CAMKK1

Summary

CAMKK1 (calcium/calmodulin dependent protein kinase kinase 1, HGNC:1469) is a protein-coding gene on chromosome 17p13.2, encoding Calcium/calmodulin-dependent protein kinase kinase 1 (Q8N5S9). Calcium/calmodulin-dependent protein kinase that belongs to a proposed calcium-triggered signaling cascade involved in a number of cellular processes.

The product of this gene belongs to the Serine/Threonine protein kinase family, and to the Ca(2+)/calmodulin-dependent protein kinase subfamily. This protein plays a role in the calcium/calmodulin-dependent (CaM) kinase cascade. Three transcript variants encoding two distinct isoforms have been identified for this gene.

Source: NCBI Gene 84254 — RefSeq curated summary.

At a glance

• GWAS associations: 2
• Clinical variants (ClinVar): 96 total
• Druggable target: yes — 17 molecules with ChEMBL bioactivity
• MANE Select transcript: NM_032294

Identifiers

Gene identifiers

Field	Value
HGNC ID	HGNC:1469
Approved symbol	CAMKK1
Name	calcium/calmodulin dependent protein kinase kinase 1
Location	17p13.2
Locus type	gene with protein product
Status	Approved
Aliases	DKFZp761M0423, CAMKKA, MGC34095
Ensembl gene	ENSG00000004660
Ensembl biotype	protein_coding
OMIM	611411
Entrez	84254

Gene structure

Transcript identifiers

Ensembl transcripts: 6 — 5 protein_coding, 1 retained_intron

ENST00000158166, ENST00000348335, ENST00000381769, ENST00000573483, ENST00000895459, ENST00000959110

RefSeq mRNA: 3 — MANE Select: NM_032294 NM_032294, NM_172206, NM_172207

CCDS: CCDS11038, CCDS11039, CCDS86560

Canonical transcript exons

ENST00000348335 — 16 exons

Exon	Start	End
ENSE00000343735	3876223	3876422
ENSE00000343738	3869801	3869888
ENSE00000670749	3869487	3869615
ENSE00000670753	3872554	3872627
ENSE00000875828	3882528	3882564
ENSE00000875830	3880346	3880434
ENSE00001048672	3881627	3881648
ENSE00001284636	3865908	3866011
ENSE00001489779	3860315	3862283
ENSE00002390564	3873409	3873462
ENSE00003518045	3883042	3883175
ENSE00003562587	3884380	3884427
ENSE00003564299	3885328	3885730
ENSE00003671228	3883884	3883937
ENSE00003684520	3883429	3883480
ENSE00003892021	3892939	3893053

Expression profiles

Bgee: expression breadth ubiquitous, 210 present calls, max score 95.07.

FANTOM5 (CAGE): breadth ubiquitous, TPM avg 4.4004 / max 95.1084, expressed in 1291 samples.

FANTOM5 promoters (4 alternative TSS)

Promoter ID	TPM avg	Samples expressed
163884	2.6486	761
163883	1.2476	696
163882	0.4313	250
163881	0.0728	36

Top tissues by expression

251 total, by Bgee expression score (0-100, higher = more expressed):

Tissue	Anatomy ID	Expression score	Quality
right frontal lobe	UBERON:0002810	95.07	gold quality
pancreatic ductal cell	CL:0002079	94.92	gold quality
Brodmann (1909) area 9	UBERON:0013540	94.84	gold quality
prefrontal cortex	UBERON:0000451	93.90	gold quality
right hemisphere of cerebellum	UBERON:0014890	93.45	gold quality
cerebellar hemisphere	UBERON:0002245	93.35	gold quality
cerebellar cortex	UBERON:0002129	93.27	gold quality
middle temporal gyrus	UBERON:0002771	92.98	gold quality
frontal cortex	UBERON:0001870	92.72	gold quality
dorsolateral prefrontal cortex	UBERON:0009834	92.72	gold quality
cerebellum	UBERON:0002037	92.44	gold quality
primary visual cortex	UBERON:0002436	92.23	gold quality
endothelial cell	CL:0000115	92.00	gold quality
neocortex	UBERON:0001950	91.85	gold quality
occipital lobe	UBERON:0002021	91.42	gold quality
anterior cingulate cortex	UBERON:0009835	91.21	gold quality
putamen	UBERON:0001874	90.59	gold quality
nucleus accumbens	UBERON:0001882	90.50	gold quality
cerebral cortex	UBERON:0000956	89.94	gold quality
caudate nucleus	UBERON:0001873	89.93	gold quality
forebrain	UBERON:0001890	88.60	gold quality
brain	UBERON:0000955	88.33	gold quality
Brodmann (1909) area 23	UBERON:0013554	88.04	gold quality
cerebellar vermis	UBERON:0004720	87.87	silver quality
amygdala	UBERON:0001876	87.57	gold quality
adenohypophysis	UBERON:0002196	87.45	gold quality
superior frontal gyrus	UBERON:0002661	86.91	gold quality
pituitary gland	UBERON:0000007	86.67	gold quality
parotid gland	UBERON:0001831	86.10	gold quality
upper arm skin	UBERON:0004263	85.98	gold quality

Single-cell (SCXA)

Detected in 1 experiment(s), a significant marker in 0.

Experiment	Marker?	Max mean expression
E-ANND-3	no	4.22

Regulation

Is transcription factor: no

miRNA regulators (miRDB)

89 targeting CAMKK1, 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-4262	100.00	73.26	3931
HSA-MIR-6867-5P	100.00	82.21	3464
HSA-MIR-181A-5P	99.99	72.96	2995
HSA-MIR-181B-5P	99.99	72.97	2996
HSA-MIR-181C-5P	99.99	72.95	2996
HSA-MIR-181D-5P	99.99	73.04	2997
HSA-MIR-3185	99.99	68.12	1959
HSA-MIR-4775	99.98	75.00	6394
HSA-MIR-23B-5P	99.98	66.07	587
HSA-MIR-548N	99.98	71.94	4170
HSA-MIR-103A-3P	99.98	69.14	1595
HSA-MIR-107	99.98	69.14	1595
HSA-MIR-3065-5P	99.97	71.56	3281
HSA-MIR-2110	99.96	66.68	1930
HSA-MIR-23A-5P	99.94	65.39	468
HSA-MIR-6721-5P	99.93	68.92	2981
HSA-MIR-3119	99.92	71.34	2390
HSA-MIR-515-5P	99.92	69.82	2343
HSA-MIR-519E-5P	99.92	69.62	2358
HSA-MIR-145-5P	99.92	71.13	1836
HSA-MIR-5195-3P	99.92	70.92	1877
HSA-MIR-3529-3P	99.90	73.55	3045
HSA-MIR-6783-3P	99.89	67.92	2059
HSA-MIR-1343-3P	99.89	66.78	1815
HSA-MIR-6857-5P	99.87	65.32	985
HSA-MIR-6756-5P	99.82	67.97	2466
HSA-MIR-3180-5P	99.82	69.12	2422
HSA-MIR-3150A-3P	99.76	64.44	1640
HSA-MIR-6763-5P	99.76	64.68	1767
HSA-MIR-6752-3P	99.72	66.71	1587

Literature-anchored findings (GeneRIF, showing 7)

• role for CaMKKalpha in the differentiation of monocytic cells (PMID:18270593)
• CaMKIalpha is a widely expressed protein kinase, suggesting that Ca2+ is likely to be functionally important in the control of mitochondrial dynamics through regulation of Drp1 phosphorylation in neurons and other cell types.[CaMKIalpha] (PMID:18695047)
• Adiponectin activates AMP-activated protein kinase in muscle cells via APPL1/LKB1-dependent and phospholipase C/Ca2+/Ca2+/calmodulin-dependent protein kinase kinase-dependent pathways (PMID:19520843)
• CAMKK1 might contribute to the risk of lung cancer in Chinese populations. (PMID:23737288)
• CaMKK1 does not play a pivotal role in the calcium signaling cascade regulating adrenal aldosterone production. (PMID:25679868)
• Site-directed mutagenesis analysis revealed that Leu(358) in CaMKKbeta/Ile(322) in CaMKKalpha confer, at least in part, a distinct recognition of AMPK but not of CaMKIalpha. (PMID:27151216)
• Polymorphism rs7214723 in CAMKK1: a new genetic variant associated with cardiovascular diseases. (PMID:34165505)

Cross-species orthologs

6 orthologs

Organism	Symbol	Gene ID
danio_rerio	camkk1b	ENSDARG00000015134
danio_rerio	camkk1a	ENSDARG00000035452
mus_musculus	Camkk1	ENSMUSG00000020785
rattus_norvegicus	Camkk1	ENSRNOG00000018242
drosophila_melanogaster	CG17698	FBGN0040056
caenorhabditis_elegans		WBGENE00000518

Paralogs (22): CAMK1G (ENSG00000008118), CAMK2B (ENSG00000058404), CAMK2A (ENSG00000070808), MYLK2 (ENSG00000101306), CAMKK2 (ENSG00000110931), STK11 (ENSG00000118046), STK33 (ENSG00000130413), PNCK (ENSG00000130822), DCLK1 (ENSG00000133083), CAMK1 (ENSG00000134072), 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 kinase 1 — Q8N5S9 (reviewed: Q8N5S9)

Alternative names: CaM-kinase IV kinase, Calcium/calmodulin-dependent protein kinase kinase alpha

All UniProt accessions (2): Q8N5S9, J3KPJ3

UniProt curated annotations — full annotation on UniProt →

Function. Calcium/calmodulin-dependent protein kinase that belongs to a proposed calcium-triggered signaling cascade involved in a number of cellular processes. Phosphorylates CAMK1, CAMK1D, CAMK1G and CAMK4. Involved in regulating cell apoptosis. Promotes cell survival by phosphorylating AKT1/PKB that inhibits pro-apoptotic BAD/Bcl2-antagonist of cell death.

Subunit / interactions. Interacts with CAMK4 and calmodulin.

Subcellular location. Cytoplasm. Nucleus.

Post-translational modifications. Appears to be autophosphorylated in a Ca(2+)/calmodulin-dependent manner. Phosphorylated at multiple sites by PRCAKA/PKA. Phosphorylation of Ser-458 is blocked upon binding to Ca(2+)/calmodulin. In vitro, phosphorylated by CAMK1 and CAMK4.

Activity regulation. Activated by Ca(2+)/calmodulin. Binding of calmodulin may relieve intrasteric autoinhibition. Partially inhibited upon phosphorylation by PRCAKA/PKA. May be regulated through phosphorylation by CAMK1 and CAMK4.

Domain organisation. The autoinhibitory domain overlaps with the calmodulin binding region and may be involved in intrasteric autoinhibition. The RP domain (arginine/proline-rich) is involved in the recognition of CAMKI and CAMK4 as substrates.

Similarity. Belongs to the protein kinase superfamily. Ser/Thr protein kinase family.

Isoforms (2)

UniProt ID	Names	Canonical?
Q8N5S9-1	1, A, Variant 3	yes
Q8N5S9-2	2, B, Variant 1

RefSeq proteins (3): NP_115670, NP_757343, NP_757344 (=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

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 (42 total): helix 10, modified residue 8, strand 8, region of interest 5, turn 3, splice variant 2, binding site 2, chain 1, domain 1, sequence variant 1, active site 1

Structure

Experimental structures (PDB)

2 structures.

PDB	Method	Resolution (Å)
6CCF	X-RAY DIFFRACTION	2.1
6CD6	X-RAY DIFFRACTION	2.2

Predicted structure (AlphaFold)

Model	pLDDT	Fraction very-high
AF-Q8N5S9-F1	72.06	0.44

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): 275 (proton acceptor)

Ligand- & substrate-binding residues (2): 134–142; 157

Post-translational modifications (8): 67, 74, 78, 100, 108, 458, 475, 492

Function

Pathways and Gene Ontology

Reactome pathways

20 pathways

ID	Pathway
R-HSA-111932	CaMK IV-mediated phosphorylation of CREB
R-HSA-442729	CREB1 phosphorylation through the activation of CaMKII/CaMKK/CaMKIV cascasde
R-HSA-9619229	Activation of RAC1 downstream of NMDARs
R-HSA-111885	Opioid Signalling
R-HSA-111933	Calmodulin induced events
R-HSA-111996	Ca-dependent events
R-HSA-111997	CaM pathway
R-HSA-112040	G-protein mediated events
R-HSA-112043	PLC beta mediated events
R-HSA-112314	Neurotransmitter receptors and postsynaptic signal transmission
R-HSA-112315	Transmission across Chemical Synapses
R-HSA-112316	Neuronal System
R-HSA-1489509	DAG and IP3 signaling
R-HSA-162582	Signal Transduction
R-HSA-372790	Signaling by GPCR
R-HSA-388396	GPCR downstream signalling
R-HSA-418594	G alpha (i) signalling events
R-HSA-438064	Post NMDA receptor activation events
R-HSA-442755	Activation of NMDA receptors and postsynaptic events
R-HSA-9006925	Intracellular signaling by second messengers

MSigDB gene sets: 162 (showing top): GSE45365_CTRL_VS_MCMV_INFECTION_NK_CELL_UP, RNGTGGGC_UNKNOWN, KEGG_ADIPOCYTOKINE_SIGNALING_PATHWAY, REACTOME_CREB1_PHOSPHORYLATION_THROUGH_THE_ACTIVATION_OF_CAMKII_CAMKK_CAMKIV_CASCASDE, GCANCTGNY_MYOD_Q6, AREB6_01, SP1_Q2_01, AP1_Q4_01, BACH2_01, TGANTCA_AP1_C, REACTOME_TRANSMISSION_ACROSS_CHEMICAL_SYNAPSES, AP1FJ_Q2, GOMF_PROTEIN_KINASE_ACTIVITY, GOMF_KINASE_ACTIVITY, GOMF_CALCIUM_CALMODULIN_DEPENDENT_PROTEIN_KINASE_ACTIVITY

GO Biological Process (2): intracellular signal transduction (GO:0035556), protein phosphorylation (GO:0006468)

GO Molecular Function (10): 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), protein kinase activity (GO:0004672), protein serine/threonine kinase activity (GO:0004674), protein binding (GO:0005515), kinase activity (GO:0016301), transferase activity (GO:0016740)

GO Cellular Component (4): nucleoplasm (GO:0005654), cytoplasm (GO:0005737), cytosol (GO:0005829), nucleus (GO:0005634)

Reactome top-level categories

Rollup of top-17 pathways:

Category	Pathways
Post NMDA receptor activation events	2
Signal Transduction	2
Calmodulin induced events	1
G alpha (i) signalling events	1
CaM pathway	1
PLC beta mediated events	1
Ca-dependent events	1
DAG and IP3 signaling	1
Opioid Signalling	1
G-protein mediated events	1
Transmission across Chemical Synapses	1
Neuronal System	1
Intracellular signaling by second messengers	1
Signaling by GPCR	1
GPCR downstream signalling	1

GO top-level categories

Rollup of top GO terms by namespace:

Category	Terms
cellular anatomical structure	3
intracellular anatomical structure	2
protein kinase activity	2
signal transduction	1
phosphorylation	1
protein modification process	1
protein serine/threonine kinase activity	1
protein binding	1
adenyl ribonucleotide binding	1
purine ribonucleoside triphosphate binding	1
nucleoside phosphate binding	1
heterocyclic compound binding	1
kinase activity	1
phosphotransferase activity, alcohol group as acceptor	1
catalytic activity, acting on a protein	1
binding	1
transferase activity, transferring phosphorus-containing groups	1
catalytic activity	1
nuclear lumen	1
cytoplasm	1
intracellular membrane-bounded organelle	1

Protein interactions and networks

STRING

842 interactions, top by confidence (×1000):

Protein A	Protein B	Partner UniProt	Score
CAMKK1	CALML3	P27482	873
CAMKK1	CALML5	Q9NZT1	873
CAMKK1	CALML6	Q8TD86	862
CAMKK1	CALML4	Q96GE6	862
CAMKK1	CALM1	P02593	818
CAMKK1	CREB1	P16220	470
CAMKK1	GGA2	Q9UJY4	460
CAMKK1	UNKL	Q9H9P5	452
CAMKK1	FAM171A1	Q5VUB5	427
CAMKK1	PRKAG1	P54619	417
CAMKK1	AKT1	P31749	417
CAMKK1	CDC42BPB	Q9Y5S2	412
CAMKK1	GGA1	Q9UJY5	412
CAMKK1	RABEP1	Q15276	408
CAMKK1	PRKAB1	Q9Y478	403

IntAct

33 interactions, top by confidence:

A	B	Type	Score
YWHAH	CAMKK1	psi-mi:“MI:0407”(direct interaction)	0.760
CAMKK1	YWHAH	psi-mi:“MI:0915”(physical association)	0.760
YWHAH	CAMKK1	psi-mi:“MI:0915”(physical association)	0.760
LPIN3	CSNK2A2	psi-mi:“MI:0914”(association)	0.640
GARRE1	CAMKK1	psi-mi:“MI:0915”(physical association)	0.620
YWHAB	BLTP3B	psi-mi:“MI:0914”(association)	0.610
YWHAH	BLTP3B	psi-mi:“MI:0914”(association)	0.570
CAMKK1	YWHAE	psi-mi:“MI:0915”(physical association)	0.560
GARRE1	APOD	psi-mi:“MI:0914”(association)	0.530
CAMKK1	RUVBL2	psi-mi:“MI:0914”(association)	0.530
SFN	CAMKK1	psi-mi:“MI:0915”(physical association)	0.400
HSP90AB1	CAMKK1	psi-mi:“MI:0915”(physical association)	0.400
CAMKK1		psi-mi:“MI:0914”(association)	0.350
TRIM11	BTN3A3	psi-mi:“MI:0914”(association)	0.350
CAMK1	PSMD12	psi-mi:“MI:0914”(association)	0.350
CAMKK1	CTSA	psi-mi:“MI:0914”(association)	0.350
MKNK1	SEC16A	psi-mi:“MI:0914”(association)	0.350
CALM2	MYO1C	psi-mi:“MI:0914”(association)	0.350
CALM3	PLEKHG3	psi-mi:“MI:0914”(association)	0.350
TRIM11	RABGAP1L	psi-mi:“MI:0914”(association)	0.350
PADI6	PER1	psi-mi:“MI:0914”(association)	0.350
SELENBP1	ZNF24	psi-mi:“MI:0914”(association)	0.350
IRGM	HOXD13	psi-mi:“MI:0914”(association)	0.350

BioGRID (78): PRKAA1 (Biochemical Activity), ANXA7 (Affinity Capture-MS), CSNK1E (Affinity Capture-MS), DDB1 (Affinity Capture-MS), H3F3A (Affinity Capture-MS), NTHL1 (Affinity Capture-MS), RPS10 (Affinity Capture-MS), SAFB2 (Affinity Capture-MS), NSA2 (Affinity Capture-MS), C3orf17 (Affinity Capture-MS), FBXL6 (Affinity Capture-MS), ELAC2 (Affinity Capture-MS), KIAA2013 (Affinity Capture-MS), BRINP1 (Affinity Capture-MS), CAMKK1 (Affinity Capture-MS)

ESM2 similar proteins: A5PKJ4, B1AK53, B8Y466, D3ZG83, O14976, O54967, O60307, O70405, O75385, O96013, P0C865, P80192, P97756, Q02779, Q13164, Q17R13, Q2YDU3, Q3U1V8, Q3U214, Q3U2S4, Q3ULB5, Q3V016, Q4KMP7, Q4V793, Q5I1X5, Q5R8Z4, Q5TCX8, Q5U2X5, Q66HA1, Q66L42, Q6NZR5, Q6ZRS2, Q80XI6, Q80Y86, Q8BHL3, Q8BTW9, Q8C078, Q8CIP4, Q8N5S9, Q8TD08

Diamond homologs: A2XFF4, A3B529, A6ZU08, A8WYE4, A8X0C4, B3DL84, B4J3F1, B4KYX8, B4LDJ6, B8BBT7, D4AE59, F1QGZ6, O08679, O14965, O22932, O55099, O59790, O70126, O88445, O88831, P25341, P25389, P32801, P38990, P43637, P50526, P54645, P59241, P92958, P97756, Q05512, Q0D4B2, Q0GGW5, Q0JI49, Q10SC8, Q12263, Q13131, Q14680, Q15831, Q16W24

SIGNOR signaling

13 interactions.

A	Effect	B	Mechanism
CAMKK1	up-regulates	CAMK4	phosphorylation
CAMKK1	up-regulates	PRKAA1	phosphorylation
CALM1	up-regulates	CAMKK1	binding
CALM2	up-regulates	CAMKK1	binding
CALM3	up-regulates	CAMKK1	binding
CAMKK1	“up-regulates activity”	BRSK1	phosphorylation
PRKACA	“down-regulates activity”	CAMKK1	phosphorylation
CAMKK1	“up-regulates activity”	AKT	phosphorylation
CAMKK1	“up-regulates activity”	CAMK1D	phosphorylation
CAMKK1	“up-regulates activity”	CAMK1	phosphorylation
CAMKK1	“up-regulates activity”	AKT1	phosphorylation

Enriched among interaction partners

Reactome pathways and GO biological processes over-represented among this gene’s 32 IntAct physical interaction partners (hypergeometric vs the genome-wide background, BH-FDR, gene-set size 15–500, ranked by fold). A functional readout of the neighbourhood — distinct from this gene’s own memberships above, and biased toward well-studied / hub proteins, so read it as themes rather than proof.

Reactome pathways:

Pathway	Partners	Fold	FDR
Translocation of SLC2A4 (GLUT4) to the plasma membrane	6	35.6×	3e-06
G2/M Checkpoints	5	25.8×	5e-05
RHO GTPase Effectors	5	13.1×	7e-04
Membrane Trafficking	7	10.0×	1e-04
Vesicle-mediated transport	7	9.4×	2e-04
Cell Cycle	6	8.3×	1e-03
Signaling by Rho GTPases	6	7.9×	1e-03
Signaling by Rho GTPases, Miro GTPases and RHOBTB3	6	7.7×	1e-03

GO biological processes:

GO term	Partners	Fold	FDR
substantia nigra development	6	68.7×	4e-08

Disease & clinical

Clinical variants and AI predictions

ClinVar

96 variants total. Per-class counts are floors (≥ shown; pagination cap):

Classification	Count (floor)
Pathogenic	0
Likely pathogenic	0
Uncertain significance	75
Likely benign	3
Benign	0

Top pathogenic / likely-pathogenic (0)

SpliceAI

2878 predictions. Top by Δscore:

Variant	Effect	Δscore
17:3861559:C:CT	acceptor_gain	1.0000
17:3865902:ACTT:A	donor_loss	1.0000
17:3865905:TA:T	donor_loss	1.0000
17:3865906:A:AC	donor_gain	1.0000
17:3865906:A:T	donor_loss	1.0000
17:3865906:ACAC:A	donor_gain	1.0000
17:3865907:C:CA	donor_gain	1.0000
17:3865907:CA:C	donor_gain	1.0000
17:3865907:CACC:C	donor_gain	1.0000
17:3865907:CACCA:C	donor_gain	1.0000
17:3866012:C:CC	acceptor_gain	1.0000
17:3869486:CCA:C	donor_gain	1.0000
17:3869526:AACCT:A	donor_gain	1.0000
17:3869612:GCAA:G	acceptor_gain	1.0000
17:3869613:CAA:C	acceptor_gain	1.0000
17:3869613:CAAC:C	acceptor_gain	1.0000
17:3869616:C:CC	acceptor_gain	1.0000
17:3869626:C:CT	acceptor_gain	1.0000
17:3869626:C:T	acceptor_gain	1.0000
17:3869627:G:T	acceptor_gain	1.0000
17:3869634:C:CT	acceptor_gain	1.0000
17:3869889:C:CC	acceptor_gain	1.0000
17:3872552:A:AC	donor_gain	1.0000
17:3872552:ACT:A	donor_gain	1.0000
17:3872553:C:CA	donor_gain	1.0000
17:3872553:CT:C	donor_gain	1.0000
17:3872553:CTC:C	donor_gain	1.0000
17:3872553:CTCCT:C	donor_gain	1.0000
17:3873404:CTCA:C	donor_loss	1.0000
17:3873405:TCA:T	donor_loss	1.0000

AlphaMissense

3286 scored. Top likely-pathogenic:

Variant	Protein change	am_pathogenicity
17:3869822:T:A	R397S	1.000
17:3869822:T:G	R397S	1.000
17:3869823:C:G	R397T	1.000
17:3873450:A:G	W337R	1.000
17:3873450:A:T	W337R	1.000
17:3876271:G:C	F316L	1.000
17:3876271:G:T	F316L	1.000
17:3876273:A:G	F316L	1.000
17:3876340:G:C	D293E	1.000
17:3876340:G:T	D293E	1.000
17:3876341:T:A	D293V	1.000
17:3876341:T:C	D293G	1.000
17:3876341:T:G	D293A	1.000
17:3876342:C:G	D293H	1.000
17:3876377:A:G	L281P	1.000
17:3876388:C:A	K277N	1.000
17:3876388:C:G	K277N	1.000
17:3876394:G:C	D275E	1.000
17:3876394:G:T	D275E	1.000
17:3876395:T:A	D275V	1.000
17:3876395:T:C	D275G	1.000
17:3876395:T:G	D275A	1.000
17:3876396:C:G	D275H	1.000
17:3883460:T:A	K161N	1.000
17:3883460:T:G	K161N	1.000
17:3883472:T:A	K157N	1.000
17:3883472:T:G	K157N	1.000
17:3869606:A:G	W408R	0.999
17:3869606:A:T	W408R	0.999
17:3869823:C:A	R397I	0.999

dbSNP variants (sampled 300 via entrez): RS1000002416 (17:3879303 A>G), RS1000119243 (17:3887561 C>G), RS1000205315 (17:3893083 G>A,C), RS1000227626 (17:3860819 C>T), RS1000232169 (17:3874136 CCAGA>C), RS1000361327 (17:3875355 C>G,T), RS1000387117 (17:3865793 C>A,T), RS1000433931 (17:3890398 C>A), RS1000587407 (17:3866871 C>T), RS1000693250 (17:3866457 G>A), RS1000718433 (17:3886129 T>C), RS1000736647 (17:3879828 G>A,C), RS1000761603 (17:3870806 G>T), RS1000915379 (17:3874488 C>T), RS1001169656 (17:3865441 G>A)

Disease associations

OMIM: gene MIM:611411 | disease phenotypes:

GenCC curated gene-disease

Mondo (0):

Orphanet (0):

HPO phenotypes

0 total (0 of 0 shown, HPO-id order):

GWAS associations

2 associations (top):

Study	Trait	p-value
GCST000349_20	Smoking behavior	7.000000e-06
GCST011353_23	Serum alkaline phosphatase levels	4.000000e-09

EFO canonical traits (2, from GWAS)

EFO ID	Trait name
EFO:0004318	smoking behavior
EFO:0004533	alkaline phosphatase measurement

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (1): CHEMBL5256 (SINGLE PROTEIN)

Molecules with ChEMBL bioactivity

17 molecules (phase ≥1), by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 166,109 (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
CHEMBL1289926	AXITINIB	4	15,732
CHEMBL502835	NINTEDANIB	4	8,545
CHEMBL535	SUNITINIB	4	79,020
CHEMBL576982	QUIZARTINIB	4	4,432
CHEMBL608533	MIDOSTAURIN	4	7,259
CHEMBL428690	ALVOCIDIB	3	27,781
CHEMBL522892	DOVITINIB	3	4,944
CHEMBL603469	LESTAURTINIB	3
CHEMBL91829	RUBOXISTAURIN	3	77
CHEMBL1230609	FORETINIB	2	3,096
CHEMBL1721885	SU-014813	2	363
CHEMBL513909	BI-2536	2	895
CHEMBL572878	TOZASERTIB	2	2,998
CHEMBL607707	PELITINIB	2	6,340
CHEMBL1908397	KW-2449	1	622
CHEMBL574738	AST-487	1	451

PharmGKB: 1 entry (VIP=true, CPIC=false)

GtoPdb / IUPHAR curated pharmacology

(IUPHAR/BPS Guide to Pharmacology — expert-curated)

Target class: enzyme — Meta subfamily

Most potent curated ligand interactions (1 total), top 1:

Ligand	Action	Affinity	Parameter
STO609	Inhibition	6.85	pIC50

Binding affinities (BindingDB)

10 measured of 10 human assays (10 total across all organisms); most potent 10 below. Values come from heterogeneous assays and are not directly comparable.

Ligand	Measure	Value
Staurosporine	KD	1.7 nM
PKC-412	KD	190 nM
(3Z)-4-amino-5-fluoro-3-[5-(4-methylpiperazino)-1,3-dihydrobenzimidazol-2-ylidene]carbostyril	KD	520 nM
(18S)-18-[(dimethylamino)methyl]-17-oxa-4,14,21-triazahexacyclo[19.6.1.1^{7,14}.0^{2,6}.0^{8,13}.0^{22,27}]nonacosa-1(28),2(6),7(29),8(13),9,11,22(27),23,25-nonaene-3,5-dione	KD	700 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
1-Acyl-1H-[1,2,4]triazole-3,5-diamine Analogue 3b	KD	3100 nM
(E)-N-[4-(3-chloro-4-fluoro-anilino)-3-cyano-7-ethoxy-6-quinolyl]-4-(dimethylamino)but-2-enamide	KD	3500 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
2-(2-chlorophenyl)-5,7-dihydroxy-8-[(3S)-3-hydroxy-1-methyl-4-piperidinyl]-1-benzopyran-4-one	KD	5300 nM

ChEMBL bioactivities

73 potent at pChembl≥5 of 74 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).

pChembl	Type	Value	Unit	Molecule
10.41	Kd	0.039	nM	STAUROSPORINE
10.30	Kd	0.05	nM	STAUROSPORINE
8.51	IC50	3.1	nM	GSK-650394
7.96	Kd	11	nM	CHEMBL4465866
7.96	IC50	11	nM	CHEMBL5397685
7.92	IC50	12	nM	CHEMBL5439578
7.92	IC50	12	nM	CHEMBL5431962
7.85	Kd	14	nM	CHEMBL4576489
7.72	Kd	19	nM	ALVOCIDIB
7.66	Kd	22	nM	BI-2536
7.64	Kd	23	nM	LESTAURTINIB
7.58	IC50	26	nM	CHEMBL5426746
7.57	IC50	27	nM	CHEMBL4870467
7.53	IC50	29.8	nM	STAUROSPORINE
7.51	IC50	31	nM	CHEMBL4857253
7.48	IC50	33	nM	GSK-650394
7.38	IC50	42	nM	STAUROSPORINE
7.33	IC50	47	nM	CHEMBL5421767
7.31	Kd	49	nM	CHEMBL4752776
7.30	Kd	50	nM	TAE-684
7.27	IC50	54	nM	CHEMBL5396413
7.27	IC50	54	nM	STAUROSPORINE
7.19	Kd	64	nM	PHA-665752
7.10	Kd	79	nM	ALVOCIDIB
7.03	IC50	94	nM	CHEMBL5422255
6.92	IC50	120	nM	CHEMBL1182777
6.92	IC50	120	nM	CHEMBL265470
6.89	Kd	130	nM	MIDOSTAURIN
6.71	IC50	195	nM	CHEMBL4125686
6.68	Kd	210	nM	KW-2449
6.66	Kd	220	nM	AST-487
6.62	IC50	238	nM	CHEMBL4877552
6.62	IC50	239	nM	CHEMBL4852523
6.42	IC50	384	nM	CHEMBL4875005
6.39	IC50	407	nM	CHEMBL4862562
6.38	Kd	420	nM	SUNITINIB
6.26	Kd	550	nM	FORETINIB
6.20	Kd	630	nM	NINTEDANIB
6.12	Kd	760	nM	CGP-52421
6.09	Kd	810	nM	CHEMBL379218
6.07	Kd	850	nM	SU-014813
6.05	Kd	900	nM	SUNITINIB
6.02	IC50	961	nM	CHEMBL4866741
6.00	IC50	1000	nM	TP-030n
5.87	IC50	1345	nM	CHEMBL4873692
5.85	Kd	1400	nM	AXITINIB
5.83	IC50	1480	nM	CHEMBL4851892
5.82	Kd	1500	nM	RUBOXISTAURIN
5.75	Kd	1800	nM	FEDRATINIB
5.74	IC50	1838	nM	CHEMBL4877634

PubChem BioAssay actives

71 with measured affinity, of 416 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
(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	435521: Binding constant for CAMKK1 kinase domain	kd	<0.0001	uM
2-cyclopentyl-4-(5-phenyl-1H-pyrrolo[2,3-b]pyridin-3-yl)benzoic acid	2023208: Inhibition of CaMKK1 (unknown origin) incubated for 20 mins in presence of kinase tracer 236 by TR-FRET	ic50	0.0031	uM
3-(2,2-difluoro-10,12-dimethyl-1-aza-3-azonia-2-boranuidatricyclo[7.3.0.03,7]dodeca-3,5,7,9,11-pentaen-4-yl)-N-[2-[2-[2-[2-[[(2S,3R,4R,6R)-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]amino]ethoxy]ethoxy]ethoxy]ethyl]propanamide	1526208: Binding affinity to recombinant full-length N-terminal His-FLAG-GST-tagged CAMKK1 (unknown origin) expressed in baculovirus infected Sf9 insect cells incubated for 1 hr in presence of calmodulin by TR-FRET assay	kd	0.0110	uM
4-(7-ethoxy-6-fluoroquinazolin-4-yl)-2-propan-2-ylbenzoic acid	2023208: Inhibition of CaMKK1 (unknown origin) incubated for 20 mins in presence of kinase tracer 236 by TR-FRET	ic50	0.0110	uM
2-cyclopentyl-4-(7-ethoxy-5-fluoroquinazolin-4-yl)benzoic acid	2023208: Inhibition of CaMKK1 (unknown origin) incubated for 20 mins in presence of kinase tracer 236 by TR-FRET	ic50	0.0120	uM
4-(7-ethoxy-5-fluoroquinazolin-4-yl)-2-propan-2-ylbenzoic acid	2023208: Inhibition of CaMKK1 (unknown origin) incubated for 20 mins in presence of kinase tracer 236 by TR-FRET	ic50	0.0120	uM
3-(2,2-difluoro-10,12-dimethyl-1-aza-3-azonia-2-boranuidatricyclo[7.3.0.03,7]dodeca-3,5,7,9,11-pentaen-4-yl)-N-[2-[2-[2-[2-[[(2S,3R,4R,6R)-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]-methylamino]ethoxy]ethoxy]ethoxy]ethyl]propanamide	1526208: Binding affinity to recombinant full-length N-terminal His-FLAG-GST-tagged CAMKK1 (unknown origin) expressed in baculovirus infected Sf9 insect cells incubated for 1 hr in presence of calmodulin by TR-FRET assay	kd	0.0140	uM
2-(2-chlorophenyl)-5,7-dihydroxy-8-[(3S,4R)-3-hydroxy-1-methylpiperidin-4-yl]chromen-4-one	256583: Average Binding Constant for CAMKK1; NA=Not Active at 10 uM	kd	0.0190	uM
4-[[(7R)-8-cyclopentyl-7-ethyl-5-methyl-6-oxo-7H-pteridin-2-yl]amino]-3-methoxy-N-(1-methylpiperidin-4-yl)benzamide	625143: Binding constant for CAMKK1 kinase domain	kd	0.0220	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	507860: Binding affinity to CAMKK1	kd	0.0230	uM
2-cyclopentyl-4-(7-ethoxyquinazolin-4-yl)benzoic acid	2023208: Inhibition of CaMKK1 (unknown origin) incubated for 20 mins in presence of kinase tracer 236 by TR-FRET	ic50	0.0260	uM
2-cyclopentyl-4-(2-phenyl-1H-imidazo[4,5-b]pyridin-7-yl)benzoic acid	1768403: Inhibition of human CAMKK1 using CAMKKtide as substrate assessed as residual activity by [gamma-33P]-ATP assay relative to control	ic50	0.0270	uM
4-(2-anilinopyrimidin-4-yl)-2-cyclopentylbenzoic acid	1768403: Inhibition of human CAMKK1 using CAMKKtide as substrate assessed as residual activity by [gamma-33P]-ATP assay relative to control	ic50	0.0310	uM
4-(7-ethoxyquinazolin-4-yl)-2-propan-2-ylbenzoic acid	2023208: Inhibition of CaMKK1 (unknown origin) incubated for 20 mins in presence of kinase tracer 236 by TR-FRET	ic50	0.0470	uM
2-[6-(1-benzothiophen-2-yl)thieno[3,2-d]pyrimidin-4-yl]sulfanylacetic acid	1718396: Binding affinity to human CAMKK1 assessed as displacement of immobilized ligand by KINOMEscan scanMAX assay relative to control	kd	0.0490	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	625143: Binding constant for CAMKK1 kinase domain	kd	0.0500	uM
2-cyclopentyl-4-(7-ethoxy-6-fluoroquinazolin-4-yl)benzoic acid	2023208: Inhibition of CaMKK1 (unknown origin) incubated for 20 mins in presence of kinase tracer 236 by TR-FRET	ic50	0.0540	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	625143: Binding constant for CAMKK1 kinase domain	kd	0.0640	uM
2-cyclopentyl-4-[7-[10-[[(2S)-1-[(2S,4R)-4-hydroxy-2-[[4-(4-methyl-1,3-thiazol-5-yl)phenyl]methylcarbamoyl]pyrrolidin-1-yl]-3,3-dimethyl-1-oxobutan-2-yl]amino]-10-oxodecoxy]quinazolin-4-yl]benzoic acid	2023208: Inhibition of CaMKK1 (unknown origin) incubated for 20 mins in presence of kinase tracer 236 by TR-FRET	ic50	0.0940	uM
acetic acid;11-oxo-3,10-diazapentacyclo[10.7.1.02,10.04,9.016,20]icosa-1(20),2,4,6,8,12,14,16,18-nonaene-17-carboxylic acid	435947: Inhibition of CAMKKalpha in the presence of 20uM ATP	ic50	0.1200	uM
11-oxo-3,10-diazapentacyclo[10.7.1.02,10.04,9.016,20]icosa-1(20),2,4,6,8,12,14,16,18-nonaene-17-carboxylic acid	2023208: Inhibition of CaMKK1 (unknown origin) incubated for 20 mins in presence of kinase tracer 236 by TR-FRET	ic50	0.1200	uM
Midostaurin	435521: Binding constant for CAMKK1 kinase domain	kd	0.1300	uM
2-cyclopentyl-4-(1H-pyrrolo[2,3-b]pyridin-3-yl)benzoic acid	1768403: Inhibition of human CAMKK1 using CAMKKtide as substrate assessed as residual activity by [gamma-33P]-ATP assay relative to control	ic50	0.1950	uM
[4-[(E)-2-(1H-indazol-3-yl)ethenyl]phenyl]-piperazin-1-ylmethanone	625143: Binding constant for CAMKK1 kinase domain	kd	0.2100	uM
1-[4-[(4-ethylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl]-3-[4-[6-(methylamino)pyrimidin-4-yl]oxyphenyl]urea	435521: Binding constant for CAMKK1 kinase domain	kd	0.2200	uM
2-cyclopentyl-4-(5-phenylpyrazolo[1,5-a]pyrimidin-3-yl)benzoic acid	1768403: Inhibition of human CAMKK1 using CAMKKtide as substrate assessed as residual activity by [gamma-33P]-ATP assay relative to control	ic50	0.2380	uM
2-cyclopentyl-4-quinolin-4-ylbenzoic acid	1768403: Inhibition of human CAMKK1 using CAMKKtide as substrate assessed as residual activity by [gamma-33P]-ATP assay relative to control	ic50	0.2390	uM
2-cyclopentyl-4-(5-phenylthieno[2,3-b]pyridin-3-yl)benzoic acid	1768403: Inhibition of human CAMKK1 using CAMKKtide as substrate assessed as residual activity by [gamma-33P]-ATP assay relative to control	ic50	0.3840	uM
2-cyclopentyl-4-thieno[3,2-d]pyrimidin-4-ylbenzoic acid	1768403: Inhibition of human CAMKK1 using CAMKKtide as substrate assessed as residual activity by [gamma-33P]-ATP assay relative to control	ic50	0.4070	uM
Sunitinib	435521: Binding constant for CAMKK1 kinase domain	kd	0.4200	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	625143: Binding constant for CAMKK1 kinase domain	kd	0.5500	uM
methyl 2-hydroxy-3-[N-[4-[methyl-[2-(4-methylpiperazin-1-yl)acetyl]amino]phenyl]-C-phenylcarbonimidoyl]-1H-indole-6-carboxylate	625143: Binding constant for CAMKK1 kinase domain	kd	0.6300	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	507860: Binding affinity to CAMKK1	kd	0.7600	uM
(2S)-1-[[5-(3-methyl-2H-indazol-5-yl)-3-pyridinyl]oxy]-3-phenylpropan-2-amine	625143: Binding constant for CAMKK1 kinase domain	kd	0.8100	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	435521: Binding constant for CAMKK1 kinase domain	kd	0.8500	uM
2-cyclopentyl-4-(5-phenylfuro[2,3-b]pyridin-3-yl)benzoic acid	1768403: Inhibition of human CAMKK1 using CAMKKtide as substrate assessed as residual activity by [gamma-33P]-ATP assay relative to control	ic50	0.9610	uM
2-cyclopentyl-4-(1-methylpyrrolo[2,3-b]pyridin-4-yl)benzoic acid	1768403: Inhibition of human CAMKK1 using CAMKKtide as substrate assessed as residual activity by [gamma-33P]-ATP assay relative to control	ic50	1.3450	uM
Axitinib	625143: Binding constant for CAMKK1 kinase domain	kd	1.4000	uM
2-cyclopentyl-4-(5-phenylpyrazolo[1,5-a]pyridin-3-yl)benzoic acid	1768403: Inhibition of human CAMKK1 using CAMKKtide as substrate assessed as residual activity by [gamma-33P]-ATP assay relative to control	ic50	1.4800	uM
(18S)-18-[(dimethylamino)methyl]-17-oxa-4,14,21-triazahexacyclo[19.6.1.17,14.02,6.08,13.022,27]nonacosa-1(28),2(6),7(29),8,10,12,22,24,26-nonaene-3,5-dione	256583: Average Binding Constant for CAMKK1; NA=Not Active at 10 uM	kd	1.5000	uM
Fedratinib	625143: Binding constant for CAMKK1 kinase domain	kd	1.8000	uM
2-cyclopentyl-4-(6-phenylquinolin-4-yl)benzoic acid	1768403: Inhibition of human CAMKK1 using CAMKKtide as substrate assessed as residual activity by [gamma-33P]-ATP assay relative to control	ic50	1.8380	uM
2-cyclopentyl-4-pyrazolo[1,5-a]pyridin-3-ylbenzoic acid	1768403: Inhibition of human CAMKK1 using CAMKKtide as substrate assessed as residual activity by [gamma-33P]-ATP assay relative to control	ic50	2.0130	uM
2-cyclopentyl-4-(6-phenylquinazolin-4-yl)benzoic acid	1768403: Inhibition of human CAMKK1 using CAMKKtide as substrate assessed as residual activity by [gamma-33P]-ATP assay relative to control	ic50	2.6140	uM
5-cyano-N-[2-(cyclohexen-1-yl)-4-[1-[2-(dimethylamino)acetyl]piperidin-4-yl]phenyl]-1H-imidazole-2-carboxamide;hydrochloride	625143: Binding constant for CAMKK1 kinase domain	kd	2.8000	uM
4-[[5-amino-1-(2,6-difluorobenzoyl)-1,2,4-triazol-3-yl]amino]benzenesulfonamide	435521: Binding constant for CAMKK1 kinase domain	kd	2.9000	uM
4-amino-5-fluoro-3-[6-(4-methylpiperazin-1-yl)-1H-benzimidazol-2-yl]-1H-quinolin-2-one	435521: Binding constant for CAMKK1 kinase domain	kd	3.1000	uM
N-[4-[4-(4-methylpiperazin-1-yl)-6-[(5-methyl-1H-pyrazol-3-yl)amino]pyrimidin-2-yl]sulfanylphenyl]cyclopropanecarboxamide	625143: Binding constant for CAMKK1 kinase domain	kd	4.6000	uM
(E)-N-[4-(3-chloro-4-fluoroanilino)-3-cyano-7-ethoxyquinolin-6-yl]-4-(dimethylamino)but-2-enamide	435521: Binding constant for CAMKK1 kinase domain	kd	5.1000	uM
2-cyclopentyl-4-quinazolin-4-ylbenzoic acid	1768403: Inhibition of human CAMKK1 using CAMKKtide as substrate assessed as residual activity by [gamma-33P]-ATP assay relative to control	ic50	5.4810	uM

CTD chemical–gene interactions

37 total (human), top 30 by PubMed support.

Chemical	Actions (top 5)	PubMed papers
sodium arsenite	decreases expression, increases expression	2
perfluorooctanoic acid	increases expression, decreases expression	2
Air Pollutants	affects cotreatment, increases abundance, increases oxidation, affects expression	2
Ozone	affects cotreatment, increases oxidation, increases abundance, affects expression	2
aristolochic acid I	decreases expression	1
FR900359	decreases phosphorylation	1
triphenyl phosphate	affects expression	1
alpha-pinene	affects cotreatment, increases oxidation, increases abundance	1
bisphenol A	increases expression	1
benzo(e)pyrene	increases methylation	1
aflatoxin B2	increases methylation	1
methacrylaldehyde	affects cotreatment, increases oxidation, increases abundance	1
di-n-butylphosphoric acid	affects expression	1
jinfukang	increases expression	1
(+)-JQ1 compound	decreases expression	1
Sunitinib	increases expression	1
Acrolein	affects cotreatment, increases oxidation, increases abundance	1
Benzo(a)pyrene	affects methylation, increases methylation	1
Cisplatin	decreases expression	1
Dichlorodiphenyl Dichloroethylene	increases expression	1
Diethylhexyl Phthalate	decreases expression	1
Estradiol	increases expression	1
Folic Acid	decreases expression	1
Lead	affects methylation	1
Methapyrilene	increases methylation	1
Smoke	decreases expression	1
Thiram	decreases expression	1
Tobacco Smoke Pollution	decreases expression	1
Tretinoin	increases expression	1
Valproic Acid	increases methylation	1

ChEMBL screening assays

178 unique, capped per target: 178 binding

Representative assays (with source publication via chembl_document):

Assay ID	Type	Description	Source paper
CHEMBL1034115	Binding	Inhibition of CAMKK1 at 3 uM	Discovery of substituted 4-(pyrazol-4-yl)-phenylbenzodioxane-2-carboxamides as potent and highly selective Rho kinase (ROCK-II) inhibitors. — J Med Chem

Cellosaurus cell lines

4 cell lines: 4 cancer cell line

First 10 cell lines (id-ordered, not curated):

Cellosaurus	Name	Category	Sex
CVCL_B1M2	Abcam HeLa CAMKK1 KO	Cancer cell line	Female
CVCL_SG68	HAP1 CAMKK1 (-) 1	Cancer cell line	Male
CVCL_SG69	HAP1 CAMKK1 (-) 2	Cancer cell line	Male
CVCL_SG70	HAP1 CAMKK1 (-) 3	Cancer cell line	Male

Clinical trials (associated diseases)

0 trials via MONDO — disease-level, not drug-specific.