PIM2

Summary

PIM2 (Pim-2 proto-oncogene, serine/threonine kinase, HGNC:8987) is a protein-coding gene on chromosome Xp11.23, encoding Serine/threonine-protein kinase pim-2 (Q9P1W9). Proto-oncogene with serine/threonine kinase activity involved in cell survival and cell proliferation.

This gene encodes a protooncogene that acts as a serine/threonine protein kinase. Studies determined the encoded protein functions to prevent apoptosis and to promote cell survival.

Source: NCBI Gene 11040 — RefSeq curated summary.

At a glance

• Clinical variants (ClinVar): 60 total
• Druggable target: yes — 17 molecules with ChEMBL bioactivity
• MANE Select transcript: NM_006875

Identifiers

Gene identifiers

Field	Value
HGNC ID	HGNC:8987
Approved symbol	PIM2
Name	Pim-2 proto-oncogene, serine/threonine kinase
Location	Xp11.23
Locus type	gene with protein product
Status	Approved
Ensembl gene	ENSG00000102096
Ensembl biotype	protein_coding
OMIM	300295
Entrez	11040

Gene structure

Transcript identifiers

Ensembl transcripts: 4 — 2 protein_coding, 2 retained_intron

ENST00000376509, ENST00000442430, ENST00000485431, ENST00000710360

RefSeq mRNA: 1 — MANE Select: NM_006875 NM_006875

CCDS: CCDS14312

Canonical transcript exons

ENST00000376509 — 6 exons

Exon	Start	End
ENSE00000670819	48918536	48918645
ENSE00000670821	48917781	48917831
ENSE00000670823	48915020	48915392
ENSE00000670825	48914395	48914571
ENSE00001470750	48913182	48914294
ENSE00001470752	48918774	48919024

Expression profiles

Bgee: expression breadth ubiquitous, 197 present calls, max score 96.95.

FANTOM5 (CAGE): breadth ubiquitous, TPM avg 54.1533 / max 1694.2406, expressed in 1714 samples.

FANTOM5 promoters (2 alternative TSS)

Promoter ID	TPM avg	Samples expressed
199201	53.5614	1712
199199	0.5919	264

Top tissues by expression

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

Tissue	Anatomy ID	Expression score	Quality
granulocyte	CL:0000094	96.95	gold quality
spleen	UBERON:0002106	95.67	gold quality
rectum	UBERON:0001052	95.42	gold quality
vermiform appendix	UBERON:0001154	93.97	gold quality
lymph node	UBERON:0000029	93.89	gold quality
blood	UBERON:0000178	93.74	gold quality
colonic epithelium	UBERON:0000397	93.44	gold quality
bone marrow cell	CL:0002092	89.67	gold quality
small intestine Peyer’s patch	UBERON:0003454	89.51	gold quality
mucosa of transverse colon	UBERON:0004991	88.90	gold quality
minor salivary gland	UBERON:0001830	88.86	gold quality
caecum	UBERON:0001153	88.20	gold quality
transverse colon	UBERON:0001157	87.87	gold quality
small intestine	UBERON:0002108	87.43	gold quality
gall bladder	UBERON:0002110	87.03	gold quality
primordial germ cell in gonad	CL:0000670 ∩ UBERON:0000991	86.95	gold quality
saliva-secreting gland	UBERON:0001044	86.10	gold quality
upper lobe of left lung	UBERON:0008952	86.08	gold quality
right uterine tube	UBERON:0001302	85.08	gold quality
olfactory segment of nasal mucosa	UBERON:0005386	85.08	gold quality
bone marrow	UBERON:0002371	84.44	gold quality
upper lobe of lung	UBERON:0008948	84.21	gold quality
leukocyte	CL:0000738	83.60	gold quality
body of stomach	UBERON:0001161	83.50	gold quality
mouth mucosa	UBERON:0003729	83.33	gold quality
right lung	UBERON:0002167	83.15	gold quality
right hemisphere of cerebellum	UBERON:0014890	82.63	gold quality
cerebellar hemisphere	UBERON:0002245	82.54	gold quality
cerebellar cortex	UBERON:0002129	82.43	gold quality
mononuclear cell	CL:0000842	82.34	gold quality

Single-cell (SCXA)

Detected in 17 experiment(s), a significant marker in 12.

Experiment	Marker?	Max mean expression
E-CURD-88	yes	82.67
E-HCAD-1	yes	60.97
E-CURD-122	yes	50.43
E-MTAB-8410	yes	45.98
E-MTAB-9467	yes	45.13
E-CURD-46	yes	33.56
E-HCAD-11	yes	27.67
E-HCAD-9	yes	22.98
E-MTAB-8142	yes	21.93
E-MTAB-10553	yes	12.23
E-MTAB-9388	yes	8.17
E-CURD-97	no	1811.30
E-HCAD-8	no	45.30
E-CURD-120	no	30.57
E-CURD-112	no	3.56

Regulation

Is transcription factor: no

Upstream regulators (CollecTRI, top): BRD4, E2F4, FLT3, FOXN3, FOXP3, JMJD6, PAX5, STAT5A

miRNA regulators (miRDB)

95 targeting PIM2, 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-4673	100.00	66.64	1490
HSA-MIR-200B-3P	100.00	73.31	2693
HSA-MIR-200C-3P	100.00	73.35	2685
HSA-MIR-429	100.00	73.44	2698
HSA-MIR-5692A	100.00	74.40	6850
HSA-MIR-3667-3P	99.99	67.17	1636
HSA-MIR-548P	99.98	72.25	3784
HSA-MIR-4645-5P	99.98	65.81	1284
HSA-MIR-3692-3P	99.98	70.27	2139
HSA-MIR-1229-3P	99.97	66.49	906
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-1468-3P	99.96	72.74	3797
HSA-MIR-3912-5P	99.95	66.11	925
HSA-MIR-6835-3P	99.93	70.49	2904
HSA-MIR-6721-5P	99.93	68.92	2981
HSA-MIR-3119	99.92	71.34	2390
HSA-MIR-498-3P	99.91	71.27	1114
HSA-MIR-3121-3P	99.82	71.96	3630
HSA-MIR-548AJ-5P	99.78	71.12	3085
HSA-MIR-548F-5P	99.78	71.02	3093
HSA-MIR-548G-5P	99.78	71.12	3085
HSA-MIR-548X-5P	99.78	71.12	3085
HSA-MIR-4699-3P	99.71	70.15	3142
HSA-MIR-6887-3P	99.66	67.83	1778
HSA-MIR-1827	99.63	68.57	3265
HSA-MIR-4516	99.61	67.78	3390
HSA-MIR-24-3P	99.59	69.97	1934
HSA-MIR-7106-5P	99.53	67.47	3574

Literature-anchored findings (GeneRIF, showing 40)

• pim-2 functions similarly to pim-1 as a pro-survival kinase; BAD is a legitimate PIM-2 substrate (PMID:12954615)
• hPim-2 mRNA expression in NHL was 1.5 to 2.6 times higher in involved splenic foci compared to nearby uninvolved regions. hPim-2 mRNA was increased 3-folds in B-CLL over normal B-cells (PMID:15291354)
• transcriptional induction of Pim-2 initiates a novel NF-kappaB activation pathway that regulates cell survival (PMID:15548703)
• EBV-induced upregulation of Pim kinases and Pim-stimulated EBNA2 transcriptional activity may contribute to the ability of EBV to immortalize B-cells and predispose them to malignant growth. (PMID:15721354)
• Up-regulation of Pim-2 is associated with disease progression and perineural invasion in prostate cancer. (PMID:16015593)
• All three Pim kinase family members predominantly phosphorylate Bad on Ser112 and in addition are capable of phosphorylating Bad on multiple sites associated with the inhibition of the pro-apoptotic function of Bad in HEK-293 cells (PMID:16403219)
• expression of the Myc and Pim proto-oncogenes by Jak2V617F was found to be FERM domain dependent. (PMID:18216297)
• Foxp3 can regulate pim 2 expression. (PMID:18424697)
• Pim kinases promote cell cycle progression and tumorigenesis by down-regulating p27(Kip1) expression at both transcriptional and posttranslational levels. (PMID:18593906)
• pim-2 acts as a pro-survival kinase to inhibit apoptosis and keep liver cell survival in IL-3-deprived medium. Pim-2 might participate in the tumorigenesis of hepatocellular carcinoma induction through its downstream molecules 4E-BP1 and Bad. (PMID:18675992)
• we infer that Pim-2 could activate API-5 to inhibit the apoptosis of liver cells, and NF-kappaB is the key regulator (PMID:19821157)
• structural analysis of the PIM2 kinase in complex with an organoruthenium inhibitor (PMID:19841674)
• PIM2 controls the expression of the pro-inflammatory cytokine IL-6. (PMID:20465571)
• Data show that Pim-2 can induce malignant transformation of human liver cell line L02. (PMID:20592892)
• A cell-based test system useful for rapid and inexpensive pre-screening of compounds capable of preventing Pim-mediated phosphorylation is discussed. (PMID:20939820)
• Pax-5 may act as a transcription factor to modulate the expression of Pim-2 in B-cells (PMID:21299464)
• IL-6 and TNF family cytokines upregulate Pim-2 in bone marrow stromal cells and osteoclasts in multiple myeloma. This appears to be a novel anti-apoptotic mechanism for MM cell survival. (PMID:21475253)
• Targeting cap-dependent translation blocks converging survival signals by AKT and PIM 1, 2 kinases in lymphoma (PMID:21859846)
• While PIM-2 can function as a potent survival factor, it can, under certain circumstances, exhibit pro-apoptotic effects as well. (PMID:22506047)
• PIM kinases promote the production of IFNgamma, the hallmark cytokine produced by Th1 cells. (PMID:23209281)
• our results identify eIF4B as a critical substrate of Pim kinases in mediating the activity of Abl oncogenes (PMID:23749639)
• Our data indicate that PIM-2 and NF-kappaB gene expression is increased in patients with acute myeloid leukemia and acute lymphoblastic leukemia. High PIM-2 expression is associated with complete remission rate in AML patients. (PMID:23752607)
• Data indicate that PIM-2 is an upstream activator of E2F-1 and ATM in the ultraviolet damage response. (PMID:23760264)
• Overexpression of pim-2 may inhibit the apoptosis of prostate cancer cells through phosphorylation of eIF4B, thus promoting tumorigenesis. (PMID:23813671)
• Pim2 directly phosphorylates TSC2 on Ser-1798 and relieves the suppression of TSC2 on mTOR-C1, leading to multiple myeloma cells proliferation. (PMID:23818547)
• PIM2 could directly phosphorylate PKM2 on the Thr-454 residue, resulting in an increase of PKM2 protein levels. Compared with wild type, PKM2 with the phosphorylation-defective mutation displayed a reduced effect on glycolysis. (PMID:24142698)
• HIF-1A induced PIM2 expression in HepG2 cells via binding to the hypoxia-responsive elements (HREs) of the PIM2 promoter. (PMID:24505470)
• Blocking the activities of PIM kinases(PIM1, PIM2 and PIM3) could prevent pancreatic cancer development. PIM kinases(PIM1, PIM2 and PIM3) may be a novel target for cancer therapy (PMID:24799066)
• Data demonstrate the role of PIM kinases in driving myeloid leukemia, and as candidate molecules for therapy against human malignancies. (PMID:25238262)
• Persistent activation of STAT3 by PIM2-driven positive feedback loop for epithelial-mesenchymal transition in breast cancer. (PMID:25854938)
• our findings will help to uncover novel signaling pathways between inflammations and oxidative stress in rheumatoid arthritis development and imply that Pim-2/mTORC1 pathway may be critical for the initiation of inflammatory reactions. (PMID:26064888)
• Our findings suggest that Pim-2-mediated aerobic glycolysis is critical for monitoring Warburg effect in colorectal tumor cells, highlighting Pim-2 as a potential metabolic target for colorectal tumor therapy. (PMID:26078709)
• We show that Pim2 inhibitors and proteasome inhibitors, such as bortezomib, have additive effects to inhibit the growth of myeloma cells, suggesting that Pim2 could be an interesting target for the treatment of multiple myeloma. (PMID:26500282)
• A high percentage of urothelial carcinomas express Pim kinases. Pim expression differs in NILG, NIHG, and IHG lesions. (PMID:26551340)
• PIM2 gene knockdown enhances the anti-proliferative effect of AZD1208 in non-Hodgkin lymphoma cell line. (PMID:26643319)
• the elevated expression of PIM2 in blastic cells is associated with poor prognosis of AML patients and their resistance to induction therapy. (PMID:26764044)
• show that PIM1 contributes to melanoma cell proliferation and tumor growth in vivo; however, the presence of PIM2 and PIM3 could also influence the outcome. (PMID:27448973)
• Our data provide evidence for a novel role for Pim2 in the regulation of the DNA damage response (DDR). Knockdown of Pim2 upregulates several downstream DDR markers, mimicking the effects of doxorubicin (Dox) treatment of MM cells, and suggesting a role for the kinase as a negative regulator of this pathway. (PMID:27564460)
• data suggest that PIM1/2 kinase overexpression is a common feature of male reproductive organs tumors, which provoke tissue alterations and a large inflammatory response that may act synergistically during the process of tumorigenesis. (PMID:27901106)
• PIM kinases in classical Hodgkin lymphoma exhibit pleiotropic effects, orchestrating tumor immune escape and supporting Reed-Sternberg cell survival. (PMID:28698206)

Cross-species orthologs

2 orthologs

Organism	Symbol	Gene ID
mus_musculus	Pim2	ENSMUSG00000031155
rattus_norvegicus	Pim2	ENSRNOG00000008177

Paralogs (2): PIM1 (ENSG00000137193), PIM3 (ENSG00000198355)

Protein

Protein identifiers

Serine/threonine-protein kinase pim-2 — Q9P1W9 (reviewed: Q9P1W9)

Alternative names: Pim-2h

All UniProt accessions (2): Q9P1W9, A0AA34QVH7

UniProt curated annotations — full annotation on UniProt →

Function. Proto-oncogene with serine/threonine kinase activity involved in cell survival and cell proliferation. Exerts its oncogenic activity through: the regulation of MYC transcriptional activity, the regulation of cell cycle progression, the regulation of cap-dependent protein translation and through survival signaling by phosphorylation of a pro-apoptotic protein, BAD. Phosphorylation of MYC leads to an increase of MYC protein stability and thereby an increase transcriptional activity. The stabilization of MYC exerted by PIM2 might explain partly the strong synergism between these 2 oncogenes in tumorigenesis. Regulates cap-dependent protein translation in a mammalian target of rapamycin complex 1 (mTORC1)-independent manner and in parallel to the PI3K-Akt pathway. Mediates survival signaling through phosphorylation of BAD, which induces release of the anti-apoptotic protein Bcl-X(L)/BCL2L1. Promotes cell survival in response to a variety of proliferative signals via positive regulation of the I-kappa-B kinase/NF-kappa-B cascade; this process requires phosphorylation of MAP3K8/COT. Promotes growth factor-independent proliferation by phosphorylation of cell cycle factors such as CDKN1A and CDKN1B. Involved in the positive regulation of chondrocyte survival and autophagy in the epiphyseal growth plate.

Subunit / interactions. Interacts with MYC.

Tissue specificity. Highly expressed in hematopoietic tissues, in leukemic and lymphoma cell lines, testis, small intestine, colon and colorectal adenocarcinoma cells. Weakly expressed in normal liver, but highly expressed in hepatocellular carcinoma tissues.

Post-translational modifications. Autophosphorylated.

Induction. Down-regulated in response to enterovirus 71 (EV71) infection.

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

RefSeq proteins (1): NP_006866* (*=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
IPR017348	PIM1/2/3	Family
IPR017441	Protein_kinase_ATP_BS	Binding_site
IPR051138	PIM_Ser/Thr_kinase	Family

Pfam: PF00069

Catalyzed reactions (Rhea), 2 shown:

• L-seryl-[protein] + ATP = O-phospho-L-seryl-[protein] + ADP + H(+) (RHEA:17989)
• L-threonyl-[protein] + ATP = O-phospho-L-threonyl-[protein] + ADP + H(+) (RHEA:46608)

UniProt features (36 total): helix 14, strand 9, turn 3, binding site 2, sequence variant 2, chain 1, domain 1, region of interest 1, compositionally biased region 1, active site 1, sequence conflict 1

Structure

Experimental structures (PDB)

2 structures.

PDB	Method	Resolution (Å)
4X7Q	X-RAY DIFFRACTION	2.33
2IWI	X-RAY DIFFRACTION	2.8

Predicted structure (AlphaFold)

Model	pLDDT	Fraction very-high
AF-Q9P1W9-F1	90.38	0.83

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): 163 (proton acceptor)

Ligand- & substrate-binding residues (2): 38–46; 61

Function

Pathways and Gene Ontology

Reactome pathways

0 pathways

MSigDB gene sets: 378 (showing top): RNGTGGGC_UNKNOWN, GOBP_REGULATION_OF_AUTOPHAGY, WALLACE_PROSTATE_CANCER_RACE_UP, MCLACHLAN_DENTAL_CARIES_UP, TGCGCANK_UNKNOWN, BROWNE_HCMV_INFECTION_8HR_UP, GCANCTGNY_MYOD_Q6, MODULE_45, AREB6_03, AAGCCAT_MIR135A_MIR135B, GOBP_CANONICAL_NF_KAPPAB_SIGNAL_TRANSDUCTION, GOBP_CELL_CYCLE_PHASE_TRANSITION, DACOSTA_UV_RESPONSE_VIA_ERCC3_UP, BROWNE_HCMV_INFECTION_12HR_UP, GGGTGGRR_PAX4_03

GO Biological Process (14): G1/S transition of mitotic cell cycle (GO:0000082), protein phosphorylation (GO:0006468), regulation of mitotic cell cycle (GO:0007346), negative regulation of cell population proliferation (GO:0008285), apoptotic mitochondrial changes (GO:0008637), response to virus (GO:0009615), positive regulation of autophagy (GO:0010508), macroautophagy (GO:0016236), positive regulation of macroautophagy (GO:0016239), negative regulation of apoptotic process (GO:0043066), positive regulation of canonical NF-kappaB signal transduction (GO:0043123), positive regulation of DNA-templated transcription (GO:0045893), protein stabilization (GO:0050821), apoptotic process (GO:0006915)

GO Molecular Function (8): protein serine/threonine kinase activity (GO:0004674), ATP binding (GO:0005524), protein serine kinase activity (GO:0106310), nucleotide binding (GO:0000166), protein kinase activity (GO:0004672), protein binding (GO:0005515), kinase activity (GO:0016301), transferase activity (GO:0016740)

GO Cellular Component (1): cytoplasm (GO:0005737)

GO top-level categories

Rollup of top GO terms by namespace:

Category	Terms
mitotic cell cycle	2
apoptotic process	2
autophagy	2
protein kinase activity	2
mitotic cell cycle phase transition	1
cell cycle G1/S phase transition	1
phosphorylation	1
protein modification process	1
regulation of cell cycle	1
cell population proliferation	1
regulation of cell population proliferation	1
negative regulation of cellular process	1
mitochondrion organization	1
response to other organism	1
positive regulation of catabolic process	1
regulation of autophagy	1
autophagosome assembly	1
positive regulation of autophagy	1
macroautophagy	1
regulation of macroautophagy	1
regulation of apoptotic process	1
negative regulation of programmed cell death	1
canonical NF-kappaB signal transduction	1
regulation of canonical NF-kappaB signal transduction	1
positive regulation of intracellular signal transduction	1
DNA-templated transcription	1
regulation of DNA-templated transcription	1
positive regulation of RNA biosynthetic process	1
regulation of protein stability	1
programmed cell death	1
apoptotic signaling pathway	1
execution phase of apoptosis	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

Protein interactions and networks

STRING

1965 interactions, top by confidence (×1000):

Protein A	Protein B	Partner UniProt	Score
PIM2	ZNF830	Q96NB3	646
PIM2	PPP4R1	Q8TF05	646
PIM2	CRNKL1	Q9BZJ0	636
PIM2	PRCC	Q92733	624
PIM2	KANSL2	Q9H9L4	616
PIM2	IL2	P01585	606
PIM2	FOXP3	Q9BZS1	559
PIM2	EIF4EBP1	Q13541	505
PIM2	DAD1	P46966	490
PIM2	MYC	P01106	479
PIM2	FLT3	P36888	454
PIM2	MCL1	Q07820	451
PIM2	ZFP36	P26651	449
PIM2	BCL2	P10415	432
PIM2	STAT5A	P42229	422

IntAct

20 interactions, top by confidence:

A	B	Type	Score
ATXN1	PIM2	psi-mi:“MI:0915”(physical association)	0.670
PIM2	ZNF821	psi-mi:“MI:0915”(physical association)	0.560
ZNF821	PIM2	psi-mi:“MI:0915”(physical association)	0.560
PIM2	DAPK1	psi-mi:“MI:0407”(direct interaction)	0.440
PIM2	MDM2	psi-mi:“MI:0217”(phosphorylation reaction)	0.440
HSP90AB1	PIM2	psi-mi:“MI:0915”(physical association)	0.400
GSK3B	PIM2	psi-mi:“MI:0915”(physical association)	0.370
PIM2	CUTC	psi-mi:“MI:0915”(physical association)	0.370
PIM2	NUP98	psi-mi:“MI:0914”(association)	0.350
PIM2	HSP90AA1	psi-mi:“MI:0914”(association)	0.350
PIM2	IKBKG	psi-mi:“MI:0407”(direct interaction)	0.000
HNRNPH3	PIM2	psi-mi:“MI:0915”(physical association)	0.000
NDUFB8	PIM2	psi-mi:“MI:0915”(physical association)	0.000
FBH1	PIM2	psi-mi:“MI:0915”(physical association)	0.000
RPL21	PIM2	psi-mi:“MI:0915”(physical association)	0.000
PIM2	ATXN1	psi-mi:“MI:0915”(physical association)	0.000

BioGRID (54): ZNF821 (Two-hybrid), CUTC (Two-hybrid), NUP98 (Affinity Capture-MS), PRCC (Affinity Capture-MS), PPIL2 (Affinity Capture-MS), TIMM13 (Affinity Capture-MS), GPKOW (Affinity Capture-MS), CLK4 (Affinity Capture-MS), TOE1 (Affinity Capture-MS), CCDC84 (Affinity Capture-MS), PIM2 (Biochemical Activity), PIM2 (Two-hybrid), PIM2 (Reconstituted Complex), PIM2 (Affinity Capture-MS), PIM2 (Negative Genetic)

ESM2 similar proteins: A7E3N7, A8VU90, B1WBU5, D3KCC4, O95382, P08923, P0C263, P0C264, P0C5K0, P0C5K1, P54265, Q06418, Q09013, Q13470, Q14296, Q16671, Q28616, Q4FZD7, Q53GL7, Q58EX7, Q60806, Q62070, Q62893, Q643R3, Q6DT37, Q6F5E8, Q6NVG1, Q6P5Z2, Q6VY05, Q76MJ5, Q80UW5, Q8CIE4, Q8CJ00, Q8IYX4, Q8K045, Q8K592, Q8NAG6, Q8NCV1, Q95JV3, Q96LW2

Diamond homologs: A0AUV4, A1A5Q6, B2DD29, B7XHR6, C0HKC8, C0HKC9, D3ZML2, F1QGZ6, O08679, O22932, O22971, O54863, O59697, O60285, O70444, O94168, P06803, P11309, P26794, P31374, P52497, P54645, P57059, P58750, P92958, Q00372, Q00771, Q05512, Q08217, Q0JI49, Q13131, Q14680, Q19469, Q1PFH8, Q20443, Q28GW8, Q38997, Q54DF2, Q54MV2, Q54WX4

SIGNOR signaling

24 interactions.

A	Effect	B	Mechanism
PIM2	“up-regulates quantity by stabilization”	CDKN1A	phosphorylation
SGI-1776	down-regulates	PIM2	“chemical inhibition”
PIM2	“down-regulates activity”	BAD	phosphorylation
PIM2	“up-regulates quantity by stabilization”	PKM	phosphorylation
FOXN3	“down-regulates quantity by repression”	PIM2	“transcriptional regulation”
PIM2	“down-regulates activity”	PK	phosphorylation
PIM2	“up-regulates quantity by stabilization”	PK	phosphorylation
PIM2	“down-regulates activity”	PRKAA1	phosphorylation
PIM2	“up-regulates quantity by stabilization”	PFKFB3	phosphorylation
PIM2	“up-regulates activity”	EIF4EBP1	phosphorylation
PIM2	“down-regulates quantity by destabilization”	CDC25A	phosphorylation
PIM2	down-regulates	BAD	phosphorylation
FLT3	“up-regulates quantity by expression”	PIM2	“transcriptional regulation”
STAT5A	“up-regulates quantity by expression”	PIM2	“transcriptional regulation”
PIM2	down-regulates	Apoptosis
SOX2/POU5F1	“up-regulates quantity by expression”	PIM2	“transcriptional regulation”
SOX17/POU5F1	“up-regulates quantity by expression”	PIM2	“transcriptional regulation”
PIM2	“up-regulates activity”	PSMD2	phosphorylation
PIM2	“up-regulates activity”	NFATC1	phosphorylation

Disease & clinical

Cancer significance

Clinical variants and AI predictions

ClinVar

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

Classification	Count (floor)
Pathogenic	0
Likely pathogenic	0
Uncertain significance	16
Likely benign	1
Benign	0

Top pathogenic / likely-pathogenic (0)

SpliceAI

677 predictions. Top by Δscore:

Variant	Effect	Δscore
X:48914290:GCAGT:G	acceptor_gain	1.0000
X:48914291:CAGT:C	acceptor_gain	1.0000
X:48914291:CAGTC:C	acceptor_gain	1.0000
X:48914292:AGT:A	acceptor_gain	1.0000
X:48914293:GT:G	acceptor_gain	1.0000
X:48914294:TC:T	acceptor_loss	1.0000
X:48914295:C:CC	acceptor_gain	1.0000
X:48914295:CTGT:C	acceptor_loss	1.0000
X:48914296:T:G	acceptor_loss	1.0000
X:48914303:C:CT	acceptor_gain	1.0000
X:48914303:C:T	acceptor_gain	1.0000
X:48914304:A:T	acceptor_gain	1.0000
X:48915014:CCTTA:C	donor_loss	1.0000
X:48915015:CTTAC:C	donor_loss	1.0000
X:48915016:TTA:T	donor_loss	1.0000
X:48915017:TA:T	donor_loss	1.0000
X:48915018:A:AC	donor_gain	1.0000
X:48915019:C:CA	donor_loss	1.0000
X:48915019:C:CC	donor_gain	1.0000
X:48915019:CCAT:C	donor_gain	1.0000
X:48915402:CAGG:C	acceptor_gain	1.0000
X:48915403:A:T	acceptor_gain	1.0000
X:48917775:ACT:A	donor_loss	1.0000
X:48917776:CTC:C	donor_loss	1.0000
X:48917777:TCAC:T	donor_loss	1.0000
X:48917778:CACCA:C	donor_loss	1.0000
X:48917779:A:AC	donor_gain	1.0000
X:48917779:A:AT	donor_loss	1.0000
X:48917780:C:CC	donor_gain	1.0000
X:48917830:ACC:A	acceptor_loss	1.0000

AlphaMissense

1988 scored. Top likely-pathogenic:

Variant	Protein change	am_pathogenicity
X:48914571:C:T	G199E	1.000
X:48915069:A:C	D182E	1.000
X:48915069:A:T	D182E	1.000
X:48915070:T:A	D182V	1.000
X:48915111:G:C	N168K	1.000
X:48915111:G:T	N168K	1.000
X:48915112:T:A	N168I	1.000
X:48915112:T:C	N168S	1.000
X:48915115:T:A	E167V	1.000
X:48915120:C:A	K165N	1.000
X:48915120:C:G	K165N	1.000
X:48915122:T:C	K165E	1.000
X:48915126:G:C	D163E	1.000
X:48915126:G:T	D163E	1.000
X:48915127:T:A	D163V	1.000
X:48915127:T:C	D163G	1.000
X:48915127:T:G	D163A	1.000
X:48915130:C:G	R162P	1.000
X:48917820:T:A	K61N	1.000
X:48917820:T:G	K61N	1.000
X:48918578:A:C	F43L	1.000
X:48918578:A:T	F43L	1.000
X:48918580:A:G	F43L	1.000
X:48914453:A:C	F238L	0.999
X:48914453:A:T	F238L	0.999
X:48914455:A:G	F238L	0.999
X:48914455:A:T	F238I	0.999
X:48914493:C:A	G225V	0.999
X:48914493:C:T	G225D	0.999
X:48914494:C:G	G225R	0.999

dbSNP variants (sampled 300 via entrez): RS1000450660 (X:48914426 A>C), RS1000800400 (X:48914101 C>T), RS1001402990 (X:48916178 T>G), RS1001850951 (X:48916510 G>A,C), RS1002810103 (X:48918258 G>A), RS1003862240 (X:48920970 C>T), RS1003964262 (X:48913837 C>A), RS1004316838 (X:48913469 C>T), RS1004915079 (X:48915526 C>G), RS1005374287 (X:48915953 A>G), RS1005966314 (X:48918136 C>G), RS1006915996 (X:48919775 C>T), RS1007380874 (X:48920235 A>T), RS1007934553 (X:48912712 T>C), RS1008937642 (X:48914459 A>T)

Disease associations

OMIM: gene MIM:300295 | 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 (2): CHEMBL3559682 (PROTEIN FAMILY), CHEMBL4523 (SINGLE PROTEIN)

Molecules with ChEMBL bioactivity

17 molecules (phase ≥1), by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 135,313 (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
CHEMBL3301610	ABEMACICLIB	4	7,045
CHEMBL535	SUNITINIB	4	79,020
CHEMBL608533	MIDOSTAURIN	4	7,259
CHEMBL300138	ENZASTAURIN	3	3,209
CHEMBL428690	ALVOCIDIB	3	27,781
CHEMBL522892	DOVITINIB	3	4,944
CHEMBL603469	LESTAURTINIB	3
CHEMBL91829	RUBOXISTAURIN	3	77
CHEMBL1230165	SILMITASERTIB	2	593
CHEMBL3975308	NUVISERTIB	2	100
CHEMBL4467168	DAPOLSERTIB	2	22
CHEMBL565612	SOTRASTAURIN	2	1,355
CHEMBL1952329	SGI-1776	1	400
CHEMBL3545083	RGB-286638	1	551
CHEMBL3651966	LGH-447	1	805
CHEMBL4225966	SEL-120 FREE BASE	1	91
CHEMBL494089	GSK-690693	1	2,061

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

GtoPdb / IUPHAR curated pharmacology

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

Target class: enzyme — PIM family

Most potent curated ligand interactions (11 total), top 11:

Ligand	Action	Affinity	Parameter
LGB321	Inhibition	11.68	pKi
PIM447	Inhibition	10.74	pKi
GDC-0339	Inhibition	10.0	pKi
AZD1208	Inhibition	9.8	pKi
compound 14k [PMID: 21982499]	Inhibition	8.22	pIC50
CX-6258	Inhibition	7.6	pIC50
uzansertib	Inhibition	7.52	pIC50
compound 28 [PMID: 30624936]	Inhibition	7.3	pIC50
nuvisertib	Inhibition	6.62	pKi
SGI-1776	Inhibition	6.44	pIC50
ruboxistaurin	Inhibition	4.7	pIC50

Binding affinities (BindingDB)

1830 measured of 2543 human assays (2543 total across all organisms); most potent 50 below. Values come from heterogeneous assays and are not directly comparable.

Ligand	Measure	Value	Patent
5-amino-N-[4-[(1R,3R,4S,5S)-3-amino-4-(2-cyanoethoxy)-5-methylcyclohexyl]-3-pyridinyl]-2-(2,6-difluorophenyl)-1,3-thiazole-4-carboxamide	IC50	0.01 nM	US-8987457: Ring-substituted N-pyridinyl amides as kinase inhibitors
N-[4-[(1R,3R,4S,5S)-3-amino-4-(2-cyanoethoxy)-5-methylcyclohexyl]-3-pyridinyl]-6-(2,6-difluoro-4-methylphenyl)-5-fluoropyridine-2-carboxamide	IC50	0.01 nM	US-8987457: Ring-substituted N-pyridinyl amides as kinase inhibitors
N-[4-[(1R,3R,4S,5S)-3-amino-4-methoxy-5-methylcyclohexyl]-3-pyridinyl]-6-[2,6-difluoro-4-(oxan-4-yl)phenyl]-5-fluoropyridine-2-carboxamide	IC50	0.01 nM	US-8987457: Ring-substituted N-pyridinyl amides as kinase inhibitors
N-[4-[(1R,3R,4S,5S)-3-amino-4-(2-cyanoethoxy)-5-methylcyclohexyl]-3-pyridinyl]-6-[2,6-difluoro-4-(4-fluorooxan-4-yl)phenyl]-5-fluoropyridine-2-carboxamide	IC50	0.01 nM	US-8987457: Ring-substituted N-pyridinyl amides as kinase inhibitors
N-[4-[(1R,3R,4S,5S)-3-amino-4-(2-cyanoethoxy)-5-methylcyclohexyl]-3-pyridinyl]-6-[2,6-difluoro-4-(oxan-4-yloxy)phenyl]-5-fluoropyridine-2-carboxamide	IC50	0.01 nM	US-8987457: Ring-substituted N-pyridinyl amides as kinase inhibitors
2-(tert-butylamino)-7-fluoro-3-methyl-8-[(6R)-6-methyl-4-oxo-5,6-dihydro-1H-pyrrolo[3,4-b]pyrrol-2-yl]quinazolin-4-one	IC50	0.012 nM	US-9394297: Amides as pim inhibitors
5-[1-[6-(1,4-diazepan-1-yl)-2-pyridinyl]pyrazolo[4,3-c]pyridin-6-yl]-3-methylpyrazin-2-amine	KI	0.012 nM	US-9434725: 5-azaindazole compounds and methods of use
3-ethyl-7-fluoro-2-[(1-methylcyclopropyl)amino]-8-[(6R)-6-methyl-4-oxo-5,6-dihydro-1H-pyrrolo[3,4-b]pyrrol-2-yl]quinazolin-4-one	IC50	0.013 nM	US-9394297: Amides as pim inhibitors
(3S)-1-[3-cyclopropyl-6-[6-(6-methylpyrazin-2-yl)pyrazolo[4,3-c]pyridin-1-yl]-2-pyridinyl]piperidin-3-amine	KI	0.014 nM	US-9434725: 5-azaindazole compounds and methods of use
(3S)-1-[3-methyl-6-[6-(6-methylpyrazin-2-yl)pyrazolo[4,3-c]pyridin-1-yl]-2-pyridinyl]piperidin-3-amine	KI	0.018 nM	US-9434725: 5-azaindazole compounds and methods of use
N-[4-[(1R,3R,4S,5S)-3-amino-5-methyl-4-methylsulfanylcyclohexyl]-3-pyridinyl]-6-(2,6-difluorophenyl)-5-fluoropyridine-2-carboxamide	IC50	0.02 nM	US-8987457: Ring-substituted N-pyridinyl amides as kinase inhibitors
N-[4-[(3R,4S,5S)-3-amino-5-methyl-4-(1,2,4-triazol-1-yl)piperidin-1-yl]-3-pyridinyl]-6-(2,6-difluorophenyl)-5-fluoropyridine-2-carboxamide	IC50	0.02 nM	US-8987457: Ring-substituted N-pyridinyl amides as kinase inhibitors
methyl N-[(3R,4S,5S)-3-amino-1-[3-[[6-(2,6-difluoro-4-methylphenyl)-5-fluoropyridine-2-carbonyl]amino]-4-pyridinyl]-5-methylpiperidin-4-yl]-N-methylcarbamate	IC50	0.02 nM	US-8987457: Ring-substituted N-pyridinyl amides as kinase inhibitors
N-[4-[(1R,3R,4S,5S)-3-amino-5-methyl-4-(2-methylsulfonylethoxy)cyclohexyl]-3-pyridinyl]-6-(2,6-difluoro-4-methylphenyl)-5-fluoropyridine-2-carboxamide	IC50	0.02 nM	US-8987457: Ring-substituted N-pyridinyl amides as kinase inhibitors
N-[4-[(1R,3R,4S,5S)-3-amino-4-methoxy-5-methylcyclohexyl]-3-pyridinyl]-6-(2,6-difluoro-4-propan-2-ylphenyl)-5-fluoropyridine-2-carboxamide	IC50	0.02 nM	US-8987457: Ring-substituted N-pyridinyl amides as kinase inhibitors
N-[4-[(1R,3R,4S,5S)-3-amino-4-methoxy-5-methylcyclohexyl]-3-pyridinyl]-6-(2,6-difluoro-4-propan-2-yloxyphenyl)-5-fluoropyridine-2-carboxamide	IC50	0.02 nM	US-8987457: Ring-substituted N-pyridinyl amides as kinase inhibitors
N-[4-[(1R,3R,4S,5S)-3-amino-5-methyl-4-(2-methylsulfonylethoxy)cyclohexyl]-3-pyridinyl]-6-[2,6-difluoro-4-(4-hydroxyoxan-4-yl)phenyl]-5-fluoropyridine-2-carboxamide	IC50	0.02 nM	US-8987457: Ring-substituted N-pyridinyl amides as kinase inhibitors
5-amino-N-[4-[(1R,3R,4S,5S)-3-amino-5-methyl-4-(2-methylsulfonylethoxy)cyclohexyl]-3-pyridinyl]-2-(2,6-difluorophenyl)-1,3-thiazole-4-carboxamide	IC50	0.02 nM	US-8987457: Ring-substituted N-pyridinyl amides as kinase inhibitors
N-[4-[(1R,3R,4R,5S)-3-amino-4-methoxy-5-methylcyclohexyl]-3-pyridinyl]-6-[2,6-difluoro-4-(oxan-4-yloxy)phenyl]-5-fluoropyridine-2-carboxamide	IC50	0.02 nM	US-8987457: Ring-substituted N-pyridinyl amides as kinase inhibitors
N-[4-[(1R,3R,4R,5S)-3-amino-5-methyl-4-(2-methylsulfonylethoxy)cyclohexyl]-3-pyridinyl]-6-[2,6-difluoro-4-(1-hydroxycyclobutyl)phenyl]-5-fluoropyridine-2-carboxamide	IC50	0.02 nM	US-8987457: Ring-substituted N-pyridinyl amides as kinase inhibitors
N-[4-[(1R,3R,4R,5S)-3-amino-5-methyl-4-(2-methylsulfonylethoxy)cyclohexyl]-3-pyridinyl]-6-[2,6-difluoro-4-(oxan-4-yloxy)phenyl]-5-fluoropyridine-2-carboxamide	IC50	0.02 nM	US-8987457: Ring-substituted N-pyridinyl amides as kinase inhibitors
N-[4-[(1R,3R,4S,5S)-3-amino-5-methyl-4-(2-methylsulfonylethoxy)cyclohexyl]-3-pyridinyl]-6-(2,6-difluoro-4-propan-2-yloxyphenyl)-5-fluoropyridine-2-carboxamide	IC50	0.02 nM	US-8987457: Ring-substituted N-pyridinyl amides as kinase inhibitors
N-[4-[(1R,3R,4R,5S)-3-amino-4-methoxy-5-methylcyclohexyl]-3-pyridinyl]-6-(2,6-difluoro-4-propan-2-yloxyphenyl)-5-fluoropyridine-2-carboxamide	IC50	0.02 nM	US-8987457: Ring-substituted N-pyridinyl amides as kinase inhibitors
N-[4-[(1R,3R,4S,5S)-3-amino-5-methyl-4-(2-methylsulfonylethoxy)cyclohexyl]-3-pyridinyl]-6-(2,6-difluoro-4-methoxyphenyl)-5-fluoropyridine-2-carboxamide	IC50	0.02 nM	US-8987457: Ring-substituted N-pyridinyl amides as kinase inhibitors
3-amino-N-[4-[(1R,3R,4S,5S)-3-amino-5-methyl-4-(2-methylsulfonylethoxy)cyclohexyl]-3-pyridinyl]-6-(2,6-difluorophenyl)-5-fluoropyridine-2-carboxamide	IC50	0.02 nM	US-8987457: Ring-substituted N-pyridinyl amides as kinase inhibitors
methyl N-[(3R,4S,5S)-3-amino-1-[3-[[6-(2,6-difluoro-4-propan-2-yloxyphenyl)-5-fluoropyridine-2-carbonyl]amino]-4-pyridinyl]-5-methylpiperidin-4-yl]carbamate	IC50	0.02 nM	US-8987457: Ring-substituted N-pyridinyl amides as kinase inhibitors
methyl N-[(3R,4S,5S)-3-amino-1-[3-[[6-[2,6-difluoro-4-(oxan-4-yloxy)phenyl]-5-fluoropyridine-2-carbonyl]amino]-4-pyridinyl]-5-methylpiperidin-4-yl]carbamate	IC50	0.02 nM	US-8987457: Ring-substituted N-pyridinyl amides as kinase inhibitors
N-[4-[(3R,4S,5S)-3-amino-5-methyl-4-(triazol-1-yl)piperidin-1-yl]-3-pyridinyl]-6-(2,6-difluoro-4-methylphenyl)-5-fluoropyridine-2-carboxamide	IC50	0.02 nM	US-8987457: Ring-substituted N-pyridinyl amides as kinase inhibitors
N-[4-[(1R,3R,4S,5S)-3-amino-4-(2-cyanoethoxy)-5-methylcyclohexyl]-3-pyridinyl]-6-(2,6-difluoro-4-methoxyphenyl)-5-fluoropyridine-2-carboxamide	IC50	0.02 nM	US-8987457: Ring-substituted N-pyridinyl amides as kinase inhibitors
3-amino-N-[4-[(1R,3R,4S,5S)-3-amino-4-(2-cyanoethoxy)-5-methylcyclohexyl]-3-pyridinyl]-6-(2,6-difluorophenyl)-5-fluoropyridine-2-carboxamide	IC50	0.02 nM	US-8987457: Ring-substituted N-pyridinyl amides as kinase inhibitors
N-[4-[(1R,3R,4S,5S)-3-amino-5-methyl-4-(triazol-1-yl)cyclohexyl]-3-pyridinyl]-6-[2,6-difluoro-4-(oxan-4-yloxy)phenyl]-5-fluoropyridine-2-carboxamide	IC50	0.02 nM	US-8987457: Ring-substituted N-pyridinyl amides as kinase inhibitors
methyl N-[(3R,4S,5S)-3-amino-1-[3-[[3-amino-6-(2,6-difluorophenyl)-5-fluoropyridine-2-carbonyl]amino]-4-pyridinyl]-5-methylpiperidin-4-yl]carbamate	IC50	0.02 nM	US-8987457: Ring-substituted N-pyridinyl amides as kinase inhibitors
3-amino-N-[4-[(1R,3R,4S,5S)-3-amino-5-methyl-4-(triazol-1-yl)cyclohexyl]-3-pyridinyl]-6-(2,6-difluorophenyl)-5-fluoropyridine-2-carboxamide	IC50	0.02 nM	US-8987457: Ring-substituted N-pyridinyl amides as kinase inhibitors
N-[4-[(1R,3R,4S,5S)-3-amino-4-(2-cyanoethoxy)-5-methylcyclohexyl]-3-pyridinyl]-6-[2,6-difluoro-4-(1-hydroxycyclobutyl)phenyl]-5-fluoropyridine-2-carboxamide	IC50	0.02 nM	US-8987457: Ring-substituted N-pyridinyl amides as kinase inhibitors
6-[6-(azetidin-1-yl)pyrazin-2-yl]-1-(6-piperazin-1-yl-2-pyridinyl)pyrazolo[4,3-c]pyridine	KI	0.02 nM	US-9434725: 5-azaindazole compounds and methods of use
1-[6-(1,4-diazepan-1-yl)-2-pyridinyl]-6-(6-methylpyrazin-2-yl)pyrazolo[4,3-c]pyridine	KI	0.0204 nM	US-9434725: 5-azaindazole compounds and methods of use
1-[6-(1,4-diazepan-1-yl)-2-pyridinyl]-6-(6-ethylpyrazin-2-yl)pyrazolo[4,3-c]pyridine	KI	0.021 nM	US-9434725: 5-azaindazole compounds and methods of use
(3S)-1-[3-methoxy-6-[6-(6-methylpyrazin-2-yl)pyrazolo[4,3-c]pyridin-1-yl]-2-pyridinyl]piperidin-3-amine	KI	0.0212 nM	US-9434725: 5-azaindazole compounds and methods of use
6-[1-[6-(1,4-diazepan-1-yl)-2-pyridinyl]pyrazolo[4,3-c]pyridin-6-yl]pyrazin-2-amine	KI	0.023 nM	US-9434725: 5-azaindazole compounds and methods of use
5-amino-N-[5-[(4R)-4-aminoazepan-1-yl]-1-methylpyrazol-4-yl]-2-(2,6-difluorophenyl)-1,3-thiazole-4-carboxamide	KI	0.024 nM	US-8669361: Pyrazol-4-yl-heterocyclyl-carboxamide compounds and methods of use
(3S)-1-[3-cyclopropyl-6-[6-(6-methylpyrazin-2-yl)pyrazolo[4,3-c]pyridin-1-yl]pyrazin-2-yl]piperidin-3-amine	KI	0.026 nM	US-9434725: 5-azaindazole compounds and methods of use
2-[[6-[1-(6-piperazin-1-yl-2-pyridinyl)pyrazolo[4,3-c]pyridin-6-yl]pyrazin-2-yl]amino]ethanol	KI	0.026 nM	US-9434725: 5-azaindazole compounds and methods of use
5-amino-N-[5-(4-aminoazepan-1-yl)-1-methylpyrazol-4-yl]-2-(2,6-difluorophenyl)-1,3-thiazole-4-carboxamide	KI	0.027 nM	US-8669361: Pyrazol-4-yl-heterocyclyl-carboxamide compounds and methods of use
6-methyl-1-[6-[6-(6-methylpyrazin-2-yl)pyrazolo[4,3-c]pyridin-1-yl]-2-pyridinyl]piperidin-3-amine	KI	0.028 nM	US-9434725: 5-azaindazole compounds and methods of use
3-(tert-butylamino)-5-(4-oxo-1,5,6,7-tetrahydropyrrolo[3,2-c]pyridin-2-yl)-3,4,4a,5,6,7,8,8a-octahydro-1H-quinoxalin-2-one	IC50	0.0282 nM	US-9394297: Amides as pim inhibitors
2-(tert-butylamino)-3-ethyl-7-fluoro-8-[(6R)-6-methyl-4-oxo-5,6-dihydro-1H-pyrrolo[3,4-b]pyrrol-2-yl]quinazolin-4-one	IC50	0.029 nM	US-9394297: Amides as pim inhibitors
2-[6-fluoro-2-methyl-3-[(1-methylcyclopropyl)amino]quinoxalin-5-yl]spiro[1,5-dihydropyrrolo[3,4-b]pyrrole-6,1’-cyclopropane]-4-one	IC50	0.0295 nM	US-9394297: Amides as pim inhibitors
N-[4-[(3R,4S,5S)-3-amino-5-methyl-4-(triazol-1-yl)piperidin-1-yl]-3-pyridinyl]-6-(2,6-difluorophenyl)-5-fluoropyridine-2-carboxamide	IC50	0.03 nM	US-8987457: Ring-substituted N-pyridinyl amides as kinase inhibitors
N-[4-[(1R,3R,4S,5S)-3-amino-5-methyl-4-(1,2,4-triazol-1-yl)cyclohexyl]-3-pyridinyl]-6-(2,6-difluorophenyl)-5-fluoropyridine-2-carboxamide	IC50	0.03 nM	US-8987457: Ring-substituted N-pyridinyl amides as kinase inhibitors
methyl N-[(3R,4S,5S)-3-amino-1-[3-[[6-(2,6-difluorophenyl)-5-fluoropyridine-2-carbonyl]amino]-4-pyridinyl]-5-methylpiperidin-4-yl]-N-methylcarbamate	IC50	0.03 nM	US-8987457: Ring-substituted N-pyridinyl amides as kinase inhibitors

ChEMBL bioactivities

3461 potent at pChembl≥5 of 3490 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).

pChembl	Type	Value	Unit	Molecule
10.92	IC50	0.012	nM	CHEMBL3902148
10.92	IC50	0.012	nM	CHEMBL3940091
10.74	Ki	0.018	nM	LGH-447
10.74	IC50	0.018	nM	LGH-447
10.74	IC50	0.018	nM	CHEMBL4741714
10.70	IC50	0.02	nM	CHEMBL3909351
10.49	Ki	0.032	nM	CHEMBL2387464
10.45	IC50	0.0354	nM	CHEMBL3949102
10.45	IC50	0.0358	nM	CHEMBL3903686
10.43	Ki	0.037	nM	CHEMBL2387465
10.42	IC50	0.0378	nM	CHEMBL3918907
10.42	IC50	0.0378	nM	CHEMBL3895124
10.40	Ki	0.04	nM	CHEMBL3623150
10.40	Ki	0.04	nM	CHEMBL4459538
10.32	IC50	0.0484	nM	CHEMBL3949318
10.31	Ki	0.049	nM	CHEMBL3634783
10.30	IC50	0.05	nM	CHEMBL3808669
10.30	IC50	0.05	nM	CHEMBL3808887
10.30	Ki	0.05	nM	CHEMBL3676285
10.30	Ki	0.05	nM	CHEMBL4439756
10.30	IC50	0.05	nM	CHEMBL4568404
10.22	IC50	0.06	nM	CHEMBL3949175
10.18	IC50	0.0667	nM	CHEMBL3896195
10.15	IC50	0.07	nM	CHEMBL3810121
10.13	IC50	0.0741	nM	CHEMBL3960373
10.12	Ki	0.076	nM	CHEMBL2387471
10.12	IC50	0.076	nM	CHEMBL3919725
10.11	IC50	0.0783	nM	CHEMBL3933056
10.11	IC50	0.077	nM	CHEMBL3909217
10.11	Ki	0.077	nM	CHEMBL3932475
10.10	IC50	0.08	nM	CHEMBL3808662
10.10	IC50	0.08	nM	CHEMBL3966732
10.10	IC50	0.08	nM	CHEMBL4441708
10.06	Ki	0.088	nM	CHEMBL3634760
10.05	IC50	0.09	nM	CHEMBL3950251
10.05	IC50	0.09	nM	CHEMBL3958862
10.03	Ki	0.094	nM	CHEMBL2387463
10.03	IC50	0.094	nM	CHEMBL3942186
10.00	IC50	0.1	nM	CHEMBL3965946
10.00	IC50	0.1	nM	CHEMBL3930148
10.00	IC50	0.1	nM	CHEMBL4110951
10.00	IC50	0.1	nM	CHEMBL3901766
10.00	IC50	0.1	nM	CHEMBL3958862
10.00	IC50	0.1	nM	CHEMBL3944421
10.00	IC50	0.1	nM	CHEMBL3918273
10.00	IC50	0.1	nM	CHEMBL3941050
10.00	Ki	0.1	nM	CHEMBL4437940
10.00	Ki	0.1	nM	CHEMBL3648680
10.00	IC50	0.1	nM	CHEMBL3979182
10.00	IC50	0.1	nM	CHEMBL3902148

PubChem BioAssay actives

1255 with measured affinity, of 3670 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
N-[2-[(1R,3S,5S)-3-amino-5-methylcyclohexyl]phenyl]-6-(2,6-difluorophenyl)-5-fluoropyridine-2-carboxamide	1692890: Inhibition of PIM2 (unknown origin)	ic50	<0.0001	uM
5-amino-N-[5-[(3S,5R)-5-amino-3-methoxyazepan-1-yl]-1-methylpyrazol-4-yl]-2-(2,6-difluorophenyl)-1,3-thiazole-4-carboxamide	1520509: Inhibition of recombinant human PIM2 using FAM-pimtide as substrate after 90 mins by Z-LYTE assay	ki	<0.0001	uM
3-amino-N-[4-[(3S)-3-aminopiperidin-1-yl]-3-pyridinyl]-6-(2,6-difluorophenyl)pyridine-2-carboxamide	1062193: Inhibition of PIM2 (unknown origin) using Biotin-AGAGRSRHSSYPAGT-OH as substrate after 2 hrs by AlphaScreen assay	ki	<0.0001	uM
N-[4-[(1R,3S,5S)-3-amino-5-methylcyclohexyl]-3-pyridinyl]-6-(2,6-difluorophenyl)-5-fluoropyridine-2-carboxamide	1266532: Inhibition of PIM2 kinase (unknown origin) using Biotin-AGAGRSRHSSYPAGT-OH as substrate after 2 hrs by alphascreen assay	ki	<0.0001	uM
N-[4-[(3R,4R,5S)-3-amino-4-hydroxy-5-methylpiperidin-1-yl]-3-pyridinyl]-6-(2,6-difluorophenyl)-5-fluoropyridine-2-carboxamide	1062197: Inhibition of PIM2 (unknown origin)	ki	<0.0001	uM
3-amino-N-[4-[(3R,4R,5S)-3-amino-4-hydroxy-5-methylpiperidin-1-yl]-3-pyridinyl]-6-(2,6-difluorophenyl)-5-fluoropyridine-2-carboxamide	1062197: Inhibition of PIM2 (unknown origin)	ki	<0.0001	uM
3-amino-N-[4-[(3R,4R)-3-amino-4-hydroxypiperidin-1-yl]-3-pyridinyl]-6-(2,6-difluorophenyl)pyridine-2-carboxamide	1062197: Inhibition of PIM2 (unknown origin)	ki	<0.0001	uM
5-(6-methylpyrazin-2-yl)-3-(6-piperazin-1-yl-2-pyridinyl)-1H-pyrazolo[3,4-c]pyridine	1256222: Inhibition of Pim2 (unknown origin) using 5FAM-ARKRRRHPSGPPTA as substrate after 90 mins	ki	<0.0001	uM
N-[5-(2-fluorophenyl)-1H-pyrrolo[2,3-b]pyridin-3-yl]-5-[[(3R,4R)-3-fluoropiperidin-4-yl]methylamino]pyrazolo[1,5-a]pyrimidine-3-carboxamide	749897: Inhibition of PIM2 (unknown origin) using FAM-pimtide as substrate after 90 mins by spectrophotometry in presence of ATP	ki	<0.0001	uM
5-amino-N-[5-[(5R)-5-amino-3,3-difluoroazepan-1-yl]-1-methylpyrazol-4-yl]-2-(2,6-difluorophenyl)-1,3-thiazole-4-carboxamide	1520509: Inhibition of recombinant human PIM2 using FAM-pimtide as substrate after 90 mins by Z-LYTE assay	ki	<0.0001	uM
N-[5-(2,6-difluorophenyl)-1H-pyrrolo[2,3-b]pyridin-3-yl]-5-[[(3R,4R)-3-fluoropiperidin-4-yl]methylamino]pyrazolo[1,5-a]pyrimidine-3-carboxamide	749897: Inhibition of PIM2 (unknown origin) using FAM-pimtide as substrate after 90 mins by spectrophotometry in presence of ATP	ki	<0.0001	uM
(3S,5R)-3,5-diamino-1-[3-[[2-(2,6-difluorophenyl)imidazo[1,5-b]pyridazin-7-yl]amino]-4-pyridinyl]piperidin-4-ol	1325331: Inhibition of recombinant Pim2 (unknown origin) by electrochemiluminescence assay	ic50	0.0001	uM
3-(1-methylcyclopropyl)-2-[(1-methylcyclopropyl)amino]-8-[(6R)-6-methyl-4-oxo-5,6-dihydro-1H-pyrrolo[3,4-b]pyrrol-2-yl]quinazolin-4-one	1572117: Inhibition of full length recombinant PIM2 (unknown origin) assessed as reduction in BAD phosphorylation at Ser112 residues preincubated for 30 mins followed by biotinylated BAD addition and measured after 1 hr by HTRF assay	ic50	0.0001	uM
3-(cyclopropylmethyl)-2-[(1-methylcyclopropyl)amino]-8-[(6R)-6-methyl-4-oxo-5,6-dihydro-1H-pyrrolo[3,4-b]pyrrol-2-yl]quinazolin-4-one	1572117: Inhibition of full length recombinant PIM2 (unknown origin) assessed as reduction in BAD phosphorylation at Ser112 residues preincubated for 30 mins followed by biotinylated BAD addition and measured after 1 hr by HTRF assay	ic50	0.0001	uM
2-(tert-butylamino)-3-(cyclopropylmethyl)-8-[(6R)-6-methyl-4-oxo-5,6-dihydro-1H-pyrrolo[3,4-b]pyrrol-2-yl]quinazolin-4-one	1572117: Inhibition of full length recombinant PIM2 (unknown origin) assessed as reduction in BAD phosphorylation at Ser112 residues preincubated for 30 mins followed by biotinylated BAD addition and measured after 1 hr by HTRF assay	ic50	0.0001	uM
2-[(1-methylcyclopropyl)amino]-3-[(1S)-1-(1-methylimidazol-4-yl)ethyl]-8-[(6R)-6-methyl-4-oxo-5,6-dihydro-1H-pyrrolo[3,4-b]pyrrol-2-yl]quinazolin-4-one	1572117: Inhibition of full length recombinant PIM2 (unknown origin) assessed as reduction in BAD phosphorylation at Ser112 residues preincubated for 30 mins followed by biotinylated BAD addition and measured after 1 hr by HTRF assay	ic50	0.0001	uM
2-(tert-butylamino)-8-[(6R)-6-methyl-4-oxo-5,6-dihydro-1H-pyrrolo[3,4-b]pyrrol-2-yl]-3-[[(2R)-oxolan-2-yl]methyl]quinazolin-4-one	1572117: Inhibition of full length recombinant PIM2 (unknown origin) assessed as reduction in BAD phosphorylation at Ser112 residues preincubated for 30 mins followed by biotinylated BAD addition and measured after 1 hr by HTRF assay	ic50	0.0001	uM
2-[(1-methylcyclopropyl)amino]-3-[1-(1-methylimidazol-4-yl)ethyl]-8-[(6R)-6-methyl-4-oxo-5,6-dihydro-1H-pyrrolo[3,4-b]pyrrol-2-yl]quinazolin-4-one	1572117: Inhibition of full length recombinant PIM2 (unknown origin) assessed as reduction in BAD phosphorylation at Ser112 residues preincubated for 30 mins followed by biotinylated BAD addition and measured after 1 hr by HTRF assay	ic50	0.0001	uM
5-amino-N-[4-[(3S)-3-aminopiperidin-1-yl]-3-pyridinyl]-2-(2,6-difluorophenyl)-1,3-thiazole-4-carboxamide	1520509: Inhibition of recombinant human PIM2 using FAM-pimtide as substrate after 90 mins by Z-LYTE assay	ki	0.0001	uM
5-amino-N-[5-[(4S)-4-aminoazepan-1-yl]-1-methylpyrazol-4-yl]-2-(2,6-difluorophenyl)-1,3-thiazole-4-carboxamide	1520509: Inhibition of recombinant human PIM2 using FAM-pimtide as substrate after 90 mins by Z-LYTE assay	ki	0.0001	uM
N-[4-[(3S,5R)-3-amino-5-methylpiperidin-1-yl]-3-pyridinyl]-2-(2,6-difluorophenyl)imidazo[1,5-b]pyridazin-7-amine	1325331: Inhibition of recombinant Pim2 (unknown origin) by electrochemiluminescence assay	ic50	0.0001	uM
(3S)-1-[3-methyl-6-[5-(1-methylpyrazol-4-yl)-1H-pyrazolo[3,4-c]pyridin-3-yl]-2-pyridinyl]piperidin-3-amine	1256222: Inhibition of Pim2 (unknown origin) using 5FAM-ARKRRRHPSGPPTA as substrate after 90 mins	ki	0.0001	uM
3-ethyl-5-[3-(6-piperazin-1-yl-2-pyridinyl)-1H-pyrazolo[3,4-c]pyridin-5-yl]pyrimidin-4-one	1256222: Inhibition of Pim2 (unknown origin) using 5FAM-ARKRRRHPSGPPTA as substrate after 90 mins	ki	0.0001	uM
3-[6-(1,4-diazepan-1-yl)-2-pyridinyl]-5-(6-methylpyrazin-2-yl)-1H-pyrazolo[3,4-c]pyridine	1483005: Inhibition of PIM2 (unknown origin) using 5FAM-ARKRRRHPSGPPTA as substrate after 90 mins in presence of ATP by caliper microfluidic mobility shift assay	ki	0.0001	uM
2-[4-[3-(6-piperazin-1-yl-2-pyridinyl)-1H-pyrazolo[3,4-c]pyridin-5-yl]pyrazol-1-yl]acetonitrile	1256222: Inhibition of Pim2 (unknown origin) using 5FAM-ARKRRRHPSGPPTA as substrate after 90 mins	ki	0.0001	uM
N-[5-(2,6-difluorophenyl)-1H-pyrrolo[2,3-b]pyridin-3-yl]-5-(piperidin-4-ylmethylamino)pyrazolo[1,5-a]pyrimidine-3-carboxamide	749897: Inhibition of PIM2 (unknown origin) using FAM-pimtide as substrate after 90 mins by spectrophotometry in presence of ATP	ki	0.0001	uM
N-[5-(2-fluorophenyl)-1H-pyrrolo[2,3-b]pyridin-3-yl]-5-(piperidin-4-ylmethylamino)pyrazolo[1,5-a]pyrimidine-3-carboxamide	749897: Inhibition of PIM2 (unknown origin) using FAM-pimtide as substrate after 90 mins by spectrophotometry in presence of ATP	ki	0.0001	uM
(6R)-2-[3-(tert-butylamino)-6-fluoro-2-methylquinoxalin-5-yl]-6-methyl-5,6-dihydro-1H-pyrrolo[3,4-b]pyrrol-4-one	1635822: Inhibition of full length recombinant Pim-2 (unknown origin) assessed as reduction in phosphorylation of biotinylated-BAD peptide at Serine 112 residue preincubated for 30 mins followed by substrate addition for 1 hr by HTRF assay	ic50	0.0001	uM
5-amino-N-[5-[(4R,5R)-4-amino-5-fluoroazepan-1-yl]-1-methylpyrazol-4-yl]-2-(2,6-difluorophenyl)-1,3-thiazole-4-carboxamide	1520509: Inhibition of recombinant human PIM2 using FAM-pimtide as substrate after 90 mins by Z-LYTE assay	ki	0.0001	uM
(3S)-1-[3-methoxy-6-[6-(6-methylpyrazin-2-yl)pyrazolo[4,3-c]pyridin-1-yl]-2-pyridinyl]piperidin-3-amine	1483005: Inhibition of PIM2 (unknown origin) using 5FAM-ARKRRRHPSGPPTA as substrate after 90 mins in presence of ATP by caliper microfluidic mobility shift assay	ki	0.0001	uM
5-amino-N-[5-(5-amino-3-fluoroazepan-1-yl)-1-methylpyrazol-4-yl]-2-(2,6-difluorophenyl)-1,3-thiazole-4-carboxamide	1520509: Inhibition of recombinant human PIM2 using FAM-pimtide as substrate after 90 mins by Z-LYTE assay	ki	0.0001	uM
3-cyclopropyl-2-[(1-methylcyclopropyl)amino]-8-[(6R)-6-methyl-4-oxo-5,6-dihydro-1H-pyrrolo[3,4-b]pyrrol-2-yl]quinazolin-4-one	1572117: Inhibition of full length recombinant PIM2 (unknown origin) assessed as reduction in BAD phosphorylation at Ser112 residues preincubated for 30 mins followed by biotinylated BAD addition and measured after 1 hr by HTRF assay	ic50	0.0001	uM
2-[3-(tert-butylamino)-6-fluoro-2-methylquinoxalin-5-yl]-1,5-dihydropyrrolo[3,2-c]pyridin-4-one	1635822: Inhibition of full length recombinant Pim-2 (unknown origin) assessed as reduction in phosphorylation of biotinylated-BAD peptide at Serine 112 residue preincubated for 30 mins followed by substrate addition for 1 hr by HTRF assay	ic50	0.0001	uM
2-(tert-butylamino)-7-fluoro-3-methyl-8-[(6R)-6-methyl-4-oxo-5,6-dihydro-1H-pyrrolo[3,4-b]pyrrol-2-yl]quinazolin-4-one	1635822: Inhibition of full length recombinant Pim-2 (unknown origin) assessed as reduction in phosphorylation of biotinylated-BAD peptide at Serine 112 residue preincubated for 30 mins followed by substrate addition for 1 hr by HTRF assay	ic50	0.0001	uM
2-(tert-butylamino)-3-cyclopropyl-8-[(6R)-6-methyl-4-oxo-5,6-dihydro-1H-pyrrolo[3,4-b]pyrrol-2-yl]quinazolin-4-one	1572117: Inhibition of full length recombinant PIM2 (unknown origin) assessed as reduction in BAD phosphorylation at Ser112 residues preincubated for 30 mins followed by biotinylated BAD addition and measured after 1 hr by HTRF assay	ic50	0.0001	uM
2-(tert-butylamino)-8-[(6R)-6-methyl-4-oxo-5,6-dihydro-1H-pyrrolo[3,4-b]pyrrol-2-yl]-3-propan-2-ylquinazolin-4-one	1572117: Inhibition of full length recombinant PIM2 (unknown origin) assessed as reduction in BAD phosphorylation at Ser112 residues preincubated for 30 mins followed by biotinylated BAD addition and measured after 1 hr by HTRF assay	ic50	0.0001	uM
(9S,11E)-12,16-dimethyl-3,7,14,17,23-pentazapentacyclo[13.6.2.12,5.04,9.018,22]tetracosa-1(22),2(24),4,11,15(23),16,18,20-octaen-6-one	1303115: Inhibition of human full-length Pim2 expressed in Escherichia coli assessed as phosphorylation of biotinylated BAD peptide at Ser 112 preincubated for 30 mins followed by substrate addition measured after 1 hr by HTRF assay	ic50	0.0001	uM
(9S)-16-methyl-3,7,14,17,23-pentazapentacyclo[13.6.2.12,5.04,9.018,22]tetracosa-1(22),2(24),4,15(23),16,18,20-heptaen-6-one	1303115: Inhibition of human full-length Pim2 expressed in Escherichia coli assessed as phosphorylation of biotinylated BAD peptide at Ser 112 preincubated for 30 mins followed by substrate addition measured after 1 hr by HTRF assay	ic50	0.0001	uM
(9S,11E,13R)-13,16-dimethyl-3,7,14,17,23-pentazapentacyclo[13.6.2.12,5.04,9.018,22]tetracosa-1(22),2(24),4,11,15(23),16,18,20-octaen-6-one	1303115: Inhibition of human full-length Pim2 expressed in Escherichia coli assessed as phosphorylation of biotinylated BAD peptide at Ser 112 preincubated for 30 mins followed by substrate addition measured after 1 hr by HTRF assay	ic50	0.0001	uM
(9S,11Z)-16-methyl-3,7,14,17,23-pentazapentacyclo[13.6.2.12,5.04,9.018,22]tetracosa-1(22),2(24),4,11,15(23),16,18,20-octaen-6-one	1303115: Inhibition of human full-length Pim2 expressed in Escherichia coli assessed as phosphorylation of biotinylated BAD peptide at Ser 112 preincubated for 30 mins followed by substrate addition measured after 1 hr by HTRF assay	ic50	0.0001	uM
3-[6-(1,4-diazepan-1-yl)-2-pyridinyl]-5-(1-methylpyrazol-4-yl)-1H-pyrazolo[3,4-c]pyridine	1256222: Inhibition of Pim2 (unknown origin) using 5FAM-ARKRRRHPSGPPTA as substrate after 90 mins	ki	0.0002	uM
3-[(1-hydroxycyclopropyl)methyl]-2-[(1-methylcyclopropyl)amino]-8-[(6R)-6-methyl-4-oxo-5,6-dihydro-1H-pyrrolo[3,4-b]pyrrol-2-yl]quinazolin-4-one	1572117: Inhibition of full length recombinant PIM2 (unknown origin) assessed as reduction in BAD phosphorylation at Ser112 residues preincubated for 30 mins followed by biotinylated BAD addition and measured after 1 hr by HTRF assay	ic50	0.0002	uM
5-amino-N-[5-[(4R,5S)-4-amino-5-hydroxyazepan-1-yl]-1-methylpyrazol-4-yl]-2-(2,6-difluorophenyl)-1,3-thiazole-4-carboxamide	1520509: Inhibition of recombinant human PIM2 using FAM-pimtide as substrate after 90 mins by Z-LYTE assay	ki	0.0002	uM
2-(tert-butylamino)-3-(1-methylcyclopropyl)-8-[(6R)-6-methyl-4-oxo-5,6-dihydro-1H-pyrrolo[3,4-b]pyrrol-2-yl]quinazolin-4-one	1572117: Inhibition of full length recombinant PIM2 (unknown origin) assessed as reduction in BAD phosphorylation at Ser112 residues preincubated for 30 mins followed by biotinylated BAD addition and measured after 1 hr by HTRF assay	ic50	0.0002	uM
3-[(1-aminocyclopropyl)methyl]-2-(tert-butylamino)-8-[(6R)-6-methyl-4-oxo-5,6-dihydro-1H-pyrrolo[3,4-b]pyrrol-2-yl]quinazolin-4-one	1572117: Inhibition of full length recombinant PIM2 (unknown origin) assessed as reduction in BAD phosphorylation at Ser112 residues preincubated for 30 mins followed by biotinylated BAD addition and measured after 1 hr by HTRF assay	ic50	0.0002	uM
3-cyclobutyl-2-[(1-methylcyclopropyl)amino]-8-[(6R)-6-methyl-4-oxo-5,6-dihydro-1H-pyrrolo[3,4-b]pyrrol-2-yl]quinazolin-4-one	1572117: Inhibition of full length recombinant PIM2 (unknown origin) assessed as reduction in BAD phosphorylation at Ser112 residues preincubated for 30 mins followed by biotinylated BAD addition and measured after 1 hr by HTRF assay	ic50	0.0002	uM
3-[(1-aminocyclopropyl)methyl]-2-[(1-methylcyclopropyl)amino]-8-[(6R)-6-methyl-4-oxo-5,6-dihydro-1H-pyrrolo[3,4-b]pyrrol-2-yl]quinazolin-4-one	1572117: Inhibition of full length recombinant PIM2 (unknown origin) assessed as reduction in BAD phosphorylation at Ser112 residues preincubated for 30 mins followed by biotinylated BAD addition and measured after 1 hr by HTRF assay	ic50	0.0002	uM
2-(tert-butylamino)-3-[(1-methylimidazol-4-yl)methyl]-8-[(6R)-6-methyl-4-oxo-5,6-dihydro-1H-pyrrolo[3,4-b]pyrrol-2-yl]quinazolin-4-one	1572117: Inhibition of full length recombinant PIM2 (unknown origin) assessed as reduction in BAD phosphorylation at Ser112 residues preincubated for 30 mins followed by biotinylated BAD addition and measured after 1 hr by HTRF assay	ic50	0.0002	uM
2-(tert-butylamino)-3-[(1-hydroxycyclopropyl)methyl]-8-[(6R)-6-methyl-4-oxo-5,6-dihydro-1H-pyrrolo[3,4-b]pyrrol-2-yl]quinazolin-4-one	1572117: Inhibition of full length recombinant PIM2 (unknown origin) assessed as reduction in BAD phosphorylation at Ser112 residues preincubated for 30 mins followed by biotinylated BAD addition and measured after 1 hr by HTRF assay	ic50	0.0002	uM
(5Z)-5-[[2-[(3R)-3-aminopiperidin-1-yl]-3-phenylphenyl]methylidene]-1,3-thiazolidine-2,4-dione	1062197: Inhibition of PIM2 (unknown origin)	ki	0.0002	uM

CTD chemical–gene interactions

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

Chemical	Actions (top 5)	PubMed papers
Benzo(a)pyrene	affects methylation, increases expression	4
sodium arsenite	decreases expression, affects cotreatment, increases abundance, increases expression	3
entinostat	increases expression, affects cotreatment	2
Leflunomide	decreases expression	2
Nickel	increases expression	2
triphenyl phosphate	affects expression	1
propionaldehyde	increases expression	1
bisphenol A	increases methylation	1
trichostatin A	affects expression	1
tris(1,3-dichloro-2-propyl)phosphate	decreases expression	1
butyraldehyde	increases expression	1
manganese chloride	increases abundance, increases expression, affects cotreatment	1
2-amino-3,8-dimethylimidazo(4,5-f)quinoxaline	decreases expression	1
S-(1,2-dichlorovinyl)cysteine	affects response to substance, increases expression, affects cotreatment	1
epigallocatechin gallate	increases expression	1
CGP 52608	increases reaction, affects binding	1
nickel acetate	decreases reaction, increases expression	1
pinostrobin	increases expression	1
N-(oxo-5,6-dihydrophenanthridin-2-yl)-N,N-dimethylacetamide hydrochloride	affects binding, decreases activity	1
4-(5-benzo(1,3)dioxol-5-yl-4-pyridin-2-yl-1H-imidazol-2-yl)benzamide	affects cotreatment, increases expression	1
nutlin 3	affects cotreatment, increases expression	1
ICG 001	increases expression	1
abrine	decreases expression	1
dorsomorphin	increases expression, affects cotreatment	1
jinfukang	increases expression, affects cotreatment	1
PF 3758309	decreases expression	1
(+)-JQ1 compound	increases expression	1
Zoledronic Acid	increases expression	1
Acetylcysteine	increases expression	1
Arsenic	affects cotreatment, increases abundance, increases expression	1

ChEMBL screening assays

605 unique, capped per target: 574 binding, 30 functional, 1 toxicity

Representative assays (with source publication via chembl_document):

Assay ID	Type	Description	Source paper
CHEMBL3812019	Binding	Inhibition of Pim1/2 in human KMS-12-BM cells assessed as phosphorylation of full-length BAD protein at Ser-112 incubated for 110 mins by flow cytometric analysis in presence of 20% FBS	Discovery and Optimization of Macrocyclic Quinoxaline-pyrrolo-dihydropiperidinones as Potent Pim-1/2 Kinase Inhibitors. — ACS Med Chem Lett
CHEMBL1963820	Functional	PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member name: PIM2	PubChem BioAssay data set
CHEMBL5160045	Toxicity	Binding affinity to human PIM2	Discovery and Preclinical Pharmacology of INE963, a Potent and Fast-Acting Blood-Stage Antimalarial with a High Barrier to Resistance and Potential for Single-Dose Cures in Uncomplicated Malaria. — J Med Chem

Cellosaurus cell lines

6 cell lines: 6 cancer cell line

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

Cellosaurus	Name	Category	Sex
CVCL_D1PT	Abcam K-562 PIM2 KO	Cancer cell line	Female
CVCL_D2LE	Abcam Raji PIM2 KO	Cancer cell line	Male
CVCL_TD79	HAP1 PIM2 (-) 1	Cancer cell line	Male
CVCL_TD80	HAP1 PIM2 (-) 2	Cancer cell line	Male
CVCL_TD81	HAP1 PIM2 (-) 3	Cancer cell line	Male
CVCL_WQ29	Abcam Jurkat PIM2 KO	Cancer cell line	Male

Clinical trials (associated diseases)

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