DPP7

Summary

DPP7 (dipeptidyl peptidase 7, HGNC:14892) is a protein-coding gene on chromosome 9q34.3, encoding Dipeptidyl peptidase 2 (Q9UHL4). Plays an important role in the degradation of some oligopeptides.

The protein encoded by this gene is a post-proline cleaving aminopeptidase expressed in quiescent lymphocytes. The resting lymphocytes are maintained through suppression of apoptosis, a state which is disrupted by inhibition of this novel serine protease. The enzyme has strong sequence homology with prolylcarboxypeptidase and is active at both acidic and neutral pH.

Source: NCBI Gene 29952 — RefSeq curated summary.

At a glance

• GWAS associations: 1
• Clinical variants (ClinVar): 173 total
• Druggable target: yes — 3 molecules with ChEMBL bioactivity
• MANE Select transcript: NM_013379

Identifiers

Gene identifiers

Field	Value
HGNC ID	HGNC:14892
Approved symbol	DPP7
Name	dipeptidyl peptidase 7
Location	9q34.3
Locus type	gene with protein product
Status	Approved
Aliases	DPPII, DPP2
Ensembl gene	ENSG00000176978
Ensembl biotype	protein_coding
OMIM	610537
Entrez	29952

Gene structure

Transcript identifiers

Ensembl transcripts: 38 — 14 protein_coding, 13 retained_intron, 6 nonsense_mediated_decay, 5 protein_coding_CDS_not_defined

ENST00000371579, ENST00000460830, ENST00000463619, ENST00000470766, ENST00000472306, ENST00000473532, ENST00000473703, ENST00000478597, ENST00000482088, ENST00000483783, ENST00000485456, ENST00000491807, ENST00000497375, ENST00000706871, ENST00000706872, ENST00000706873, ENST00000706874, ENST00000706875, ENST00000706876, ENST00000706877, ENST00000706878, ENST00000706879, ENST00000706880, ENST00000706881, ENST00000706882, ENST00000718334, ENST00000718335, ENST00000894943, ENST00000894944, ENST00000894945, ENST00000894946, ENST00000894947, ENST00000894948, ENST00000894949, ENST00000894950, ENST00000960839, ENST00000960840, ENST00000960841

RefSeq mRNA: 1 — MANE Select: NM_013379 NM_013379

CCDS: CCDS7030

Canonical transcript exons

ENST00000371579 — 13 exons

Exon	Start	End
ENSE00001455574	137114647	137114733
ENSE00001923377	137114463	137114576
ENSE00003495678	137114243	137114382
ENSE00003538243	137113361	137113496
ENSE00003567909	137113206	137113287
ENSE00003570670	137112953	137113119
ENSE00003576072	137112112	137112230
ENSE00003609068	137113865	137114028
ENSE00003670167	137112745	137112805
ENSE00004034807	137111690	137111754
ENSE00004034808	137111873	137112029
ENSE00004034809	137110546	137110783
ENSE00004034810	137110880	137110950

Expression profiles

Bgee: expression breadth ubiquitous, 243 present calls, max score 99.31.

FANTOM5 (CAGE): breadth ubiquitous, TPM avg 61.1705 / max 398.7661, expressed in 1755 samples.

FANTOM5 promoters (1 alternative TSS)

Promoter ID	TPM avg	Samples expressed
103305	61.1705	1755

Top tissues by expression

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

Tissue	Anatomy ID	Expression score	Quality
adenohypophysis	UBERON:0002196	99.31	gold quality
right hemisphere of cerebellum	UBERON:0014890	99.14	gold quality
right uterine tube	UBERON:0001302	99.07	gold quality
granulocyte	CL:0000094	99.00	gold quality
right lobe of thyroid gland	UBERON:0001119	98.95	gold quality
cerebellar hemisphere	UBERON:0002245	98.93	gold quality
left testis	UBERON:0004533	98.93	gold quality
left lobe of thyroid gland	UBERON:0001120	98.91	gold quality
apex of heart	UBERON:0002098	98.91	gold quality
right testis	UBERON:0004534	98.91	gold quality
right frontal lobe	UBERON:0002810	98.88	gold quality
cerebellar cortex	UBERON:0002129	98.84	gold quality
left adrenal gland cortex	UBERON:0035825	98.72	gold quality
Brodmann (1909) area 9	UBERON:0013540	98.69	gold quality
right adrenal gland cortex	UBERON:0035827	98.64	gold quality
pituitary gland	UBERON:0000007	98.62	gold quality
left adrenal gland	UBERON:0001234	98.61	gold quality
right atrium auricular region	UBERON:0006631	98.59	gold quality
lower esophagus mucosa	UBERON:0035834	98.58	gold quality
C1 segment of cervical spinal cord	UBERON:0006469	98.54	gold quality
right adrenal gland	UBERON:0001233	98.50	gold quality
minor salivary gland	UBERON:0001830	98.49	gold quality
anterior cingulate cortex	UBERON:0009835	98.44	gold quality
body of stomach	UBERON:0001161	98.32	gold quality
metanephros cortex	UBERON:0010533	98.32	gold quality
muscle layer of sigmoid colon	UBERON:0035805	98.31	gold quality
olfactory segment of nasal mucosa	UBERON:0005386	98.23	gold quality
esophagogastric junction muscularis propria	UBERON:0035841	98.20	gold quality
right coronary artery	UBERON:0001625	98.19	gold quality
lower esophagus	UBERON:0013473	98.19	gold quality

Single-cell (SCXA)

Detected in 4 experiment(s), a significant marker in 3.

Experiment	Marker?	Max mean expression
E-HCAD-13	yes	11.77
E-GEOD-93593	yes	4.01
E-MTAB-9221	no	685.06
E-ANND-3	no	0.00

Regulation

Is transcription factor: no

Upstream regulators (CollecTRI, top): KLF2

Literature-anchored findings (GeneRIF, showing 5)

• catalytic properties and inhibition of this proline-specific enzyme (PMID:12529175)
• DPP II plays a minor role in the progression of malignant melanocytic lesions (PMID:18823758)
• DPP2 is essential for maintaining lymphocytes and fibroblasts in G(0), and its inhibition results in apoptosis mediated by induction of c-Myc and p53. (PMID:19556882)
• The constitutive expression of dipeptidyl peptidase II mRNA in chronic lymphocytic leukemia was demonstrated. (PMID:20534982)
• human DPP7 structures reveal the molecular basis of specific inhibition and the architectural diversity of proline-specific peptidases (PMID:22952628)

Cross-species orthologs

8 orthologs

Organism	Symbol	Gene ID
danio_rerio	dpp7	ENSDARG00000027750
mus_musculus	Dpp7	ENSMUSG00000026958
rattus_norvegicus	Dpp7	ENSRNOG00000012640
drosophila_melanogaster	CG3734	FBGN0038700
drosophila_melanogaster	CG18493	FBGN0038701
drosophila_melanogaster	CG3739	FBGN0038702
drosophila_melanogaster	CG11626	FBGN0038705
caenorhabditis_elegans		WBGENE00019682

Paralogs (2): PRSS16 (ENSG00000112812), PRCP (ENSG00000137509)

Protein

Protein identifiers

Dipeptidyl peptidase 2 — Q9UHL4 (reviewed: Q9UHL4)

Alternative names: Dipeptidyl aminopeptidase II, Dipeptidyl peptidase 7, Dipeptidyl peptidase II, Quiescent cell proline dipeptidase

All UniProt accessions (6): A0A9L9PXE7, A0A9L9PXM1, A0A9L9PY12, Q9UHL4, R4GMV4, R4GN05

UniProt curated annotations — full annotation on UniProt →

Function. Plays an important role in the degradation of some oligopeptides.

Subunit / interactions. Homodimer.

Subcellular location. Lysosome. Cytoplasmic vesicle. Secreted.

Tissue specificity. Detected in seminal plasma (at protein level).

Post-translational modifications. N-glycosylated.

Similarity. Belongs to the peptidase S28 family.

RefSeq proteins (1): NP_037511* (*=MANE)

Domains & families (InterPro)

ID	Name	Type
IPR008758	Peptidase_S28	Family
IPR029058	AB_hydrolase_fold	Homologous_superfamily
IPR042269	Ser_carbopepase_S28_SKS	Homologous_superfamily

Pfam: PF05577

Enzyme classification (BRENDA):

• EC 3.4.14.2 — dipeptidyl-peptidase II (BRENDA: 10 organisms, 103 substrates, 205 inhibitors, 54 Km, 32 kcat entries)

Substrate kinetics (BRENDA)

37 substrates with measured Km, best-characterized 15. Km ranges are aggregated across organisms/conditions.

Substrate	Km (mM)	Measurements
GLY-PRO-4-NITROANILIDE	0.018–0.59	5
LYS-ALA-2-NAPHTHYLAMIDE	0.087–0.555	4
ALA-PRO-P-NITROANILIDE	0.009–0.041	3
GLY-PRO-P-NITROANILIDE	0.07–0.227	3
ALA-ALA-4-NITROANILIDE	0.487–1.22	2
ARG-PRO-4-NITROANILIDE	0.068–0.086	2
GLY-L-PRO-4-NITROANILIDE	0.36–1.1	2
L-LYS-L-ALA-7-AMIDO-4-METHYLCOUMARIN	0.36–0.93	2
LYS-ALA-P-NITROANILIDE	0.04–0.57	2
LYS-PRO-P-NITROANILIDE	0.019	2
ALA-ALA-ALA	1.67	1
ALA-PRO-4-NITROANILIDE	0.0457	1
ALA-PRO-AMINO-4-TRIFLUOROMETHYLCOUMARIN	0.032	1
ARG-PRO-2-NAPHTHYLAMIDE	0.0086	1
ARG-PRO-P-NITROANILIDE	0.04	1

UniProt features (50 total): helix 19, strand 13, glycosylation site 6, turn 4, active site 3, signal peptide 1, propeptide 1, sequence variant 1, sequence conflict 1, chain 1

Structure

Experimental structures (PDB)

3 structures.

PDB	Method	Resolution (Å)
4EBB	X-RAY DIFFRACTION	2
3JYH	X-RAY DIFFRACTION	2.19
3N0T	X-RAY DIFFRACTION	2.45

Predicted structure (AlphaFold)

Model	pLDDT	Fraction very-high
AF-Q9UHL4-F1	94.44	0.92

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 (3): 162 (charge relay system); 418 (charge relay system); 443 (charge relay system)

Glycosylation sites (6): 363, 428, 50, 86, 315, 356

Function

Pathways and Gene Ontology

Reactome pathways

1 pathways

ID	Pathway
R-HSA-6798695	Neutrophil degranulation

MSigDB gene sets: 145 (showing top): REACTOME_INNATE_IMMUNE_SYSTEM, GOCC_SECRETORY_GRANULE, MODULE_151, GRAESSMANN_APOPTOSIS_BY_DOXORUBICIN_UP, GRAESSMANN_RESPONSE_TO_MC_AND_DOXORUBICIN_UP, GOBP_MACROMOLECULE_CATABOLIC_PROCESS, SHETH_LIVER_CANCER_VS_TXNIP_LOSS_PAM1, GROSS_HYPOXIA_VIA_ELK3_UP, BYSTRYKH_HEMATOPOIESIS_STEM_CELL_AND_BRAIN_QTL_CIS, KINSEY_TARGETS_OF_EWSR1_FLII_FUSION_DN, GOBP_PROTEIN_CATABOLIC_PROCESS, BURTON_ADIPOGENESIS_9, MODULE_114, GOCC_SECRETORY_VESICLE, GOCC_VESICLE_LUMEN

GO Biological Process (2): proteolysis (GO:0006508), lysosomal protein catabolic process (GO:1905146)

GO Molecular Function (6): aminopeptidase activity (GO:0004177), serine-type peptidase activity (GO:0008236), dipeptidyl-peptidase activity (GO:0008239), serine-type exopeptidase activity (GO:0070008), peptidase activity (GO:0008233), hydrolase activity (GO:0016787)

GO Cellular Component (7): extracellular region (GO:0005576), Golgi apparatus (GO:0005794), vesicle (GO:0031982), azurophil granule lumen (GO:0035578), extracellular exosome (GO:0070062), lysosome (GO:0005764), cytoplasmic vesicle (GO:0031410)

Reactome top-level categories

Rollup of top-1 pathways:

Category	Pathways
Innate Immune System	1

GO top-level categories

Rollup of top GO terms by namespace:

Category	Terms
exopeptidase activity	3
cytoplasm	2
protein metabolic process	1
lysosome	1
protein catabolic process in the vacuole	1
peptidase activity	1
serine hydrolase activity	1
serine-type peptidase activity	1
hydrolase activity	1
catalytic activity, acting on a protein	1
catalytic activity	1
cellular anatomical structure	1
endomembrane system	1
intracellular membrane-bounded organelle	1
membrane-bounded organelle	1
vacuolar lumen	1
secretory granule lumen	1
azurophil granule	1
extracellular vesicle	1
lytic vacuole	1
intracellular vesicle	1

Protein interactions and networks

STRING

996 interactions, top by confidence (×1000):

Protein A	Protein B	Partner UniProt	Score
DPP7	DPP8	Q6V1X1	878
DPP7	DPP9	Q86TI2	877
DPP7	DPP4	P27487	871
DPP7	TIMM8B	Q9Y5J9	844
DPP7	TIMM8A	O60220	762
DPP7	PREP	P48147	710
DPP7	DPP3	Q9NY33	692
DPP7	FAP	Q12884	680
DPP7	SDHD	O14521	650
DPP7	SDHC	Q99643	648
DPP7	CTSC	P53634	646
DPP7	PEPD	P12955	632
DPP7	SDHB	P21912	632
DPP7	DPP10	Q8N608	556
DPP7	GOLGA3	Q08378	532

IntAct

42 interactions, top by confidence:

A	B	Type	Score
DPP7	CFTR	psi-mi:“MI:0915”(physical association)	0.370
DPP7		psi-mi:“MI:0915”(physical association)	0.370
DPP7	TFAP2A	psi-mi:“MI:0915”(physical association)	0.370
DPP7	TFAP2C	psi-mi:“MI:0915”(physical association)	0.370
	ESYT2	psi-mi:“MI:0914”(association)	0.350
	PGRMC1	psi-mi:“MI:0914”(association)	0.350
	HAX1	psi-mi:“MI:0914”(association)	0.350
BFRF1A	SHTN1	psi-mi:“MI:0914”(association)	0.350
SPHK1	TAF4	psi-mi:“MI:0914”(association)	0.350
APP	RTL1	psi-mi:“MI:0914”(association)	0.350
RASA1		psi-mi:“MI:0914”(association)	0.350
DOK2	MYO1C	psi-mi:“MI:0914”(association)	0.350
RAB5A	PSMD14	psi-mi:“MI:0914”(association)	0.350
RASA1	MYO1C	psi-mi:“MI:0914”(association)	0.350
SH2D3C	ANXA2P2	psi-mi:“MI:0914”(association)	0.350
SH3GL3	RBFOX3	psi-mi:“MI:0914”(association)	0.350
CSK	HSPB1	psi-mi:“MI:0914”(association)	0.350
ABI1	HSPB1	psi-mi:“MI:0914”(association)	0.350
PTPN12	HSPB1	psi-mi:“MI:0914”(association)	0.350
PRKCE	PAPSS1	psi-mi:“MI:0914”(association)	0.350
DOK2	ARPC2	psi-mi:“MI:0914”(association)	0.350
HCK	MAGEB2	psi-mi:“MI:0914”(association)	0.350
RAB5A	EIF3CL	psi-mi:“MI:0914”(association)	0.350
MAP2K1	SLC16A3	psi-mi:“MI:0914”(association)	0.350
TRIM24	DDTL	psi-mi:“MI:0914”(association)	0.350
	VPS37C	psi-mi:“MI:0914”(association)	0.350
MAPT	SHTN1	psi-mi:“MI:0914”(association)	0.350

BioGRID (40): DPP7 (Affinity Capture-RNA), DPP7 (Affinity Capture-MS), DPP7 (Affinity Capture-MS), DPP7 (Affinity Capture-MS), DPP7 (Affinity Capture-MS), DPP7 (Affinity Capture-MS), DPP7 (Affinity Capture-MS), DPP7 (Affinity Capture-MS), DPP7 (Affinity Capture-MS), DPP7 (Affinity Capture-MS), DPP7 (Affinity Capture-MS), DPP7 (Affinity Capture-MS), DPP7 (Affinity Capture-MS), DPP7 (Affinity Capture-MS), TRIM24 (Affinity Capture-MS)

ESM2 similar proteins: A4FV98, A5PK51, A6NDG6, E1BE10, O00587, O35595, O95294, P60487, Q12788, Q17QS4, Q1JPJ0, Q2T9S4, Q2TBI8, Q32NY4, Q3T063, Q3ZBF9, Q501J2, Q5E9V4, Q5F4B1, Q5IS64, Q5SUV1, Q5T9C9, Q6AYG0, Q6AYR8, Q6XQN1, Q6XQN6, Q6ZMM2, Q80US4, Q8BNV1, Q8BZG5, Q8CC86, Q8IZ69, Q8N9H8, Q8NE01, Q8R2H9, Q8TCT1, Q8VCA8, Q8VD52, Q969S8, Q96AZ1

Diamond homologs: D4AYS6, P34610, P34676, P42785, Q1PF50, Q2TA14, Q5RBU7, Q7TMR0, Q9EPB1, Q9ET22, Q9NQE7, Q9QXE5, Q9UHL4, W7DQR8, P34528

SIGNOR signaling

0 interactions.

Enriched among interaction partners

Reactome pathways and GO biological processes over-represented among this gene’s 49 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
Signaling by Receptor Tyrosine Kinases	5	8.1×	1e-02
Infectious disease	7	5.4×	8e-03

Disease & clinical

Clinical variants and AI predictions

ClinVar

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

Classification	Count (floor)
Pathogenic	0
Likely pathogenic	0
Uncertain significance	134
Likely benign	8
Benign	0

Top pathogenic / likely-pathogenic (0)

SpliceAI

1740 predictions. Top by Δscore:

Variant	Effect	Δscore
9:137110782:CT:C	acceptor_gain	1.0000
9:137110784:C:CC	acceptor_gain	1.0000
9:137110870:C:A	donor_gain	1.0000
9:137110874:CCGCA:C	donor_loss	1.0000
9:137110875:CGCA:C	donor_loss	1.0000
9:137110876:GCAC:G	donor_loss	1.0000
9:137110877:CA:C	donor_loss	1.0000
9:137110879:C:CT	donor_loss	1.0000
9:137110946:CGAAT:C	acceptor_gain	1.0000
9:137110951:C:CA	acceptor_loss	1.0000
9:137110951:C:CC	acceptor_gain	1.0000
9:137110958:C:CT	acceptor_gain	1.0000
9:137110959:A:T	acceptor_gain	1.0000
9:137111871:ACCAC:A	donor_gain	1.0000
9:137111872:CCACC:C	donor_gain	1.0000
9:137111920:C:CA	donor_gain	1.0000
9:137111921:C:A	donor_gain	1.0000
9:137111940:CCG:C	donor_gain	1.0000
9:137112123:AGGC:A	donor_gain	1.0000
9:137112126:C:CA	donor_gain	1.0000
9:137112947:CCTCA:C	donor_loss	1.0000
9:137112948:CTCA:C	donor_loss	1.0000
9:137112949:TCA:T	donor_loss	1.0000
9:137112950:CA:C	donor_loss	1.0000
9:137112952:C:CT	donor_loss	1.0000
9:137113116:TAGG:T	acceptor_gain	1.0000
9:137113116:TAGGC:T	acceptor_loss	1.0000
9:137113117:AGGC:A	acceptor_loss	1.0000
9:137113118:GG:G	acceptor_gain	1.0000
9:137113118:GGCT:G	acceptor_loss	1.0000

AlphaMissense

3187 scored. Top likely-pathogenic:

Variant	Protein change	am_pathogenicity
9:137112121:C:A	W347C	0.998
9:137112121:C:G	W347C	0.998
9:137111977:A:C	F368C	0.997
9:137112025:C:T	C352Y	0.997
9:137110896:G:C	H443D	0.996
9:137111935:C:G	C382S	0.996
9:137111936:A:T	C382S	0.996
9:137112024:G:C	C352W	0.996
9:137112025:C:G	C352S	0.996
9:137112026:A:T	C352S	0.996
9:137111934:G:C	C382W	0.995
9:137111935:C:T	C382Y	0.994
9:137112123:A:G	W347R	0.994
9:137112123:A:T	W347R	0.994
9:137111709:T:A	D418V	0.993
9:137111709:T:C	D418G	0.993
9:137111976:G:C	F368L	0.993
9:137111976:G:T	F368L	0.993
9:137111978:A:G	F368L	0.993
9:137112026:A:G	C352R	0.993
9:137113424:G:C	S186R	0.993
9:137113424:G:T	S186R	0.993
9:137113425:C:A	S186I	0.993
9:137113426:T:G	S186R	0.993
9:137113467:C:A	R172M	0.993
9:137111702:C:A	W420C	0.992
9:137111702:C:G	W420C	0.992
9:137111710:C:G	D418H	0.992
9:137111719:C:A	G415W	0.992
9:137111977:A:G	F368S	0.992

dbSNP variants (sampled 300 via entrez): RS1000152032 (9:137110936 C>G,T), RS1000534307 (9:137117961 G>A), RS1000928527 (9:137113788 G>A,T), RS1001201395 (9:137110049 G>A,C), RS1001229725 (9:137112337 C>T), RS1001307640 (9:137115857 G>T), RS1002118424 (9:137120029 A>G), RS1002310082 (9:137116722 T>C), RS1002977899 (9:137115207 C>T), RS1003028459 (9:137115388 T>G), RS1003072095 (9:137115964 C>T), RS1003086269 (9:137119272 A>C), RS1003311379 (9:137111616 C>A,G,T), RS1003322320 (9:137110404 GCGTTGTGGAGCCTCTA>G), RS1003405750 (9:137115230 G>A)

Disease associations

OMIM: gene MIM:610537 | disease phenotypes: MIM:614254

GenCC curated gene-disease

Mondo (1): neurodevelopmental disorder with or without hyperkinetic movements and seizures, autosomal dominant (MONDO:0013655)

Orphanet (0):

HPO phenotypes

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

GWAS associations

1 associations (top):

Study	Trait	p-value
GCST005024_58	Pursuit maintenance gain	2.000000e-06

EFO canonical traits (1, from GWAS)

EFO ID	Trait name
EFO:0008433	pursuit maintenance gain measurement

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (2): CHEMBL2111469 (SELECTIVITY GROUP), CHEMBL3976 (SINGLE PROTEIN)

Molecules with ChEMBL bioactivity

3 molecules (phase ≥1), by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 37,626 (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
CHEMBL1422	SITAGLIPTIN	4	26,582
CHEMBL515387	GOSOGLIPTIN	4	785
CHEMBL67279	TALABOSTAT	3	10,259

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

GtoPdb / IUPHAR curated pharmacology

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

Target class: enzyme — S28: Lysosomal Pro-Xaa carboxypeptidase

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

Ligand	Action	Affinity	Parameter
UAMC00039	Inhibition	10.1	pKi

Binding affinities (BindingDB)

319 measured of 465 human assays (468 total across all organisms); most potent 50 below. Values come from heterogeneous assays and are not directly comparable.

Ligand	Measure	Value	Patent
(2S)-1-{2-[(3-hydroxyadamantan-1-yl)amino]acetyl}pyrrolidine-2-carbonitrile	IC50	51 nM
(2S,3S)-3-{4-[3-(5-cyclopropyl-1,2,4-oxadiazol-3-yl)phenyl]phenyl}-1-[(3S)-3-fluoropyrrolidin-1-yl]-1-oxobutan-2-aminium; 2,2,2-trifluoroacetate	IC50	96 nM
(2S,3S)-3-{4-[4-(ethoxycarbonyl)phenyl]phenyl}-1-[(3S)-3-fluoropyrrolidin-1-yl]-1-oxobutan-2-aminium; 2,2,2-trifluoroacetate	IC50	120 nM
oxadiazole based amide	IC50	160 nM
(2S,3S)-1-[(3S)-3-fluoropyrrolidin-1-yl]-3-[4-(3-methanesulfonamidophenyl)phenyl]-1-oxobutan-2-aminium; 2,2,2-trifluoroacetate	IC50	250 nM
(2S,3S)-1-[(3S)-3-fluoropyrrolidin-1-yl]-3-[4-(4-methoxyphenyl)phenyl]-1-oxobutan-2-aminium; 2,2,2-trifluoroacetate	IC50	330 nM
(2S,3S)-1-[(3S)-3-fluoropyrrolidin-1-yl]-1-oxo-3-{4-[3-(1H-1,2,4-triazol-3-yl)phenyl]phenyl}butan-2-aminium; 2,2,2-trifluoroacetate	IC50	350 nM
1-[(1-Adamantylamino)acetyl]-2-pyrrolidinecarbonitrile	IC50	350 nM
(2S,3S)-3-[4-(2-chlorophenyl)phenyl]-1-[(3S)-3-fluoropyrrolidin-1-yl]-1-oxobutan-2-aminium; 2,2,2-trifluoroacetate	IC50	380 nM
(2S,3S)-3-{4-[3-(ethoxycarbonyl)phenyl]phenyl}-1-[(3S)-3-fluoropyrrolidin-1-yl]-1-oxobutan-2-aminium; 2,2,2-trifluoroacetate	IC50	490 nM
(2S,3S)-1-(3,3-difluoropyrrolidin-1-yl)-3-[4-(1-methyl-6-oxo-1,6-dihydropyridin-3-yl)phenyl]-1-oxobutan-2-aminium; 2,2,2-trifluoroacetate	IC50	550 nM
N-[2-(2-cyanopyrrolidin-1-yl)-2-oxoethyl]isoquinoline-4-carboxamide	IC50	610 nM	US-9346814: FAP inhibitors
(2S,3S)-1-[(3S)-3-fluoropyrrolidin-1-yl]-1-oxo-3-{4-[4-(trifluoromethyl)phenyl]phenyl}butan-2-aminium; 2,2,2-trifluoroacetate	IC50	670 nM
(2S,3R)-3-[4-(4-fluorophenyl)phenyl]-1-[(3S)-3-fluoropyrrolidin-1-yl]-1-oxo-4-(pyrrolidin-1-yl)butan-2-aminium; 2,2,2-trifluoroacetate	IC50	700 nM
(2S,3S)-1-[(3S)-3-fluoropyrrolidin-1-yl]-1-oxo-3-[4-(1,3-thiazol-2-yl)phenyl]butan-2-aminium; 2,2,2-trifluoroacetate	IC50	720 nM
(2S,3S)-3-[4-(1-methyl-6-oxo-1,6-dihydropyridin-3-yl)phenyl]-1-oxo-1-(1,3-thiazolidin-3-yl)butan-2-aminium; 2,2,2-trifluoroacetate	IC50	810 nM
(2S,3S)-3-[4-(3-carbamoylphenyl)phenyl]-1-[(3S)-3-fluoropyrrolidin-1-yl]-1-oxobutan-2-aminium; 2,2,2-trifluoroacetate	IC50	820 nM
(2S,3S)-1-[(3S)-3-fluoropyrrolidin-1-yl]-1-oxo-3-{4-[3-(2-oxo-2,3-dihydro-1H-imidazol-4-yl)phenyl]phenyl}butan-2-aminium; 2,2,2-trifluoroacetate	IC50	830 nM
(2S,3S)-3-[5-(2,4-dichlorophenyl)-1,3,4-oxadiazol-2-yl]-1-oxo-1-(pyrrolidin-1-yl)butan-2-aminium; 2,2,2-trifluoroacetate	IC50	850 nM
N-[2-[(2S)-2-cyanopyrrolidin-1-yl]-2-oxoethyl]quinoline-4-carboxamide	IC50	860 nM	US-9346814: FAP inhibitors
(2S,3S)-1-[(3S)-3-fluoropyrrolidin-1-yl]-1-oxo-3-{4-[3-(1H-1,2,3,4-tetrazol-1-yl)phenyl]phenyl}butan-2-aminium; 2,2,2-trifluoroacetate	IC50	870 nM
(2S,3S)-1-[(3S)-3-fluoropyrrolidin-1-yl]-3-{4-[3-(1,3,4-oxadiazol-2-yl)phenyl]phenyl}-1-oxobutan-2-aminium; 2,2,2-trifluoroacetate	IC50	960 nM
oxadiazole based amide	IC50	1000 nM
9.8k	IC50	1040 nM
(2S,3S)-3-[4-(2,4-dichlorophenyl)-1,3-oxazol-2-yl]-1-oxo-1-(pyrrolidin-1-yl)butan-2-aminium; 2,2,2-trifluoroacetate	IC50	1050 nM
(2S,3S)-1-(4-fluoropiperidin-1-yl)-3-[4-(1-methyl-6-oxo-1,6-dihydropyridin-3-yl)phenyl]-1-oxobutan-2-aminium; 2,2,2-trifluoroacetate	IC50	1100 nM
(2S,3S)-3-[4-(2-fluorophenyl)phenyl]-1-[(3S)-3-fluoropyrrolidin-1-yl]-1-oxobutan-2-aminium; 2,2,2-trifluoroacetate	IC50	1100 nM
(2S,3S)-1-[(3S)-3-fluoropyrrolidin-1-yl]-3-[4-(4-methylphenyl)phenyl]-1-oxobutan-2-aminium; 2,2,2-trifluoroacetate	IC50	1100 nM
(2S,3S)-1-[(3S)-3-fluoropyrrolidin-1-yl]-1-oxo-3-{4-[3-(5-oxo-4,5-dihydro-1H-1,2,4-triazol-3-yl)phenyl]phenyl}butan-2-aminium; 2,2,2-trifluoroacetate	IC50	1100 nM
(2S,3S)-1-[(3S)-3-fluoropyrrolidin-1-yl]-1-oxo-3-{4-[3-(5-oxo-4,5-dihydro-1,2,4-oxadiazol-3-yl)phenyl]phenyl}butan-2-aminium; 2,2,2-trifluoroacetate	IC50	1100 nM
(2S,3S)-1-[(3S)-3-fluoropyrrolidin-1-yl]-3-[4-(4-methanesulfonylphenyl)phenyl]-1-oxobutan-2-aminium; 2,2,2-trifluoroacetate	IC50	1200 nM
(2S,3S)-1-[(3S)-3-fluoropyrrolidin-1-yl]-1-oxo-3-{4-[3-(trifluoromethanesulfonamido)phenyl]phenyl}butan-2-aminium; 2,2,2-trifluoroacetate	IC50	1300 nM
(2S,3S)-3-[4-(2,5-difluorophenyl)phenyl]-1-[(3S)-3-fluoropyrrolidin-1-yl]-1-oxobutan-2-aminium; 2,2,2-trifluoroacetate	IC50	1300 nM
oxadiazole based amide	IC50	1300 nM
9.7g	IC50	1300 nM
(2S,3S)-2-amino-3-[3-(2,4-dichlorophenyl)-1,2,4-oxadiazol-5-yl]-1-(pyrrolidin-1-yl)butan-1-one	IC50	1400 nM
oxadiazole based amide	IC50	1400 nM
(2S,3S)-1-[(3S)-3-fluoropyrrolidin-1-yl]-1-oxo-3-[4-(1H-pyrazol-1-yl)phenyl]butan-2-aminium; 2,2,2-trifluoroacetate	IC50	1500 nM
(2S,3S)-3-[3-(2-chloro-4-methanesulfonamidophenyl)-1,2,4-oxadiazol-5-yl]-1-[(3R)-3-fluoropyrrolidin-1-yl]-1-oxobutan-2-aminium; 2,2,2-trifluoroacetate	IC50	1700 nM
(2S,3S)-3-[3-(2-chloro-4-methanesulfonylphenyl)-1,2,4-oxadiazol-5-yl]-4-cyclopropyl-1-[(3S)-3-fluoropyrrolidin-1-yl]-1-oxobutan-2-aminium; 2,2,2-trifluoroacetate	IC50	1700 nM
(2S,3S)-1-[(3S)-3-fluoropyrrolidin-1-yl]-3-[4-(4-methanesulfonamidophenyl)phenyl]-1-oxobutan-2-aminium; 2,2,2-trifluoroacetate	IC50	1800 nM
(2S,3S)-2-amino-1-(pyrrolidin-1-yl)-3-{3-[2-(trifluoromethyl)phenyl]-1,2,4-oxadiazol-5-yl}butan-1-one	IC50	1800 nM
(3R)-3-amino-4-(2,5-difluorophenyl)-1-{2-[4-(methylsulfanyl)phenyl]-4H,5H,6H,7H-pyrido[4,3-d][1,3]thiazol-5-yl}butan-1-one	IC50	1900 nM
(2S,3S)-3-[4-(3,5-difluorophenyl)phenyl]-1-[(3S)-3-fluoropyrrolidin-1-yl]-1-oxobutan-2-aminium; 2,2,2-trifluoroacetate	IC50	2000 nM
(2S,3S)-3-[4-(3,4-difluorophenyl)phenyl]-1-[(3S)-3-fluoropyrrolidin-1-yl]-1-oxobutan-2-aminium; 2,2,2-trifluoroacetate	IC50	2000 nM
2-(adamantan-1-ylamino)-1-[(S)-2-(5-methyl-[1,3,4]oxadiazole-2-carbonyl)-pyrrolidin-1-yl]-ethanone	IC50	2070 nM
(2S,3S)-3-{4-[1-(4-fluorophenyl)-6-oxo-1,6-dihydropyridin-3-yl]phenyl}-1-[(3S)-3-fluoropyrrolidin-1-yl]-1-oxobutan-2-aminium; 2,2,2-trifluoroacetate	IC50	2100 nM
(2S,3S)-2-amino-3-[3-(2-chlorophenyl)-1,2,4-oxadiazol-5-yl]-1-(pyrrolidin-1-yl)butan-1-one	IC50	2200 nM
N-[2-(2-cyanopyrrolidin-1-yl)-2-oxoethyl]quinoline-4-carboxamide	IC50	2400 nM	US-9346814: FAP inhibitors
(2S,3S)-3-{4-[1-(2-ethoxy-1,1-difluoro-2-oxoethyl)-6-oxo-1,6-dihydropyridin-3-yl]phenyl}-1-[(3S)-3-fluoropyrrolidin-1-yl]-1-oxobutan-2-aminium; 2,2,2-trifluoroacetate	IC50	2500 nM

ChEMBL bioactivities

647 potent at pChembl≥5 of 1214 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).

pChembl	Type	Value	Unit	Molecule
10.09	Ki	0.082	nM	CHEMBL98869
10.09	Ki	0.082	nM	CHEMBL5723377
9.85	IC50	0.14	nM	CHEMBL5723377
9.68	IC50	0.21	nM	CHEMBL5723377
9.66	IC50	0.22	nM	CHEMBL98869
9.66	IC50	0.22	nM	CHEMBL98801
9.64	IC50	0.23	nM	CHEMBL98762
9.41	IC50	0.39	nM	CHEMBL99506
9.41	IC50	0.39	nM	CHEMBL418979
9.39	IC50	0.41	nM	CHEMBL99247
9.32	IC50	0.48	nM	CHEMBL194354
9.32	IC50	0.48	nM	CHEMBL398076
9.32	IC50	0.48	nM	CHEMBL5723377
9.32	IC50	0.48	nM	CHEMBL98869
9.26	IC50	0.55	nM	CHEMBL98148
9.22	IC50	0.6	nM	CHEMBL97970
9.21	IC50	0.62	nM	CHEMBL215299
9.21	IC50	0.62	nM	CHEMBL98060
9.18	IC50	0.66	nM	CHEMBL99047
9.14	IC50	0.72	nM	CHEMBL194428
9.12	IC50	0.75	nM	CHEMBL99111
9.10	IC50	0.8	nM	CHEMBL98423
9.06	IC50	0.88	nM	CHEMBL397057
9.05	IC50	0.9	nM	CHEMBL317312
9.00	IC50	1	nM	CHEMBL372180
8.96	IC50	1.1	nM	CHEMBL98860
8.96	IC50	1.1	nM	CHEMBL100370
8.96	IC50	1.1	nM	CHEMBL97977
8.95	IC50	1.13	nM	CHEMBL317950
8.88	IC50	1.31	nM	CHEMBL97884
8.87	IC50	1.34	nM	CHEMBL317949
8.82	IC50	1.5	nM	CHEMBL98415
8.82	IC50	1.5	nM	CHEMBL440325
8.75	IC50	1.77	nM	CHEMBL327499
8.74	IC50	1.8	nM	CHEMBL196933
8.74	IC50	1.8	nM	CHEMBL101401
8.72	IC50	1.91	nM	CHEMBL430661
8.70	IC50	2	nM	CHEMBL194852
8.69	IC50	2.03	nM	CHEMBL99263
8.66	IC50	2.2	nM	CHEMBL196267
8.64	IC50	2.3	nM	CHEMBL319520
8.57	IC50	2.7	nM	CHEMBL237336
8.57	IC50	2.7	nM	CHEMBL330600
8.57	IC50	2.7	nM	CHEMBL99260
8.47	IC50	3.4	nM	CHEMBL215244
8.43	IC50	3.7	nM	CHEMBL194517
8.42	IC50	3.8	nM	CHEMBL214630
8.40	IC50	4	nM	CHEMBL382974
8.40	IC50	4	nM	CHEMBL329314
8.39	IC50	4.1	nM	CHEMBL371130

PubChem BioAssay actives

728 with measured affinity, of 2395 total; 50 most potent distinct compounds. Largely complementary to BindingDB; screening values are coarse (µM, 4 dp), so sub-nM hits tie at the floor.

Compound	Assay	Type	Value	Unit
(2S)-2-amino-4-[(4-chlorophenyl)methylamino]-1-piperidin-1-ylbutan-1-one	343975: Inhibition of DPP2	ki	0.0001	uM
(2S)-2-amino-4-[(4-chlorophenyl)methyl-methylamino]-1-piperidin-1-ylbutan-1-one	56221: Inhibition of human Dipeptidylpeptidase II (DPP II)	ic50	0.0002	uM
(2S)-2-amino-4-[(2-chlorophenyl)methylamino]-1-piperidin-1-ylbutan-1-one	56221: Inhibition of human Dipeptidylpeptidase II (DPP II)	ic50	0.0002	uM
(2S)-2-amino-4-[(4-phenylmethoxyphenyl)methylamino]-1-piperidin-1-ylbutan-1-one	56221: Inhibition of human Dipeptidylpeptidase II (DPP II)	ic50	0.0004	uM
(2S)-2-amino-4-[(2-phenylmethoxyphenyl)methylamino]-1-piperidin-1-ylbutan-1-one	56221: Inhibition of human Dipeptidylpeptidase II (DPP II)	ic50	0.0004	uM
(2S)-2-amino-4-[(4-chlorophenyl)methylamino]-1-(4-fluoropiperidin-1-yl)butan-1-one	56221: Inhibition of human Dipeptidylpeptidase II (DPP II)	ic50	0.0004	uM
[(1R)-1-[[(2S)-2,4-diaminobutanoyl]amino]pentyl]boronic acid	305098: Inhibition of human DPP2	ic50	0.0005	uM
[(1S)-1-[[(2S)-2,4-diaminobutanoyl]amino]pentyl]boronic acid	254911: Inhibitory concentration against human dipeptidylpeptidase 7	ic50	0.0005	uM
(2S)-2-amino-4-[(4-chlorophenyl)methylamino]-1-(4-methylpiperidin-1-yl)butan-1-one	56221: Inhibition of human Dipeptidylpeptidase II (DPP II)	ic50	0.0006	uM
(2S)-2-amino-4-[(4-chlorophenyl)methylamino]-1-(3-fluoropiperidin-1-yl)butan-1-one	56221: Inhibition of human Dipeptidylpeptidase II (DPP II)	ic50	0.0006	uM
(2S)-2-amino-4-(dibenzylamino)-1-piperidin-1-ylbutan-1-one	56221: Inhibition of human Dipeptidylpeptidase II (DPP II)	ic50	0.0006	uM
(2S,4S)-2-amino-4-[(4-chlorophenyl)methylamino]-1-piperidin-1-ylpentan-1-one	270815: Inhibition of DPP2	ic50	0.0006	uM
(2S)-2-amino-4-[(4-methoxyphenyl)methylamino]-1-piperidin-1-ylbutan-1-one	56221: Inhibition of human Dipeptidylpeptidase II (DPP II)	ic50	0.0007	uM
[(2S)-1-[(2S)-2,4-diaminobutanoyl]pyrrolidin-2-yl]boronic acid	254911: Inhibitory concentration against human dipeptidylpeptidase 7	ic50	0.0007	uM
(2S)-2-amino-1-piperidin-1-yl-4-(thiophen-2-ylmethylamino)butan-1-one	56221: Inhibition of human Dipeptidylpeptidase II (DPP II)	ic50	0.0008	uM
(2S)-2-amino-1-piperidin-1-yl-4-(pyridin-4-ylmethylamino)butan-1-one	56221: Inhibition of human Dipeptidylpeptidase II (DPP II)	ic50	0.0008	uM
(2S)-2-amino-4-(2-phenylethylamino)-1-piperidin-1-ylbutan-1-one	56221: Inhibition of human Dipeptidylpeptidase II (DPP II)	ic50	0.0009	uM
(2S)-1-[(3aR,6aR)-3,3a,4,5,6,6a-hexahydro-2H-cyclopenta[b]pyrrol-1-yl]-2,4-diaminobutan-1-one	305098: Inhibition of human DPP2	ic50	0.0009	uM
[(2R)-1-[2-[(4-pentyl-1-bicyclo[2.2.2]octanyl)amino]acetyl]pyrrolidin-2-yl]boronic acid	255032: Inhibitory activity against human DPP7 using Ala-Pro-AMC in fluorometric assay	ic50	0.0010	uM
(2S)-2-amino-4-(naphthalen-2-ylmethylamino)-1-piperidin-1-ylbutan-1-one	56221: Inhibition of human Dipeptidylpeptidase II (DPP II)	ic50	0.0011	uM
(2S)-2-amino-4-(cyclohexylmethylamino)-1-piperidin-1-ylbutan-1-one	56221: Inhibition of human Dipeptidylpeptidase II (DPP II)	ic50	0.0011	uM
(2S)-2-amino-4-[(4-chlorophenyl)methylamino]-1-(3,6-dihydro-2H-pyridin-1-yl)butan-1-one	56221: Inhibition of human Dipeptidylpeptidase II (DPP II)	ic50	0.0011	uM
(2S)-2-amino-4-[(4-chlorophenyl)methylamino]-1-(3-methylpiperidin-1-yl)butan-1-one	56221: Inhibition of human Dipeptidylpeptidase II (DPP II)	ic50	0.0011	uM
(2S)-2-amino-4-(naphthalen-1-ylmethylamino)-1-piperidin-1-ylbutan-1-one	56221: Inhibition of human Dipeptidylpeptidase II (DPP II)	ic50	0.0013	uM
(2S)-2-amino-4-[(3-chlorophenyl)methylamino]-1-piperidin-1-ylbutan-1-one	56221: Inhibition of human Dipeptidylpeptidase II (DPP II)	ic50	0.0013	uM
N-[(3S)-3-amino-4-oxo-4-piperidin-1-ylbutyl]acetamide	56221: Inhibition of human Dipeptidylpeptidase II (DPP II)	ic50	0.0015	uM
(2S)-2-amino-4-anilino-1-piperidin-1-ylbutan-1-one	56221: Inhibition of human Dipeptidylpeptidase II (DPP II)	ic50	0.0015	uM
2-[(3S)-3-amino-4-oxo-4-piperidin-1-ylbutyl]guanidine	56221: Inhibition of human Dipeptidylpeptidase II (DPP II)	ic50	0.0018	uM
(2S)-2-amino-4-[(3-methoxyphenyl)methylamino]-1-piperidin-1-ylbutan-1-one	56221: Inhibition of human Dipeptidylpeptidase II (DPP II)	ic50	0.0018	uM
[(2R)-1-[2-(cycloheptylamino)acetyl]pyrrolidin-2-yl]boronic acid	255032: Inhibitory activity against human DPP7 using Ala-Pro-AMC in fluorometric assay	ic50	0.0018	uM
(2S)-2-amino-4-(3-phenylpropylamino)-1-piperidin-1-ylbutan-1-one	56221: Inhibition of human Dipeptidylpeptidase II (DPP II)	ic50	0.0019	uM
[(2S)-1-[(2S)-2-aminohexanoyl]pyrrolidin-2-yl]boronic acid	254911: Inhibitory concentration against human dipeptidylpeptidase 7	ic50	0.0020	uM
(2S)-2-amino-4-(benzylamino)-1-piperidin-1-ylbutan-1-one	56221: Inhibition of human Dipeptidylpeptidase II (DPP II)	ic50	0.0020	uM
[(2R)-1-[2-(cyclodecylamino)acetyl]pyrrolidin-2-yl]boronic acid	255032: Inhibitory activity against human DPP7 using Ala-Pro-AMC in fluorometric assay	ic50	0.0022	uM
(2S)-2-amino-4-[(4-chlorophenyl)methylamino]-1-(2-methylpiperidin-1-yl)butan-1-one	56221: Inhibition of human Dipeptidylpeptidase II (DPP II)	ic50	0.0023	uM
3-[[[(3S)-3-amino-4-oxo-4-piperidin-1-ylbutyl]amino]methyl]benzonitrile	56221: Inhibition of human Dipeptidylpeptidase II (DPP II)	ic50	0.0027	uM
(2S)-2-amino-4-[(2,4-dimethoxyphenyl)methylamino]-1-piperidin-1-ylbutan-1-one	56221: Inhibition of human Dipeptidylpeptidase II (DPP II)	ic50	0.0027	uM
(2S,3S)-2-amino-3-[4-(4-fluorophenyl)phenyl]-1-[(3S)-3-fluoropyrrolidin-1-yl]butan-1-one	393710: Inhibition of QPP	ic50	0.0027	uM
(2S,4S)-2-amino-4-[(4-chlorophenyl)methylamino]-1-piperidin-1-ylhexan-1-one	270815: Inhibition of DPP2	ic50	0.0034	uM
[(1S)-1-[[(2S)-2,6-diaminohexanoyl]amino]pentyl]boronic acid	254911: Inhibitory concentration against human dipeptidylpeptidase 7	ic50	0.0037	uM
(2S,4S)-2-amino-4-[(4-chlorophenyl)methylamino]-5-phenyl-1-piperidin-1-ylpentan-1-one	270815: Inhibition of DPP2	ic50	0.0038	uM
1-[(2S)-2-amino-4-(benzylamino)butanoyl]piperidine-2-carbonitrile	56221: Inhibition of human Dipeptidylpeptidase II (DPP II)	ic50	0.0040	uM
[(2R)-1-[2-(cyclooctylamino)acetyl]pyrrolidin-2-yl]boronic acid	255032: Inhibitory activity against human DPP7 using Ala-Pro-AMC in fluorometric assay	ic50	0.0040	uM
[(2R)-1-[2-(cyclohexylamino)acetyl]pyrrolidin-2-yl]boronic acid	255032: Inhibitory activity against human DPP7 using Ala-Pro-AMC in fluorometric assay	ic50	0.0041	uM
(2S)-2-amino-4-[bis[(4-chlorophenyl)methyl]amino]-1-piperidin-1-ylbutan-1-one	56221: Inhibition of human Dipeptidylpeptidase II (DPP II)	ic50	0.0042	uM
6-[[(3S)-3-amino-4-oxo-4-piperidin-1-ylbutyl]amino]pyridine-3-carbonitrile	56221: Inhibition of human Dipeptidylpeptidase II (DPP II)	ic50	0.0046	uM
[(1S)-1-[[(2S)-2,5-diaminopentanoyl]amino]pentyl]boronic acid	254911: Inhibitory concentration against human dipeptidylpeptidase 7	ic50	0.0047	uM
4-methyl-3-[(1-methyl-6-pyridin-3-ylpyrazolo[3,4-d]pyrimidin-4-yl)amino]-N-[3-(trifluoromethyl)phenyl]benzamide	2148261: Binding affinity to human DPP7 incubated for 45 mins by Kinobead based pull down assay	kd	0.0053	uM
[(2R)-1-[(2R)-2-aminopropanoyl]pyrrolidin-2-yl]boronic acid	255032: Inhibitory activity against human DPP7 using Ala-Pro-AMC in fluorometric assay	ic50	0.0063	uM
1-[(2S)-2-amino-4-[(4-chlorophenyl)methylamino]butanoyl]piperidine-2-carbonitrile	56221: Inhibition of human Dipeptidylpeptidase II (DPP II)	ic50	0.0065	uM

CTD chemical–gene interactions

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

Chemical	Actions (top 5)	PubMed papers
sodium arsenite	decreases expression, increases expression	2
UAMC00039	decreases reaction, increases cleavage, increases abundance, decreases activity	2
Valproic Acid	decreases expression, increases methylation	2
bisphenol F	increases expression	1
methylmercuric chloride	decreases expression	1
sodium arsenate	increases abundance, increases expression	1
4-nitroaniline	decreases reaction, increases abundance, increases cleavage, increases reaction	1
ferrous chloride	decreases expression	1
nickel sulfate	decreases expression	1
benzyloxycarbonylleucyl-leucyl-leucine aldehyde	increases cleavage, increases reaction, increases abundance	1
alanylproline-4-nitroanilide	increases cleavage, decreases reaction	1
ICG 001	increases expression	1
bisphenol B	increases expression	1
bisphenol S	increases expression	1
jinfukang	affects cotreatment, increases expression	1
(+)-JQ1 compound	decreases expression	1
bisphenol AF	increases expression	1
Temozolomide	decreases expression	1
Sunitinib	increases expression	1
Air Pollutants	affects expression, increases abundance	1
Arbutin	decreases expression	1
Arsenic	increases abundance, increases expression	1
Benzo(a)pyrene	increases expression	1
Cisplatin	affects cotreatment, increases expression	1
Diazinon	increases methylation	1
Dipeptides	increases abundance, increases cleavage, increases reaction, decreases reaction	1
Estradiol	increases expression	1
Ethyl Methanesulfonate	decreases expression	1
Etoposide	increases abundance, increases cleavage, increases reaction	1
Formaldehyde	decreases expression	1

ChEMBL screening assays

147 unique, capped per target: 142 binding, 4 functional, 1 admet

Representative assays (with source publication via chembl_document):

Assay ID	Type	Description	Source paper
CHEMBL665781	Binding	Selectivity index of compound was determined for human Dipeptidylpeptidase IV to that of Dipeptidyl-peptidase II	Design, synthesis, and SAR of potent and selective dipeptide-derived inhibitors for dipeptidyl peptidases. — J Med Chem
CHEMBL4617710	ADMET	Inhibition of mammalian DPP7 (unknown origin) using H-Lys-Pro-AMC as substrate preincubated for 10 mins followed by substrate addition measured after 30 mins	Discovery of Cyclic Boronic Acid QPX7728, an Ultrabroad-Spectrum Inhibitor of Serine and Metallo-β-lactamases. — J Med Chem
CHEMBL5723296	Functional	Affinity Biochemical interaction: (enzymatic assay (fluorogenic substrate cleavage)) EUB0002750aCl DPP7	Affinity Biochemical Literature for EUbOPEN Chemogenomic Library

Clinical trials (associated diseases)

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