DCLK3

Summary

DCLK3 (doublecortin like kinase 3, HGNC:19005) is a protein-coding gene on chromosome 3p22.2, encoding Serine/threonine-protein kinase DCLK3 (Q9C098).

Predicted to enable protein serine/threonine kinase activity. Predicted to be involved in protein localization to nucleus. Predicted to act upstream of or within negative regulation of protein localization to nucleus and peptidyl-serine phosphorylation. Predicted to be active in cytoplasm and nucleus.

Source: NCBI Gene 85443 — RefSeq curated summary.

At a glance

• GWAS associations: 6
• Clinical variants (ClinVar): 108 total
• Druggable target: yes — 20 molecules with ChEMBL bioactivity
• MANE Select transcript: NM_001394672

Identifiers

Gene identifiers

Field	Value
HGNC ID	HGNC:19005
Approved symbol	DCLK3
Name	doublecortin like kinase 3
Location	3p22.2
Locus type	gene with protein product
Status	Approved
Aliases	KIAA1765, DCDC3C
Ensembl gene	ENSG00000163673
Ensembl biotype	protein_coding
OMIM	613167
Entrez	85443

Gene structure

Transcript identifiers

Ensembl transcripts: 4 — 3 protein_coding, 1 protein_coding_CDS_not_defined

ENST00000416516, ENST00000498047, ENST00000636136, ENST00000929032

RefSeq mRNA: 2 — MANE Select: NM_001394672 NM_001394672, NM_033403

CCDS: CCDS43064, CCDS93239

Canonical transcript exons

ENST00000636136 — 5 exons

Exon	Start	End
ENSE00001077122	36718010	36718177
ENSE00003560573	36721527	36721659
ENSE00003796785	36764182	36764553
ENSE00003796849	36737208	36739084
ENSE00003926181	36712421	36715521

Expression profiles

Bgee: expression breadth ubiquitous, 132 present calls, max score 90.06.

FANTOM5 (CAGE): breadth tissue_specific, TPM avg 0.0631 / max 7.3247, expressed in 34 samples.

FANTOM5 promoters (2 alternative TSS)

Promoter ID	TPM avg	Samples expressed
41659	0.0518	29
41658	0.0114	8

Top tissues by expression

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

Tissue	Anatomy ID	Expression score	Quality
sural nerve	UBERON:0015488	90.06	gold quality
male germ line stem cell (sensu Vertebrata) in testis	CL:0000089 ∩ UBERON:0000473	83.50	gold quality
tibial nerve	UBERON:0001323	82.75	gold quality
primordial germ cell in gonad	CL:0000670 ∩ UBERON:0000991	78.08	gold quality
ganglionic eminence	UBERON:0004023	76.35	gold quality
nucleus accumbens	UBERON:0001882	69.35	gold quality
trigeminal ganglion	UBERON:0001675	69.07	gold quality
cortical plate	UBERON:0005343	67.32	gold quality
caudate nucleus	UBERON:0001873	65.28	gold quality
putamen	UBERON:0001874	65.25	gold quality
dorsal root ganglion	UBERON:0000044	61.80	gold quality
prefrontal cortex	UBERON:0000451	61.06	gold quality
hindlimb stylopod muscle	UBERON:0004252	59.72	gold quality
muscle of leg	UBERON:0001383	59.28	gold quality
gastrocnemius	UBERON:0001388	58.87	gold quality
jejunal mucosa	UBERON:0000399	58.34	gold quality
left testis	UBERON:0004533	58.11	gold quality
testis	UBERON:0000473	57.98	gold quality
right testis	UBERON:0004534	57.12	gold quality
vermiform appendix	UBERON:0001154	56.50	gold quality
frontal cortex	UBERON:0001870	55.19	gold quality
pituitary gland	UBERON:0000007	55.12	gold quality
Brodmann (1909) area 9	UBERON:0013540	54.98	gold quality
adenohypophysis	UBERON:0002196	54.80	gold quality
forebrain	UBERON:0001890	54.40	gold quality
cardiac muscle of right atrium	UBERON:0003379	54.34	gold quality
left ventricle myocardium	UBERON:0006566	54.23	gold quality
neocortex	UBERON:0001950	54.22	gold quality
kidney epithelium	UBERON:0004819	53.93	gold quality
skin of hip	UBERON:0001554	53.88	gold quality

Single-cell (SCXA)

Detected in 2 experiment(s), a significant marker in 0.

Experiment	Marker?	Max mean expression
E-GEOD-36552	no	19.78
E-ANND-3	no	3.26

Regulation

Is transcription factor: no

miRNA regulators (miRDB)

124 targeting DCLK3, 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-LET-7A-3P	100.00	74.03	3932
HSA-LET-7B-3P	100.00	74.08	3913
HSA-LET-7F-1-3P	100.00	74.02	3928
HSA-MIR-98-3P	100.00	74.08	3907
HSA-MIR-3646	100.00	73.56	5283
HSA-MIR-450A-1-3P	100.00	69.33	1837
HSA-MIR-4262	100.00	73.26	3931
HSA-MIR-6833-3P	100.00	70.63	3197
HSA-MIR-4283	100.00	66.42	2097
HSA-MIR-29A-3P	100.00	73.11	1835
HSA-MIR-29B-3P	100.00	73.18	1833
HSA-MIR-29C-3P	100.00	73.15	1833
HSA-MIR-4768-5P	100.00	69.49	2861
HSA-MIR-4668-3P	100.00	68.74	2635
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-6870-5P	99.99	68.55	2115
HSA-MIR-4775	99.98	75.00	6394
HSA-MIR-302C-5P	99.97	72.56	3642
HSA-MIR-4723-5P	99.97	68.70	2034
HSA-MIR-5698	99.97	68.49	2029
HSA-MIR-7111-5P	99.97	68.48	2062
HSA-MIR-4666A-3P	99.96	71.71	3434
HSA-MIR-185-3P	99.95	67.01	1743
HSA-MIR-6772-5P	99.94	67.01	577
HSA-MIR-1236-3P	99.94	68.04	1695
HSA-MIR-381-3P	99.93	71.87	2854
HSA-MIR-6835-3P	99.93	70.49	2904

Cross-species orthologs

4 orthologs

Organism	Symbol	Gene ID
danio_rerio	dclk3	ENSDARG00000078997
mus_musculus	Dclk3	ENSMUSG00000032500
rattus_norvegicus	Dclk3	ENSRNOG00000033026
caenorhabditis_elegans		WBGENE00009326

Paralogs (22): CAMKK1 (ENSG00000004660), 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), CAMKV (ENSG00000164076), PHKG1 (ENSG00000164776), DCLK2 (ENSG00000170390), CAMK1D (ENSG00000183049)

Protein

Protein identifiers

Serine/threonine-protein kinase DCLK3 — Q9C098 (reviewed: Q9C098)

Alternative names: Doublecortin domain-containing protein 3C, Doublecortin-like and CAM kinase-like 3, Doublecortin-like kinase 3

All UniProt accessions (2): A0A1B0GTZ4, Q9C098

UniProt curated annotations — full annotation on UniProt →

Subcellular location. Cytoplasm. Nucleus.

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

RefSeq proteins (2): NP_001381601, NP_208382 (=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 (21 total): sequence variant 8, compositionally biased region 5, region of interest 3, binding site 2, chain 1, domain 1, active site 1

Structure

Experimental structures (PDB)

0 structures.

Predicted structure (AlphaFold)

Model	pLDDT	Fraction very-high
AF-Q9C098-F1	63.27	0.35

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): 477 (proton acceptor)

Ligand- & substrate-binding residues (2): 362–370; 385

Function

Pathways and Gene Ontology

Reactome pathways

0 pathways

MSigDB gene sets: 57 (showing top): TERAMOTO_OPN_TARGETS_CLUSTER_1, chr3p22, ACEVEDO_METHYLATED_IN_LIVER_CANCER_DN, GOMF_PROTEIN_KINASE_ACTIVITY, GOMF_KINASE_ACTIVITY, GOMF_PROTEIN_SERINE_THREONINE_KINASE_ACTIVITY, GOMF_ADENYL_NUCLEOTIDE_BINDING, GOMF_TRANSFERASE_ACTIVITY_TRANSFERRING_PHOSPHORUS_CONTAINING_GROUPS, MIKKELSEN_MEF_HCP_WITH_H3K27ME3, PEDRIOLI_MIR31_TARGETS_DN, ZNF618_TARGET_GENES, MIR3646, LET_7A_3P, MIR4262, MIR98_3P

GO Biological Process (4): protein localization to nucleus (GO:0034504), protein phosphorylation (GO:0006468), intracellular signal transduction (GO:0035556), negative regulation of protein localization to nucleus (GO:1900181)

GO Molecular Function (7): protein serine/threonine kinase activity (GO:0004674), ATP binding (GO:0005524), protein serine kinase activity (GO:0106310), nucleotide binding (GO:0000166), protein kinase activity (GO:0004672), kinase activity (GO:0016301), transferase activity (GO:0016740)

GO Cellular Component (2): nucleus (GO:0005634), cytoplasm (GO:0005737)

GO top-level categories

Rollup of top GO terms by namespace:

Category	Terms
intracellular anatomical structure	2
protein kinase activity	2
protein localization to organelle	1
phosphorylation	1
protein modification process	1
signal transduction	1
protein localization to nucleus	1
regulation of protein localization to nucleus	1
negative regulation of protein localization	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
transferase activity, transferring phosphorus-containing groups	1
catalytic activity	1
intracellular membrane-bounded organelle	1
cellular anatomical structure	1

Protein interactions and networks

STRING

1343 interactions, top by confidence (×1000):

Protein A	Protein B	Partner UniProt	Score
DCLK3	KLRB1	Q12918	828
DCLK3	SHOC2	Q9UQ13	632
DCLK3	DCX	O43602	572
DCLK3	INPPL1	O15357	496
DCLK3	BMP1	P13497	492
DCLK3	DNPH1	O43598	453
DCLK3	MGMT	P16455	446
DCLK3	CRYM	Q14894	432
DCLK3	PLXNA2	O75051	425
DCLK3	FGF20	Q9NP95	423
DCLK3	FGF22	Q9HCT0	423
DCLK3	FGF16	O43320	423
DCLK3	GPRIN2	O60269	417
DCLK3	ZNF366	Q8N895	415
DCLK3	FGF18	O76093	412

IntAct

11 interactions, top by confidence:

A	B	Type	Score
CDK5	FIBP	psi-mi:“MI:0914”(association)	0.840
DCLK3	BTBD9	psi-mi:“MI:0915”(physical association)	0.370
DCLK3	SALL1	psi-mi:“MI:0915”(physical association)	0.370
DCLK3	TRIM39	psi-mi:“MI:0915”(physical association)	0.370
DCLK3	TADA3	psi-mi:“MI:0915”(physical association)	0.370
DCLK3	ZNF12	psi-mi:“MI:0915”(physical association)	0.370
DCLK3	ZNF292	psi-mi:“MI:0915”(physical association)	0.370
DCLK3	ZNF366	psi-mi:“MI:0915”(physical association)	0.370
	CAMK2B	psi-mi:“MI:0914”(association)	0.350

BioGRID (7): DCLK3 (Affinity Capture-MS), RAMP1 (Reconstituted Complex), DCLK3 (Affinity Capture-MS), ADM (Reconstituted Complex), DCLK3 (Cross-Linking-MS (XL-MS)), PPIC (Cross-Linking-MS (XL-MS)), DCLK3 (Affinity Capture-MS)

ESM2 similar proteins: A2YBX5, B1WAR9, B5X564, F4I114, F4I4F2, F4ICB6, F4J394, O13839, P15792, P25341, P83101, Q05999, Q09831, Q0DCT8, Q0PKV7, Q17QV9, Q1PFB9, Q39183, Q4R7T5, Q5R667, Q5U2N4, Q5XIT0, Q63553, Q64FQ2, Q66I46, Q6DBX4, Q6NTJ3, Q6P431, Q6UDG0, Q7T0B0, Q7TNL3, Q7TSJ6, Q8CDB0, Q8N2I9, Q8VDU5, Q8W490, Q922Y0, Q924X7, Q9BUB5, Q9BYT3

Diamond homologs: A2ASS6, A2CG49, A4IFM7, A8C984, A8WXF6, E9PT87, F1M0Z1, G4SLH0, O02827, O08875, O43293, O44997, O54784, O60229, O62305, O70150, O75962, O88764, O94768, O94806, P07313, P08414, P10911, P13234, P18652, P18653, P18654, P20689, P22216, P25323, P29294, P51812, P53355, P97924, Q00168, Q0KHT7, Q0KL02, Q14012, Q15139, Q15418

SIGNOR signaling

0 interactions.

Disease & clinical

Clinical variants and AI predictions

ClinVar

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

Classification	Count (floor)
Pathogenic	0
Likely pathogenic	0
Uncertain significance	88
Likely benign	3
Benign	0

Top pathogenic / likely-pathogenic (0)

SpliceAI

673 predictions. Top by Δscore:

Variant	Effect	Δscore
3:36715517:AGCAG:A	acceptor_gain	1.0000
3:36715518:GCAG:G	acceptor_gain	1.0000
3:36715519:CAG:C	acceptor_gain	1.0000
3:36715519:CAGC:C	acceptor_gain	1.0000
3:36715520:AG:A	acceptor_gain	1.0000
3:36715520:AGCT:A	acceptor_loss	1.0000
3:36715521:GC:G	acceptor_loss	1.0000
3:36715522:C:CC	acceptor_gain	1.0000
3:36715522:C:T	acceptor_loss	1.0000
3:36715525:T:C	acceptor_gain	1.0000
3:36715525:T:TC	acceptor_gain	1.0000
3:36718058:G:C	donor_gain	1.0000
3:36721522:CTTA:C	donor_loss	1.0000
3:36721523:TTAC:T	donor_loss	1.0000
3:36721524:TA:T	donor_loss	1.0000
3:36721525:ACCT:A	donor_loss	1.0000
3:36721526:CCTTT:C	donor_gain	1.0000
3:36721658:ACCT:A	acceptor_loss	1.0000
3:36721660:CT:C	acceptor_loss	1.0000
3:36721661:T:A	acceptor_loss	1.0000
3:36721671:C:T	acceptor_gain	1.0000
3:36737202:GCTTA:G	donor_loss	1.0000
3:36737203:CTTAC:C	donor_loss	1.0000
3:36737204:TTAC:T	donor_loss	1.0000
3:36737205:TACC:T	donor_loss	1.0000
3:36737206:A:AC	donor_gain	1.0000
3:36737207:C:CC	donor_gain	1.0000
3:36715530:A:AC	acceptor_gain	0.9900
3:36715530:A:C	acceptor_gain	0.9900
3:36718047:A:AC	donor_gain	0.9900

AlphaMissense

5392 scored. Top likely-pathogenic:

Variant	Protein change	am_pathogenicity
3:36718152:C:A	W537C	1.000
3:36718152:C:G	W537C	1.000
3:36718154:A:G	W537R	1.000
3:36718154:A:T	W537R	1.000
3:36721615:A:C	D499E	1.000
3:36721615:A:T	D499E	1.000
3:36721616:T:A	D499V	1.000
3:36737212:A:G	L483P	1.000
3:36737230:T:A	D477V	1.000
3:36737230:T:G	D477A	1.000
3:36737233:C:G	R476P	1.000
3:36737239:A:T	V474D	1.000
3:36737559:A:C	F367L	1.000
3:36737559:A:T	F367L	1.000
3:36737561:A:G	F367L	1.000
3:36715474:G:T	R601S	0.999
3:36718026:C:A	W579C	0.999
3:36718026:C:G	W579C	0.999
3:36718028:A:G	W579R	0.999
3:36718028:A:T	W579R	0.999
3:36718104:G:C	F553L	0.999
3:36718104:G:T	F553L	0.999
3:36718105:A:G	F553S	0.999
3:36718106:A:G	F553L	0.999
3:36718108:G:T	P552Q	0.999
3:36718117:C:T	G549D	0.999
3:36718144:C:T	G540D	0.999
3:36718145:C:G	G540R	0.999
3:36718153:C:G	W537S	0.999
3:36718159:T:A	D535V	0.999

dbSNP variants (sampled 300 via entrez): RS1000003626 (3:36761566 C>T), RS1000067720 (3:36731080 G>A), RS1000141950 (3:36728889 T>C), RS1000182275 (3:36737869 G>A,T), RS1000344252 (3:36743932 C>T), RS1000363680 (3:36717365 G>A), RS1000374407 (3:36719944 A>T), RS1000381550 (3:36743596 C>A,T), RS1000420958 (3:36725594 G>A), RS1000544525 (3:36754933 A>G), RS1000573500 (3:36756464 A>C,G,T), RS1000582565 (3:36713781 C>A), RS1000608140 (3:36737264 C>T), RS1000757536 (3:36719946 C>G), RS1000778563 (3:36761999 T>C)

Disease associations

OMIM: gene MIM:613167 | disease phenotypes:

GenCC curated gene-disease

Mondo (0):

Orphanet (0):

HPO phenotypes

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

GWAS associations

6 associations (top):

Study	Trait	p-value
GCST004946_15	Schizophrenia	3.000000e-11
GCST006575_3	Takayasu arteritis	5.000000e-06
GCST007565_148	Morning person	1.000000e-13
GCST007576_4	Chronotype	1.000000e-13
GCST009600_86	Anorexia nervosa, attention-deficit/hyperactivity disorder, autism spectrum disorder, bipolar disorder, major depression, obsessive-compulsive disorder, schizophrenia, or Tourette syndrome (pleiotropy)	2.000000e-17
GCST010147_2	White matter hyperintensity volume	2.000000e-07

EFO canonical traits (2, from GWAS)

EFO ID	Trait name
EFO:0008328	chronotype measurement
EFO:0005665	white matter hyperintensity measurement

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (1): CHEMBL6123 (SINGLE PROTEIN)

Molecules with ChEMBL bioactivity

20 molecules (phase ≥1), by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 295,468 (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
CHEMBL288441	BOSUTINIB	4	12,255
CHEMBL502835	NINTEDANIB	4	8,545
CHEMBL535	SUNITINIB	4	79,020
CHEMBL939	GEFITINIB	4	117,814
CHEMBL428690	ALVOCIDIB	3	27,781
CHEMBL522892	DOVITINIB	3	4,944
CHEMBL603469	LESTAURTINIB	3
CHEMBL1721885	SU-014813	2	363
CHEMBL384304	RG-547	2	93
CHEMBL445813	AT-7519	2	2,614
CHEMBL475251	R-406	2	762
CHEMBL572878	TOZASERTIB	2	2,998
CHEMBL607707	PELITINIB	2	6,340
CHEMBL1908397	KW-2449	1	622
CHEMBL296468	BMS-387032	1	2,075
CHEMBL494089	GSK-690693	1	2,061

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

GtoPdb / IUPHAR curated pharmacology

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

Target class: enzyme — DCAMKL family

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
(3Z)-4-amino-5-fluoro-3-[5-(4-methylpiperazino)-1,3-dihydrobenzimidazol-2-ylidene]carbostyril	KD	520 nM
N-[4-({4-[(3-methyl-1H-pyrazol-5-yl)amino]-6-(4-methylpiperazin-1-yl)pyrimidin-2-yl}sulfanyl)phenyl]cyclopropanecarboxamide	KD	1100 nM
BMS-387072	KD	1800 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
3-((3R,4R)-4-methyl-3-(methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino)piperidin-1-yl)-3-oxopropanenitrile	KD	5000 nM
2-(2-chlorophenyl)-5,7-dihydroxy-8-[(3S)-3-hydroxy-1-methyl-4-piperidinyl]-1-benzopyran-4-one	KD	5300 nM

ChEMBL bioactivities

47 potent at pChembl≥5 of 47 total, top 37 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).

pChembl	Type	Value	Unit	Molecule
8.35	Kd	4.5	nM	TOFACITINIB CITRATE
8.35	Kd	4.5	nM	TOFACITINIB
7.92	Kd	12	nM	TOFACITINIB CITRATE
7.92	Kd	12	nM	TOFACITINIB
7.89	Kd	13	nM	FEDRATINIB
7.85	Kd	14	nM	TAE-684
7.77	Kd	17	nM	STAUROSPORINE
7.22	Kd	60	nM	CHEMBL4465866
7.07	Kd	86	nM	KW-2449
6.98	Kd	104	nM	CHEMBL4576489
6.96	Kd	110	nM	SUNITINIB
6.96	Kd	110	nM	GSK-690693
6.62	Kd	240	nM	SU-014813
6.58	Kd	260	nM	RUXOLITINIB
6.22	Kd	600	nM	R-406
6.21	Kd	620	nM	RG-547
6.11	Kd	770	nM	NINTEDANIB
6.09	Kd	820	nM	CHEMBL1241674
6.04	Kd	910	nM	CHEMBL1229592
6.00	IC50	1000	nM	TP-030-1
6.00	IC50	1000	nM	TP-030-2
6.00	IC50	1000	nM	TP-030n
5.96	Kd	1100	nM	ALVOCIDIB
5.96	Kd	1100	nM	LESTAURTINIB
5.96	Kd	1100	nM	AT-7519
5.89	Kd	1300	nM	DOVITINIB
5.80	Kd	1600	nM	BMS-387032
5.77	Kd	1700	nM	BMS-345541
5.75	Kd	1800	nM	CHEMBL2425628
5.75	Kd	1800	nM	CHEMBL4564337
5.60	Kd	2500	nM	PLX-4720
5.54	Kd	2900	nM	GEFITINIB
5.44	Kd	3600	nM	TOZASERTIB
5.35	Kd	4500	nM	PHA-665752
5.31	Kd	4900	nM	PELITINIB
5.27	Kd	5400	nM	BOSUTINIB
5.19	Kd	6500	nM	JNJ-7706621

PubChem BioAssay actives

42 with measured affinity, of 198 total; 31 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
Tofacitinib	413573: Binding affinity to DCamkL3	kd	0.0045	uM
Fedratinib	624707: Binding constant for DCAMKL3 kinase domain	kd	0.0130	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	624707: Binding constant for DCAMKL3 kinase domain	kd	0.0140	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	435399: Binding constant for DCAMKL3 kinase domain	kd	0.0170	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	1526176: Binding affinity to recombinant full-length N-terminal His-FLAG-tagged DCLK3 (unknown origin) expressed in baculovirus infected Sf9 insect cells incubated for 1 hr by TR-FRET assay	kd	0.0600	uM
[4-[(E)-2-(1H-indazol-3-yl)ethenyl]phenyl]-piperazin-1-ylmethanone	624707: Binding constant for DCAMKL3 kinase domain	kd	0.0860	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	1526176: Binding affinity to recombinant full-length N-terminal His-FLAG-tagged DCLK3 (unknown origin) expressed in baculovirus infected Sf9 insect cells incubated for 1 hr by TR-FRET assay	kd	0.1040	uM
4-[2-(4-amino-1,2,5-oxadiazol-3-yl)-1-ethyl-7-[[(3S)-piperidin-3-yl]methoxy]imidazo[4,5-c]pyridin-4-yl]-2-methylbut-3-yn-2-ol	624707: Binding constant for DCAMKL3 kinase domain	kd	0.1100	uM
Sunitinib	435399: Binding constant for DCAMKL3 kinase domain	kd	0.1100	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	435399: Binding constant for DCAMKL3 kinase domain	kd	0.2400	uM
Ruxolitinib	624707: Binding constant for DCAMKL3 kinase domain	kd	0.2600	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	624707: Binding constant for DCAMKL3 kinase domain	kd	0.6000	uM
[4-amino-2-[(1-methylsulfonylpiperidin-4-yl)amino]pyrimidin-5-yl]-(2,3-difluoro-6-methoxyphenyl)methanone	624707: Binding constant for DCAMKL3 kinase domain	kd	0.6200	uM
methyl 2-hydroxy-3-[N-[4-[methyl-[2-(4-methylpiperazin-1-yl)acetyl]amino]phenyl]-C-phenylcarbonimidoyl]-1H-indole-6-carboxylate	624707: Binding constant for DCAMKL3 kinase domain	kd	0.7700	uM
2-(4-amino-1-propan-2-ylpyrazolo[3,4-d]pyrimidin-3-yl)-1H-indol-5-ol	624707: Binding constant for DCAMKL3 kinase domain	kd	0.8200	uM
N-[3-[5-chloro-2-[2-methoxy-4-(4-methylpiperazin-1-yl)anilino]pyrimidin-4-yl]oxyphenyl]prop-2-enamide	2185060: Binding affinity to DCAMKL3 (unknown origin) assessed as dissociation constant	kd	0.9100	uM
4-[(2,6-dichlorobenzoyl)amino]-N-piperidin-4-yl-1H-pyrazole-5-carboxamide	624707: Binding constant for DCAMKL3 kinase domain	kd	1.1000	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	507897: Binding affinity to DCAMKL3	kd	1.1000	uM
2-(2-chlorophenyl)-5,7-dihydroxy-8-[(3S,4R)-3-hydroxy-1-methylpiperidin-4-yl]chromen-4-one	435399: Binding constant for DCAMKL3 kinase domain	kd	1.1000	uM
4-amino-5-fluoro-3-[6-(4-methylpiperazin-1-yl)-1H-benzimidazol-2-yl]-1H-quinolin-2-one	435399: Binding constant for DCAMKL3 kinase domain	kd	1.3000	uM
N-[5-[(5-tert-butyl-1,3-oxazol-2-yl)methylsulfanyl]-1,3-thiazol-2-yl]piperidine-4-carboxamide	435399: Binding constant for DCAMKL3 kinase domain	kd	1.6000	uM
N’-(1,8-dimethylimidazo[1,2-a]quinoxalin-4-yl)ethane-1,2-diamine	624707: Binding constant for DCAMKL3 kinase domain	kd	1.7000	uM
5-(6-bromo-5-methoxy-1H-indol-3-yl)-2-(1H-pyrrol-2-yl)-1,3-oxazole	1541246: Binding affinity to wild-type human partial length DCAMKL3 (E140 to V628 residues) expressed in bacterial expression system by active-site directed competition binding assay based Kinomescan method	kd	1.8000	uM
(4-hydroxypiperidin-1-yl)-[4-[[4-[4-(3-methylsulfonylpropoxy)indol-1-yl]pyrimidin-2-yl]amino]cyclohexyl]methanone	769522: Binding affinity to DCAMKL3 (unknown origin)	kd	1.8000	uM
N-[3-(5-chloro-1H-pyrrolo[2,3-b]pyridine-3-carbonyl)-2,4-difluorophenyl]propane-1-sulfonamide	624707: Binding constant for DCAMKL3 kinase domain	kd	2.5000	uM
Gefitinib	624707: Binding constant for DCAMKL3 kinase domain	kd	2.9000	uM
N-[4-[4-(4-methylpiperazin-1-yl)-6-[(5-methyl-1H-pyrazol-3-yl)amino]pyrimidin-2-yl]sulfanylphenyl]cyclopropanecarboxamide	435399: Binding constant for DCAMKL3 kinase domain	kd	3.6000	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	624707: Binding constant for DCAMKL3 kinase domain	kd	4.5000	uM
(E)-N-[4-(3-chloro-4-fluoroanilino)-3-cyano-7-ethoxyquinolin-6-yl]-4-(dimethylamino)but-2-enamide	435399: Binding constant for DCAMKL3 kinase domain	kd	4.9000	uM
Bosutinib	624707: Binding constant for DCAMKL3 kinase domain	kd	5.4000	uM
4-[[5-amino-1-(2,6-difluorobenzoyl)-1,2,4-triazol-3-yl]amino]benzenesulfonamide	435399: Binding constant for DCAMKL3 kinase domain	kd	6.5000	uM

CTD chemical–gene interactions

10 total (human), top 10 by PubMed support.

Chemical	Actions (top 5)	PubMed papers
ethyl-p-hydroxybenzoate	decreases expression	1
CGP 52608	affects binding, increases reaction	1
abrine	increases expression	1
Resveratrol	affects cotreatment, decreases expression	1
Copper	affects cotreatment, decreases expression	1
Formaldehyde	decreases expression	1
Rotenone	decreases expression	1
Silicon Dioxide	increases expression	1
Triclosan	decreases expression	1
Valproic Acid	increases methylation	1

ChEMBL screening assays

108 unique, capped per target: 108 binding

Representative assays (with source publication via chembl_document):

Assay ID	Type	Description	Source paper
CHEMBL1017885	Binding	Inhibition of DCAMKL3 assessed as enzyme activity relative to control	Examining the chirality, conformation and selective kinase inhibition of 3-((3R,4R)-4-methyl-3-(methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino)piperidin-1-yl)-3-oxopropanenitrile (CP-690,550). — J Med Chem

Clinical trials (associated diseases)

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