TNK1

Summary

TNK1 (tyrosine kinase non receptor 1, HGNC:11940) is a protein-coding gene on chromosome 17p13.1, encoding Non-receptor tyrosine-protein kinase TNK1 (Q13470). Involved in negative regulation of cell growth.

The protein encoded by this gene belongs to the tyrosine protein kinase family. Tyrosine protein kinases are important regulators of intracellular signal transduction pathways, mediating cellular proliferation, survival, and development. This gene is highly expressed in fetal tissues and at lower levels in few adult tissues, thus may function in signaling pathways utilized broadly during fetal development, and more selectively in adult tissues. It plays a negative regulatory role in the Ras-Raf1-MAPK pathway, and knockout mice have been shown to develop spontaneous tumors, suggesting a role as a tumor suppressor gene. Alternatively spliced transcript variants encoding different isoforms have been found for this gene.

Source: NCBI Gene 8711 — RefSeq curated summary.

At a glance

• Clinical variants (ClinVar): 129 total
• Druggable target: yes — 49 molecules with ChEMBL bioactivity
• MANE Select transcript: NM_003985

Identifiers

Gene identifiers

Field	Value
HGNC ID	HGNC:11940
Approved symbol	TNK1
Name	tyrosine kinase non receptor 1
Location	17p13.1
Locus type	gene with protein product
Status	Approved
Aliases	KOS1
Ensembl gene	ENSG00000174292
Ensembl biotype	protein_coding
OMIM	608076
Entrez	8711

Gene structure

Transcript identifiers

Ensembl transcripts: 9 — 4 protein_coding, 3 retained_intron, 2 nonsense_mediated_decay

ENST00000570896, ENST00000574794, ENST00000575268, ENST00000576136, ENST00000576207, ENST00000576716, ENST00000576812, ENST00000577009, ENST00000688331

RefSeq mRNA: 2 — MANE Select: NM_003985 NM_001251902, NM_003985

CCDS: CCDS45602, CCDS58510

Canonical transcript exons

ENST00000639010 — 0 exons

Expression profiles

Bgee: expression breadth ubiquitous, 133 present calls, max score 84.10.

FANTOM5 (CAGE): breadth broad, TPM avg 2.1950 / max 98.1469, expressed in 670 samples.

FANTOM5 promoters (2 alternative TSS)

Promoter ID	TPM avg	Samples expressed
159162	2.0369	594
159163	0.1581	71

Top tissues by expression

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

Tissue	Anatomy ID	Expression score	Quality
mucosa of transverse colon	UBERON:0004991	84.10	gold quality
cerebellar hemisphere	UBERON:0002245	83.34	gold quality
right hemisphere of cerebellum	UBERON:0014890	83.33	gold quality
cerebellum	UBERON:0002037	83.31	gold quality
cerebellar cortex	UBERON:0002129	83.31	gold quality
male germ line stem cell (sensu Vertebrata) in testis	CL:0000089 ∩ UBERON:0000473	81.65	gold quality
body of stomach	UBERON:0001161	80.87	gold quality
transverse colon	UBERON:0001157	80.29	gold quality
skin of leg	UBERON:0001511	79.84	gold quality
zone of skin	UBERON:0000014	79.69	gold quality
minor salivary gland	UBERON:0001830	79.62	gold quality
duodenum	UBERON:0002114	79.50	gold quality
skin of abdomen	UBERON:0001416	79.47	gold quality
saliva-secreting gland	UBERON:0001044	79.20	gold quality
small intestine Peyer’s patch	UBERON:0003454	79.18	gold quality
body of pancreas	UBERON:0001150	79.16	gold quality
stomach	UBERON:0000945	79.02	gold quality
small intestine	UBERON:0002108	79.01	gold quality
esophagus mucosa	UBERON:0002469	78.95	gold quality
lower esophagus mucosa	UBERON:0035834	78.31	gold quality
primordial germ cell in gonad	CL:0000670 ∩ UBERON:0000991	78.28	gold quality
pancreas	UBERON:0001264	78.22	gold quality
prostate gland	UBERON:0002367	78.08	gold quality
olfactory segment of nasal mucosa	UBERON:0005386	77.79	gold quality
intestine	UBERON:0000160	76.86	gold quality
islet of Langerhans	UBERON:0000006	76.83	gold quality
colon	UBERON:0001155	76.69	gold quality
right lobe of thyroid gland	UBERON:0001119	76.64	gold quality
fundus of stomach	UBERON:0001160	76.56	gold quality
metanephros cortex	UBERON:0010533	76.56	gold quality

Single-cell (SCXA)

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

Experiment	Marker?	Max mean expression
E-ANND-3	no	2.28

Regulation

Is transcription factor: no

Upstream regulators (CollecTRI, top): SP1, SP3, TFAP2A

miRNA regulators (miRDB)

28 targeting TNK1, 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-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-380-3P	99.89	70.18	1978
HSA-MIR-4728-5P	99.85	69.39	4718
HSA-MIR-6785-5P	99.82	68.68	4428
HSA-MIR-4668-5P	99.79	70.58	3782
HSA-MIR-149-3P	99.72	68.22	3963
HSA-MIR-548AU-3P	99.70	68.22	1373
HSA-MIR-6883-5P	99.69	68.05	3785
HSA-MIR-646	99.68	67.84	1645
HSA-MIR-580-3P	99.67	69.23	1841
HSA-MIR-7106-5P	99.53	67.47	3574
HSA-MIR-3171	99.49	69.06	776
HSA-MIR-297	99.40	69.58	1418
HSA-MIR-4520-2-3P	99.14	69.28	1009
HSA-MIR-6852-3P	98.54	67.60	1468
HSA-MIR-224-5P	98.33	70.12	1256
HSA-MIR-7850-5P	98.12	67.28	1111
HSA-MIR-3691-3P	97.90	65.97	791
HSA-MIR-10526-3P	97.86	64.97	1342
HSA-MIR-6783-5P	97.67	67.21	1528
HSA-MIR-663B	97.40	62.91	664
HSA-MIR-3173-5P	97.35	65.82	1282
HSA-MIR-6799-3P	97.35	65.60	1302
HSA-MIR-4776-5P	97.14	66.63	405

Literature-anchored findings (GeneRIF, showing 11)

• TNK1 therefore acts as a novel molecular switch that can determine the properties of TNFalpha signaling and therefore cell death. (PMID:17471239)
• Activated Tnk1 kinase is associated with Hodgkin’s lymphoma. (PMID:20090780)
• The application of functional genomics by using high-throughput-RNAi screens has allowed us to identify TNK1 as a growth-associated kinase in pancreatic cancer cells. (PMID:21536687)
• The activated TNK1 potentiates JAK-STAT signaling through dual phosphorylation of STAT1 at tyrosine 701 and serine 727 amino acid positions. (PMID:24449862)
• the Single nucleotide polymorphisms rs11136000 of CLU, rs541458 of PICALM, and rs1554948 of TNK1 according to the three age groups 50-65 years (group 1), 66-80 years (group 2), and 80+ years (group 3) in 569 older subjects without cognitive impairment (NoCI) and 520 Alzheimer’s disease (AD) patients, were studied. (PMID:28631188)
• TNK1 was found to be deregulated in the gut in murine and porcine trauma models and human inflammatory bowel disease. Thus, TNK1 might be a target during MODS to prevent damage in several organs, notably the gut. (PMID:30320600)
• Thirty-Eight-Negative Kinase 1 Is a Mediator of Acute Kidney Injury in Experimental and Clinical Traumatic Hemorrhagic Shock. (PMID:32983160)
• Polymorphism rs11867353 of Tyrosine Kinase Non-Receptor 1 (TNK1) Gene Is a Novel Genetic Marker for Alzheimer’s Disease. (PMID:33070267)
• TNK1 is a ubiquitin-binding and 14-3-3-regulated kinase that can be targeted to block tumor growth. (PMID:34504101)
• The noncatalytic regions of the tyrosine kinase Tnk1 are important for activity and substrate specificity. (PMID:36334623)
• Fusion crystallization reveals the behavior of both the 1TEL crystallization chaperone and the TNK1 UBA domain. (PMID:37776857)

Cross-species orthologs

2 orthologs

Organism	Symbol	Gene ID
mus_musculus	Tnk1	ENSMUSG00000001583
rattus_norvegicus	Tnk1	ENSRNOG00000015578

Paralogs (32): FGR (ENSG00000000938), MATK (ENSG00000007264), BTK (ENSG00000010671), FYN (ENSG00000010810), STYK1 (ENSG00000060140), TNK2 (ENSG00000061938), TXK (ENSG00000074966), JAK2 (ENSG00000096968), ABL1 (ENSG00000097007), PTK6 (ENSG00000101213), HCK (ENSG00000101336), BMX (ENSG00000102010), CSK (ENSG00000103653), TYK2 (ENSG00000105397), JAK3 (ENSG00000105639), FRK (ENSG00000111816), ITK (ENSG00000113263), ZAP70 (ENSG00000115085), PTK2B (ENSG00000120899), SRMS (ENSG00000125508), TEC (ENSG00000135605), BLK (ENSG00000136573), ABL2 (ENSG00000143322), FER (ENSG00000151422), JAK1 (ENSG00000162434), SYK (ENSG00000165025), PTK2 (ENSG00000169398), YES1 (ENSG00000176105), FES (ENSG00000182511), LCK (ENSG00000182866), SRC (ENSG00000197122), LYN (ENSG00000254087)

Protein

Protein identifiers

Non-receptor tyrosine-protein kinase TNK1 — Q13470 (reviewed: Q13470)

Alternative names: CD38 negative kinase 1

All UniProt accessions (3): Q13470, I3L334, U3KPR9

UniProt curated annotations — full annotation on UniProt →

Function. Involved in negative regulation of cell growth. Has tumor suppressor properties. Plays a negative regulatory role in the Ras-MAPK pathway. May function in signaling pathways utilized broadly during fetal development and more selectively in adult tissues and in cells of the lymphohematopoietic system. Could specifically be involved in phospholipid signal transduction.

Subunit / interactions. Interacts with the SH3 domain of PLCG1 via its Pro-rich domain.

Subcellular location. Cytoplasm. Membrane.

Tissue specificity. Expressed in all umbilical cord blood, bone marrow and adult blood cell sub-populations and in several leukemia cell lines. Highly expressed in fetal blood, brain, lung, liver and kidney. Detected at lower levels in adult prostate, testis, ovary, small intestine and colon. Not expressed in adult lung, liver, kidney or brain.

Post-translational modifications. Autophosphorylated on tyrosine residues.

Similarity. Belongs to the protein kinase superfamily. Tyr protein kinase family.

Isoforms (2)

UniProt ID	Names	Canonical?
Q13470-1	1	yes
Q13470-2	2

RefSeq proteins (2): NP_001238831, NP_003976* (*=MANE)

Domains & families (InterPro)

ID	Name	Type
IPR000719	Prot_kinase_dom	Domain
IPR001245	Ser-Thr/Tyr_kinase_cat_dom	Domain
IPR001452	SH3_domain	Domain
IPR008266	Tyr_kinase_AS	Active_site
IPR011009	Kinase-like_dom_sf	Homologous_superfamily
IPR017441	Protein_kinase_ATP_BS	Binding_site
IPR020635	Tyr_kinase_cat_dom	Domain
IPR049587	TNK-like_SAM	Domain
IPR050198	Non-receptor_tyrosine_kinases	Family
IPR055175	ACK/TNK-like_SAM	Domain

Pfam: PF07714, PF22931

Catalyzed reactions (Rhea), 1 shown:

• L-tyrosyl-[protein] + ATP = O-phospho-L-tyrosyl-[protein] + ADP + H(+) (RHEA:10596)

UniProt features (48 total): sequence conflict 15, modified residue 8, sequence variant 6, helix 5, domain 2, region of interest 2, turn 2, compositionally biased region 2, binding site 2, chain 1, splice variant 1, strand 1, active site 1

Structure

Experimental structures (PDB)

10 structures.

PDB	Method	Resolution (Å)
7TDY	X-RAY DIFFRACTION	1.53
7TCY	X-RAY DIFFRACTION	1.54
7T8J	X-RAY DIFFRACTION	1.89
9ZVU	X-RAY DIFFRACTION	1.96
9NGE	X-RAY DIFFRACTION	2.02
9Z2L	X-RAY DIFFRACTION	2.02
7U4Z	X-RAY DIFFRACTION	2.03
7U4W	X-RAY DIFFRACTION	2.1
9O0H	X-RAY DIFFRACTION	2.24
9CPL	X-RAY DIFFRACTION	2.4

Predicted structure (AlphaFold)

Model	pLDDT	Fraction very-high
AF-Q13470-F1	73.01	0.41

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): 245 (proton acceptor)

Ligand- & substrate-binding residues (2): 122–130; 148

Post-translational modifications (8): 60, 96, 255, 502, 514, 519, 582, 411

Function

Pathways and Gene Ontology

Reactome pathways

0 pathways

MSigDB gene sets: 82 (showing top): GSE45365_CD8A_DC_VS_CD11B_DC_IFNAR_KO_DN, MORF_RAD51L3, MODULE_120, MORF_CTSB, MORF_IL4, MODULE_99, MORF_THPO, MODULE_175, HAN_SATB1_TARGETS_DN, RGAGGAARY_PU1_Q6, MORF_ATF2, GOBP_PROTEIN_AUTOPHOSPHORYLATION, GOMF_PROTEIN_KINASE_ACTIVITY, GOMF_KINASE_ACTIVITY, MORF_PAX7

GO Biological Process (2): protein phosphorylation (GO:0006468), protein autophosphorylation (GO:0046777)

GO Molecular Function (8): protein tyrosine kinase activity (GO:0004713), non-membrane spanning protein tyrosine kinase activity (GO:0004715), ATP binding (GO:0005524), nucleotide binding (GO:0000166), protein kinase activity (GO:0004672), protein binding (GO:0005515), kinase activity (GO:0016301), transferase activity (GO:0016740)

GO Cellular Component (3): cytoplasm (GO:0005737), plasma membrane (GO:0005886), membrane (GO:0016020)

GO top-level categories

Rollup of top GO terms by namespace:

Category	Terms
cellular anatomical structure	2
phosphorylation	1
protein modification process	1
protein phosphorylation	1
protein kinase activity	1
protein tyrosine kinase activity	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
intracellular anatomical structure	1
membrane	1
cell periphery	1

Protein interactions and networks

STRING

466 interactions, top by confidence (×1000):

Protein A	Protein B	Partner UniProt	Score
TNK1	CD38	P28907	690
TNK1	PGBD1	Q96JS3	573
TNK1	TNKS	O95271	537
TNK1	EXOC3L2	Q2M3D2	507
TNK1	GALP	Q9UBC7	487
TNK1	SH3BP2	P78314	451
TNK1	SH3BP5	O60239	408
TNK1	PICALM	Q13492	393
TNK1	SORL1	Q92673	366
TNK1	SH3RF3	Q8TEJ3	353
TNK1	GAB2	Q9UQC2	350
TNK1	SORCS1	Q8WY21	324
TNK1	MYH13	Q9UKX3	313
TNK1	CLU	P10909	311
TNK1	GAK	O14976	305

IntAct

32 interactions, top by confidence:

A	B	Type	Score
SFN	TNK1	psi-mi:“MI:0915”(physical association)	0.690
TNK1	SFN	psi-mi:“MI:0915”(physical association)	0.690
YWHAE	TNK1	psi-mi:“MI:0915”(physical association)	0.670
ZNRD2	MYO9A	psi-mi:“MI:0914”(association)	0.530
	TNK1	psi-mi:“MI:0915”(physical association)	0.400
HSP90AB1	TNK1	psi-mi:“MI:0915”(physical association)	0.400
TNK1		psi-mi:“MI:0915”(physical association)	0.400
TNK1	CDC37	psi-mi:“MI:0915”(physical association)	0.400
TNK1	DDX5	psi-mi:“MI:0914”(association)	0.350
JUN		psi-mi:“MI:0914”(association)	0.350
	PLK4	psi-mi:“MI:0914”(association)	0.350
	CAMK2B	psi-mi:“MI:0914”(association)	0.350
	GAK	psi-mi:“MI:0914”(association)	0.350
	CDK1	psi-mi:“MI:0914”(association)	0.350
	AURKA	psi-mi:“MI:0914”(association)	0.350
	SGK1	psi-mi:“MI:0914”(association)	0.350
	TBKBP1	psi-mi:“MI:0914”(association)	0.350
	AHRR	psi-mi:“MI:0914”(association)	0.350
M		psi-mi:“MI:0914”(association)	0.350
TNK1	ACP1	psi-mi:“MI:0914”(association)	0.350
	HLA-C	psi-mi:“MI:0914”(association)	0.350

BioGRID (57): DDX5 (Affinity Capture-MS), ILF3 (Affinity Capture-MS), SFN (Affinity Capture-MS), YWHAB (Affinity Capture-MS), YWHAE (Affinity Capture-MS), YWHAG (Affinity Capture-MS), YWHAH (Affinity Capture-MS), YWHAQ (Affinity Capture-MS), YWHAZ (Affinity Capture-MS), TNK1 (Affinity Capture-MS), TNK1 (Affinity Capture-MS), TNK1 (Affinity Capture-MS), TNK1 (Affinity Capture-MS), TNK1 (Affinity Capture-MS), TNK1 (Affinity Capture-MS)

ESM2 similar proteins: A0A061IR73, A0A7N9VSG0, A7YSY2, D3KCC4, D3ZU57, D4A2B7, O08644, O15197, O19179, O43542, O75064, O95382, P0C0K6, P0C0K7, P51840, P52785, P52824, P54777, Q02846, Q05932, Q13470, Q13608, Q1HG60, Q3ZBE0, Q4KM32, Q5JZY3, Q643R3, Q6MG64, Q6NVG1, Q6ZPS2, Q76MJ5, Q7TNJ2, Q80SX8, Q8BYG9, Q8IZY2, Q8NFF5, Q8R5G7, Q8TDZ2, Q8WWN8, Q91V24

Diamond homologs: F1N9Y5, F1RDG9, G5EBZ8, G5EE56, O02466, O18735, O45539, O54967, P00519, P00520, P00521, P00522, P00525, P00526, P00528, P00533, P00534, P00535, P03949, P04412, P04626, P06239, P06240, P06494, P07948, P08103, P08630, P08631, P0CY46, P10447, P11273, P15209, P17713, P24786, P25911, P27446, P29317, P42679, P42680, P42681

SIGNOR signaling

7 interactions.

A	Effect	B	Mechanism
TNK1	“up-regulates quantity”	PLCG1	binding
MARK4	“down-regulates activity”	TNK1	phosphorylation
MARK1	“down-regulates activity”	TNK1	phosphorylation
MARK2	“down-regulates activity”	TNK1	phosphorylation
MARK3	“down-regulates activity”	TNK1	phosphorylation
14-3-3	“down-regulates activity”	TNK1	binding
TNK1	“up-regulates activity”	TNK1	phosphorylation

Enriched among interaction partners

Reactome pathways and GO biological processes over-represented among this gene’s 20 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
Transcriptional Regulation by TP53	6	23.3×	4e-05

Disease & clinical

Clinical variants and AI predictions

ClinVar

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

Classification	Count (floor)
Pathogenic	0
Likely pathogenic	0
Uncertain significance	87
Likely benign	12
Benign	12

Top pathogenic / likely-pathogenic (0)

SpliceAI

2147 predictions. Top by Δscore:

Variant	Effect	Δscore
17:7383613:GAGT:G	donor_gain	1.0000
17:7383615:GT:G	donor_gain	1.0000
17:7383861:GATG:G	donor_gain	1.0000
17:7386560:GGCC:G	acceptor_gain	1.0000
17:7386988:A:AG	acceptor_gain	1.0000
17:7386989:G:GG	acceptor_gain	1.0000
17:7386989:GCCCC:G	acceptor_gain	1.0000
17:7387142:G:GT	donor_gain	1.0000
17:7387150:GATGG:G	donor_gain	1.0000
17:7387151:A:G	donor_gain	1.0000
17:7388783:CACA:C	acceptor_loss	1.0000
17:7388785:CA:C	acceptor_loss	1.0000
17:7388786:A:AG	acceptor_gain	1.0000
17:7388786:AGGT:A	acceptor_gain	1.0000
17:7388787:G:GC	acceptor_loss	1.0000
17:7388787:G:GG	acceptor_gain	1.0000
17:7388787:GGT:G	acceptor_gain	1.0000
17:7388787:GGTG:G	acceptor_gain	1.0000
17:7388880:CAAG:C	donor_loss	1.0000
17:7388882:AGGTA:A	donor_loss	1.0000
17:7388885:T:A	donor_loss	1.0000
17:7383612:AGAGT:A	donor_gain	0.9900
17:7383613:GAGTG:G	donor_gain	0.9900
17:7383617:G:GG	donor_gain	0.9900
17:7383705:CCA:C	acceptor_loss	0.9900
17:7383706:CAG:C	acceptor_loss	0.9900
17:7383708:G:A	acceptor_loss	0.9900
17:7383862:ATGG:A	donor_loss	0.9900
17:7383863:TGGTG:T	donor_loss	0.9900
17:7383866:T:A	donor_loss	0.9900

AlphaMissense

0 scored. Top likely-pathogenic:

dbSNP variants (sampled 300 via entrez): RS1000533068 (17:7388340 G>A), RS1000547127 (17:7387289 G>A), RS1000562666 (17:7386051 T>G), RS1000641794 (17:7387011 G>A), RS1002262081 (17:7384552 C>G), RS1002356948 (17:7384232 C>G), RS1002471812 (17:7389776 A>C), RS1002665972 (17:7384897 C>T), RS1003200525 (17:7379341 T>C), RS1003202464 (17:7379489 G>A,C), RS1003476 (17:7386013 C>T), RS1003477 (17:7385941 C>A), RS1003522330 (17:7383947 C>G,T), RS1003621893 (17:7379107 C>T), RS1003805088 (17:7389178 G>A)

Disease associations

OMIM: gene MIM:608076 | disease phenotypes:

GenCC curated gene-disease

Mondo (0):

Orphanet (0):

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): CHEMBL5334 (SINGLE PROTEIN)

Molecules with ChEMBL bioactivity

49 molecules (phase ≥1), by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 400,916 (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
CHEMBL1171837	PONATINIB	4	8,955
CHEMBL1287853	FEDRATINIB	4	3,554
CHEMBL1289926	AXITINIB	4	15,732
CHEMBL1336	SORAFENIB	4	86,060
CHEMBL1983268	ENTRECTINIB	4	3,510
CHEMBL2028663	DABRAFENIB	4	12,430
CHEMBL2035187	PACRITINIB	4	3,345
CHEMBL2103743	TOFACITINIB CITRATE	4	1,672
CHEMBL2103830	FOSTAMATINIB	4	3,841
CHEMBL2105759	BARICITINIB	4	6,741
CHEMBL221959	TOFACITINIB	4	10,408
CHEMBL2403108	CERITINIB	4	8,551
CHEMBL3301622	GILTERITINIB	4	2,395
CHEMBL477772	PAZOPANIB	4	15,540
CHEMBL502835	NINTEDANIB	4	8,545
CHEMBL535	SUNITINIB	4	79,020
CHEMBL5416410	DASATINIB	4	655
CHEMBL553	ERLOTINIB	4	108,300
CHEMBL601719	CRIZOTINIB	4	14,403
CHEMBL608533	MIDOSTAURIN	4	7,259
CHEMBL300138	ENZASTAURIN	3
CHEMBL3137331	DEFACTINIB	3
CHEMBL3545154	POZIOTINIB	3
CHEMBL3545308	ROCILETINIB	3
CHEMBL483158	ALISERTIB	3
CHEMBL603469	LESTAURTINIB	3
CHEMBL1230609	FORETINIB	2
CHEMBL1231124	AZD-1480	2
CHEMBL1721885	SU-014813	2
CHEMBL1738757	REBASTINIB	2

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

GtoPdb / IUPHAR curated pharmacology

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

Target class: enzyme — Ack family

Most potent curated ligand interactions (2 total), top 2:

Ligand	Action	Affinity	Parameter
xiliertinib	Inhibition	6.59	pIC50
XMD8-92	Inhibition	6.05	pKd

Binding affinities (BindingDB)

12 measured of 12 human assays (12 total across all organisms); most potent 12 below. Values come from heterogeneous assays and are not directly comparable.

Ligand	Measure	Value	Patent
Staurosporine	KD	1.7 nM
PKC-412	KD	190 nM
4-[[7-[2,6-bis(fluoranyl)phenyl]-9-chloranyl-5H-pyrimido[5,4-d][2]benzazepin-2-yl]amino]benzoic acid	KD	300 nM
4-[4-({[4-chloro-3-(trifluoromethyl)phenyl]carbamoyl}amino)phenoxy]-N-methylpyridine-2-carboxamide	KD	370 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
ERLOTINIB HYDROCHLORIDE	KD	1200 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
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
13-[2-methoxy-4-[4-(4-methylpiperazin-1-yl)piperidin-1-yl]anilino]-2,5,9-trimethyl-4-thia-2,6,9,12,14-pentazatricyclo[8.4.0.03,7]tetradeca-1(14),3(7),5,10,12-pentaen-8-one	IC50	3610 nM	US-12365696: Small-molecule focal adhesion kinase (FAK) inhibitors
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

205 potent at pChembl≥5 of 208 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).

pChembl	Type	Value	Unit	Molecule
9.23	IC50	0.584	nM	STAUROSPORINE
8.87	IC50	1.34	nM	STAUROSPORINE
8.86	IC50	1.37	nM	CHEMBL5772004
8.74	Kd	1.8	nM	TAE-684
8.73	IC50	1.84	nM	STAUROSPORINE
8.60	Kd	2.5	nM	STAUROSPORINE
8.56	IC50	2.77	nM	CHEMBL5756581
8.52	Kd	3	nM	XL-228
8.48	IC50	3.33	nM	CHEMBL5853387
8.47	IC50	3.36	nM	CHEMBL6022678
8.45	IC50	3.59	nM	CHEMBL6058132
8.41	IC50	3.92	nM	CHEMBL5993654
8.40	Kd	4	nM	CHEMBL4465866
8.39	IC50	4.04	nM	CHEMBL5822783
8.38	IC50	4.15	nM	CHEMBL5758369
8.36	IC50	4.42	nM	CHEMBL5955353
8.30	IC50	4.96	nM	CHEMBL5863835
8.30	IC50	5	nM	CHEMBL6054797
8.29	IC50	5.07	nM	NESUPARIB
8.26	IC50	5.56	nM	CHEMBL5795408
8.25	IC50	5.59	nM	CHEMBL5924751
8.24	IC50	5.77	nM	CHEMBL5968204
8.23	IC50	5.82	nM	CHEMBL5772340
8.22	Kd	6	nM	MK-5108
8.20	IC50	6.29	nM	CHEMBL5851052
8.17	IC50	6.77	nM	CHEMBL5932989
8.14	IC50	7.28	nM	CHEMBL5989650
8.09	IC50	8.05	nM	CHEMBL5879210
8.07	IC50	8.46	nM	CHEMBL5758790
8.05	IC50	8.81	nM	CHEMBL5785121
8.03	Kd	9.3	nM	LESTAURTINIB
8.02	IC50	9.65	nM	CHEMBL6001595
8.01	IC50	9.89	nM	CHEMBL5750491
7.99	IC50	10.2	nM	CHEMBL6013549
7.98	IC50	10.4	nM	CHEMBL5954322
7.98	IC50	10.4	nM	CHEMBL5949390
7.97	IC50	10.7	nM	CHEMBL5788476
7.97	IC50	10.6	nM	CHEMBL6015205
7.97	IC50	10.7	nM	CHEMBL6064240
7.96	IC50	11	nM	CHEMBL5997953
7.95	IC50	11.3	nM	CHEMBL5869375
7.94	IC50	11.4	nM	CHEMBL6032977
7.94	IC50	11.4	nM	CHEMBL5981093
7.94	IC50	11.4	nM	CHEMBL5958241
7.94	IC50	11.6	nM	CHEMBL6056405
7.93	IC50	11.8	nM	CHEMBL5985547
7.92	IC50	12.1	nM	CHEMBL5921357
7.91	IC50	12.4	nM	CHEMBL5890554
7.90	IC50	12.5	nM	CHEMBL6023648
7.90	IC50	12.6	nM	CHEMBL6060400

PubChem BioAssay actives

93 with measured affinity, of 526 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	1531911: Inhibition of human TNK1 using poly[Glu:Tyr] (4:1) as substrate by [gamma-33P]-ATP assay	ic50	0.0006	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	624930: Binding constant for TNK1 kinase domain	kd	0.0018	uM
4-N-(5-cyclopropyl-1H-pyrazol-3-yl)-6-(4-methylpiperazin-1-yl)-2-N-[(3-propan-2-yl-1,2-oxazol-5-yl)methyl]pyrimidine-2,4-diamine	1425200: Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	kd	0.0030	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	1526152: Binding affinity to recombinant human N-terminal GST-tagged TNK1 (106 to 390 residues) expressed in baculovirus expression system using CSKtide as substrate incubated for 1 hr by TR-FRET assay	kd	0.0040	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	508114: Binding affinity to TNK1	kd	0.0093	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	1526152: Binding affinity to recombinant human N-terminal GST-tagged TNK1 (106 to 390 residues) expressed in baculovirus expression system using CSKtide as substrate incubated for 1 hr by TR-FRET assay	kd	0.0130	uM
2,6-difluoro-N-[3-fluoro-4-[6-methoxy-7-[3-(4-methylpiperazin-1-yl)propoxy]quinolin-4-yl]oxyphenyl]benzenesulfonamide	1573275: Binding affinity to TNK1 in SILAC-labeled human MDA-MB-231 cells lysate by mass spectrometry based kinAffinity assay	kd	0.0140	uM
N-[3-[2-[2-ethoxy-4-(4-methylpiperazin-1-yl)anilino]-7-oxo-8-[[(2R)-oxolan-2-yl]methyl]pyrido[2,3-d]pyrimidin-6-yl]phenyl]-3-(trifluoromethyl)benzamide	1988555: Binding affinity to TNK1 (unknown origin) assessed as dissociation constant by KINOME scan assay	kd	0.0150	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	624930: Binding constant for TNK1 kinase domain	kd	0.0210	uM
2,5-difluoro-N-[3-fluoro-4-[6-methoxy-7-[3-(4-methylpiperazin-1-yl)propoxy]quinolin-4-yl]oxyphenyl]benzenesulfonamide	1573275: Binding affinity to TNK1 in SILAC-labeled human MDA-MB-231 cells lysate by mass spectrometry based kinAffinity assay	kd	0.0240	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	624930: Binding constant for TNK1 kinase domain	kd	0.0250	uM
2-N-[2-methoxy-4-[4-(4-methylpiperazin-1-yl)piperidin-1-yl]phenyl]-4-N-(2-propan-2-ylsulfonylphenyl)-1,3,5-triazine-2,4-diamine	2161838: Inhibition of human N-terminal GST-fused TNK1 isoform 2 catalytic domain (106 to 390 residues) expressed in baculovirus expression system using CSKtide as substrate measured after 5 hrs by off-chip mobility shift assay relative to control	ic50	0.0268	uM
Ceritinib	1425200: Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	kd	0.0270	uM
4-methyl-3-[(2-methyl-6-pyridin-3-ylpyrazolo[3,4-d]pyrimidin-4-yl)amino]-N-[3-(trifluoromethyl)phenyl]benzamide	2149625: Binding affinity to human TNK1 incubated for 45 mins by Kinobead based pull down assay	kd	0.0277	uM
2-[2-methoxy-4-(4-methylpiperazin-1-yl)anilino]-5,11-dimethylpyrimido[4,5-b][1,4]benzodiazepin-6-one	570548: Binding affinity to TNK1 by immobilized ligand displacement assay	kd	0.0290	uM
Gilteritinib	1425200: Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	kd	0.0390	uM
(2R)-2-methyl-2-[[2-(1H-pyrrolo[2,3-b]pyridin-3-yl)pyrimidin-4-yl]amino]-N-(2,2,2-trifluoroethyl)butanamide	1425200: Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	kd	0.0460	uM
N-[5-[(2R)-2-methoxy-2-phenylacetyl]-4,6-dihydro-1H-pyrrolo[3,4-d]pyrazol-3-yl]-4-(4-methylpiperazin-1-yl)benzamide	1425200: Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	kd	0.0490	uM
4-[4-[(3-tert-butyl-1-quinolin-6-ylpyrazol-5-yl)carbamoylamino]-3-fluorophenoxy]-N-methylpyridine-2-carboxamide	1425200: Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	kd	0.0550	uM
1-[4-[(4-ethylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl]-3-[4-[6-(methylamino)pyrimidin-4-yl]oxyphenyl]urea	435833: Binding constant for full-length TNK1	kd	0.0600	uM
Dabrafenib	1425200: Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	kd	0.0660	uM
N-[4-[4-(4-methylpiperazin-1-yl)-6-[(5-methyl-1H-pyrazol-3-yl)amino]pyrimidin-2-yl]sulfanylphenyl]cyclopropanecarboxamide	435833: Binding constant for full-length TNK1	kd	0.0830	uM
Midostaurin	435833: Binding constant for full-length TNK1	kd	0.0830	uM
Ponatinib	1425200: Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	kd	0.0840	uM
Tofacitinib	624930: Binding constant for TNK1 kinase domain	kd	0.1200	uM
(2S)-1-[4-[(5-cyclopropyl-1H-pyrazol-3-yl)amino]pyrrolo[2,1-f][1,2,4]triazin-2-yl]-N-(6-fluoro-3-pyridinyl)-2-methylpyrrolidine-2-carboxamide	1425200: Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	kd	0.1520	uM
Fostamatinib	1425200: Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	kd	0.1600	uM
Axitinib	624930: Binding constant for TNK1 kinase domain	kd	0.1600	uM
methyl 2-hydroxy-3-[N-[4-[methyl-[2-(4-methylpiperazin-1-yl)acetyl]amino]phenyl]-C-phenylcarbonimidoyl]-1H-indole-6-carboxylate	624930: Binding constant for TNK1 kinase domain	kd	0.2100	uM
methyl (15S,16R,18R)-16-hydroxy-15-methyl-3-oxo-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-nonaene-16-carboxylate	1425200: Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	kd	0.2870	uM
N-[3-[[2-[4-(4-acetylpiperazin-1-yl)-2-methoxyanilino]-5-(trifluoromethyl)pyrimidin-4-yl]amino]phenyl]prop-2-enamide	1425200: Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	kd	0.2890	uM
Crizotinib	624930: Binding constant for TNK1 kinase domain	kd	0.3200	uM
Fedratinib	624930: Binding constant for TNK1 kinase domain	kd	0.3600	uM
6-(2,6-dichlorophenyl)-8-methyl-2-(3-methylsulfanylanilino)pyrido[2,3-d]pyrimidin-7-one	624930: Binding constant for TNK1 kinase domain	kd	0.3600	uM
N-[2-[4-[[4-(cyclobutylamino)-5-(trifluoromethyl)pyrimidin-2-yl]amino]-11-azatricyclo[6.2.1.02,7]undeca-2(7),3,5-trien-11-yl]-2-oxoethyl]acetamide	1425200: Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	kd	0.3690	uM
3-[4-[4-[2-[3-[(dimethylamino)methyl]phenyl]-1H-pyrrolo[2,3-b]pyridin-4-yl]-1-ethylpyrazol-3-yl]phenyl]-1,1-dimethylurea	1425200: Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	kd	0.5360	uM
5-(3-ethylsulfonylphenyl)-3,8-dimethyl-N-(1-methylpiperidin-4-yl)-9H-pyrido[2,3-b]indole-7-carboxamide	1425200: Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	kd	0.5580	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	508114: Binding affinity to TNK1	kd	0.5700	uM
[4-[(E)-2-(1H-indazol-3-yl)ethenyl]phenyl]-piperazin-1-ylmethanone	624930: Binding constant for TNK1 kinase domain	kd	0.5800	uM
Baricitinib	1425200: Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	kd	0.6220	uM
Erlotinib	435833: Binding constant for full-length TNK1	kd	0.6300	uM
N-(2-chloro-6-methylphenyl)-2-[[6-[4-(2-hydroxyethyl)piperazin-1-yl]-2-methylpyrimidin-4-yl]amino]-1,3-thiazole-5-carboxamide;hydrate	1425200: Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	kd	0.6780	uM
Sunitinib	435833: Binding constant for full-length TNK1	kd	0.6800	uM
Pacritinib	1425200: Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	kd	0.8880	uM
2-[2-ethoxy-4-(4-hydroxypiperidin-1-yl)anilino]-5,11-dimethylpyrimido[4,5-b][1,4]benzodiazepin-6-one	2160995: Binding affinity to TNK1 (unknown origin) assessed as dissociation constant by ATP-competition binding assay	kd	0.8900	uM
Pazopanib	435833: Binding constant for full-length TNK1	kd	0.9800	uM
2-(4-amino-1-propan-2-ylpyrazolo[3,4-d]pyrimidin-3-yl)-1H-indol-5-ol	624930: Binding constant for TNK1 kinase domain	kd	1.2000	uM
5-chloro-2-N-[(1S)-1-(5-fluoropyrimidin-2-yl)ethyl]-4-N-(5-methyl-1H-pyrazol-3-yl)pyrimidine-2,4-diamine	1425200: Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	kd	1.2640	uM
1-[4-[4-amino-6-(methoxymethyl)-7-(morpholin-4-ylmethyl)pyrrolo[2,1-f][1,2,4]triazin-5-yl]-2-fluorophenyl]-3-[2-fluoro-5-(trifluoromethyl)phenyl]urea	1425200: Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	kd	1.2650	uM
4-[[9-chloro-7-(2-fluoro-6-methoxyphenyl)-5H-pyrimido[5,4-d][2]benzazepin-2-yl]amino]-2-methoxybenzoic acid	1425200: Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	kd	1.2700	uM

CTD chemical–gene interactions

25 total (human), top 25 by PubMed support.

Chemical	Actions (top 5)	PubMed papers
aristolochic acid I	increases expression	1
sodium bichromate	decreases expression	1
nickel subsulfide	decreases expression	1
sodium arsenite	increases abundance, increases expression	1
coumarin	increases phosphorylation	1
nutlin 3	increases expression, affects cotreatment	1
ON 01910	increases phosphorylation	1
licochalcone B	increases expression	1
Resveratrol	affects cotreatment, decreases expression	1
Arsenic Trioxide	decreases response to substance	1
Leflunomide	decreases expression	1
Arsenic	increases abundance, increases expression	1
Benzo(a)pyrene	affects methylation	1
Calcitriol	increases expression	1
Dactinomycin	affects cotreatment, increases expression	1
Dichlorodiphenyl Dichloroethylene	decreases expression	1
Mustard Gas	increases phosphorylation	1
Plant Extracts	affects cotreatment, decreases expression	1
Selenium	increases expression	1
Smoke	decreases expression	1
Valproic Acid	increases methylation	1
Metribolone	decreases expression	1
Antirheumatic Agents	decreases expression	1
Okadaic Acid	increases expression	1
Acrylamide	increases expression	1

ChEMBL screening assays

153 unique, capped per target: 153 binding

Representative assays (with source publication via chembl_document):

Assay ID	Type	Description	Source paper
CHEMBL1017051	Binding	Binding affinity to Tnk1	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

Cellosaurus cell lines

2 cell lines: 2 cancer cell line

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

Cellosaurus	Name	Category	Sex
CVCL_B2J7	Abcam HeLa TNK1 KO	Cancer cell line	Female
CVCL_TT14	HAP1 TNK1 (-)	Cancer cell line	Male

Clinical trials (associated diseases)

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