CAMK1
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Also known as CaMKICaMKI-alpha
Summary
CAMK1 (calcium/calmodulin dependent protein kinase I, HGNC:1459) is a protein-coding gene on chromosome 3p25.3, encoding Calcium/calmodulin-dependent protein kinase type 1 (Q14012). Calcium/calmodulin-dependent protein kinase that operates in the calcium-triggered CaMKK-CaMK1 signaling cascade and, upon calcium influx, regulates transcription activators activity, cell cycle, hormone production, cell differentiation, actin filament organization and neurite o….
Calcium/calmodulin-dependent protein kinase I is expressed in many tissues and is a component of a calmodulin-dependent protein kinase cascade. Calcium/calmodulin directly activates calcium/calmodulin-dependent protein kinase I by binding to the enzyme and indirectly promotes the phosphorylation and synergistic activation of the enzyme by calcium/calmodulin-dependent protein kinase I kinase.
Source: NCBI Gene 8536 — RefSeq curated summary.
At a glance
- Clinical variants (ClinVar): 76 total
- Druggable target: yes — 19 molecules with ChEMBL bioactivity
- MANE Select transcript:
NM_003656
Identifiers
Gene identifiers
| Field | Value |
|---|---|
| HGNC ID | HGNC:1459 |
| Approved symbol | CAMK1 |
| Name | calcium/calmodulin dependent protein kinase I |
| Location | 3p25.3 |
| Locus type | gene with protein product |
| Status | Approved |
| Aliases | CaMKI, CaMKI-alpha |
| Ensembl gene | ENSG00000134072 |
| Ensembl biotype | protein_coding |
| OMIM | 604998 |
| Entrez | 8536 |
Gene structure
Transcript identifiers
Ensembl transcripts: 15 — 12 protein_coding, 2 retained_intron, 1 nonsense_mediated_decay
ENST00000256460, ENST00000397277, ENST00000411972, ENST00000421120, ENST00000482803, ENST00000496534, ENST00000856591, ENST00000856592, ENST00000856593, ENST00000856594, ENST00000856595, ENST00000856596, ENST00000856597, ENST00000962076, ENST00000962077
RefSeq mRNA: 1 — MANE Select: NM_003656
NM_003656
CCDS: CCDS2582
Canonical transcript exons
ENST00000256460 — 12 exons
| Exon | Start | End |
|---|---|---|
| ENSE00001135141 | 9767667 | 9767781 |
| ENSE00001165098 | 9769832 | 9769947 |
| ENSE00001954612 | 9757347 | 9757621 |
| ENSE00003466603 | 9759672 | 9759750 |
| ENSE00003493373 | 9759488 | 9759575 |
| ENSE00003511946 | 9761631 | 9761757 |
| ENSE00003541626 | 9763139 | 9763213 |
| ENSE00003541736 | 9762914 | 9763052 |
| ENSE00003567355 | 9765759 | 9765890 |
| ENSE00003570225 | 9760656 | 9760768 |
| ENSE00003593007 | 9761461 | 9761536 |
| ENSE00003687552 | 9757729 | 9757846 |
Expression profiles
Bgee: expression breadth ubiquitous, 208 present calls, max score 97.23.
FANTOM5 (CAGE): breadth ubiquitous, TPM avg 16.8621 / max 290.7500, expressed in 1696 samples.
FANTOM5 promoters (2 alternative TSS)
| Promoter ID | TPM avg | Samples expressed |
|---|---|---|
| 40976 | 16.5125 | 1693 |
| 40977 | 0.3496 | 154 |
Top tissues by expression
279 total, by Bgee expression score (0-100, higher = more expressed):
| Tissue | Anatomy ID | Expression score | Quality |
|---|---|---|---|
| right adrenal gland cortex | UBERON:0035827 | 97.23 | gold quality |
| right adrenal gland | UBERON:0001233 | 97.16 | gold quality |
| left adrenal gland cortex | UBERON:0035825 | 96.97 | gold quality |
| left adrenal gland | UBERON:0001234 | 96.80 | gold quality |
| adrenal cortex | UBERON:0001235 | 96.50 | gold quality |
| right frontal lobe | UBERON:0002810 | 95.47 | gold quality |
| prefrontal cortex | UBERON:0000451 | 94.87 | gold quality |
| nucleus accumbens | UBERON:0001882 | 94.87 | gold quality |
| caudate nucleus | UBERON:0001873 | 94.78 | gold quality |
| monocyte | CL:0000576 | 94.49 | gold quality |
| amygdala | UBERON:0001876 | 94.44 | gold quality |
| adrenal gland | UBERON:0002369 | 94.39 | gold quality |
| left uterine tube | UBERON:0001303 | 94.22 | gold quality |
| mononuclear cell | CL:0000842 | 93.95 | gold quality |
| putamen | UBERON:0001874 | 93.88 | gold quality |
| omental fat pad | UBERON:0010414 | 93.87 | gold quality |
| peritoneum | UBERON:0002358 | 93.80 | gold quality |
| leukocyte | CL:0000738 | 93.73 | gold quality |
| cingulate cortex | UBERON:0003027 | 93.73 | gold quality |
| anterior cingulate cortex | UBERON:0009835 | 93.63 | gold quality |
| left coronary artery | UBERON:0001626 | 93.38 | gold quality |
| adipose tissue of abdominal region | UBERON:0007808 | 93.38 | gold quality |
| right ovary | UBERON:0002118 | 93.37 | gold quality |
| Brodmann (1909) area 9 | UBERON:0013540 | 93.33 | gold quality |
| esophagogastric junction muscularis propria | UBERON:0035841 | 93.32 | gold quality |
| granulocyte | CL:0000094 | 93.17 | gold quality |
| dorsolateral prefrontal cortex | UBERON:0009834 | 93.07 | gold quality |
| lower esophagus muscularis layer | UBERON:0035833 | 92.81 | gold quality |
| popliteal artery | UBERON:0002250 | 92.76 | gold quality |
| lower esophagus | UBERON:0013473 | 92.76 | gold quality |
Single-cell (SCXA)
Detected in 2 experiment(s), a significant marker in 1.
| Experiment | Marker? | Max mean expression |
|---|---|---|
| E-ANND-3 | yes | 4.62 |
| E-ENAD-17 | no | 15.41 |
Regulation
Is transcription factor: yes
Downstream targets (CollecTRI)
2 targets.
| Target | Regulation |
|---|---|
| ERVW-1 | Activation |
| HDAC5 | Activation |
Upstream regulators (CollecTRI, top): GLI2, NR5A1
miRNA regulators (miRDB)
35 targeting CAMK1, 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-3163 | 100.00 | 77.23 | 8605 |
| HSA-MIR-1252-5P | 100.00 | 69.80 | 2774 |
| HSA-MIR-3688-3P | 99.97 | 72.02 | 2834 |
| HSA-MIR-3148 | 99.97 | 75.06 | 6478 |
| HSA-MIR-95-5P | 99.89 | 72.17 | 3973 |
| HSA-MIR-6124 | 99.87 | 69.78 | 3551 |
| HSA-MIR-4728-5P | 99.85 | 69.39 | 4718 |
| HSA-MIR-3121-3P | 99.82 | 71.96 | 3630 |
| HSA-MIR-6785-5P | 99.82 | 68.68 | 4428 |
| HSA-MIR-204-5P | 99.79 | 71.62 | 2439 |
| HSA-MIR-211-5P | 99.79 | 71.65 | 2440 |
| HSA-MIR-623 | 99.76 | 68.16 | 1170 |
| HSA-MIR-556-3P | 99.74 | 68.75 | 1203 |
| HSA-MIR-149-3P | 99.72 | 68.22 | 3963 |
| HSA-MIR-4755-5P | 99.71 | 70.34 | 2716 |
| HSA-MIR-5006-3P | 99.71 | 70.26 | 2728 |
| HSA-MIR-494-3P | 99.70 | 71.45 | 2795 |
| HSA-MIR-6883-5P | 99.69 | 68.05 | 3785 |
| HSA-MIR-141-5P | 99.57 | 67.86 | 897 |
| HSA-MIR-6832-3P | 99.52 | 70.44 | 1726 |
| HSA-MIR-4441 | 99.49 | 66.56 | 3216 |
| HSA-MIR-297 | 99.40 | 69.58 | 1418 |
| HSA-MIR-10399-5P | 99.17 | 69.87 | 2610 |
| HSA-MIR-6504-3P | 99.17 | 69.31 | 2891 |
| HSA-MIR-4784 | 99.15 | 67.41 | 1733 |
| HSA-MIR-4270 | 99.02 | 66.26 | 1987 |
| HSA-MIR-3150B-3P | 98.81 | 67.21 | 1728 |
| HSA-MIR-3149 | 98.77 | 67.13 | 1639 |
| HSA-MIR-9500 | 98.62 | 66.54 | 1845 |
| HSA-MIR-12120 | 98.05 | 68.44 | 1768 |
Literature-anchored findings (GeneRIF, showing 15)
- CaMKI is involved in angiotensin II and K(+) stimulation of CYP11B2 transcription and the capacity of the adrenal to produce aldosterone (PMID:12193581)
- we cloned a novel calmodulin-kinase (CaM-KIdelta) from HeLa cells and characterized its activation mechanism. CaM-KIdelta exhibits Ca(2+)/CaM-dependent activity that is enhanced in vitro by phosphorylation of its Thr180 by CaM-K kinase (CaM-KK)alpha (PMID:12935886)
- calcium/calmodulin-dependent protein kinase I regulates of cyclin D1/Cdk4 complexes (PMID:14754892)
- Calcium/calmodulin-dependent protein kinase I inhibits neuronal nitric-oxide synthase activity through serine 741 phosphorylation (PMID:15251453)
- Dioxin-mediated up-regulation of aryl hydrocarbon receptor target genes is dependent on the calcium/calmodulin/CaMKIalpha pathway. (PMID:18089838)
- variants in doublecortin- and calmodulin kinase like 1, a gene up-regulated by BDNF, have roles in memory and general cognitive abilities (PMID:19844571)
- CaMKI was significantly upregulated in adrenal adenomas. (PMID:21249615)
- structures of three CaMKIalpha truncates in apo form and in complexes with ATP (PMID:23028635)
- Fbxl12-induced CaMKI degradation attenuates p27 phosphorylation at these sites in early G1 and iii) activation of CaMKI during G1 transition followed by p27 phosphorylation appears to be upstream to other p27 phosphorylation events (PMID:23707388)
- It is one of Ca(2+)-sensing proteins and substantial age- and Alzheimer disease(AD)-related alterations in Ca(2+)-sensing proteins most likely contribute to selective vulnerability of basal forebrain cholinergic neurons to degeneration in AD. (PMID:24461366)
- CAMK1 functional regulation subnetwork in hepatocellular carcinoma (PMID:24825433)
- this study suggests that the tightly linked regulatory loop comprised of the SIK2-PP2A and CaMKI and PME-1 networks may function in fine-tuning cell proliferation and stress response. (PMID:24841198)
- Barettin has inhibitory activity against two protein kinases related to inflammation, namely the receptor-interacting serine/threonine kinase 2 (RIPK2) and calcium/calmodulin-dependent protein kinase 1alpha (CAMK1alpha). (PMID:26466644)
- The mRNA expressions of PPP3CB and MEF2C were significantly up-regulated, and CAMK1 and PPP3R1 were significantly down-regulated in mitral regurgitation(MR) patients compared to normal subjects. Moreover, MR patients had significantly increased mRNA levels of PPP3CB, MEF2C and PLCE1 compared to aortic valve disease patients (PMID:27907007)
- Expression of CAMK1 and its association with clinicopathologic characteristics in pancreatic cancer. (PMID:33342045)
Cross-species orthologs
6 orthologs
| Organism | Symbol | Gene ID |
|---|---|---|
| danio_rerio | camk1b | ENSDARG00000029474 |
| danio_rerio | camk1a | ENSDARG00000060116 |
| danio_rerio | ENSDARG00000116980 | |
| mus_musculus | Camk1 | ENSMUSG00000030272 |
| rattus_norvegicus | Camk1 | ENSRNOG00000021781 |
| caenorhabditis_elegans | WBGENE00000553 |
Paralogs (22): CAMKK1 (ENSG00000004660), CAMK1G (ENSG00000008118), CAMK2B (ENSG00000058404), CAMK2A (ENSG00000070808), MYLK2 (ENSG00000101306), CAMKK2 (ENSG00000110931), STK11 (ENSG00000118046), STK33 (ENSG00000130413), PNCK (ENSG00000130822), DCLK1 (ENSG00000133083), MYLK3 (ENSG00000140795), CAMK2D (ENSG00000145349), MYLK4 (ENSG00000145949), PSKH2 (ENSG00000147613), CAMK2G (ENSG00000148660), PHKG2 (ENSG00000156873), PSKH1 (ENSG00000159792), DCLK3 (ENSG00000163673), CAMKV (ENSG00000164076), PHKG1 (ENSG00000164776), DCLK2 (ENSG00000170390), CAMK1D (ENSG00000183049)
Protein
Protein identifiers
Calcium/calmodulin-dependent protein kinase type 1 — Q14012 (reviewed: Q14012)
Alternative names: CaM kinase I, CaM kinase I alpha
All UniProt accessions (5): B0YIY3, C9JES6, Q14012, F8W6S9, H7C071
UniProt curated annotations — full annotation on UniProt →
Function. Calcium/calmodulin-dependent protein kinase that operates in the calcium-triggered CaMKK-CaMK1 signaling cascade and, upon calcium influx, regulates transcription activators activity, cell cycle, hormone production, cell differentiation, actin filament organization and neurite outgrowth. Recognizes the substrate consensus sequence [MVLIF]-x-R-x(2)-[ST]-x(3)-[MVLIF]. Regulates axonal extension and growth cone motility in hippocampal and cerebellar nerve cells. Upon NMDA receptor-mediated Ca(2+) elevation, promotes dendritic growth in hippocampal neurons and is essential in synapses for full long-term potentiation (LTP) and ERK2-dependent translational activation. Downstream of NMDA receptors, promotes the formation of spines and synapses in hippocampal neurons by phosphorylating ARHGEF7/BETAPIX on ‘Ser-694’, which results in the enhancement of ARHGEF7 activity and activation of RAC1. Promotes neuronal differentiation and neurite outgrowth by activation and phosphorylation of MARK2 on ‘Ser-91’, ‘Ser-92’, ‘Ser-93’ and ‘Ser-294’. Promotes nuclear export of HDAC5 and binding to 14-3-3 by phosphorylation of ‘Ser-259’ and ‘Ser-498’ in the regulation of muscle cell differentiation. Regulates NUMB-mediated endocytosis by phosphorylation of NUMB on ‘Ser-276’ and ‘Ser-295’. Involved in the regulation of basal and estrogen-stimulated migration of medulloblastoma cells through ARHGEF7/BETAPIX phosphorylation. Is required for proper activation of cyclin-D1/CDK4 complex during G1 progression in diploid fibroblasts. Plays a role in K(+) and ANG2-mediated regulation of the aldosterone synthase (CYP11B2) to produce aldosterone in the adrenal cortex. Phosphorylates EIF4G3/eIF4GII. In vitro phosphorylates CREB1, ATF1, CFTR, MYL9 and SYN1/synapsin I.
Subunit / interactions. Monomer. Interacts with XPO1. Interacts with MARK2, ARHGEF7/BETAPIX and GIT1.
Subcellular location. Cytoplasm. Nucleus.
Tissue specificity. Widely expressed. Expressed in cells of the zona glomerulosa of the adrenal cortex.
Post-translational modifications. Phosphorylated by CaMKK1 and CaMKK2 on Thr-177. Polybiquitinated by the E3 ubiquitin-protein ligase complex SCF(FBXL12), leading to proteasomal degradation.
Activity regulation. Activated by Ca(2+)/calmodulin. Binding of calmodulin results in conformational change that relieves intrasteric autoinhibition and allows phosphorylation of Thr-177 within the activation loop by CaMKK1 or CaMKK2. Phosphorylation of Thr-177 results in several fold increase in total activity. Unlike CaMK4, is unable to exhibit autonomous activity after Ca(2+)/calmodulin activation.
Domain organisation. The autoinhibitory domain overlaps with the calmodulin binding region and interacts in the inactive folded state with the catalytic domain as a pseudosubstrate.
Similarity. Belongs to the protein kinase superfamily. CAMK Ser/Thr protein kinase family. CaMK subfamily.
RefSeq proteins (1): NP_003647* (*=MANE)
Domains & families (InterPro)
| ID | Name | Type |
|---|---|---|
| IPR000719 | Prot_kinase_dom | Domain |
| IPR008271 | Ser/Thr_kinase_AS | Active_site |
| IPR011009 | Kinase-like_dom_sf | Homologous_superfamily |
| IPR017441 | Protein_kinase_ATP_BS | Binding_site |
Pfam: PF00069
Enzyme classification (BRENDA):
- EC 2.7.11.17 — Ca2+/calmodulin-dependent protein kinase (BRENDA: 38 organisms, 300 substrates, 137 inhibitors, 35 Km, 17 kcat entries)
Substrate kinetics (BRENDA)
12 substrates with measured Km, best-characterized 12. Km ranges are aggregated across organisms/conditions.
| Substrate | Km (mM) | Measurements |
|---|---|---|
| ATP | 0.0071–178.29 | 13 |
| BIOTINYLATED THR-ARG-SER-ALA-ILE-ARG-ARG-ALA-SER | 0.0064–0.0158 | 4 |
| GST-TAGGED GLUN2A | 6.05–11.75 | 2 |
| GST-TAGGED GLUN2B | 0.35–5.93 | 2 |
| MAP2 | 0.0007–0.0008 | 2 |
| CALDESMON | 0.0049 | 1 |
| HISTONE IIIS | 0.0445 | 1 |
| LYS-LYS-ALA-LEU-ARG-ARG-GLN-GLU-ALA-VAL-ASP-ALA- | 0.063 | 1 |
| MICROTUBULE ASSOCIATED PROTEIN 2 | 0.0016 | 1 |
| SYNTIDE-2 | 0.02 | 1 |
| SYNTIDE-2 PEPTIDE | 0.0221 | 1 |
| MYELIN BASIC PROTEIN | — | 0 |
Catalyzed reactions (Rhea), 2 shown:
- L-seryl-[protein] + ATP = O-phospho-L-seryl-[protein] + ADP + H(+) (RHEA:17989)
- L-threonyl-[protein] + ATP = O-phospho-L-threonyl-[protein] + ADP + H(+) (RHEA:46608)
UniProt features (43 total): helix 15, strand 8, turn 4, mutagenesis site 3, sequence variant 2, region of interest 2, binding site 2, modified residue 2, chain 1, domain 1, cross-link 1, short sequence motif 1, active site 1
Structure
Experimental structures (PDB)
4 structures.
| PDB | Method | Resolution (Å) |
|---|---|---|
| 4FG8 | X-RAY DIFFRACTION | 2.2 |
| 4FG9 | X-RAY DIFFRACTION | 2.4 |
| 4FGB | X-RAY DIFFRACTION | 2.6 |
| 4FG7 | X-RAY DIFFRACTION | 2.7 |
Predicted structure (AlphaFold)
| Model | pLDDT | Fraction very-high |
|---|---|---|
| AF-Q14012-F1 | 79.87 | 0.51 |
Functional residue map
Curated UniProt residues grouped by drug-discovery relevance — catalytic, ligand-binding, modification, and mutation-validated positions. Source: UniProtKB sequence features.
Catalytic / active sites (1): 141 (proton acceptor)
Ligand- & substrate-binding residues (2): 26–34; 49
Post-translational modifications (3): 59, 177, 363
Mutagenesis-validated functional residues (3):
| Position | Phenotype |
|---|---|
| 49 | catalytically inactive form; prevents cdk4 activation. |
| 177 | loss of activation by camkk1. |
| 177 | partial activation in absence of camkk1. |
Function
Pathways and Gene Ontology
Reactome pathways
7 pathways
| ID | Pathway |
|---|---|
| R-HSA-9617324 | Negative regulation of NMDA receptor-mediated neuronal transmission |
| R-HSA-9619229 | Activation of RAC1 downstream of NMDARs |
| R-HSA-112314 | Neurotransmitter receptors and postsynaptic signal transmission |
| R-HSA-112315 | Transmission across Chemical Synapses |
| R-HSA-112316 | Neuronal System |
| R-HSA-438064 | Post NMDA receptor activation events |
| R-HSA-442755 | Activation of NMDA receptors and postsynaptic events |
MSigDB gene sets: 261 (showing top):
GOBP_DENDRITE_DEVELOPMENT, BIOCARTA_FMLP_PATHWAY, GOBP_INTRACELLULAR_PROTEIN_TRANSPORT, GOBP_POSITIVE_REGULATION_OF_MUSCLE_CELL_DIFFERENTIATION, GOBP_POSITIVE_REGULATION_OF_INTRACELLULAR_PROTEIN_TRANSPORT, GOBP_DENDRITIC_SPINE_DEVELOPMENT, GOBP_POSITIVE_REGULATION_OF_PROTEIN_LOCALIZATION, ACEVEDO_NORMAL_TISSUE_ADJACENT_TO_LIVER_TUMOR_DN, GOBP_REGULATION_OF_PROTEIN_EXPORT_FROM_NUCLEUS, GOBP_NEUROGENESIS, MEF2_02, GOBP_POSITIVE_REGULATION_OF_INTRACELLULAR_TRANSPORT, GOBP_NUCLEAR_TRANSPORT, GOBP_REGULATION_OF_CELL_PROJECTION_ORGANIZATION, GOBP_CELL_JUNCTION_ORGANIZATION
GO Biological Process (20): nucleocytoplasmic transport (GO:0006913), signal transduction (GO:0007165), nervous system development (GO:0007399), positive regulation of neuron projection development (GO:0010976), cell differentiation (GO:0030154), regulation of protein localization (GO:0032880), intracellular signal transduction (GO:0035556), positive regulation of transcription by RNA polymerase II (GO:0045944), positive regulation of protein export from nucleus (GO:0046827), regulation of synapse organization (GO:0050807), regulation of muscle cell differentiation (GO:0051147), positive regulation of muscle cell differentiation (GO:0051149), positive regulation of synapse structural plasticity (GO:0051835), positive regulation of syncytium formation by plasma membrane fusion (GO:0060143), positive regulation of dendritic spine development (GO:0060999), protein phosphorylation (GO:0006468), regulation of neuron projection development (GO:0010975), negative regulation of protein binding (GO:0032091), regulation of protein binding (GO:0043393), positive regulation of protein serine/threonine kinase activity (GO:0071902)
GO Molecular Function (11): protein serine/threonine kinase activity (GO:0004674), calcium/calmodulin-dependent protein kinase activity (GO:0004683), calmodulin binding (GO:0005516), ATP binding (GO:0005524), protein serine kinase activity (GO:0106310), nucleotide binding (GO:0000166), catalytic activity (GO:0003824), protein kinase activity (GO:0004672), protein binding (GO:0005515), kinase activity (GO:0016301), transferase activity (GO:0016740)
GO Cellular Component (4): nucleus (GO:0005634), cytoplasm (GO:0005737), cytosol (GO:0005829), postsynaptic density (GO:0014069)
Reactome top-level categories
Rollup of top-5 pathways:
| Category | Pathways |
|---|---|
| Activation of NMDA receptors and postsynaptic events | 2 |
| Post NMDA receptor activation events | 1 |
| Transmission across Chemical Synapses | 1 |
| Neuronal System | 1 |
| Neurotransmitter receptors and postsynaptic signal transmission | 1 |
GO top-level categories
Rollup of top GO terms by namespace:
| Category | Terms |
|---|---|
| protein binding | 3 |
| neuron projection development | 2 |
| intracellular anatomical structure | 2 |
| muscle cell differentiation | 2 |
| positive regulation of cellular component organization | 2 |
| protein serine/threonine kinase activity | 2 |
| protein kinase activity | 2 |
| cellular anatomical structure | 2 |
| nuclear transport | 1 |
| cell communication | 1 |
| cellular process | 1 |
| signaling | 1 |
| regulation of cellular process | 1 |
| cellular response to stimulus | 1 |
| system development | 1 |
| regulation of neuron projection development | 1 |
| positive regulation of cell projection organization | 1 |
| cellular developmental process | 1 |
| intracellular protein localization | 1 |
| regulation of localization | 1 |
| signal transduction | 1 |
| regulation of transcription by RNA polymerase II | 1 |
| transcription by RNA polymerase II | 1 |
| positive regulation of DNA-templated transcription | 1 |
| protein export from nucleus | 1 |
| positive regulation of nucleocytoplasmic transport | 1 |
| regulation of protein export from nucleus | 1 |
| positive regulation of intracellular protein transport | 1 |
| regulation of synapse structure or activity | 1 |
| synapse organization | 1 |
| regulation of cellular component organization | 1 |
| regulation of cell differentiation | 1 |
| positive regulation of cell differentiation | 1 |
| regulation of muscle cell differentiation | 1 |
| regulation of synapse structural plasticity | 1 |
| syncytium formation by cell-cell fusion | 1 |
| regulation of syncytium formation by plasma membrane fusion | 1 |
| positive regulation of developmental process | 1 |
| dendritic spine development | 1 |
| regulation of dendritic spine development | 1 |
Protein interactions and networks
STRING
1491 interactions, top by confidence (×1000):
| Protein A | Protein B | Partner UniProt | Score |
|---|---|---|---|
| CAMK1 | CALM1 | P02593 | 916 |
| CAMK1 | CALML4 | Q96GE6 | 845 |
| CAMK1 | CALML3 | P27482 | 844 |
| CAMK1 | CALML5 | Q9NZT1 | 844 |
| CAMK1 | CALML6 | Q8TD86 | 834 |
| CAMK1 | ARPP21 | Q9UBL0 | 637 |
| CAMK1 | CYP11B2 | P19099 | 632 |
| CAMK1 | CREB1 | P16220 | 603 |
| CAMK1 | KCNN2 | Q9H2S1 | 550 |
| CAMK1 | SYN2 | Q92777 | 537 |
| CAMK1 | HSP90AB1 | P08238 | 515 |
| CAMK1 | HSP90AA1 | P07900 | 513 |
| CAMK1 | MEF2A | Q02078 | 502 |
| CAMK1 | KCNMA1 | Q12791 | 490 |
| CAMK1 | PPP2CA | P05323 | 460 |
IntAct
80 interactions, top by confidence:
| A | B | Type | Score |
|---|---|---|---|
| PHF19 | EED | psi-mi:“MI:0914”(association) | 0.730 |
| ATXN1 | CAMK1 | psi-mi:“MI:0915”(physical association) | 0.720 |
| CAMK1D | CAMK1 | psi-mi:“MI:0915”(physical association) | 0.620 |
| CALM1 | CAMK1 | psi-mi:“MI:0407”(direct interaction) | 0.590 |
| IL16 | CAMK1 | psi-mi:“MI:0915”(physical association) | 0.560 |
| HTT | CAMK1 | psi-mi:“MI:0915”(physical association) | 0.560 |
| EPHA1 | EXOC5 | psi-mi:“MI:0914”(association) | 0.530 |
| CCDC106 | NEFM | psi-mi:“MI:0914”(association) | 0.530 |
| CDO1 | DBT | psi-mi:“MI:0914”(association) | 0.530 |
| HTR2C | KLRG2 | psi-mi:“MI:0914”(association) | 0.530 |
| CER1 | POTEF | psi-mi:“MI:0914”(association) | 0.530 |
| SAMTOR | PER1 | psi-mi:“MI:0914”(association) | 0.530 |
| PHF19 | EPOP | psi-mi:“MI:0914”(association) | 0.530 |
| ANKRD22 | ESYT2 | psi-mi:“MI:0914”(association) | 0.530 |
| PTPN6 | CAMK1 | psi-mi:“MI:0915”(physical association) | 0.400 |
| CAMK1 | psi-mi:“MI:0915”(physical association) | 0.400 | |
| CAMK1 | BLK | psi-mi:“MI:0915”(physical association) | 0.400 |
| CAMK1 | PIK3R3 | psi-mi:“MI:0915”(physical association) | 0.370 |
BioGRID (115): CAMK1 (Affinity Capture-MS), CAMK1 (Affinity Capture-MS), CAMK1 (Affinity Capture-MS), CAMK1 (Affinity Capture-MS), CAMK1 (Affinity Capture-MS), BLK (Affinity Capture-MS), CAMK1 (Biochemical Activity), PPME1 (Biochemical Activity), CAMK1 (Two-hybrid), CAMK1 (Two-hybrid), CAMK1 (Affinity Capture-MS), CAMK1 (Affinity Capture-MS), CAMK1 (Affinity Capture-MS), CAMK1 (Affinity Capture-MS), CAMK1 (Affinity Capture-MS)
ESM2 similar proteins: A8X6H4, O70150, O75582, P10665, P11275, P11798, P18652, P18653, P18654, P28583, P51812, Q13557, Q14012, Q15349, Q2HJF7, Q38869, Q38871, Q38872, Q39016, Q42396, Q54CY9, Q54SJ5, Q5F3L1, Q5R4K3, Q5RCC4, Q5ZKI0, Q63450, Q63531, Q6DEH3, Q6GLS4, Q6P2M8, Q6PFQ0, Q6PHZ2, Q7TPS0, Q869W6, Q8BW96, Q8IU85, Q8RWL2, Q8VDF3, Q91YS8
Diamond homologs: A0A2I0BVG8, A0A509AFG4, A0A509AHB6, A0A509ALV6, A0A509AQE6, A0A5K1K8H0, A0AAR7, A5A7I7, A5A7I8, A8X6H4, O15865, O49717, O70150, P25323, P28582, P28583, P34101, P49101, P53681, P53682, P53683, P53684, P62343, P62344, P62345, P93759, Q06850, Q0D715, Q0DYK7, Q10KY3, Q14012, Q1PE17, Q1PFH8, Q2QQR2, Q2QVG8, Q2QX45, Q38868, Q38869, Q38870, Q38871
SIGNOR signaling
22 interactions.
| A | Effect | B | Mechanism |
|---|---|---|---|
| CAMK1 | down-regulates | NUMB | phosphorylation |
| CAMK1 | unknown | EIF4G3 | phosphorylation |
| CAMK1 | “up-regulates activity” | GCM1 | phosphorylation |
| RAP1A | “up-regulates activity” | CAMK1 | |
| CAMK1 | “down-regulates activity” | PPME1 | phosphorylation |
| CAMK1 | unknown | KRT18 | phosphorylation |
| CAMK1 | “up-regulates activity” | PPME1 | phosphorylation |
| PPM1F | “down-regulates activity” | CAMK1 | dephosphorylation |
| CAMK1 | “up-regulates activity” | ARHGEF2 | phosphorylation |
| CAMK1 | down-regulates | HDAC5 | phosphorylation |
| FBXL12 | “down-regulates quantity” | CAMK1 | ubiquitination |
| CAMK1 | “up-regulates activity” | CDKN1B | phosphorylation |
| CAMK1 | “up-regulates activity” | ATF1 | phosphorylation |
| CAMK1 | “up-regulates activity” | CAMK1 | phosphorylation |
| CAMK1 | “down-regulates activity” | NOS1 | phosphorylation |
| CAMK1 | “down-regulates activity” | SYN1 | phosphorylation |
| CAMKK2 | “up-regulates activity” | CAMK1 | phosphorylation |
| CAMKK1 | “up-regulates activity” | CAMK1 | phosphorylation |
| CAMK1 | “up-regulates activity” | DNM1L | phosphorylation |
Disease & clinical
Clinical variants and AI predictions
ClinVar
76 variants total. Per-class counts are floors (≥ shown; pagination cap):
| Classification | Count (floor) |
|---|---|
| Pathogenic | 0 |
| Likely pathogenic | 0 |
| Uncertain significance | 53 |
| Likely benign | 5 |
| Benign | 0 |
Top pathogenic / likely-pathogenic (0)
SpliceAI
1811 predictions. Top by Δscore:
| Variant | Effect | Δscore |
|---|---|---|
| 3:9757853:T:C | acceptor_gain | 1.0000 |
| 3:9757853:T:TC | acceptor_gain | 1.0000 |
| 3:9757860:CA:C | acceptor_gain | 1.0000 |
| 3:9757861:A:AC | acceptor_gain | 1.0000 |
| 3:9757861:A:C | acceptor_gain | 1.0000 |
| 3:9757861:A:T | acceptor_gain | 1.0000 |
| 3:9757862:T:C | acceptor_gain | 1.0000 |
| 3:9757862:T:TC | acceptor_gain | 1.0000 |
| 3:9759483:CTCA:C | donor_loss | 1.0000 |
| 3:9759484:TCA:T | donor_loss | 1.0000 |
| 3:9759485:CACCT:C | donor_loss | 1.0000 |
| 3:9759670:A:AC | donor_gain | 1.0000 |
| 3:9759671:C:CC | donor_gain | 1.0000 |
| 3:9759746:TTTGG:T | acceptor_gain | 1.0000 |
| 3:9759747:TTGG:T | acceptor_gain | 1.0000 |
| 3:9759748:TGG:T | acceptor_gain | 1.0000 |
| 3:9759749:GG:G | acceptor_gain | 1.0000 |
| 3:9759751:C:CC | acceptor_gain | 1.0000 |
| 3:9759760:C:CT | acceptor_gain | 1.0000 |
| 3:9759760:C:T | acceptor_gain | 1.0000 |
| 3:9759761:A:T | acceptor_gain | 1.0000 |
| 3:9759765:C:CT | acceptor_gain | 1.0000 |
| 3:9761457:TTACA:T | donor_loss | 1.0000 |
| 3:9761459:A:AC | donor_gain | 1.0000 |
| 3:9761460:C:CA | donor_gain | 1.0000 |
| 3:9761460:CA:C | donor_gain | 1.0000 |
| 3:9761460:CAA:C | donor_gain | 1.0000 |
| 3:9761460:CAAG:C | donor_gain | 1.0000 |
| 3:9761460:CAAGA:C | donor_gain | 1.0000 |
| 3:9761532:AGGGG:A | acceptor_gain | 1.0000 |
AlphaMissense
2448 scored. Top likely-pathogenic:
| Variant | Protein change | am_pathogenicity |
|---|---|---|
| 3:9759673:A:G | W275R | 1.000 |
| 3:9759673:A:T | W275R | 1.000 |
| 3:9760664:G:A | S246F | 1.000 |
| 3:9760677:A:G | W242R | 1.000 |
| 3:9760677:A:T | W242R | 1.000 |
| 3:9760747:G:C | F218L | 1.000 |
| 3:9760747:G:T | F218L | 1.000 |
| 3:9760749:A:G | F218L | 1.000 |
| 3:9760751:G:T | P217H | 1.000 |
| 3:9760760:C:A | G214V | 1.000 |
| 3:9760760:C:T | G214D | 1.000 |
| 3:9760766:A:G | L212P | 1.000 |
| 3:9761479:C:T | G205D | 1.000 |
| 3:9761480:C:G | G205R | 1.000 |
| 3:9761489:A:G | W202R | 1.000 |
| 3:9761489:A:T | W202R | 1.000 |
| 3:9761495:C:G | D200H | 1.000 |
| 3:9761637:A:G | Y184H | 1.000 |
| 3:9761648:C:T | G180E | 1.000 |
| 3:9761701:G:C | D162E | 1.000 |
| 3:9761701:G:T | D162E | 1.000 |
| 3:9761702:T:A | D162V | 1.000 |
| 3:9761702:T:C | D162G | 1.000 |
| 3:9761702:T:G | D162A | 1.000 |
| 3:9761703:C:G | D162H | 1.000 |
| 3:9761744:A:G | L148P | 1.000 |
| 3:9761747:A:G | L147P | 1.000 |
| 3:9761749:A:C | N146K | 1.000 |
| 3:9761749:A:T | N146K | 1.000 |
| 3:9761751:T:C | N146D | 1.000 |
dbSNP variants (sampled 300 via entrez): RS1000255179 (3:9769578 C>T), RS1000349198 (3:9769287 C>A,T), RS1000523584 (3:9764563 C>T), RS1000716628 (3:9770583 G>A,C), RS1001226359 (3:9769638 T>G), RS1001436923 (3:9762597 T>G), RS1001531576 (3:9767469 C>T), RS1001594385 (3:9763783 C>T), RS1001808155 (3:9761160 C>G,T), RS1001847020 (3:9765552 C>T), RS1001931268 (3:9765161 A>G), RS1002026457 (3:9764934 T>C), RS1002158550 (3:9769904 A>T), RS1003304691 (3:9770974 T>C), RS1003376079 (3:9759110 G>C,T)
Disease associations
OMIM: gene MIM:604998 | disease phenotypes: MIM:144700
GenCC curated gene-disease
Mondo (1): nonpapillary renal cell carcinoma (MONDO:0007763)
Orphanet (1): Hereditary clear cell renal cell carcinoma (Orphanet:422526)
HPO phenotypes
0 total (0 of 0 shown, HPO-id order):
GWAS associations
0 associations (top):
Drugs & pharmacology
Drug and pharmacology data
Is drug target: yes
ChEMBL targets (1): CHEMBL2493 (SINGLE PROTEIN)
Molecules with ChEMBL bioactivity
19 molecules (phase ≥1), by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 156,708 (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 |
|---|---|---|---|
| CHEMBL1287853 | FEDRATINIB | 4 | 3,554 |
| CHEMBL1789941 | RUXOLITINIB | 4 | 11,547 |
| CHEMBL2103743 | TOFACITINIB CITRATE | 4 | 1,672 |
| CHEMBL221959 | TOFACITINIB | 4 | 10,408 |
| CHEMBL477772 | PAZOPANIB | 4 | 15,540 |
| CHEMBL502835 | NINTEDANIB | 4 | 8,545 |
| CHEMBL535 | SUNITINIB | 4 | 79,020 |
| CHEMBL608533 | MIDOSTAURIN | 4 | 7,259 |
| CHEMBL223360 | LINIFANIB | 3 | 3,925 |
| CHEMBL603469 | LESTAURTINIB | 3 | |
| CHEMBL1230609 | FORETINIB | 2 | 3,096 |
| CHEMBL1721885 | SU-014813 | 2 | 363 |
| CHEMBL1980297 | ILORASERTIB | 2 | 581 |
| CHEMBL1980715 | LAUROGUADINE | 2 | 294 |
| CHEMBL475251 | R-406 | 2 | 762 |
| CHEMBL521851 | PICTILISIB | 2 | 6,071 |
| CHEMBL572878 | TOZASERTIB | 2 | 2,998 |
| CHEMBL1908397 | KW-2449 | 1 | 622 |
| CHEMBL574738 | AST-487 | 1 | 451 |
PharmGKB: 1 entry (VIP=true, CPIC=false)
PharmGKB variants
2 variants.
| Variant | Genes | Level | Score | #Clin annots | Drugs |
|---|---|---|---|---|---|
| rs1052133 | CAMK1, OGG1 | 0.00 | 0 | ||
| rs293795 | CAMK1, OGG1 | 0.00 | 0 |
GtoPdb / IUPHAR curated pharmacology
(IUPHAR/BPS Guide to Pharmacology — expert-curated)
Target class: enzyme — CAMK1 family
Binding affinities (BindingDB)
7 measured of 7 human assays (7 total across all organisms); most potent 7 below. Values come from heterogeneous assays and are not directly comparable.
| Ligand | Measure | Value |
|---|---|---|
| Staurosporine | KD | 1.7 nM |
| PKC-412 | KD | 190 nM |
| 1-[4-[(4-ethyl-1-piperazinyl)methyl]-3-(trifluoromethyl)phenyl]-3-[4-[[6-(methylamino)-4-pyrimidinyl]oxy]phenyl]urea | KD | 1400 nM |
| 5-[(Z)-(5-fluoranyl-2-oxidanylidene-1H-indol-3-ylidene)methyl]-2,4-dimethyl-N-[(2S)-3-morpholin-4-yl-2-oxidanyl-propyl]-1H-pyrrole-3-carboxamide | KD | 2600 nM |
| 5-({4-[(2,3-dimethyl-2H-indazol-6-yl)(methyl)amino]pyrimidin-2-yl}amino)-2-methylbenzene-1-sulfonamide | KD | 2900 nM |
| N-[2-(diethylamino)ethyl]-5-[(Z)-(5-fluoro-2-oxo-1,2-dihydro-3H-indol-3-ylidene)methyl]-2,4-dimethyl-1H-pyrrole-3-carboxamide | KD | 3500 nM |
| 3-((3R,4R)-4-methyl-3-(methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino)piperidin-1-yl)-3-oxopropanenitrile | KD | 5000 nM |
ChEMBL bioactivities
126 potent at pChembl≥5 of 128 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).
| pChembl | Type | Value | Unit | Molecule |
|---|---|---|---|---|
| 9.00 | IC50 | 1 | nM | CHEMBL4635883 |
| 8.70 | IC50 | 2 | nM | CHEMBL4640712 |
| 8.61 | IC50 | 2.43 | nM | STAUROSPORINE |
| 8.52 | IC50 | 3.02 | nM | STAUROSPORINE |
| 8.52 | IC50 | 3 | nM | CHEMBL4635883 |
| 8.48 | IC50 | 3.33 | nM | STAUROSPORINE |
| 8.09 | IC50 | 8.2 | nM | CHEMBL4635883 |
| 7.96 | IC50 | 11 | nM | CHEMBL4635883 |
| 7.90 | Ki | 12.59 | nM | CHEMBL1980995 |
| 7.64 | IC50 | 23 | nM | CHEMBL4635883 |
| 7.57 | Kd | 27 | nM | STAUROSPORINE |
| 7.52 | Kd | 30 | nM | STAUROSPORINE |
| 7.50 | Ki | 31.62 | nM | CHEMBL2000271 |
| 7.10 | Ki | 79.43 | nM | CHEMBL1984162 |
| 7.00 | Ki | 100 | nM | CHEMBL1974870 |
| 6.90 | Ki | 125.9 | nM | CHEMBL2002726 |
| 6.89 | Kd | 130 | nM | LESTAURTINIB |
| 6.70 | Ki | 199.5 | nM | CHEMBL2004716 |
| 6.64 | Kd | 230 | nM | R-406 |
| 6.60 | Ki | 251.2 | nM | CHEMBL1971029 |
| 6.60 | Ki | 251.2 | nM | CHEMBL1991063 |
| 6.50 | Ki | 316.2 | nM | CHEMBL1987034 |
| 6.50 | Ki | 316.2 | nM | CHEMBL1965836 |
| 6.50 | Ki | 316.2 | nM | CHEMBL1993661 |
| 6.40 | Ki | 398.1 | nM | CHEMBL1987054 |
| 6.33 | Kd | 470 | nM | RUXOLITINIB |
| 6.30 | Ki | 501.2 | nM | CHEMBL1998159 |
| 6.20 | Ki | 631 | nM | CHEMBL1974328 |
| 6.10 | Ki | 794.3 | nM | CHEMBL1977041 |
| 6.10 | Ki | 794.3 | nM | CHEMBL1241473 |
| 6.01 | Kd | 970 | nM | SUNITINIB |
| 6.00 | IC50 | 1000 | nM | TP-030n |
| 6.00 | Ki | 1000 | nM | CHEMBL504950 |
| 6.00 | Ki | 1000 | nM | ILORASERTIB |
| 5.96 | Kd | 1100 | nM | TAE-684 |
| 5.92 | Kd | 1200 | nM | TOFACITINIB CITRATE |
| 5.92 | Kd | 1200 | nM | TOFACITINIB |
| 5.90 | Ki | 1259 | nM | CHEMBL1972584 |
| 5.90 | Ki | 1259 | nM | CHEMBL2002479 |
| 5.90 | Ki | 1259 | nM | CHEMBL2001751 |
| 5.90 | Ki | 1259 | nM | CHEMBL1979577 |
| 5.90 | Ki | 1259 | nM | CHEMBL1990885 |
| 5.85 | Kd | 1400 | nM | KW-2449 |
| 5.80 | Kd | 1600 | nM | FEDRATINIB |
| 5.80 | Ki | 1585 | nM | CHEMBL2002165 |
| 5.80 | Ki | 1585 | nM | CHEMBL2000832 |
| 5.80 | Ki | 1585 | nM | CHEMBL1965988 |
| 5.80 | Ki | 1585 | nM | CHEMBL2000685 |
| 5.80 | Ki | 1585 | nM | CHEMBL1979883 |
| 5.80 | Ki | 1585 | nM | CHEMBL1967720 |
PubChem BioAssay actives
45 with measured affinity, of 1622 total; 29 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 |
|---|---|---|---|---|
| 2-[(3S)-3-aminopiperidin-1-yl]-4-[[2,6-di(propan-2-yl)-4-pyridinyl]amino]pyrimidine-5-carboxamide | 1668858: Inhibition of human CAMK1A using KKALRRQETVDAL as substrate in presence of [gamma-33P]-ATP by hotspot kinase assay | ic50 | 0.0010 | uM |
| 2-[(3S)-3-aminopiperidin-1-yl]-4-[3,5-bis(2-cyanopropan-2-yl)anilino]pyrimidine-5-carboxamide | 1668858: Inhibition of human CAMK1A using KKALRRQETVDAL as substrate in presence of [gamma-33P]-ATP by hotspot kinase assay | ic50 | 0.0020 | uM |
| (2S,3R,4R,6R)-3-methoxy-2-methyl-4-(methylamino)-29-oxa-1,7,17-triazaoctacyclo[12.12.2.12,6.07,28.08,13.015,19.020,27.021,26]nonacosa-8,10,12,14,19,21,23,25,27-nonaen-16-one | 2198154: Inhibition of human CAMK1a using KKALRRQETVDAL as substrate preincubated for 20 mins followed by [gamma-33P]-ATP addition and measured after 120 mins by radiometric Hot-SpotSM Kinase assay | ic50 | 0.0024 | uM |
| Abemaciclib | 1551240: Inhibition of wild-type human full length CAMK1A (M1 to L370 residues) expressed in bacterial expression system assessed as residual activity at 50 nM by Kinomescan method relative to control | ki | 0.0100 | uM |
| (15S,16S,18R)-16-hydroxy-16-(hydroxymethyl)-15-methyl-28-oxa-4,14,19-triazaoctacyclo[12.11.2.115,18.02,6.07,27.08,13.019,26.020,25]octacosa-1,6,8,10,12,20,22,24,26-nonaen-3-one | 507852: Binding affinity to CAMK1 | kd | 0.1300 | uM |
| 6-[[5-fluoro-2-(3,4,5-trimethoxyanilino)pyrimidin-4-yl]amino]-2,2-dimethyl-4H-pyrido[3,2-b][1,4]oxazin-3-one | 624922: Binding constant for CAMK1 kinase domain | kd | 0.2300 | uM |
| Ruxolitinib | 624922: Binding constant for CAMK1 kinase domain | kd | 0.4700 | uM |
| Sunitinib | 436009: Binding constant for full-length CAMK1 | kd | 0.9700 | uM |
| 5-chloro-2-N-[2-methoxy-4-[4-(4-methylpiperazin-1-yl)piperidin-1-yl]phenyl]-4-N-(2-propan-2-ylsulfonylphenyl)pyrimidine-2,4-diamine | 624922: Binding constant for CAMK1 kinase domain | kd | 1.1000 | uM |
| Tofacitinib | 624922: Binding constant for CAMK1 kinase domain | kd | 1.2000 | uM |
| [4-[(E)-2-(1H-indazol-3-yl)ethenyl]phenyl]-piperazin-1-ylmethanone | 624922: Binding constant for CAMK1 kinase domain | kd | 1.4000 | uM |
| Fedratinib | 624922: Binding constant for CAMK1 kinase domain | kd | 1.6000 | uM |
| N-[3-(5-chloro-1H-pyrrolo[2,3-b]pyridine-3-carbonyl)-2,4-difluorophenyl]propane-1-sulfonamide | 624922: Binding constant for CAMK1 kinase domain | kd | 1.9000 | uM |
| Midostaurin | 436009: Binding constant for full-length CAMK1 | kd | 2.0000 | uM |
| Pazopanib | 436009: Binding constant for full-length CAMK1 | kd | 2.1000 | uM |
| (3Z)-5-[(2,6-dichlorophenyl)methylsulfonyl]-3-[[3,5-dimethyl-4-[(2R)-2-(pyrrolidin-1-ylmethyl)pyrrolidine-1-carbonyl]-1H-pyrrol-2-yl]methylidene]-1H-indol-2-one | 624922: Binding constant for CAMK1 kinase domain | kd | 2.1000 | uM |
| 4-[4-[3-[4-[(propan-2-ylamino)methyl]anilino]-1H-pyrazol-5-yl]phenyl]benzene-1,3-diol | 301979: Inhibition of CAMK1 | ic50 | 2.1300 | uM |
| 1-[4-[(4-ethylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl]-3-[4-[6-(methylamino)pyrimidin-4-yl]oxyphenyl]urea | 436009: Binding constant for full-length CAMK1 | kd | 3.0000 | uM |
| 1-pentyl-4-(2-phenylmethoxyphenyl)imidazol-2-amine;hydrochloride | 1734144: Inhibition of wild-type human CAMK1alpha using KKALRRQETVDAL peptide as substrate in presence of Ca2+ calmodulin and [gamma-33P]-ATP by radiometric hotspot kinase assay | ic50 | 3.0000 | uM |
| 5-[(Z)-(5-fluoro-2-oxo-1H-indol-3-ylidene)methyl]-N-[(2S)-2-hydroxy-3-morpholin-4-ylpropyl]-2,4-dimethyl-1H-pyrrole-3-carboxamide | 436009: Binding constant for full-length CAMK1 | kd | 3.3000 | uM |
| 2-N-(3,5-dichlorophenyl)-4-N-[4-(dimethylamino)cyclohexyl]-5-(3-methyl-1,2-oxazol-5-yl)pyrimidine-2,4-diamine | 721400: Inhibition of CAMK1 (unknown origin) in presence of ATP | ic50 | 3.8800 | uM |
| 14,15-diazatetracyclo[7.6.1.02,7.013,16]hexadeca-1(15),2,4,6,9(16),10,12-heptaen-8-one | 256643: Average Binding Constant for CAMK1; NA=Not Active at 10 uM | kd | 4.1000 | uM |
| (4-hydroxypiperidin-1-yl)-[4-[[4-[4-(3-methylsulfonylpropoxy)indol-1-yl]pyrimidin-2-yl]amino]cyclohexyl]methanone | 769531: Binding affinity to CAMK1 (unknown origin) | kd | 4.3000 | uM |
| 4-[2-(1H-indazol-4-yl)-6-[(4-methylsulfonylpiperazin-1-yl)methyl]thieno[3,2-d]pyrimidin-4-yl]morpholine | 624922: Binding constant for CAMK1 kinase domain | kd | 4.7000 | uM |
| methyl 2-hydroxy-3-[N-[4-[methyl-[2-(4-methylpiperazin-1-yl)acetyl]amino]phenyl]-C-phenylcarbonimidoyl]-1H-indole-6-carboxylate | 624922: Binding constant for CAMK1 kinase domain | kd | 5.9000 | uM |
| 1-N’-[3-fluoro-4-[6-methoxy-7-(3-morpholin-4-ylpropoxy)quinolin-4-yl]oxyphenyl]-1-N-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide | 624922: Binding constant for CAMK1 kinase domain | kd | 5.9000 | uM |
| 4-N-[5-(diethylamino)pentan-2-yl]-2-[(E)-2-(2,4,6-trichlorophenyl)ethenyl]quinazoline-4,6-diamine | 1452760: Inhibition of CaMK1alpha (unknown origin) | ic50 | 6.9000 | uM |
| N-[4-[4-(4-methylpiperazin-1-yl)-6-[(5-methyl-1H-pyrazol-3-yl)amino]pyrimidin-2-yl]sulfanylphenyl]cyclopropanecarboxamide | 624922: Binding constant for CAMK1 kinase domain | kd | 7.0000 | uM |
| N-[(2S,3R,4R,6R,18S)-18-hydroxy-3-methoxy-2-methyl-16-oxo-29-oxa-1,7,17-triazaoctacyclo[12.12.2.12,6.07,28.08,13.015,19.020,27.021,26]nonacosa-8,10,12,14,19,21,23,25,27-nonaen-4-yl]-N-methylbenzamide | 507852: Binding affinity to CAMK1 | kd | 7.4000 | uM |
CTD chemical–gene interactions
37 total (human), top 30 by PubMed support.
| Chemical | Actions (top 5) | PubMed papers |
|---|---|---|
| Tretinoin | increases expression | 2 |
| aristolochic acid I | increases expression | 1 |
| triphenyl phosphate | affects expression | 1 |
| bisphenol A | increases expression | 1 |
| beta-lapachone | decreases expression | 1 |
| sodium bichromate | decreases expression | 1 |
| afimoxifene | decreases response to substance | 1 |
| sodium arsenite | decreases expression, increases abundance | 1 |
| W 7 | decreases reaction, increases phosphorylation | 1 |
| cobaltous chloride | decreases expression | 1 |
| nickel sulfate | increases expression | 1 |
| S-(1,2-dichlorovinyl)cysteine | affects cotreatment, decreases expression | 1 |
| tamibarotene | increases expression | 1 |
| 1,2-bis(2-aminophenoxy)ethane N,N,N’,N’-tetraacetic acid acetoxymethyl ester | decreases reaction, increases phosphorylation | 1 |
| KN 93 | decreases activity | 1 |
| CGP 52608 | affects binding, increases reaction | 1 |
| STO 609 | increases activity, increases phosphorylation | 1 |
| bisphenol S | increases expression | 1 |
| jinfukang | affects cotreatment, increases expression | 1 |
| bisphenol AF | increases expression | 1 |
| Sunitinib | decreases expression | 1 |
| Air Pollutants | affects expression, increases abundance | 1 |
| Arsenic | decreases expression, increases abundance | 1 |
| Atrazine | decreases expression | 1 |
| Benzo(a)pyrene | increases methylation | 1 |
| Cisplatin | affects cotreatment, increases expression | 1 |
| Diuron | decreases expression | 1 |
| Enzyme Inhibitors | decreases activity, increases O-linked glycosylation | 1 |
| Ivermectin | decreases expression | 1 |
| Lipopolysaccharides | affects cotreatment, decreases expression | 1 |
ChEMBL screening assays
324 unique, capped per target: 322 binding, 2 functional
Representative assays (with source publication via chembl_document):
| Assay ID | Type | Description | Source paper |
|---|---|---|---|
| CHEMBL1004136 | Binding | Inhibition of CAMK1 at 1 uM relative to control | Novel potent BRAF inhibitors: toward 1 nM compounds through optimization of the central phenyl ring. — J Med Chem |
| CHEMBL1963816 | Functional | PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member name: CAMK1 | PubChem BioAssay data set |
Cellosaurus cell lines
4 cell lines: 3 cancer cell line, 1 transformed cell line
First 10 cell lines (id-ordered, not curated):
| Cellosaurus | Name | Category | Sex |
|---|---|---|---|
| CVCL_D7LI | Ubigene A-549 CAMK1 KO | Cancer cell line | Male |
| CVCL_D8I9 | Ubigene HCT 116 CAMK1 KO | Cancer cell line | Male |
| CVCL_D9AS | Ubigene HEK293 CAMK1 KO | Transformed cell line | Female |
| CVCL_D9Z6 | Ubigene HeLa CAMK1 KO | Cancer cell line | Female |
Clinical trials (associated diseases)
300 trials via MONDO — disease-level, not drug-specific.
| Trial | Phase | Status | Title |
|---|---|---|---|
| NCT00414765 | PHASE4 | COMPLETED | Aldesleukin in Participants With Metastatic Renal Cell Carcinoma or Metastatic Melanoma |
| NCT00777504 | PHASE4 | UNKNOWN | Study to the Optimal Duration of Therapy With Oral Angiogenesis Inhibitors |
| NCT00930345 | PHASE4 | TERMINATED | Biological, Pathological and Imagery Markers in the First-line Treatment of Metastatic Clear-cell Renal Cell Carcinoma |
| NCT01206764 | PHASE4 | COMPLETED | A Trial of Everolimis in Patients With Advanced Renal Cell Carcinoma. |
| NCT01266837 | PHASE4 | COMPLETED | Open Label, Single Arm Trial to Characterize Patients With Metastatic RCC Treated With Everolimus After Failure of the First VEGF-targeted Therapy (MARC-2) |
| NCT02056587 | PHASE4 | COMPLETED | Everolimus in Patients With Metastatic Renal Cell Carcinoma Following Progression on Prior Bevacizumab Treatment |
| NCT02338570 | PHASE4 | TERMINATED | Outcome-related Factors in Patients With Metastatic Renal Cell Carcinoma Treated With Everolimus (ORCHIDEE) |
| NCT02596035 | PHASE4 | COMPLETED | An Investigational Immuno-therapy Safety Trial of Nivolumab in Patients With Advanced or Metastatic Renal Cell Carcinoma |
| NCT02982954 | PHASE4 | COMPLETED | A Study to Evaluate the Safety of Nivolumab and Ipilimumab in Subjects With Previously Untreated Advanced or Metastatic Renal Cell Cancer |
| NCT05949424 | PHASE4 | UNKNOWN | OPTI - DOSE: Optimal Dosing of Oral Anticancer Drugs in Older Adults |
| NCT07028125 | PHASE4 | RECRUITING | Digital Monitoring of Self-reported Symptoms by Patients Treated With Cabozantinib Plus Nivolumab for Advanced Clear-cell Renal Carcinoma |
| NCT07405086 | PHASE4 | RECRUITING | Morning Versus Afternoon Administration of Immunotherapy for the Treatment of Advanced or Metastatic Solid Tumors, The Knight SHIFT Study |
| NCT00033904 | PHASE3 | COMPLETED | Survival Study Of Oncophage® vs. Observation In Patients With Kidney Cancer |
| NCT00126178 | PHASE3 | TERMINATED | Clinical Trial Studying a Personalized Cancer Vaccine in Patients With Non-metastatic Kidney Cancer |
| NCT00291369 | PHASE3 | COMPLETED | Cytokines in Patients With Metastatic Renal Cell Carcinoma of Intermediate Prognosis |
| NCT00326898 | PHASE3 | COMPLETED | Sunitinib Malate or Sorafenib Tosylate in Treating Patients With Kidney Cancer That Was Removed By Surgery |
| NCT00410124 | PHASE3 | COMPLETED | RAD001 Plus Best Supportive Care (BSC) Versus BSC Plus Placebo in Patients With Metastatic Carcinoma of the Kidney Which Has Progressed After Treatment With Sorafenib and/or Sunitinib |
| NCT00474786 | PHASE3 | COMPLETED | Temsirolimus Versus Sorafenib As Second-Line Therapy In Patients With Advanced RCC Who Have Failed First-Line Sunitinib |
| NCT00478114 | PHASE3 | COMPLETED | Efficacy and Safety of Sorafenib in Advanced Renal Cell Carcinoma (RCC) |
| NCT00606632 | PHASE3 | COMPLETED | Pre-surgical Detection of Clear Cell Renal Cell Carcinoma (ccRCC) Using Radiolabeled G250-Antibody |
| NCT00606866 | PHASE3 | COMPLETED | MRI Study of BAY 43-9006 in Metastatic Renal Cell Carcinoma |
| NCT00631371 | PHASE3 | COMPLETED | Study Comparing Bevacizumab + Temsirolimus vs. Bevacizumab + Interferon-Alfa In Advanced Renal Cell Carcinoma Subjects |
| NCT00732914 | PHASE3 | COMPLETED | Sequential Study to Treat Renal Cell Carcinoma |
| NCT00869011 | PHASE3 | UNKNOWN | Exercise for Patients With Renal Cell Cancer Receiving Sunitinib |
| NCT00930033 | PHASE3 | COMPLETED | Clinical Trial to Assess the Importance of Nephrectomy |
| NCT01030783 | PHASE3 | COMPLETED | A Study to Compare Tivozanib (AV-951) to Sorafenib in Subjects With Advanced Renal Cell Carcinoma |
| NCT01076010 | PHASE3 | COMPLETED | An Extension Treatment Protocol for Subjects Who Have Participated in a Study of Tivozanib Versus Sorafenib in Kidney Carcinoma (Protocol AV-951-09-301). |
| NCT01198158 | PHASE3 | TERMINATED | Everolimus With or Without Bevacizumab in Treating Patients With Advanced Kidney Cancer That Progressed After First-Line Therapy |
| NCT01223027 | PHASE3 | COMPLETED | Study of Dovitinib Versus Sorafenib in Patients With Metastatic Renal Cell Carcinoma |
| NCT01224288 | PHASE3 | ACTIVE_NOT_RECRUITING | Dynamic Contrast Enhancement Computed Tomography for Evaluating Tumor Perfusion in Patients With Metastatic Renal Cell Carcinoma Receiving Targeted Therapies: Renal Cell Carcinoma (RCC) Scramble |
| NCT01235962 | PHASE3 | COMPLETED | A Study to Evaluate Pazopanib as an Adjuvant Treatment for Localized Renal Cell Carcinoma (RCC) |
| NCT01265810 | PHASE3 | COMPLETED | Caphosol in Oral Mucositis Due to Targeted Therapy |
| NCT01265901 | PHASE3 | COMPLETED | IMA901 in Patients Receiving Sunitinib for Advanced/Metastatic Renal Cell Carcinoma |
| NCT01481870 | PHASE3 | UNKNOWN | Comparison of Sequential Therapies With Sunitinib and Sorafenib in Advanced Renal Cell Carcinoma |
| NCT01575548 | PHASE3 | ACTIVE_NOT_RECRUITING | Pazopanib Hydrochloride in Treating Patients With Metastatic Kidney Cancer Who Have No Evidence of Disease After Surgery |
| NCT01582672 | PHASE3 | TERMINATED | Phase 3 Trial of Autologous Dendritic Cell Immunotherapy Plus Standard Treatment of Advanced Renal Cell Carcinoma |
| NCT01613846 | PHASE3 | COMPLETED | Phase III Sequential Open-label Study to Evaluate the Efficacy and Safety of Sorafenib Followed by Pazopanib Versus Pazopanib Followed by Sorafenib in the Treatment of Advanced / Metastatic Renal Cell Carcinoma (SWITCH-II) |
| NCT01762592 | PHASE3 | WITHDRAWN | REDECT 2: REnal Masses: Pivotal Trial to DEteCT Clear Cell Renal Cell Carcinoma With PET/CT |
| NCT01865747 | PHASE3 | COMPLETED | A Study of Cabozantinib (XL184) vs Everolimus in Subjects With Metastatic Renal Cell Carcinoma |
| NCT02231749 | PHASE3 | COMPLETED | Nivolumab Combined With Ipilimumab Versus Sunitinib in Previously Untreated Advanced or Metastatic Renal Cell Carcinoma (CheckMate 214) |
Related Atlas pages
- Disease cohort memberships (association, not causation — diseases whose associated-gene cohort lists this gene; a subset are also under Associated diseases): nonpapillary renal cell carcinoma