PBK

Summary

PBK (PDZ binding kinase, HGNC:18282) is a protein-coding gene on chromosome 8p21.1, encoding Lymphokine-activated killer T-cell-originated protein kinase (Q96KB5). Phosphorylates MAP kinase p38. In precision oncology, PBK OVEREXPRESSION is associated with resistance to Gefitinib in Lung Non-small Cell Carcinoma (CIViC Level D).

This gene encodes a serine/threonine protein kinase related to the dual specific mitogen-activated protein kinase kinase (MAPKK) family. Evidence suggests that mitotic phosphorylation is required for its catalytic activity. The encoded protein may be involved in the activation of lymphoid cells and support testicular functions, with a suggested role in the process of spermatogenesis. Overexpression of this gene has been implicated in tumorigenesis. Alternative splicing results in multiple transcript variants.

Source: NCBI Gene 55872 — RefSeq curated summary.

At a glance

• Clinical variants (ClinVar): 25 total
• GTEx eGene: eQTL in 4 tissues, sQTL in 1 (q < 0.05)
• ChEMBL bioactivity: 1 clinical-phase molecule tested; no curated mechanism-of-action drug
• Precision-oncology evidence (CIViC): 1 curated variant–drug association
• Constraint (gnomAD): pLI 0.43 (intermediate), LOEUF 1.06 (unconstrained)
• MANE Select transcript: NM_018492

Identifiers

Gene identifiers

Field	Value
HGNC ID	HGNC:18282
Approved symbol	PBK
Name	PDZ binding kinase
Location	8p21.1
Locus type	gene with protein product
Status	Approved
Aliases	TOPK, FLJ14385, Nori-3, SPK, CT84
Ensembl gene	ENSG00000168078
Ensembl biotype	protein_coding
OMIM	611210
Entrez	55872

Gene structure

Transcript identifiers

Ensembl transcripts: 7 — 6 protein_coding, 1 nonsense_mediated_decay

MANE Select: ENST00000301905

Transcript support level (Ensembl TSL; 1 = fully mRNA-supported): TSL 1: 1, TSL 2: 1, TSL 3: 1, TSL 5: 1

ENST00000301905, ENST00000521226, ENST00000522944, ENST00000524266, ENST00000884617, ENST00000884618, ENST00001139121

RefSeq mRNA: 3 — MANE Select: NM_018492 NM_001278945, NM_001363040, NM_018492

CCDS: CCDS6063, CCDS64858

Canonical transcript exons

ENST00000301905 — 8 exons

Exon	Start	End
ENSE00001120145	27833056	27833133
ENSE00001120151	27809624	27810501
ENSE00001159563	27837652	27837817
ENSE00003532619	27820565	27820694
ENSE00003545989	27810958	27811134
ENSE00003648502	27822319	27822488
ENSE00003654412	27823063	27823205
ENSE00003662851	27828105	27828198

Expression profiles

Bgee: expression breadth ubiquitous, 189 present calls, max score 98.14.

FANTOM5 (CAGE): breadth ubiquitous, TPM avg 15.2858 / max 842.0722, expressed in 1343 samples.

Highest expression (Bgee): ventricular zone, sperm, male germ cell, ganglionic eminence, primordial germ cell in gonad.

Genetic regulation across tissues (GTEx eQTL / sQTL)

PBK is an eGene in GTEx v10 — its expression is genetically regulated (eQTL) in 4 tissues and its splicing (sQTL) in 1 (q < 0.05). Strongest associations first; slope = normalized effect of the lead variant’s alternative allele.

5 significant tissue × QTL associations:

Tissue	QTL	q-value	Slope	Lead variant
Testis	sqtl	2.0e-24	-0.68	8:27823393:A:G
Colon Transverse	eqtl	4.6e-03	-0.13	8:27699888:C:T
Brain Caudate basal ganglia	eqtl	1.8e-02	-1.84	8:27632723:CT:C
Testis	eqtl	2.8e-02	+0.25	8:27310515:G:T
Heart Left Ventricle	eqtl	4.0e-02	-0.71	8:28102892:G:A

FANTOM5 promoters

3 alternative TSS:

Promoter ID	TPM avg	Samples expressed
92513	14.2643	1331
92514	0.9593	562
92515	0.0621	14

Top tissues by expression

showing 100 of 278 tissues by Bgee expression score (0-100, higher = more expressed):

Tissue	Anatomy ID	Expression score	Quality
ventricular zone	UBERON:0003053	98.14	gold quality
sperm	CL:0000019	97.71	gold quality
male germ cell	CL:0000015	96.16	gold quality
ganglionic eminence	UBERON:0004023	95.39	gold quality
primordial germ cell in gonad	CL:0000670 ∩ UBERON:0000991	93.81	gold quality
adult organism	UBERON:0007023	93.58	gold quality
embryo	UBERON:0000922	92.88	gold quality
left testis	UBERON:0004533	92.31	gold quality
right testis	UBERON:0004534	92.16	gold quality
testis	UBERON:0000473	91.12	gold quality
secondary oocyte	CL:0000655	90.04	gold quality
oocyte	CL:0000023	86.46	gold quality
male germ line stem cell (sensu Vertebrata) in testis	CL:0000089 ∩ UBERON:0000473	86.11	gold quality
mucosa of transverse colon	UBERON:0004991	82.22	gold quality
rectum	UBERON:0001052	81.83	gold quality
stromal cell of endometrium	CL:0002255	81.19	gold quality
adrenal tissue	UBERON:0018303	81.12	gold quality
esophagus squamous epithelium	UBERON:0006920	79.64	gold quality
esophagus mucosa	UBERON:0002469	78.00	gold quality
epithelium of esophagus	UBERON:0001976	77.09	gold quality
vermiform appendix	UBERON:0001154	76.80	gold quality
cartilage tissue	UBERON:0002418	76.65	gold quality
lower esophagus mucosa	UBERON:0035834	76.27	gold quality
oral cavity	UBERON:0000167	76.05	gold quality
thymus	UBERON:0002370	75.46	gold quality
mucosa of sigmoid colon	UBERON:0004993	75.34	gold quality
duodenum	UBERON:0002114	75.27	gold quality
colonic mucosa	UBERON:0000317	75.24	gold quality
bone marrow	UBERON:0002371	74.88	gold quality
trabecular bone tissue	UBERON:0002483	74.62	gold quality
caecum	UBERON:0001153	74.14	gold quality
squamous epithelium	UBERON:0006914	73.51	gold quality
lymph node	UBERON:0000029	72.22	gold quality
placenta	UBERON:0001987	71.98	gold quality
tibia	UBERON:0000979	71.34	gold quality
epithelium of nasopharynx	UBERON:0001951	70.27	silver quality
endometrium	UBERON:0001295	70.02	gold quality
cortical plate	UBERON:0005343	68.83	gold quality
gingival epithelium	UBERON:0001949	68.40	silver quality
jejunal mucosa	UBERON:0000399	67.97	gold quality
gingiva	UBERON:0001828	67.97	gold quality
smooth muscle tissue	UBERON:0001135	67.75	gold quality
olfactory segment of nasal mucosa	UBERON:0005386	66.70	gold quality
transverse colon	UBERON:0001157	66.25	gold quality
bone marrow cell	CL:0002092	66.06	silver quality
small intestine	UBERON:0002108	64.93	gold quality
upper leg skin	UBERON:0004262	64.93	gold quality
tonsil	UBERON:0002372	64.70	gold quality
small intestine Peyer’s patch	UBERON:0003454	64.47	gold quality
skin of abdomen	UBERON:0001416	64.09	gold quality
islet of Langerhans	UBERON:0000006	63.53	gold quality
zone of skin	UBERON:0000014	63.11	gold quality
cervix squamous epithelium	UBERON:0006922	63.01	gold quality
ileal mucosa	UBERON:0000331	62.91	gold quality
hair follicle	UBERON:0002073	62.69	gold quality
skin of leg	UBERON:0001511	62.32	gold quality
intestine	UBERON:0000160	62.00	gold quality
skin of hip	UBERON:0001554	61.85	gold quality
amniotic fluid	UBERON:0000173	61.31	gold quality
esophagus	UBERON:0001043	61.16	gold quality
vagina	UBERON:0000996	61.06	gold quality
cervix epithelium	UBERON:0004801	60.95	silver quality
germinal epithelium of ovary	UBERON:0001304	60.77	gold quality
large intestine	UBERON:0000059	60.47	gold quality
spleen	UBERON:0002106	60.41	gold quality
nasal cavity mucosa	UBERON:0001826	59.92	gold quality
colon	UBERON:0001155	59.54	gold quality
gall bladder	UBERON:0002110	59.26	gold quality
parietal pleura	UBERON:0002400	58.80	silver quality
palpebral conjunctiva	UBERON:0001812	58.60	silver quality
eye	UBERON:0000970	58.59	silver quality
pigmented layer of retina	UBERON:0001782	58.54	gold quality
mammalian vulva	UBERON:0000997	58.50	silver quality
jejunum	UBERON:0002115	57.85	gold quality
colonic epithelium	UBERON:0000397	57.32	silver quality
right adrenal gland	UBERON:0001233	57.27	gold quality
right adrenal gland cortex	UBERON:0035827	57.08	gold quality
stomach	UBERON:0000945	56.84	gold quality
body of stomach	UBERON:0001161	56.77	gold quality
uterus	UBERON:0000995	56.67	gold quality
periodontal ligament	UBERON:0008266	56.53	gold quality
mouth mucosa	UBERON:0003729	56.24	gold quality
oviduct epithelium	UBERON:0004804	55.78	silver quality
pleura	UBERON:0000977	55.75	silver quality
female reproductive system	UBERON:0000474	55.52	gold quality
metanephros	UBERON:0000081	54.88	gold quality
adrenal gland	UBERON:0002369	54.67	gold quality
minor salivary gland	UBERON:0001830	54.65	gold quality
pancreas	UBERON:0001264	54.50	gold quality
descending thoracic aorta	UBERON:0002345	54.41	gold quality
left adrenal gland	UBERON:0001234	54.35	gold quality
omental fat pad	UBERON:0010414	53.89	gold quality
peritoneum	UBERON:0002358	53.86	gold quality
uterine cervix	UBERON:0000002	53.70	gold quality
penis	UBERON:0000989	53.45	silver quality
adipose tissue of abdominal region	UBERON:0007808	53.21	gold quality
cortex of kidney	UBERON:0001225	53.20	gold quality
lung	UBERON:0002048	53.18	gold quality
upper lobe of lung	UBERON:0008948	52.62	gold quality
adrenal cortex	UBERON:0001235	52.55	gold quality

Single-cell (SCXA)

Detected in 15 experiment(s), a significant marker in 14.

Experiment	Marker?	Max mean expression
E-MTAB-8894	yes	555.97
E-ENAD-17	yes	501.56
E-GEOD-81383	yes	476.57
E-MTAB-9435	yes	386.61
E-GEOD-75140	yes	352.68
E-MTAB-5061	yes	320.75
E-GEOD-110499	yes	294.92
E-HCAD-10	yes	260.39
E-MTAB-7052	yes	208.83
E-CURD-114	yes	95.92
E-GEOD-134144	yes	29.62
E-HCAD-13	yes	21.38
E-HCAD-5	yes	19.75
E-ANND-3	yes	4.44
E-CURD-11	no	337.60

HPA expression

RNA tissue specificity: Group enriched

showing 60 of 67 HPA tissues / cells by nTPM:

Tissue / cell	Axis	nTPM	Protein (IHC)
Testis	tissue	65.7	high
Thymus	tissue	21.3
Lymph node	tissue	11.9	low
Tonsil	tissue	11.6	low
Rectum	tissue	9.5	not detected
Bone marrow	tissue	8.6	not detected
Colon	tissue	8.3	not detected
Duodenum	tissue	7.9	not detected
Small intestine	tissue	7.6	not detected
Appendix	tissue	6.3	not detected
Esophagus	tissue	5.4	not detected
Placenta	tissue	4.8	medium
Skin 1	tissue	4.6	not detected
Caudate putamen	tissue	4.4
Stomach 1	tissue	3.4	not detected
Ovary	tissue	2.6	not detected
Smooth muscle	tissue	2.5	not detected
Vagina	tissue	2.4	not detected
Breast	tissue	2.1	not detected
Frontal cortex	tissue	1.7
Urinary bladder	tissue	1.5	not detected
Endometrium 1	tissue	1.1	not detected
Cervix	tissue	1.0	not detected
Adipose tissue	tissue	1.0	not detected
Liver	tissue	1.0	not detected
Spleen	tissue	0.9	not detected
Spinal cord	tissue	0.9
Gallbladder	tissue	0.7	not detected
Fallopian tube	tissue	0.6	not detected
Basal ganglia	tissue	0.5	not detected
Substantia nigra	tissue	0.5
Thyroid gland	tissue	0.5	not detected
Lung	tissue	0.5	not detected
Corpus callosum	tissue	0.5
Pancreas	tissue	0.4	not detected
Medulla oblongata	tissue	0.4
Thalamus	tissue	0.4
Kidney	tissue	0.4	not detected
Hippocampal formation	tissue	0.4
Olfactory bulb	tissue	0.4
Septum	tissue	0.4
Prefrontal cortex	tissue	0.3
Cerebral cortex	tissue	0.3	not detected
Pons	tissue	0.3
Putamen	tissue	0.3
Amygdala	tissue	0.3
Midbrain	tissue	0.3
Hypothalamus	tissue	0.3
Superior colliculi	tissue	0.3
Prostate	tissue	0.3	not detected
Ventral forebrain	tissue	0.3
Heart muscle	tissue	0.2	not detected
Parathyroid gland	tissue	0.2	not detected
Motor cortex	tissue	0.2
Entorhinal cortex	tissue	0.2
Retrosplenial and cingulate cortex	tissue	0.2
Retrosplenial cortex	tissue	0.2
Temporal cortex	tissue	0.2
Occipital cortex	tissue	0.2
Insular cortex	tissue	0.2

Brain sub-regions (HPA Brain Atlas): detected in 32; highest nTPM — Ventral spinal cord (0.9), Dorsal spinal cord (0.8), Anterior thalamic nucleus, ventral (0.7), Pedunculopontine tegmental nucleus (0.6), White matter (0.5).

Regulation

Is transcription factor: no

Upstream regulators (CollecTRI, top): ATM, CREB1

miRNA regulators (miRDB)

Targeting PBK by miRDB confidence (max_score; target_count = how many genes the miRNA targets in total — lower means more specific).

showing 30 of 49 miRNAs:

miRNA	Max score	Avg score	miRNA target_count
HSA-MIR-548N	99.98	71.94	4170
HSA-MIR-548P	99.98	72.25	3784
HSA-MIR-3688-3P	99.97	72.02	2834
HSA-MIR-302E	99.96	70.74	2669
HSA-MIR-3658	99.96	73.87	4379
HSA-MIR-548AA	99.96	70.64	3753
HSA-MIR-548AP-3P	99.96	70.64	3753
HSA-MIR-548T-3P	99.96	70.64	3753
HSA-MIR-545-3P	99.95	70.74	2783
HSA-MIR-145-5P	99.92	71.13	1836
HSA-MIR-5195-3P	99.92	70.92	1877
HSA-MIR-10527-5P	99.91	72.28	3754
HSA-MIR-302A-3P	99.89	71.23	1777
HSA-MIR-302B-3P	99.89	71.23	1777
HSA-MIR-302C-3P	99.89	71.20	1778
HSA-MIR-302D-3P	99.89	71.25	1777
HSA-MIR-5582-3P	99.86	72.48	4221
HSA-MIR-373-3P	99.84	70.68	1668
HSA-MIR-520E-3P	99.84	70.55	1698
HSA-MIR-372-3P	99.83	70.58	1691
HSA-MIR-520A-3P	99.83	70.59	1687
HSA-MIR-520B-3P	99.83	70.56	1699
HSA-MIR-520C-3P	99.83	70.56	1699
HSA-MIR-520D-3P	99.83	70.78	1676
HSA-MIR-520F-3P	99.82	71.32	1216
HSA-MIR-4495	99.82	72.08	3080
HSA-MIR-548AG	99.77	69.25	1492
HSA-MIR-6505-5P	99.73	69.25	1595
HSA-MIR-4255	99.72	67.70	1541
HSA-MIR-548AI	99.69	69.24	1494

Functional genomics

gnomAD constraint: pLI 0.434, LOEUF 1.06, missense Z 0.37 — population loss-of-function intolerance (pLI ≥ 0.9 = LoF-intolerant; lower LOEUF = more constrained). gnomAD

Regional missense constraint (gnomAD RMC): no regional variation along ENST00000301905 — one region, missense o/e 0.98.

Literature-anchored findings (GeneRIF, showing 40)

• PBK/TOPK is upregulated in Burkitt’s lymphoma and other highly proliferative malignant cells and during normal fetal development. (PMID:11783945)
• TOPK protein is up-regulated in a variety of hematologic malignancies and may be involved in leukemic cell growth; 4 of 5 clinical that strongly expressed TOPK also strongly expressed phosphorylated c-Myc (PMID:14757441)
• PBK/TOPK plays an important role in transiently amplifying neural progenitors in the adult subependymal zone of transgenically targeted mice. (PMID:16291951)
• PBK augments tumor cell growth following transient appearance in different types of progenitor cells in vivo as reported. (PMID:17482142)
• Findings showed that TOPK positively modulated UVB-induced JNK1 activity and played a pivotal role in JNK1-mediated cell transformation induced by H-Ras. (PMID:17545598)
• The positive feedback loop between TOPK and ERK2 increases tumorigenesis properties of HCT116 colorectal cancer cells, and TOPK-regulated signaling may serve as a potential therapeutic target in colorectal cancer (PMID:17631144)
• TOPK is indispensable for cancer cell cytokinesis throughout phosphorylation on p97. (PMID:19900192)
• PBK/TOPK protein could serve as a useful indicator for histopathologic differentiation between cholangiocarcinoma and hepatocellular carcinomas and the low expression of PBK/TOPK is predicative of poor survival in cholangiocarcinoma patients. (PMID:19954816)
• Upregulation of TOPK is associated with breast cancer. (PMID:20589935)
• increased levels of PBK/TOPK may contribute to tumor cell development and progression through suppression of p53 function and consequent reductions in the cell-cycle regulatory proteins such as p21. (PMID:20622899)
• Phosphorylation of Prx1 (Ser-32) by TOPK prevents UVB-induced apoptosis in RPMI7951 melanoma cells through regulation of Prx1 peroxidase activity and blockade of intracellular H(2)O(2) accumulation. (PMID:20647304)
• T-LAK cell-originated protein kinase (TOPK) phosphorylation of MKP1 protein prevents solar ultraviolet light-induced inflammation through inhibition of the p38 protein signaling pathway. (PMID:21715333)
• Our results indicate that overexpression of TOPK could predetermine the metastatic capability of tumors and could serve as a significant prognostic predictor of shortened overall survival and time to recurrence. (PMID:22192142)
• The 3D structure of TOPK protein has been constructed by using multiple templates. (PMID:22940854)
• that the serine-threonine kinase PBK/TOPK is frequently overexpressed in high-grade lymphomas and its expression is positively correlated to that of c-Myc and E2F1 (PMID:23237560)
• TOPK directly interacted with and phosphorylated IkappaBalpha at Ser-32, leading to p65 nuclear translocation and NF-kappaB activation. (PMID:23250755)
• These results suggest that the malignant transformation of plexiform neurofibroma is associated with distinct changes in the expression of BUB1B, PBK and NEK2 (PMID:23370767)
• Antibody screening revealed 3 candidate prognostic markers in breast cancer: the Anillin (ANLN); PDZ-Binding Kinase (PBK); and, PDZ-Domain Containing 1 (PDZK1). (PMID:23547718)
• CHFR ubiquitinates and regulates TOPK levels, which is essential for its checkpoint function. (PMID:24012691)
• PBK/TOPK expression is positively correlated with Ki67 and p53 expression, and can be used as an independent prognostic factor in non-small-cell lung cancer. (PMID:24025073)
• TOPK protein upregulates iNOS gene expression in T cell leukemia Jurkat cells or macrophage leukemic Raw 264.7 cells via NF-kappaB activation in response to LPS, and might act as a critical effector in LPS/TLR4-mediated signaling cascade. (PMID:24440499)
• Study findings suggest that the PBK/TOPK mRNA/protein expression is specific to human bladder cancer and might be used as a novel target for development of cancer immunotherapy and diagnostic biomarker. (PMID:24629784)
• PDZ-binding kinase/T-LAK cell-originated protein kinase correlates with mutant p53 and affects cell proliferation and viability as well as prognosis in lung adenocarcinoma (PMID:25466965)
• PBK/TOPK expression is closely associated with cervical cancer and cervical intraepithelial neoplasia, which may be served as a useful target for tumor diagnosis and immunotherapy. (PMID:25550851)
• Authors identified TOPK/PBK, in vitro and in vivo, as the master ZFP linker kinase. Furthermore, they show precise temporal correlation between TOPK activating phosphorylation by Cdk1 and linker phosphorylation in mitosis. (PMID:25575812)
• TOPK, overexpressed in colorectal cancer, enhances the resistance of colorectal cancer cells to anoikis. (PMID:25687885)
• TOPK was speculated to be one of a potential marker and therapeutic target in advanced prostate cancer (PMID:25881543)
• The in vitro data have been consistent with a role for PBK/TOPK in facilitating invasion in prostate cancer. PBK could be a prognostic biomarker for prostate cancer that would discriminate aggressive prostate cancer from indolent disease. (PMID:25909225)
• Overexpression of Nrf2 inhibited the PBK/TOPK KD-induced decrease in cdc2 and cyclin B expression and cell cycle arrest, and blocked ROS production and apoptosis. (PMID:26503118)
• TOPK silencing sensitizes EGFR-TKI-resistant lung cancer cells to gefitinib and increases gefitinib efficacy in preclinical lung adenocarcinoma xenograft models. (PMID:26745678)
• Upregulation of proteasome subunit beta type 8 PSMB8 and PDZ binding kinase PBK was confirmed by real-time reverse transcription-PCR analysis. (PMID:26894977)
• Study shows that BUB1beta and PDZ binding kinase are up-regulated in breast cancer tumors and their expression is associated with improved overall survival (OS) in basal-like tumors but worse OS in luminal and untreated patients. (PMID:26897635)
• Results indicate that src-family kinase (Src) is a upstream kinase of T-LAK cell-originated protein kinase (TOPK). (PMID:27016416)
• Determined the crystal structure of PBK, which has two phospho-mimicking mutations T9E and T198E. The structural data indicated that PBK may assemble into an inactive dimer in alkaline conditions. Analytical size-exclusion chromatography and analytical ultracentrifugation confirmed that PBK exists in a conformational transition between dimers and monomers at different pH conditions. (PMID:27262437)
• TOPK protein and transcriptional levels of FOXM1 were reduced by TOPK inhibitor treatment. (PMID:27334838)
• A high PBK expression level was correlated with long overall survival in oral squamous cell carcinoma. (PMID:27347940)
• High TOPK expression is associated with liver cancer. (PMID:27582549)
• PBK/TOPK plays a crucial role in tumour malignant potential through its overexpression and highlight its usefulness as a prognostic factor and potential therapeutic target in gastric cancer. (PMID:27898655)
• findings suggest that PBK/TOPK plays a crucial role in tumor malignant potential through its overexpression in ESCC (PMID:27919968)
• Data suggest that T-LAK cell-originated protein kinase (TOPK) might play a pivotal role in breast cancer invasion and metastasis. (PMID:28212583)

Cross-species orthologs

4 orthologs

Organism	Symbol	Gene ID
danio_rerio	pbk	ENSDARG00000007221
mus_musculus	Pbk	ENSMUSG00000022033
rattus_norvegicus	Pbk	ENSRNOG00000015308
drosophila_melanogaster	CG8173	FBGN0030864

Mouse-model phenotypes

Observed phenotypes of the mouse ortholog (MGI:1289156) from MGI (Alliance of Genome Resources) — knockout/mutant phenotypes, ranked by annotation count. 8 distinct phenotype terms.

Mouse phenotype (MP)	Records
thick epidermis	1
abnormal epidermis stratum corneum morphology	1
abnormal skin morphology	1
reproductive system phenotype	1
increased tumor necrosis factor secretion	1
increased interleukin-6 secretion	1
decreased interleukin-6 secretion	1
skin fibrosis	1

Additional cross-species homologs

Sequence homologs in species beyond Ensembl Compara’s model organisms, by Diamond local protein alignment (% sequence identity; best hit per species). Lower-identity rows are more distant homologs. The matched accessions’ gene symbols aren’t in biobtree yet, so each row shows the UniProt accession.

Organism	UniProt	Identity	Method
Sus scrofa	A4PES0	79.0%	Diamond

Genomic neighbors (locus context)

Genes flanking this one on the chromosome (NCBI/Entrez gene neighborhood). Positional context only — some neighbors share regulatory elements (bidirectional promoters, antisense/overlapping transcripts), but chromosomal adjacency is not itself a functional relationship (see Interactions for that).

Symbol	Type	Entrez
MIR4287	ncRNA	100422828
ESCO2	protein-coding	157570
SCARA5	protein-coding	286133
NUGGC	protein-coding	389643
MIR3622A	ncRNA	100500858
MIR3622B	ncRNA	100500871
SCARA3	protein-coding	51435
CCDC25	protein-coding	55246
ELP3	protein-coding	55140

Protein

Protein identifiers

Lymphokine-activated killer T-cell-originated protein kinase — Q96KB5 (reviewed: Q96KB5)

Alternative names: Cancer/testis antigen 84, MAPKK-like protein kinase, Nori-3, PDZ-binding kinase, Spermatogenesis-related protein kinase, T-LAK cell-originated protein kinase

All UniProt accessions (4): E5RFX4, E5RIE1, Q96KB5, V9HWH0

UniProt curated annotations — full annotation on UniProt →

Function. Phosphorylates MAP kinase p38. Seems to be active only in mitosis. May also play a role in the activation of lymphoid cells. When phosphorylated, forms a complex with TP53, leading to TP53 destabilization and attenuation of G2/M checkpoint during doxorubicin-induced DNA damage.

Subunit / interactions. Interacts with DLG1 and TP53.

Tissue specificity. Expressed in the testis and placenta. In the testis, restrictedly expressed in outer cell layer of seminiferous tubules.

Post-translational modifications. Phosphorylated; in a cell-cycle dependent manner at mitosis.

Activity regulation. Activated by phosphorylation.

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

Isoforms (2)

UniProt ID	Names	Canonical?
Q96KB5-1	1	yes
Q96KB5-2	2

RefSeq proteins (3): NP_001265874, NP_001349969, NP_060962* (*=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
IPR041989	PKc_TOPK	Domain

Pfam: PF00069

Catalyzed reactions (Rhea)

• L-tyrosyl-[protein] + ATP = O-phospho-L-tyrosyl-[protein] + ADP + H(+) (RHEA:10596)
• 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 (59 total): helix 21, strand 11, modified residue 5, mutagenesis site 4, turn 4, sequence variant 3, sequence conflict 3, binding site 2, chain 1, domain 1, cross-link 1, splice variant 1, region of interest 1, active site 1

Structure

Experimental structures (PDB)

1 structures by resolution:

PDB	Title	Method	Resolution (Å)
5J0A	Crystal structure of PDZ-binding kinase	X-RAY DIFFRACTION	2.74

Predicted structure (AlphaFold)

Model	pLDDT	Fraction very-high
AF-Q96KB5-F1	84.66	0.59

Human Protein Atlas

Protein class: Enzymes, ENZYME proteins, Transferases, Kinases, STE Ser/Thr protein kinases, Predicted intracellular proteins, Plasma proteins

Protein evidence: Evidence at protein level

Subcellular location (HPA, imaging): cytosol

Antibody reliability (HPA): IH enhanced · IF approved

Functional residue map

Curated UniProt residues grouped by drug-discovery relevance — catalytic, ligand-binding, modification, and mutation-validated positions. Source: UniProtKB sequence features.

Catalytic / active sites (1)

Position	Role
167	proton acceptor

Ligand- & substrate-binding residues (2)

Position	Role
38–46	ATP
64	ATP

Post-translational modifications (6)

Type	Positions
Phosphoserine	59, 32
Glycyl lysine isopeptide (lys-gly) (interchain with g-cter in sumo2)	169
N-acetylmethionine	1
Phosphothreonine	9, 24

Mutagenesis-validated functional residues (4)

Position	Phenotype
9	tp53-binding.
64–65	loss of activity.
320	decrease in the binding to dlg1.
322	decrease in the binding to dlg1.

Function

Pathways and Gene Ontology

Reactome pathways

0 curated (TAS) of 0; 0 disease pathways. Curated-first; evidence = TAS (manually curated) vs IEA (electronic inference).

MSigDB gene sets: 318 (showing top): WU_APOPTOSIS_BY_CDKN1A_VIA_TP53, HORIUCHI_WTAP_TARGETS_DN, GOBP_NEGATIVE_REGULATION_OF_PROTEOLYSIS, GOBP_REGULATION_OF_PROTEASOMAL_UBIQUITIN_DEPENDENT_PROTEIN_CATABOLIC_PROCESS, KANG_DOXORUBICIN_RESISTANCE_UP, RODRIGUES_THYROID_CARCINOMA_POORLY_DIFFERENTIATED_UP, GOBP_REGULATION_OF_STRESS_ACTIVATED_PROTEIN_KINASE_SIGNALING_CASCADE, GOBP_CELLULAR_RESPONSE_TO_UV, GOBP_INFLAMMATORY_RESPONSE, GOBP_CELLULAR_RESPONSE_TO_LIGHT_STIMULUS, CHIANG_LIVER_CANCER_SUBCLASS_UNANNOTATED_DN, GRAESSMANN_APOPTOSIS_BY_DOXORUBICIN_DN, GRAESSMANN_RESPONSE_TO_MC_AND_DOXORUBICIN_DN, GOBP_MACROMOLECULE_CATABOLIC_PROCESS, IVANOVA_HEMATOPOIESIS_LATE_PROGENITOR

GO Biological Process (3): mitotic cell cycle (GO:0000278), MAPK cascade (GO:0000165), protein phosphorylation (GO:0006468)

GO Molecular Function (10): protein serine/threonine kinase activity (GO:0004674), MAP kinase kinase activity (GO:0004708), protein tyrosine kinase activity (GO:0004713), ATP binding (GO:0005524), protein serine kinase activity (GO:0106310), nucleotide binding (GO:0000166), protein kinase activity (GO:0004672), protein binding (GO:0005515), kinase activity (GO:0016301), transferase activity (GO:0016740)

GO Cellular Component (1): nucleus (GO:0005634)

GO top-level categories

20 GO namespaces:

Category	Terms
protein kinase activity	3
cell cycle	1
mitotic nuclear division	1
intracellular signaling cassette	1
phosphorylation	1
protein modification process	1
MAPK cascade	1
protein serine/threonine/tyrosine kinase activity	1
adenyl ribonucleotide binding	1
purine ribonucleoside triphosphate binding	1
anion 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 membrane-bounded organelle	1

Experimentally-supported GO annotations

GO terms backed by direct experimental evidence (ECO experimental codes) — 1 of 14 annotations. The rest are phylogenetic / computational / electronic (IEA).

1 experimentally-supported GO terms:

GO term	NS	Evidence
nucleus	CC	direct assay

Protein interactions and networks

STRING

showing 15 of 1,548 interactions by confidence (×1000):

Protein A	Protein B	Partner UniProt	Score
PBK	CDK1	P06493	726
PBK	MELK	Q14680	614
PBK	DLGAP5	Q15398	591
PBK	ASF1B	Q9NVP2	591
PBK	CEP55	Q53EZ4	588
PBK	KIF20A	O95235	587
PBK	NUSAP1	Q9BXS6	582
PBK	TOP2A	P11388	580
PBK	ASPM	Q8IZT6	572
PBK	TTK	P33981	570
PBK	NCAPG	Q9BPX3	569
PBK	BUB1B	O60566	567
PBK	BUB1	O43683	543
PBK	KIF11	P52732	530
PBK	UBE2T	Q9NPD8	523

IntAct

Human interaction partners of PBK in IntAct, one row per partner (best MIscore; records = supporting IntAct interaction records).

showing 30 of 164 partners by confidence:

Partner	Interaction type	MIscore	Records
DLG1	direct interaction	0.750	10
TP53	physical association	0.710	7
SCRIB	direct interaction	0.610	6
MAST2	direct interaction	0.610	3
DDIT4L	physical association	0.560	3
MCRS1	physical association	0.560	3
ZNF526	physical association	0.560	3
TRIM37	association	0.550	2
MPDZ	direct interaction	0.440	14
PATJ	direct interaction	0.440	9
GRIP1	direct interaction	0.440	7
GRIP2	direct interaction	0.440	7
MAGI1	direct interaction	0.440	6
MAGI2	direct interaction	0.440	6
MAGI3	direct interaction	0.440	6
PDZD2	direct interaction	0.440	6
PTPN13	direct interaction	0.440	5
IL16	direct interaction	0.440	4
NHERF4	direct interaction	0.440	4
PDZK1	direct interaction	0.440	4
DLG4	direct interaction	0.440	3
FRMPD2	direct interaction	0.440	3
LNX1	direct interaction	0.440	3
LNX2	direct interaction	0.440	3
PARD3B	direct interaction	0.440	3
PDZD7	direct interaction	0.440	3
TJP1	direct interaction	0.440	3
TJP2	direct interaction	0.440	3
TJP3	direct interaction	0.440	3
USH1C	direct interaction	0.440	3

BioGRID (193 interactions; top human partners by supporting records): MSL1 (Affinity Capture-MS; 4 records), TP53 (Affinity Capture-Western; 4 records), ARRDC1 (Affinity Capture-MS; 3 records), DLG1 (Two-hybrid; 3 records), DOK4 (Affinity Capture-MS; 3 records), LGALS9 (Affinity Capture-MS; 3 records), LGALS9B (Affinity Capture-MS; 3 records), LNX1 (Affinity Capture-Western; 3 records), CDK1 (Biochemical Activity; 2 records), CHFR (Affinity Capture-Western; 2 records), FAM19A3 (Affinity Capture-MS; 2 records), FGB (Affinity Capture-MS; 2 records), H2AFX (Reconstituted Complex; 2 records), PPP1CA (Co-fractionation; 2 records), PRC1 (Affinity Capture-Western; 2 records)

SIGNOR signaling

showing 19 of 23 signaling interactions:

A	Effect	B	Mechanism
CDK1	unknown	PBK	phosphorylation
PBK	unknown	H3C1	phosphorylation
PBK	up-regulates	GPSM2	phosphorylation
PBK	up-regulates	PRDX1	phosphorylation
CyclinB/CDK1	unknown	PBK	phosphorylation
PBK	unknown	“Histone H3”	phosphorylation
CHFR	“down-regulates quantity by destabilization”	PBK	polyubiquitination
PBK	“down-regulates activity”	PTEN	phosphorylation
LNX1	“down-regulates quantity by destabilization”	PBK	ubiquitination
SRC	“up-regulates quantity by stabilization”	PBK	phosphorylation
PBK	“down-regulates activity”	ULK1	phosphorylation
PBK	“up-regulates activity”	JUN	phosphorylation
PBK	“up-regulates activity”	TP53RK	phosphorylation
PBK	“up-regulates activity”	MAPK1	phosphorylation
PBK	“up-regulates activity”	HDAC1	phosphorylation
PBK	“up-regulates activity”	HDAC2	phosphorylation
MAPK1	“up-regulates activity”	PBK	phosphorylation
PBK	“up-regulates activity”	MAPK8	phosphorylation
CyclinB/CDK1	“up-regulates activity”	PBK	phosphorylation

Enriched among interaction partners

Reactome pathways and GO biological processes over-represented among this gene’s 164 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
Dopamine Neurotransmitter Release Cycle	6	29.5×	3e-06
Ras activation upon Ca2+ influx through NMDA receptor	5	28.3×	3e-05
Neurexins and neuroligins	14	27.3×	2e-14
Unblocking of NMDA receptors, glutamate binding and activation	5	26.9×	3e-05
Negative regulation of NMDA receptor-mediated neuronal transmission	5	26.9×	3e-05
Assembly and cell surface presentation of NMDA receptors	10	25.1×	1e-09
Protein-protein interactions at synapses	9	23.7×	1e-08
Long-term potentiation	5	23.6×	6e-05

GO biological processes:

GO term	Partners	Fold	FDR
establishment or maintenance of epithelial cell apical/basal polarity	15	57.4×	7e-21
protein localization to synapse	7	35.3×	8e-08
receptor clustering	8	32.9×	1e-08
regulation of postsynaptic membrane neurotransmitter receptor levels	8	26.1×	8e-08
neurotransmitter secretion	5	23.1×	1e-04
positive regulation of excitatory postsynaptic potential	6	20.8×	3e-05
negative regulation of stress fiber assembly	5	19.1×	3e-04
establishment or maintenance of cell polarity	6	15.8×	1e-04

Disease & clinical

Genetic variants

Variant evidence for PBK: 25 ClinVar records (0 pathogenic / likely pathogenic); 2 CIViC cancer variants.

ClinVar

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

Classification	Count (floor)
Pathogenic	0
Likely pathogenic	0
Uncertain significance	20
Likely benign	0
Benign	0

SpliceAI

Top 10 splice-impact sites by Δscore (adjacent positions with the same effect merged into one range; 26 predictions of 659):

Position(s)	Effect	Δscore	Sites
8:27810512	acceptor_gain	1.0000
8:27820563–27820564	donor_loss	1.0000	5
8:27820696	acceptor_loss	1.0000	2
8:27822317–27822318	donor_loss	1.0000	5
8:27822489–27822490	acceptor_loss	1.0000	4
8:27822490	acceptor_gain	1.0000
8:27828203	acceptor_gain	1.0000
8:27828208	acceptor_gain	1.0000
8:27833134–27833135	acceptor_loss	1.0000	5
8:27810503	acceptor_gain	0.9900

AlphaMissense

755 missense substitutions predicted likely pathogenic (of 2,143 scored), across 185 residues. Top 20 hotspot residues, ranked by the number of likely-pathogenic substitutions (of those reachable by a single-nucleotide change), then by mean score:

Residue	Likely-pathogenic substitutions	Mean am_pathogenicity	Max am_pathogenicity
M240	9	0.886	0.997
D186	8	0.995	0.999
D229	8	0.991	0.996
D167	8	0.986	0.998
H165	8	0.984	0.996
H158	8	0.980	0.998
N172	8	0.962	0.992
H94	8	0.949	0.992
W212	7	0.994	0.999
E85	7	0.988	0.995
F231	7	0.986	0.997
W61	7	0.984	0.998
K64	7	0.983	1.000
E239	7	0.982	0.996
K169	7	0.968	0.998
F297	7	0.952	0.986
C185	7	0.947	0.997
W238	7	0.943	0.992
E116	7	0.941	0.983
E216	7	0.936	0.975

HPA cancer prognostics

RNA cancer specificity: Low cancer specificity

Human Protein Atlas survival analysis — favorable = higher expression predicts better survival.

8 prognostic cancer types:

Cancer	Prognostic	p-value
Kidney Chromophobe (TCGA)	unfavorable	1.21e-06
Kidney Renal Papillary Cell Carcinoma (TCGA)	unfavorable	1.47e-06
Liver Hepatocellular Carcinoma (validation)	unfavorable	3.97e-06
Liver Hepatocellular Carcinoma (TCGA)	unfavorable	7.03e-06
Lung Adenocarcinoma (TCGA)	unfavorable	2.67e-05
Pancreatic Adenocarcinoma (TCGA)	unfavorable	3.76e-05
Kidney Renal Clear Cell Carcinoma (validation)	unfavorable	0.000139
Colon Adenocarcinoma (TCGA)	favorable	0.000632

Disease associations

OMIM: gene MIM:611210 | disease phenotypes:

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (1): CHEMBL4896 (SINGLE PROTEIN)

Molecules with ChEMBL bioactivity

Phase ≥1, by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 4,094 (via chembl_molecule»patent_compound — counts attach to the compound, not the gene–compound relationship, so off-target/promiscuous molecules can dominate).

1 molecules by phase:

Molecule	Name	Phase	Patents
CHEMBL223360	LINIFANIB	3	4,094

Clinical evidence (CIViC)

Drug × variant × indication, from 1 curated evidence items; also 1 prognostic. CIViC evidence level: A (validated) → B (clinical) → C (case study) → D (preclinical) → E (inferential).

1 predictive associations by evidence level:

Variant	Therapy	Indication	Effect	Level	CIViC
PBK OVEREXPRESSION	Gefitinib	Lung Non-small Cell Carcinoma	Resistance	CIViC D	EID835

CIViC curated variants (2)

Named clinical variants curated in CIViC for this gene (the catalogue beneath the predictive evidence above):

OVEREXPRESSION, NUCLEAR EXPRESSION.

PharmGKB: 1 entry (CPIC guideline: no)

GtoPdb / IUPHAR curated pharmacology

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

Target class: enzyme — TOPK family

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

Ligand	Action	Affinity	Parameter
OTS964	Inhibition	7.55	pIC50

Binding affinities (BindingDB)

265 measured of 269 human assays (269 total across all organisms); most potent 50 below. Values come from heterogeneous assays and are not directly comparable.

Ligand	Measure	Value	Patent
9-[4-(aminomethyl)phenyl]-8-hydroxy-5,5a,6,7,8,9,9a,9b-octahydro-3aH-thieno[2,3-c]quinolin-4-one	IC50	0.38 nM	US-8962648: Tricyclic compounds and PBK inhibitors containing the same
9-[4-(2-aminopropan-2-yl)phenyl]-8-hydroxy-5,5a,6,7,8,9,9a,9b-octahydro-3aH-thieno[2,3-c]quinolin-4-one	IC50	0.43 nM	US-8962648: Tricyclic compounds and PBK inhibitors containing the same
9-[4-(2-aminoethyl)-3-fluorophenyl]-8-hydroxy-5,5a,6,7,8,9,9a,9b-octahydro-3aH-thieno[2,3-c]quinolin-4-one	IC50	0.5 nM	US-8962648: Tricyclic compounds and PBK inhibitors containing the same
CHEMBL4445123	IC50	0.5 nM
9-[4-[(1R)-1-aminoethyl]phenyl]-8-hydroxy-5,5a,6,7,8,9,9a,9b-octahydro-3aH-thieno[2,3-c]quinolin-4-one	IC50	0.54 nM	US-8962648: Tricyclic compounds and PBK inhibitors containing the same
9-[4-[[4-(aminomethyl)piperidin-1-yl]methyl]-3-fluorophenyl]-8-hydroxy-5,5a,6,7,8,9,9a,9b-octahydro-3aH-thieno[2,3-c]quinolin-4-one	IC50	0.57 nM	US-8962648: Tricyclic compounds and PBK inhibitors containing the same
9-[4-[(2R)-1-aminopropan-2-yl]phenyl]-8-hydroxy-5,5a,6,7,8,9,9a,9b-octahydro-3aH-thieno[2,3-c]quinolin-4-one	IC50	0.64 nM	US-8962648: Tricyclic compounds and PBK inhibitors containing the same
9-[4-(1-amino-2-methylpropan-2-yl)phenyl]-8-hydroxy-5,5a,6,7,8,9,9a,9b-octahydro-3aH-thieno[2,3-c]quinolin-4-one	IC50	0.67 nM	US-8962648: Tricyclic compounds and PBK inhibitors containing the same
9-[4-(1-aminoethyl)phenyl]-8-hydroxy-5,5a,6,7,8,9,9a,9b-octahydro-3aH-thieno[2,3-c]quinolin-4-one	IC50	0.73 nM	US-8962648: Tricyclic compounds and PBK inhibitors containing the same
9-[4-(3-aminopropyl)phenyl]-8-hydroxy-5,5a,6,7,8,9,9a,9b-octahydro-3aH-thieno[2,3-c]quinolin-4-one	IC50	0.74 nM	US-8962648: Tricyclic compounds and PBK inhibitors containing the same
9-[4-(1-aminobutan-2-yl)phenyl]-8-hydroxy-5,5a,6,7,8,9,9a,9b-octahydro-3aH-thieno[2,3-c]quinolin-4-one	IC50	0.74 nM	US-8962648: Tricyclic compounds and PBK inhibitors containing the same
8-hydroxy-9-(1,2,3,6-tetrahydropyridin-4-yl)-3aH-thieno[2,3-c]quinolin-4-one	IC50	0.78 nM	US-8962648: Tricyclic compounds and PBK inhibitors containing the same
9-[5-(aminomethyl)thiophen-2-yl]-8-hydroxy-3aH-thieno[2,3-c]quinolin-4-one	IC50	0.78 nM	US-8962648: Tricyclic compounds and PBK inhibitors containing the same
9-[4-[(1S)-1-aminoethyl]phenyl]-8-hydroxy-5,5a,6,7,8,9,9a,9b-octahydro-3aH-thieno[2,3-c]quinolin-4-one	IC50	0.81 nM	US-8962648: Tricyclic compounds and PBK inhibitors containing the same
9-[4-(1-aminopropyl)phenyl]-8-hydroxy-5,5a,6,7,8,9,9a,9b-octahydro-3aH-thieno[2,3-c]quinolin-4-one	IC50	0.82 nM	US-8962648: Tricyclic compounds and PBK inhibitors containing the same
9-[4-[(1R)-1-(dimethylamino)ethyl]phenyl]-8-hydroxy-5,5a,6,7,8,9,9a,9b-octahydro-3aH-thieno[2,3-c]quinolin-4-one	IC50	0.88 nM	US-8962648: Tricyclic compounds and PBK inhibitors containing the same
9-[4-[(1S)-1-aminopropyl]phenyl]-8-hydroxy-5,5a,6,7,8,9,9a,9b-octahydro-3aH-thieno[2,3-c]quinolin-4-one	IC50	0.88 nM	US-8962648: Tricyclic compounds and PBK inhibitors containing the same
8-hydroxy-9-[4-(methylaminomethyl)phenyl]-5,5a,6,7,8,9,9a,9b-octahydro-3aH-thieno[2,3-c]quinolin-4-one	IC50	0.9 nM	US-8962648: Tricyclic compounds and PBK inhibitors containing the same
9-[4-(1-aminoethyl)-3-fluorophenyl]-8-hydroxy-5,5a,6,7,8,9,9a,9b-octahydro-3aH-thieno[2,3-c]quinolin-4-one	IC50	0.92 nM	US-8962648: Tricyclic compounds and PBK inhibitors containing the same
9-[3-fluoro-4-[(3-hydroxypyrrolidin-1-yl)methyl]phenyl]-8-hydroxy-5,5a,6,7,8,9,9a,9b-octahydro-3aH-thieno[2,3-c]quinolin-4-one	IC50	0.97 nM	US-8962648: Tricyclic compounds and PBK inhibitors containing the same
9-[4-(1-amino-2-methylpropan-2-yl)-3-fluorophenyl]-8-hydroxy-5,5a,6,7,8,9,9a,9b-octahydro-3aH-thieno[2,3-c]quinolin-4-one	IC50	1 nM	US-8962648: Tricyclic compounds and PBK inhibitors containing the same
9-[4-(2-aminoethyl)phenyl]-8-hydroxy-5,5a,6,7,8,9,9a,9b-octahydro-3aH-thieno[2,3-c]quinolin-4-one	IC50	1.1 nM	US-8962648: Tricyclic compounds and PBK inhibitors containing the same
8-hydroxy-9-[4-[(1S)-1-(methylamino)ethyl]phenyl]-5,5a,6,7,8,9,9a,9b-octahydro-3aH-thieno[2,3-c]quinolin-4-one	IC50	1.1 nM	US-8962648: Tricyclic compounds and PBK inhibitors containing the same
9-(2-amino-2,3-dihydro-1H-inden-5-yl)-8-hydroxy-5,5a,6,7,8,9,9a,9b-octahydro-3aH-thieno[2,3-c]quinolin-4-one	IC50	1.2 nM	US-8962648: Tricyclic compounds and PBK inhibitors containing the same
8-hydroxy-9-[4-[(1R)-1-(methylamino)ethyl]phenyl]-5,5a,6,7,8,9,9a,9b-octahydro-3aH-thieno[2,3-c]quinolin-4-one	IC50	1.3 nM	US-8962648: Tricyclic compounds and PBK inhibitors containing the same
9-[4-(2-aminopropyl)phenyl]-8-hydroxy-5,5a,6,7,8,9,9a,9b-octahydro-3aH-thieno[2,3-c]quinolin-4-one	IC50	1.3 nM	US-8962648: Tricyclic compounds and PBK inhibitors containing the same
9-[4-(1-aminopropan-2-yl)phenyl]-8-hydroxy-5,5a,6,7,8,9,9a,9b-octahydro-3aH-thieno[2,3-c]quinolin-4-one	IC50	1.3 nM	US-8962648: Tricyclic compounds and PBK inhibitors containing the same
9-[4-[(1R)-1-aminopropyl]phenyl]-8-hydroxy-5,5a,6,7,8,9,9a,9b-octahydro-3aH-thieno[2,3-c]quinolin-4-one	IC50	1.3 nM	US-8962648: Tricyclic compounds and PBK inhibitors containing the same
8-hydroxy-9-[4-[(1S)-1-(methylamino)propyl]phenyl]-5,5a,6,7,8,9,9a,9b-octahydro-3aH-thieno[2,3-c]quinolin-4-one	IC50	1.3 nM	US-8962648: Tricyclic compounds and PBK inhibitors containing the same
9-[4-[(2S)-1-aminopropan-2-yl]phenyl]-8-hydroxy-5,5a,6,7,8,9,9a,9b-octahydro-3aH-thieno[2,3-c]quinolin-4-one	IC50	1.3 nM	US-8962648: Tricyclic compounds and PBK inhibitors containing the same
8-hydroxy-9-[4-[(2R)-1-(methylamino)propan-2-yl]phenyl]-5,5a,6,7,8,9,9a,9b-octahydro-3aH-thieno[2,3-c]quinolin-4-one	IC50	1.3 nM	US-8962648: Tricyclic compounds and PBK inhibitors containing the same
9-[4-[(1R)-1-(ethylamino)propyl]phenyl]-8-hydroxy-5,5a,6,7,8,9,9a,9b-octahydro-3aH-thieno[2,3-c]quinolin-4-one	IC50	1.4 nM	US-8962648: Tricyclic compounds and PBK inhibitors containing the same
9-[4-(1-amino-3-methylbutan-2-yl)phenyl]-8-hydroxy-5,5a,6,7,8,9,9a,9b-octahydro-3aH-thieno[2,3-c]quinolin-4-one	IC50	1.4 nM	US-8962648: Tricyclic compounds and PBK inhibitors containing the same
9-[4-(1-aminopropan-2-yl)-3-fluorophenyl]-8-hydroxy-5,5a,6,7,8,9,9a,9b-octahydro-3aH-thieno[2,3-c]quinolin-4-one	IC50	1.5 nM	US-8962648: Tricyclic compounds and PBK inhibitors containing the same
9-[4-[1-(dimethylamino)ethyl]phenyl]-8-hydroxy-5,5a,6,7,8,9,9a,9b-octahydro-3aH-thieno[2,3-c]quinolin-4-one	IC50	1.6 nM	US-8962648: Tricyclic compounds and PBK inhibitors containing the same
CHEMBL4452726	IC50	1.6 nM
9-[4-[1-(aminomethyl)cyclobutyl]phenyl]-8-hydroxy-5,5a,6,7,8,9,9a,9b-octahydro-3aH-thieno[2,3-c]quinolin-4-one	IC50	1.7 nM	US-8962648: Tricyclic compounds and PBK inhibitors containing the same
4-(8-hydroxy-4-oxo-5,5a,6,7,8,9,9a,9b-octahydro-3aH-thieno[2,3-c]quinolin-9-yl)benzenesulfonamide	IC50	1.8 nM	US-8962648: Tricyclic compounds and PBK inhibitors containing the same
9-[4-[3-(aminomethyl)pentan-3-yl]phenyl]-8-hydroxy-5,5a,6,7,8,9,9a,9b-octahydro-3aH-thieno[2,3-c]quinolin-4-one	IC50	1.8 nM	US-8962648: Tricyclic compounds and PBK inhibitors containing the same
9-[4-[2-(dimethylamino)ethyl]-3-fluorophenyl]-8-hydroxy-5,5a,6,7,8,9,9a,9b-octahydro-3aH-thieno[2,3-c]quinolin-4-one	IC50	1.9 nM	US-8962648: Tricyclic compounds and PBK inhibitors containing the same
9-[4-[1-(dimethylamino)propyl]phenyl]-8-hydroxy-5,5a,6,7,8,9,9a,9b-octahydro-3aH-thieno[2,3-c]quinolin-4-one	IC50	1.9 nM	US-8962648: Tricyclic compounds and PBK inhibitors containing the same
9-[4-[1-(aminomethyl)cyclopropyl]phenyl]-8-hydroxy-5,5a,6,7,8,9,9a,9b-octahydro-3aH-thieno[2,3-c]quinolin-4-one	IC50	1.9 nM	US-8962648: Tricyclic compounds and PBK inhibitors containing the same
9-[4-[1-(dimethylamino)ethyl]-3-fluorophenyl]-8-hydroxy-5,5a,6,7,8,9,9a,9b-octahydro-3aH-thieno[2,3-c]quinolin-4-one	IC50	1.9 nM	US-8962648: Tricyclic compounds and PBK inhibitors containing the same
N-[1-[4-(8-hydroxy-4-oxo-5,5a,6,7,8,9,9a,9b-octahydro-3aH-thieno[2,3-c]quinolin-9-yl)phenyl]ethyl]methanesulfonamide	IC50	2 nM	US-8962648: Tricyclic compounds and PBK inhibitors containing the same
9-[4-(ethylaminomethyl)phenyl]-8-hydroxy-5,5a,6,7,8,9,9a,9b-octahydro-3aH-thieno[2,3-c]quinolin-4-one	IC50	2 nM	US-8962648: Tricyclic compounds and PBK inhibitors containing the same
8-hydroxy-9-[4-(1-hydroxyethyl)phenyl]-5,5a,6,7,8,9,9a,9b-octahydro-3aH-thieno[2,3-c]quinolin-4-one	IC50	2 nM	US-8962648: Tricyclic compounds and PBK inhibitors containing the same
8-hydroxy-9-(1,2,3,4-tetrahydroisoquinolin-7-yl)-5,5a,6,7,8,9,9a,9b-octahydro-3aH-thieno[2,3-c]quinolin-4-one	IC50	2 nM	US-8962648: Tricyclic compounds and PBK inhibitors containing the same
9-[4-[(2R)-1-aminopropan-2-yl]phenyl]-8-methoxy-5,5a,6,7,8,9,9a,9b-octahydro-3aH-thieno[2,3-c]quinolin-4-one	IC50	2 nM	US-8962648: Tricyclic compounds and PBK inhibitors containing the same
9-[4-[(1S)-1-(dimethylamino)propyl]phenyl]-8-hydroxy-5,5a,6,7,8,9,9a,9b-octahydro-3aH-thieno[2,3-c]quinolin-4-one	IC50	2.2 nM	US-8962648: Tricyclic compounds and PBK inhibitors containing the same
9-(4-amino-3-hydroxyphenyl)-8-hydroxy-5,5a,6,7,8,9,9a,9b-octahydro-3aH-thieno[2,3-c]quinolin-4-one	IC50	2.3 nM	US-8962648: Tricyclic compounds and PBK inhibitors containing the same

ChEMBL bioactivities

270 potent at pChembl≥5 of 285 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).

pChembl	Type	Value	Unit	Molecule
9.30	IC50	0.5	nM	CHEMBL4445123
8.81	IC50	1.56	nM	CHEMBL4452726
8.59	IC50	2.6	nM	CHEMBL3672295
8.57	IC50	2.71	nM	CHEMBL4440222
8.53	IC50	2.94	nM	CHEMBL4527920
8.34	IC50	4.59	nM	CHEMBL4564624
8.28	IC50	5.2	nM	CHEMBL3715360
8.28	IC50	5.3	nM	CHEMBL3716544
8.26	IC50	5.44	nM	CHEMBL4536593
8.19	IC50	6.44	nM	CHEMBL4452595
8.00	Ki	10	nM	CHEMBL1974328
7.97	IC50	10.69	nM	CHEMBL4537262
7.72	IC50	19.06	nM	CHEMBL4469640
7.68	IC50	21	nM	CHEMBL4593398
7.68	IC50	20.88	nM	CHEMBL4455498
7.64	IC50	23	nM	CHEMBL3672271
7.62	IC50	24	nM	CHEMBL3715388
7.60	IC50	25.1	nM	CHEMBL4458265
7.58	IC50	26.13	nM	CHEMBL4438486
7.55	IC50	28	nM	CHEMBL3672369
7.48	IC50	33	nM	CHEMBL3716635
7.47	IC50	34	nM	CHEMBL3715121
7.47	IC50	34	nM	CHEMBL3718105
7.46	IC50	35	nM	CHEMBL3718439
7.44	IC50	36	nM	CHEMBL3715494
7.41	IC50	39	nM	CHEMBL3718039
7.35	IC50	44.89	nM	CHEMBL4451419
7.29	IC50	50.9	nM	STAUROSPORINE
7.26	IC50	55	nM	CHEMBL3718730
7.26	IC50	54.3	nM	STAUROSPORINE
7.23	IC50	59	nM	CHEMBL3717059
7.21	IC50	61.41	nM	CHEMBL4473141
7.20	IC50	63	nM	CHEMBL3717532
7.20	IC50	63	nM	CHEMBL3718268
7.20	IC50	63.83	nM	CHEMBL4444190
7.19	IC50	64.46	nM	CHEMBL4534841
7.19	IC50	65	nM	CHEMBL4534499
7.14	IC50	72	nM	CHEMBL3715032
7.13	IC50	74	nM	CHEMBL3715508
7.11	IC50	78	nM	CHEMBL3717297
7.08	IC50	83.9	nM	STAUROSPORINE
7.07	IC50	86	nM	CHEMBL3717841
7.01	IC50	98	nM	CHEMBL3718758
7.00	IC50	99	nM	CHEMBL3715825
6.96	IC50	110	nM	CHEMBL3719067
6.90	Ki	125.9	nM	CHEMBL1973098
6.85	IC50	140	nM	CHEMBL3717063
6.85	IC50	142.5	nM	CHEMBL4552688
6.84	IC50	143.9	nM	CHEMBL4455728
6.82	IC50	150	nM	CHEMBL3718368

PubChem BioAssay actives

48 with measured affinity, of 891 total; 44 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
1-[4-[(2R)-1-aminopropan-2-yl]phenyl]-2-hydroxy-4-methyl-5H-phenanthridin-6-one	1585718: Inhibition of human TOPK using MBP as substrate after 2 hrs in presence of [gamma-33P]-ATP by filter-binding method	ic50	0.0005	uM
1-[4-[(1R)-1-aminoethyl]phenyl]-2-hydroxy-4,9-dimethyl-5H-phenanthridin-6-one	1585718: Inhibition of human TOPK using MBP as substrate after 2 hrs in presence of [gamma-33P]-ATP by filter-binding method	ic50	0.0016	uM
9-[4-[(2R)-1-aminopropan-2-yl]phenyl]-8-hydroxy-6-methyl-5H-thieno[2,3-c]quinolin-4-one	1415292: Inhibition of full length N-terminal GST-fused human PBK expressed in baculovirus expression system using FITC-labeled histone H3 peptide as substrate after 1 hr by IMAP method	ic50	0.0026	uM
1-[4-[(1R)-1-aminoethyl]phenyl]-4-chloro-2-hydroxy-5H-phenanthridin-6-one	1585718: Inhibition of human TOPK using MBP as substrate after 2 hrs in presence of [gamma-33P]-ATP by filter-binding method	ic50	0.0027	uM
1-[4-[(1R)-1-aminoethyl]phenyl]-2-hydroxy-4-methyl-5H-phenanthridin-6-one	1585718: Inhibition of human TOPK using MBP as substrate after 2 hrs in presence of [gamma-33P]-ATP by filter-binding method	ic50	0.0029	uM
1-[4-[(2R)-1-aminopropan-2-yl]phenyl]-4-chloro-2-hydroxy-5H-phenanthridin-6-one	1585718: Inhibition of human TOPK using MBP as substrate after 2 hrs in presence of [gamma-33P]-ATP by filter-binding method	ic50	0.0046	uM
1-[4-[(2R)-1-aminopropan-2-yl]phenyl]-2-methoxy-4-methyl-5H-phenanthridin-6-one	1585718: Inhibition of human TOPK using MBP as substrate after 2 hrs in presence of [gamma-33P]-ATP by filter-binding method	ic50	0.0054	uM
1-[4-[(2R)-1-aminopropan-2-yl]phenyl]-2-hydroxy-4,9-dimethyl-5H-phenanthridin-6-one	1585718: Inhibition of human TOPK using MBP as substrate after 2 hrs in presence of [gamma-33P]-ATP by filter-binding method	ic50	0.0064	uM
9-[4-[(2R)-1-aminopropan-2-yl]phenyl]-8-hydroxy-6-methyl-5H-thieno[2,3-c]quinolin-4-one;hydrochloride	1585718: Inhibition of human TOPK using MBP as substrate after 2 hrs in presence of [gamma-33P]-ATP by filter-binding method	ic50	0.0107	uM
1-[4-[(2R)-1-(dimethylamino)propan-2-yl]phenyl]-2-hydroxy-4,9-dimethyl-5H-phenanthridin-6-one	1585718: Inhibition of human TOPK using MBP as substrate after 2 hrs in presence of [gamma-33P]-ATP by filter-binding method	ic50	0.0191	uM
1-[4-[(1R)-1-(dimethylamino)ethyl]phenyl]-2-hydroxy-4,9-dimethyl-5H-phenanthridin-6-one	1585718: Inhibition of human TOPK using MBP as substrate after 2 hrs in presence of [gamma-33P]-ATP by filter-binding method	ic50	0.0209	uM
7-[5-(trifluoromethyl)-1H-pyrazol-4-yl]-8,9,10,11-tetrahydro-3H-pyrazolo[4,5-a]phenanthridine	1562833: Inhibition of TOPK (unknown origin) using MBP as substrate after 3 hrs by ADP-Glo assay	ic50	0.0210	uM
9-[4-[(1R)-1-aminoethyl]phenyl]-8-hydroxy-6-methyl-5H-thieno[2,3-c]quinolin-4-one	1585718: Inhibition of human TOPK using MBP as substrate after 2 hrs in presence of [gamma-33P]-ATP by filter-binding method	ic50	0.0230	uM
1-[4-[1-(aminomethyl)cyclopropyl]phenyl]-2-hydroxy-4-methyl-5H-phenanthridin-6-one	1585718: Inhibition of human TOPK using MBP as substrate after 2 hrs in presence of [gamma-33P]-ATP by filter-binding method	ic50	0.0251	uM
4-chloro-1-[4-[(1R)-1-(dimethylamino)ethyl]phenyl]-2-hydroxy-5H-phenanthridin-6-one	1585718: Inhibition of human TOPK using MBP as substrate after 2 hrs in presence of [gamma-33P]-ATP by filter-binding method	ic50	0.0261	uM
9-[4-[(2R)-1-(dimethylamino)propan-2-yl]phenyl]-8-hydroxy-6-methyl-5H-thieno[2,3-c]quinolin-4-one	1415292: Inhibition of full length N-terminal GST-fused human PBK expressed in baculovirus expression system using FITC-labeled histone H3 peptide as substrate after 1 hr by IMAP method	ic50	0.0280	uM
1-[4-[(1R)-1-(dimethylamino)ethyl]phenyl]-2-hydroxy-4-methyl-5H-phenanthridin-6-one	1585718: Inhibition of human TOPK using MBP as substrate after 2 hrs in presence of [gamma-33P]-ATP by filter-binding method	ic50	0.0449	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	2198361: Inhibition of human PBK using myelin basic protein as substrate preincubated for 20 mins followed by [gamma-33P]-ATP addition and measured after 120 mins by radiometric Hot-SpotSM Kinase assay	ic50	0.0509	uM
1-[4-[(1R)-1-aminoethyl]phenyl]-7-fluoro-2-hydroxy-4-methyl-5H-phenanthridin-6-one	1585718: Inhibition of human TOPK using MBP as substrate after 2 hrs in presence of [gamma-33P]-ATP by filter-binding method	ic50	0.0614	uM
1-[4-[(2R)-1-(dimethylamino)propan-2-yl]phenyl]-2-hydroxy-4-methyl-5H-phenanthridin-6-one	1585718: Inhibition of human TOPK using MBP as substrate after 2 hrs in presence of [gamma-33P]-ATP by filter-binding method	ic50	0.0638	uM
1-[4-[(2R)-1-aminopropan-2-yl]phenyl]-7-fluoro-2-hydroxy-4-methyl-5H-phenanthridin-6-one	1585718: Inhibition of human TOPK using MBP as substrate after 2 hrs in presence of [gamma-33P]-ATP by filter-binding method	ic50	0.0645	uM
4-chloro-1-[4-[(2R)-1-(dimethylamino)propan-2-yl]phenyl]-2-hydroxy-5H-phenanthridin-6-one	1585718: Inhibition of human TOPK using MBP as substrate after 2 hrs in presence of [gamma-33P]-ATP by filter-binding method	ic50	0.0650	uM
1-[4-[(1R)-1-aminoethyl]phenyl]-2-methoxy-4-methyl-5H-phenanthridin-6-one	1585718: Inhibition of human TOPK using MBP as substrate after 2 hrs in presence of [gamma-33P]-ATP by filter-binding method	ic50	0.1425	uM
1-[4-[1-[(dimethylamino)methyl]cyclopropyl]phenyl]-2-hydroxy-4-methyl-5H-phenanthridin-6-one	1585718: Inhibition of human TOPK using MBP as substrate after 2 hrs in presence of [gamma-33P]-ATP by filter-binding method	ic50	0.1439	uM
1-[4-[(2R)-1-aminopropan-2-yl]phenyl]-2-hydroxy-4,8-dimethyl-5H-phenanthridin-6-one	1585718: Inhibition of human TOPK using MBP as substrate after 2 hrs in presence of [gamma-33P]-ATP by filter-binding method	ic50	0.2237	uM
6,9-dichloro-3H-[1]benzothiolo[3,2-d]pyrimidin-4-one	437693: Inhibition of PBK by HTRF assay	ki	0.3161	uM
1-[4-[(2R)-1-aminopropan-2-yl]phenyl]-4-chloro-2,7-dihydroxy-5H-phenanthridin-6-one	1585718: Inhibition of human TOPK using MBP as substrate after 2 hrs in presence of [gamma-33P]-ATP by filter-binding method	ic50	0.3213	uM
1-[4-[(2R)-1-aminopropan-2-yl]phenyl]-2,7-dihydroxy-4-methyl-5H-phenanthridin-6-one	1585718: Inhibition of human TOPK using MBP as substrate after 2 hrs in presence of [gamma-33P]-ATP by filter-binding method	ic50	0.3357	uM
4-methyl-3-[(2-methyl-6-pyridin-3-ylpyrazolo[3,4-d]pyrimidin-4-yl)amino]-N-[3-(trifluoromethyl)phenyl]benzamide	2148941: Binding affinity to human PBK incubated for 45 mins by Kinobead based pull down assay	kd	0.3630	uM
1-[4-[(2R)-1-aminopropan-2-yl]phenyl]-2-hydroxy-4,7-dimethyl-5H-phenanthridin-6-one	1585718: Inhibition of human TOPK using MBP as substrate after 2 hrs in presence of [gamma-33P]-ATP by filter-binding method	ic50	0.5861	uM
1-[4-[(1R)-1-aminoethyl]phenyl]-4-chloro-2,7-dihydroxy-5H-phenanthridin-6-one	1585718: Inhibition of human TOPK using MBP as substrate after 2 hrs in presence of [gamma-33P]-ATP by filter-binding method	ic50	0.6429	uM
1-[4-[(1R)-1-aminoethyl]phenyl]-2-hydroxy-4,7-dimethyl-5H-phenanthridin-6-one	1585718: Inhibition of human TOPK using MBP as substrate after 2 hrs in presence of [gamma-33P]-ATP by filter-binding method	ic50	0.7214	uM
1-[4-[(1R)-1-aminoethyl]phenyl]-2-hydroxy-4,8-dimethyl-5H-phenanthridin-6-one	1585718: Inhibition of human TOPK using MBP as substrate after 2 hrs in presence of [gamma-33P]-ATP by filter-binding method	ic50	0.8943	uM
1-[4-[(1R)-1-aminoethyl]phenyl]-2,7-dihydroxy-4-methyl-5H-phenanthridin-6-one	1585718: Inhibition of human TOPK using MBP as substrate after 2 hrs in presence of [gamma-33P]-ATP by filter-binding method	ic50	0.9775	uM
1-[4-[1-(aminomethyl)cyclopropyl]phenyl]-4-chloro-2,7-dihydroxy-5H-phenanthridin-6-one	1585718: Inhibition of human TOPK using MBP as substrate after 2 hrs in presence of [gamma-33P]-ATP by filter-binding method	ic50	1.2660	uM
1-[4-[1-(aminomethyl)cyclopropyl]phenyl]-2,7-dihydroxy-4-methyl-5H-phenanthridin-6-one	1585718: Inhibition of human TOPK using MBP as substrate after 2 hrs in presence of [gamma-33P]-ATP by filter-binding method	ic50	1.5050	uM
4-chloro-1-[4-[(1R)-1-(dimethylamino)ethyl]phenyl]-2,7-dihydroxy-5H-phenanthridin-6-one	1585718: Inhibition of human TOPK using MBP as substrate after 2 hrs in presence of [gamma-33P]-ATP by filter-binding method	ic50	2.4400	uM
4-chloro-1-[4-[(2R)-1-(dimethylamino)propan-2-yl]phenyl]-2,7-dihydroxy-5H-phenanthridin-6-one	1585718: Inhibition of human TOPK using MBP as substrate after 2 hrs in presence of [gamma-33P]-ATP by filter-binding method	ic50	2.6630	uM
1-[4-[(1R)-1-(dimethylamino)ethyl]phenyl]-2-hydroxy-4,7-dimethyl-5H-phenanthridin-6-one	1585718: Inhibition of human TOPK using MBP as substrate after 2 hrs in presence of [gamma-33P]-ATP by filter-binding method	ic50	3.0130	uM
1-[4-[(1R)-1-(dimethylamino)ethyl]phenyl]-2,7-dihydroxy-4-methyl-5H-phenanthridin-6-one	1585718: Inhibition of human TOPK using MBP as substrate after 2 hrs in presence of [gamma-33P]-ATP by filter-binding method	ic50	4.7900	uM
7-chloro-3-oxo-8-(1,3-thiazol-5-ylmethylamino)-11,16-dioxa-2,4,19,21-tetrazatricyclo[15.3.1.05,10]henicosa-1(20),5,7,9,17(21),18-hexaene-18-carbonitrile	310379: Inhibition of PBK	ki	5.1950	uM
4-chloro-1-[4-[1-[(dimethylamino)methyl]cyclopropyl]phenyl]-2,7-dihydroxy-5H-phenanthridin-6-one	1585718: Inhibition of human TOPK using MBP as substrate after 2 hrs in presence of [gamma-33P]-ATP by filter-binding method	ic50	5.2380	uM
1-[4-[(1R)-1-(dimethylamino)ethyl]phenyl]-2-hydroxy-4,8-dimethyl-5H-phenanthridin-6-one	1585718: Inhibition of human TOPK using MBP as substrate after 2 hrs in presence of [gamma-33P]-ATP by filter-binding method	ic50	6.4150	uM
1-[4-[(2R)-1-(dimethylamino)propan-2-yl]phenyl]-2-hydroxy-4,8-dimethyl-5H-phenanthridin-6-one	1585718: Inhibition of human TOPK using MBP as substrate after 2 hrs in presence of [gamma-33P]-ATP by filter-binding method	ic50	7.0550	uM

CTD chemical–gene interactions

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

Chemical	Actions (top 5)	PubMed papers
sodium arsenite	affects cotreatment, decreases expression, affects binding, increases reaction, increases expression	5
bisphenol A	decreases expression, increases expression, affects expression	4
Benzo(a)pyrene	decreases expression, increases methylation	4
Estradiol	increases expression, decreases expression	4
Valproic Acid	affects cotreatment, increases expression, affects expression	4
Resveratrol	affects cotreatment, increases expression, decreases expression	3
Cyclosporine	decreases expression	3
Cadmium Chloride	decreases expression, decreases reaction, increases abundance, increases palmitoylation	3
(+)-JQ1 compound	decreases expression	2
Cadmium	decreases reaction, increases abundance, increases palmitoylation, increases expression	2
Cisplatin	decreases expression, increases reaction, increases expression	2
Lipopolysaccharides	affects cotreatment, decreases expression, affects expression, affects reaction	2
Nickel	increases expression	2
Progesterone	decreases expression, increases expression	2
Tretinoin	affects cotreatment, decreases expression	2
Aflatoxin B1	affects expression, decreases methylation	2
Genistein	affects expression, increases expression	2
aristolochic acid I	decreases expression	1
afuresertib	decreases expression	1
FR900359	decreases phosphorylation	1
dicrotophos	decreases expression	1
propionaldehyde	decreases expression	1
kojic acid	decreases expression	1
trichostatin A	increases expression	1
methylparaben	decreases expression	1
tris(1,3-dichloro-2-propyl)phosphate	decreases expression	1
cobaltous chloride	decreases expression	1
2-bromopalmitate	decreases reaction, increases abundance, increases palmitoylation	1
perfluorooctanoic acid	decreases expression	1
2,3-bis(3’-hydroxybenzyl)butyrolactone	affects cotreatment, increases expression	1

ChEMBL screening assays

90 unique, capped per target: 89 binding, 1 functional

Representative assays (with source publication via chembl_document):

Assay ID	Type	Description	Source paper
CHEMBL1041173	Binding	Residual activity of PBK at 1 uM by microplate scintillation counting	Substituted 2-arylbenzothiazoles as kinase inhibitors: hit-to-lead optimization. — *Bioorg Med Chem*
CHEMBL1964100	Functional	PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member name: TOPK	PubChem BioAssay data set

Cellosaurus cell lines

9 cell lines: 8 cancer cell line, 1 transformed cell line

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

Cellosaurus	Name	Category	Sex
CVCL_B3DH	Abcam HEK293T PBK KO	Transformed cell line	Female
CVCL_B8M5	Abcam HCT 116 PBK KO	Cancer cell line	Male
CVCL_B9PC	Abcam A-549 PBK KO	Cancer cell line	Male
CVCL_E1DU	Ubigene U2OS PBK KO	Cancer cell line	Female
CVCL_TC34	HAP1 PBK (-) 1	Cancer cell line	Male
CVCL_TC35	HAP1 PBK (-) 2	Cancer cell line	Male
CVCL_XR40	HAP1 PBK (-) 3	Cancer cell line	Male
CVCL_XR41	HAP1 PBK (-) 4	Cancer cell line	Male
CVCL_XR42	HAP1 PBK (-) 5	Cancer cell line	Male

Clinical trials (associated diseases)

Via MONDO — disease-level, not drug-specific.

Predicted chemistry — Sugi Predict

The predicted patent-compound landscape for PBK across ~30M SureChEMBL compounds — explore on Sugi Predict.