2,3-c]pyridine-2-carboxamide | 216483: Inhibition of VCAM-1 in human endothelial cells | ic50 | 0.3700 | uM |
| 4-[4-[1-[2-(2-ethoxyethoxy)ethoxymethyl]cyclopropyl]phenoxy]-N-methylthieno[2,3-c]pyridine-2-carboxamide | 216483: Inhibition of VCAM-1 in human endothelial cells | ic50 | 0.4200 | uM |
| 4-[4-(1,1-difluoro-2-hydroxyethyl)phenoxy]-N-methylthieno[2,3-c]pyridine-2-carboxamide | 216483: Inhibition of VCAM-1 in human endothelial cells | ic50 | 0.4700 | uM |
| 4-(2,4-dimethylphenyl)sulfanylthieno[2,3-c]pyridine-2-carboxamide | 216491: In vitro potency against TNF alpha induced expression of VCAM-1 on human vascular endothelial cells using CAM ELISA assay | ic50 | 0.7700 | uM |
| 4-(2-prop-2-enylphenoxy)thieno[2,3-c]pyridine-2-carboxamide | 216483: Inhibition of VCAM-1 in human endothelial cells | ic50 | 0.7800 | uM |
| 4-(3-chlorophenoxy)thieno[2,3-c]pyridine-2-carboxamide | 216483: Inhibition of VCAM-1 in human endothelial cells | ic50 | 0.8500 | uM |
| 4-(4-chlorophenoxy)-N-(2-hydroxyethyl)thieno[2,3-c]pyridine-2-carboxamide | 216483: Inhibition of VCAM-1 in human endothelial cells | ic50 | 0.8800 | uM |
| 4-[4-(1,2-dihydroxyethyl)phenoxy]thieno[2,3-c]pyridine-2-carboxamide | 216483: Inhibition of VCAM-1 in human endothelial cells | ic50 | 0.9300 | uM |
| 4-chlorothieno[2,3-c]pyridine-2-carboxamide | 216491: In vitro potency against TNF alpha induced expression of VCAM-1 on human vascular endothelial cells using CAM ELISA assay | ic50 | 1.3000 | uM |
| 4-(4-methylphenyl)sulfanylthieno[2,3-c]pyridine | 216491: In vitro potency against TNF alpha induced expression of VCAM-1 on human vascular endothelial cells using CAM ELISA assay | ic50 | 2.1000 | uM |
| 2-ethyl-4-(4-methylphenyl)sulfanylthieno[2,3-c]pyridine | 216491: In vitro potency against TNF alpha induced expression of VCAM-1 on human vascular endothelial cells using CAM ELISA assay | ic50 | 2.3000 | uM |
| 2-[3-(10H-pyrazino[2,3-b][1,4]benzothiazin-8-ylmethyl)-3-azabicyclo[3.3.1]nonan-9-yl]acetic acid | 1508013: Inhibition of VCAM1 (unknown origin) | ic50 | 2.5000 | uM |
| 5-(6-ethylthieno[2,3-d]pyrimidin-4-yl)sulfanyl-1,3,4-thiadiazol-2-amine | 216491: In vitro potency against TNF alpha induced expression of VCAM-1 on human vascular endothelial cells using CAM ELISA assay | ic50 | 2.5000 | uM |
| [4-(4-methylphenyl)sulfanylthieno[2,3-c]pyridin-2-yl]-phenylmethanone | 216491: In vitro potency against TNF alpha induced expression of VCAM-1 on human vascular endothelial cells using CAM ELISA assay | ic50 | 2.7000 | uM |
| 4-chloro-N,N-diethyl-3-nitrobenzenesulfonamide | 216481: Ability to inhibit expression of Vascular cell adhesion molecule 1 | ic50 | 3.0000 | uM |
| (E)-1-[4-(4-methylphenyl)sulfanylthieno[2,3-c]pyridin-2-yl]-N-phenoxymethanimine | 216491: In vitro potency against TNF alpha induced expression of VCAM-1 on human vascular endothelial cells using CAM ELISA assay | ic50 | 3.5000 | uM |
| 6-ethyl-4-[(5-methyl-1,3,4-thiadiazol-2-yl)sulfanyl]thieno[2,3-d]pyrimidine | 216491: In vitro potency against TNF alpha induced expression of VCAM-1 on human vascular endothelial cells using CAM ELISA assay | ic50 | 3.5000 | uM |
| 4-(4-chlorophenoxy)thieno[2,3-c]pyridine-2-carboxamide | 216483: Inhibition of VCAM-1 in human endothelial cells | ic50 | 3.9000 | uM |
| 1-(4-chloro-3-nitrophenyl)sulfonylpyrrolidine | 216481: Ability to inhibit expression of Vascular cell adhesion molecule 1 | ic50 | 4.0000 | uM |
| 8-[[4-(dimethylsulfamoylamino)piperidin-1-yl]methyl]-10H-pyrazino[2,3-b][1,4]benzothiazine | 1508013: Inhibition of VCAM1 (unknown origin) | ic50 | 4.5000 | uM |
| bis(4-chloro-3-nitrophenyl)methanone | 216481: Ability to inhibit expression of Vascular cell adhesion molecule 1 | ic50 | 5.0000 | uM |
| 4-chloro-N,N-bis(2-methoxyethyl)-3-nitrobenzenesulfonamide | 216481: Ability to inhibit expression of Vascular cell adhesion molecule 1 | ic50 | 5.0000 | uM |
| methyl 4-methylsulfonyl-3-nitrobenzoate | 216481: Ability to inhibit expression of Vascular cell adhesion molecule 1 | ic50 | 5.0000 | uM |
| 4-chloro-2-nitrobenzonitrile | 216481: Ability to inhibit expression of Vascular cell adhesion molecule 1 | ic50 | 5.0000 | uM |
| 4-[2,6-ditert-butyl-4-[2-(3,5-ditert-butyl-4-hydroxyphenyl)sulfanylpropan-2-ylsulfanyl]phenoxy]-4-oxobutanoic acid | 216494: Inhibition of TNF-alpha inducible Vascular cell adhesion molecule-1 expression. | ic50 | 6.0000 | uM |
| 4-chloro-N-[3-[(4-chloro-3-nitrophenyl)sulfonyl-methylamino]propyl]-N-methyl-3-nitrobenzenesulfonamide | 216481: Ability to inhibit expression of Vascular cell adhesion molecule 1 | ic50 | 6.0000 | uM |
| 4-chloro-N-(4-chloro-3-nitrophenyl)sulfonyl-3-nitro-N-phenylbenzenesulfonamide | 216481: Ability to inhibit expression of Vascular cell adhesion molecule 1 | ic50 | 7.0000 | uM |
| 4-chloro-3-nitro-N,N-dipentylbenzenesulfonamide | 216481: Ability to inhibit expression of Vascular cell adhesion molecule 1 | ic50 | 7.0000 | uM |
| 1-fluoro-4-(4-fluoro-3-nitrophenyl)sulfonyl-2-nitrobenzene | 216481: Ability to inhibit expression of Vascular cell adhesion molecule 1 | ic50 | 7.0000 | uM |
| 1-(4-chloro-3-nitrophenyl)sulfonyl-4-methylpiperazine | 216481: Ability to inhibit expression of Vascular cell adhesion molecule 1 | ic50 | 8.0000 | uM |
CTD chemical–gene interactions
330 total (human), top 30 by PubMed support.
| Chemical | Actions (top 5) | PubMed papers |
|---|---|---|
| Lipopolysaccharides | increases expression, increases reaction, increases secretion, affects reaction, decreases reaction | 18 |
| Particulate Matter | decreases expression, decreases reaction, increases expression, increases abundance, affects expression (+1 more) | 12 |
| Vehicle Emissions | increases expression, increases reaction, affects expression, decreases expression, decreases reaction (+1 more) | 9 |
| Glucose | decreases reaction, increases expression, affects cotreatment, increases secretion | 8 |
| Valproic Acid | affects cotreatment, decreases expression, affects expression, increases expression | 8 |
| Simvastatin | increases expression, affects cotreatment, decreases expression, increases reaction, decreases reaction | 8 |
| Quercetin | affects cotreatment, decreases reaction, increases expression, increases reaction | 6 |
| bisphenol A | decreases expression, affects cotreatment, decreases reaction, increases expression | 5 |
| 3-(4-methylphenylsulfonyl)-2-propenenitrile | increases reaction, increases abundance, decreases reaction, increases expression, affects binding | 5 |
| lipopolysaccharide, Escherichia coli O111 B4 | decreases reaction, increases expression, affects reaction | 5 |
| Resveratrol | decreases reaction, increases expression, decreases expression | 5 |
| Acetylcysteine | decreases reaction, increases expression | 5 |
| Hydrogen Peroxide | decreases reaction, increases secretion, increases expression, decreases expression | 5 |
| Ascorbic Acid | affects binding, affects cotreatment, increases expression, decreases reaction, decreases expression | 4 |
| Plant Extracts | decreases reaction, increases expression, increases reaction, decreases expression | 4 |
| titanium dioxide | decreases reaction, increases expression | 3 |
| acetovanillone | decreases reaction, increases expression | 3 |
| SB 203580 | decreases reaction, increases expression | 3 |
| lipopolysaccharide, E coli O55-B5 | decreases reaction, increases expression, affects cotreatment | 3 |
| Air Pollutants | increases expression, affects reaction, affects expression | 3 |
| Arsenic | increases expression, increases secretion | 3 |
| Dexamethasone | decreases reaction, increases expression, decreases expression, affects cotreatment | 3 |
| Estradiol | affects cotreatment, decreases expression, decreases reaction, increases expression | 3 |
| Ethinyl Estradiol | affects cotreatment, decreases expression, increases reaction | 3 |
| Formaldehyde | decreases expression, increases expression | 3 |
| Hydrocortisone | affects cotreatment, increases expression, decreases reaction | 3 |
| Sulfasalazine | decreases reaction, increases expression, decreases expression | 3 |
| Smoke | decreases reaction, increases expression | 3 |
| Tetrachlorodibenzodioxin | affects expression, decreases expression, increases expression | 3 |
| Soot | increases expression | 3 |
ChEMBL screening assays
16 unique, capped per target: 15 binding, 1 functional
Representative assays (with source publication via chembl_document):
| Assay ID | Type | Description | Source paper |
|---|---|---|---|
| CHEMBL1176151 | Binding | Inhibition of VCAM1 in TNF-alpha/IL4-stimulated HUVEC assessed as inhibition of cell adhesion between HUVEC and Ramos cells at 8 uM after 20 hrs incubation relative to untreated control | Symbiopolyol, a VCAM-1 inhibitor from a symbiotic dinoflagellate of the jellyfish Mastigias papua. — *J Nat Prod* |
| CHEMBL815903 | Functional | Inhibition of TNF-alpha inducible Vascular cell adhesion molecule-1 expression. | Novel phenolic antioxidants as multifunctional inhibitors of inducible VCAM-1 expression for use in atherosclerosis. — *Bioorg Med Chem Lett* |
Cellosaurus cell lines
1 cell lines: 1 cancer cell line
First 10 cell lines (id-ordered, not curated):
| Cellosaurus | Name | Category | Sex |
|---|---|---|---|
| CVCL_B1IG | Abcam A-549 VCAM1 KO | Cancer cell line | Male |
Clinical trials (associated diseases)
Via MONDO — disease-level, not drug-specific.
Predicted chemistry — Sugi Predict
The predicted patent-compound landscape for VCAM1 across ~30M SureChEMBL compounds — explore on Sugi Predict.
Related Atlas pages
- Disease cohort memberships (association, not causation — diseases whose associated-gene cohort lists this gene; a subset are also under Associated diseases): multiple sclerosis, Sjogren syndrome