CPN1

Summary

CPN1 (carboxypeptidase N subunit 1, HGNC:2312) is a protein-coding gene on chromosome 10q24.2, encoding Carboxypeptidase N catalytic chain (P15169). Protects the body from potent vasoactive and inflammatory peptides containing C-terminal Arg or Lys (such as kinins or anaphylatoxins) which are released into the circulation.

Carboxypeptidase N is a plasma metallo-protease that cleaves basic amino acids from the C terminal of peptides and proteins. The enzyme is important in the regulation of peptides like kinins and anaphylatoxins, and has also been known as kininase-1 and anaphylatoxin inactivator. This enzyme is a tetramer comprised of two identical regulatory subunits and two identical catalytic subunits; this gene encodes the catalytic subunit. Mutations in this gene can be associated with angioedema or chronic urticaria resulting from carboxypeptidase N deficiency.

Source: NCBI Gene 1369 — RefSeq curated summary.

At a glance

• Gene–disease (curated): carboxypeptidase N deficiency (Limited, GenCC)
• GWAS associations: 10
• Clinical variants (ClinVar): 67 total — 1 pathogenic, 1 likely-pathogenic
• Druggable target: yes
• Dosage sensitivity (ClinGen): haploinsufficiency autosomal recessive, triplosensitivity no evidence
• MANE Select transcript: NM_001308

Identifiers

Gene identifiers

Field	Value
HGNC ID	HGNC:2312
Approved symbol	CPN1
Name	carboxypeptidase N subunit 1
Location	10q24.2
Locus type	gene with protein product
Status	Approved
Ensembl gene	ENSG00000120054
Ensembl biotype	protein_coding
OMIM	603103
Entrez	1369

Gene structure

Transcript identifiers

Ensembl transcripts: 8 — 8 protein_coding

ENST00000370418, ENST00000441382, ENST00000877010, ENST00000877011, ENST00000877012, ENST00000877013, ENST00000877014, ENST00000877015

RefSeq mRNA: 1 — MANE Select: NM_001308 NM_001308

CCDS: CCDS7486

Canonical transcript exons

ENST00000370418 — 9 exons

Exon	Start	End
ENSE00000811300	100065188	100065370
ENSE00000811301	100063614	100063725
ENSE00000811302	100057013	100057152
ENSE00000811303	100054347	100054446
ENSE00001452668	100081403	100081869
ENSE00001887192	100042193	100042573
ENSE00003305953	100075911	100076107
ENSE00003381123	100048758	100048876
ENSE00003404628	100069714	100069869

Expression profiles

Bgee: expression breadth broad, 35 present calls, max score 93.77.

FANTOM5 (CAGE): breadth tissue_specific, TPM avg 0.2699 / max 113.4429, expressed in 31 samples.

FANTOM5 promoters (3 alternative TSS)

Promoter ID	TPM avg	Samples expressed
111014	0.1684	17
111013	0.0849	20
111012	0.0165	7

Top tissues by expression

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

Tissue	Anatomy ID	Expression score	Quality
right lobe of liver	UBERON:0001114	93.77	gold quality
liver	UBERON:0002107	92.31	gold quality
primordial germ cell in gonad	CL:0000670 ∩ UBERON:0000991	87.53	gold quality
male germ line stem cell (sensu Vertebrata) in testis	CL:0000089 ∩ UBERON:0000473	83.98	gold quality
buccal mucosa cell	CL:0002336	74.03	silver quality
tibialis anterior	UBERON:0001385	70.70	silver quality
pancreatic ductal cell	CL:0002079	65.42	silver quality
ileal mucosa	UBERON:0000331	63.03	silver quality
triceps brachii	UBERON:0001509	62.08	gold quality
frontal pole	UBERON:0002795	62.00	gold quality
middle frontal gyrus	UBERON:0002702	61.96	gold quality
paraflocculus	UBERON:0005351	61.56	gold quality
olfactory bulb	UBERON:0002264	60.09	gold quality
type B pancreatic cell	CL:0000169	59.88	gold quality
deltoid	UBERON:0001476	59.30	gold quality
upper leg skin	UBERON:0004262	58.87	gold quality
gluteal muscle	UBERON:0002000	58.45	gold quality
endometrium epithelium	UBERON:0004811	57.18	gold quality
cranial nerve II	UBERON:0000941	56.81	silver quality
oocyte	CL:0000023	56.72	gold quality
decidua	UBERON:0002450	56.55	gold quality
epithelial cell of pancreas	CL:0000083	53.71	gold quality
nasal cavity epithelium	UBERON:0005384	53.11	gold quality
right testis	UBERON:0004534	52.46	gold quality
hair follicle	UBERON:0002073	52.43	gold quality
quadriceps femoris	UBERON:0001377	51.95	gold quality
heart right ventricle	UBERON:0002080	51.81	gold quality
thymus	UBERON:0002370	51.17	gold quality
left testis	UBERON:0004533	51.16	gold quality
testis	UBERON:0000473	50.78	gold quality

Single-cell (SCXA)

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

Experiment	Marker?	Max mean expression
E-ANND-3	yes	4.43

Regulation

Is transcription factor: no

miRNA regulators (miRDB)

12 targeting CPN1, 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-3163	100.00	77.23	8605
HSA-MIR-3121-3P	99.82	71.96	3630
HSA-MIR-4677-5P	99.70	70.09	1940
HSA-MIR-7156-5P	99.64	68.81	1369
HSA-MIR-4427	99.34	70.33	1854
HSA-MIR-488-5P	99.28	68.12	821
HSA-MIR-6739-3P	99.22	68.84	1843
HSA-MIR-6761-5P	98.71	68.03	1504
HSA-MIR-6834-3P	98.16	65.77	551
HSA-MIR-10395-3P	98.10	66.70	1726
HSA-MIR-4433A-5P	96.79	65.01	599
HSA-MIR-4433B-5P	95.91	66.56	727

Functional genomics

ClinGen dosage: haploinsufficiency 30 (autosomal recessive), triplosensitivity 0 (no evidence). ClinGen Gene Dosage Map

Literature-anchored findings (GeneRIF, showing 4)

• carboxypeptidase N regulates the biologic activity of SDF-1alpha by reducing the chemokine-specific activity (PMID:15718415)
• This review summarizes the structure, enzymatic properties and function of this enzyme, including insights gained by the recent elucidation of the crystal structure of the CPN catalytic subunit and structural modeling of the non-catalytic 83 kDa subunit. (PMID:18039526)
• circulating CPN/CPB and platelets may potentially contribute to regulating the bioactivity of leukocyte chemoattractant chemerin (PMID:19010784)
• CPN binds to fibrinogen and is present in a fibrin clot prepared from plasma. (PMID:23000409)

Cross-species orthologs

3 orthologs

Organism	Symbol	Gene ID
danio_rerio	cpn1	ENSDARG00000005185
mus_musculus	Cpn1	ENSMUSG00000025196
rattus_norvegicus	Cpn1	ENSRNOG00000013439

Paralogs (7): CPXM1 (ENSG00000088882), AEBP1 (ENSG00000106624), CPD (ENSG00000108582), CPE (ENSG00000109472), CPZ (ENSG00000109625), CPXM2 (ENSG00000121898), CPM (ENSG00000135678)

Protein

Protein identifiers

Carboxypeptidase N catalytic chain — P15169 (reviewed: P15169)

Alternative names: Anaphylatoxin inactivator, Arginine carboxypeptidase, Carboxypeptidase N polypeptide 1, Carboxypeptidase N small subunit, Kininase-1, Lysine carboxypeptidase, Plasma carboxypeptidase B, Serum carboxypeptidase N

All UniProt accessions (2): P15169, B1AP58

UniProt curated annotations — full annotation on UniProt →

Function. Protects the body from potent vasoactive and inflammatory peptides containing C-terminal Arg or Lys (such as kinins or anaphylatoxins) which are released into the circulation.

Subunit / interactions. Tetramer of two catalytic chains and two glycosylated inactive chains.

Subcellular location. Secreted. Extracellular space.

Tissue specificity. Synthesized in the liver and secreted in plasma.

Disease relevance. Carboxypeptidase N deficiency (CPND) [MIM:212070] An autosomal recessive disorder characterized by angioedema, acute or chronic urticaria, and hay fever or asthma. Affected individuals have levels of carboxypeptidase N below the reference range. The disease is caused by variants affecting the gene represented in this entry.

Cofactor. Binds 1 zinc ion per subunit.

Similarity. Belongs to the peptidase M14 family.

RefSeq proteins (1): NP_001299* (*=MANE)

Domains & families (InterPro)

ID	Name	Type
IPR000834	Peptidase_M14	Domain
IPR008969	CarboxyPept-like_regulatory	Homologous_superfamily
IPR033814	M14_CPN	Domain
IPR050753	Peptidase_M14_domain	Family
IPR057246	CARBOXYPEPT_ZN_1	Binding_site
IPR057247	CARBOXYPEPT_ZN_2	Binding_site

Pfam: PF00246, PF13620

Enzyme classification (BRENDA):

• EC 3.4.17.3 — lysine carboxypeptidase (BRENDA: 10 organisms, 75 substrates, 51 inhibitors, 42 Km, 25 kcat entries)

Substrate kinetics (BRENDA)

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

Substrate	Km (mM)	Measurements
BRADYKININ	0.0004–0.706	4
C3A69-77	0.035–0.077	3
BENZOYL-ALA-LYS	0.25–0.35	2
BENZOYL-GLY-ARG	0.1–6.7	2
BENZOYL-GLY-LYS	1.4–6.3	2
C5A66-74	0.219–0.602	2
CHEMERIN	0.1228–0.17	2
FIBRINOPEPTIDE ALPHAARG96-104	0.361–0.448	2
FIBRINOPEPTIDE BETALYS125-133	0.0532–0.143	2
FIBRINOPEPTIDE GAMMALYS54-62	0.34–0.657	2
FIBRINOPEPTIDE GAMMALYS77-85	0.238–3.727	2
HIPPURYL-ARG	0.14–1.8	2
HIPPURYL-L-ARG	1.2–6.93	2
HIPPURYL-L-LYS	3.3–35.8	2
BENZOYL-ALA-ARG	0.28	1

UniProt features (50 total): helix 16, strand 16, glycosylation site 3, binding site 3, disulfide bond 2, sequence conflict 2, turn 2, signal peptide 1, chain 1, sequence variant 1, domain 1, region of interest 1, active site 1

Structure

Experimental structures (PDB)

1 structures.

PDB	Method	Resolution (Å)
2NSM	X-RAY DIFFRACTION	2.1

Predicted structure (AlphaFold)

Model	pLDDT	Fraction very-high
AF-P15169-F1	90.71	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): 308 (proton donor/acceptor)

Ligand- & substrate-binding residues (3): 86; 89; 216

Disulfide bonds (2): 42–104, 271–311

Glycosylation sites (3): 409, 400, 402

Function

Pathways and Gene Ontology

Reactome pathways

4 pathways

ID	Pathway
R-HSA-977606	Regulation of Complement cascade
R-HSA-166658	Complement cascade
R-HSA-168249	Innate Immune System
R-HSA-168256	Immune System

MSigDB gene sets: 109 (showing top): GSE45365_NK_CELL_VS_BCELL_DN, MODULE_172, SHEPARD_BMYB_MORPHOLINO_UP, FREAC2_01, REACTOME_INNATE_IMMUNE_SYSTEM, GOMF_METALLOPEPTIDASE_ACTIVITY, GOBP_RESPONSE_TO_CORTICOSTEROID, GOBP_MACROMOLECULE_CATABOLIC_PROCESS, GOBP_PEPTIDE_METABOLIC_PROCESS, MODULE_492, GOBP_PROTEIN_MATURATION, GOBP_AMIDE_METABOLIC_PROCESS, TATCTGG_MIR488, GOBP_RESPONSE_TO_STEROID_HORMONE, GOBP_RESPONSE_TO_HORMONE

GO Biological Process (6): peptide metabolic process (GO:0006518), bradykinin catabolic process (GO:0010815), protein processing (GO:0016485), protein catabolic process (GO:0030163), response to glucocorticoid (GO:0051384), proteolysis (GO:0006508)

GO Molecular Function (8): metallocarboxypeptidase activity (GO:0004181), zinc ion binding (GO:0008270), carboxypeptidase activity (GO:0004180), protein binding (GO:0005515), peptidase activity (GO:0008233), metallopeptidase activity (GO:0008237), hydrolase activity (GO:0016787), metal ion binding (GO:0046872)

GO Cellular Component (2): extracellular region (GO:0005576), obsolete extracellular space (GO:0005615)

Reactome top-level categories

Rollup of top-3 pathways:

Category	Pathways
Complement cascade	1
Innate Immune System	1
Immune System	1

GO top-level categories

Rollup of top GO terms by namespace:

Category	Terms
protein metabolic process	2
metabolic process	1
catabolic process	1
proteolysis	1
protein maturation	1
macromolecule catabolic process	1
response to corticosteroid	1
carboxypeptidase activity	1
metalloexopeptidase activity	1
transition metal ion binding	1
exopeptidase activity	1
binding	1
hydrolase activity	1
catalytic activity, acting on a protein	1
peptidase activity	1
catalytic activity	1
cation binding	1
cellular anatomical structure	1

Protein interactions and networks

STRING

662 interactions, top by confidence (×1000):

Protein A	Protein B	Partner UniProt	Score
CPN1	CPN2	P22792	933
CPN1	CPB1	P15086	783
CPN1	A0A2R8Y809	A0A2R8Y809	769
CPN1	TBCE	Q15813	769
CPN1	TBCD	Q9BTW9	764
CPN1	HSPE1	P61604	681
CPN1	KNG1	P01042	669
CPN1	CLIP1	P30622	649
CPN1	HSPD1	P10809	621
CPN1	ACE	P12821	590
CPN1	KLK4	Q9Y5K2	583
CPN1	BDKRB2	P30411	515
CPN1	CPB2	Q96IY4	511
CPN1	FEZF2	Q8TBJ5	506
CPN1	BDKRB1	P46663	505

IntAct

31 interactions, top by confidence:

A	B	Type	Score
HLA-A	CPN1	psi-mi:“MI:0915”(physical association)	0.560
PRKCA	CPN1	psi-mi:“MI:0915”(physical association)	0.560
YWHAG	CPN1	psi-mi:“MI:0915”(physical association)	0.560
CPN1	SETDB1	psi-mi:“MI:0915”(physical association)	0.560
OPTN	CPN1	psi-mi:“MI:0915”(physical association)	0.560
KAT5	CPN1	psi-mi:“MI:0915”(physical association)	0.560
LMO3	CPN1	psi-mi:“MI:0915”(physical association)	0.560
CPN1	PRKCA	psi-mi:“MI:0915”(physical association)	0.560
CPN1	CEP170	psi-mi:“MI:0914”(association)	0.530
CPN1	PRKDC	psi-mi:“MI:0915”(physical association)	0.400
	CD5L	psi-mi:“MI:0915”(physical association)	0.400
S	IGLL5	psi-mi:“MI:0914”(association)	0.350
ITM2B	ILVBL	psi-mi:“MI:0914”(association)	0.350
CPN1	ALDH3A1	psi-mi:“MI:0914”(association)	0.350
CPN1	CDC42	psi-mi:“MI:0915”(physical association)	0.000
CPN1	CLEC4G	psi-mi:“MI:0915”(physical association)	0.000

BioGRID (14): BTBD1 (Affinity Capture-MS), CEP170 (Affinity Capture-MS), KDM3B (Affinity Capture-MS), PRKDC (Proximity Label-MS), C3 (Biochemical Activity), CEP170 (Affinity Capture-MS), BTBD1 (Affinity Capture-MS), ALDH3A1 (Affinity Capture-MS), KDM3B (Affinity Capture-MS), CPN1 (Synthetic Lethality), CPN1 (Negative Genetic), CPN1 (Reconstituted Complex), CPN1 (Two-hybrid), CPN1 (Two-hybrid)

ESM2 similar proteins: A5A6K7, O17754, O54858, O75976, O89001, P04836, P14384, P15087, P15169, P16870, P21661, P23188, P23377, P28841, P29122, P37892, P38836, P42787, Q00493, Q0II73, Q16769, Q28193, Q2KIG3, Q2KJ83, Q4R4M3, Q4R7R2, Q5REC2, Q5RFD6, Q5U901, Q63415, Q66K79, Q80V42, Q8IVL8, Q8N436, Q8QGP3, Q8R4H4, Q8R4V4, Q8WXQ8, Q90240, Q96IY4

Diamond homologs: A2RUV9, A5A6K7, O14786, O17754, O18806, O35276, O35375, O35474, O43854, O54858, O54991, O60462, O75976, O88783, O89001, P00451, P02886, P02887, P02888, P04836, P12259, P12263, P14384, P15087, P15169, P16870, P21956, P28824, P29068, P37892, P39041, P42787, P70490, P78357, P79385, P79795, P83852, P97333, P97846, P98092

SIGNOR signaling

1 interactions.

A	Effect	B	Mechanism
CPN1	“down-regulates activity”	HBA1	cleavage

Disease & clinical

Clinical variants and AI predictions

ClinVar

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

Classification	Count (floor)
Pathogenic	1
Likely pathogenic	1
Uncertain significance	52
Likely benign	5
Benign	5

Top pathogenic / likely-pathogenic (2)

Variant ID	HGVS	Classification
6622	NM_001308.3(CPN1):c.173dup (p.His59fs)	Pathogenic
3340540	NM_001308.3(CPN1):c.734C>T (p.Thr245Met)	Likely pathogenic

SpliceAI

1209 predictions. Top by Δscore:

Variant	Effect	Δscore
10:100054342:CCTA:C	donor_loss	1.0000
10:100054343:CTAC:C	donor_loss	1.0000
10:100054345:ACC:A	donor_loss	1.0000
10:100054346:C:A	donor_loss	1.0000
10:100054445:ACCT:A	acceptor_loss	1.0000
10:100054446:CCTG:C	acceptor_loss	1.0000
10:100054447:C:CC	acceptor_gain	1.0000
10:100054447:CTGC:C	acceptor_loss	1.0000
10:100057007:TTTTA:T	donor_loss	1.0000
10:100057009:TTA:T	donor_loss	1.0000
10:100057010:TACCT:T	donor_loss	1.0000
10:100057012:CC:C	donor_loss	1.0000
10:100065183:CATA:C	donor_loss	1.0000
10:100065184:ATAC:A	donor_loss	1.0000
10:100065187:C:CT	donor_loss	1.0000
10:100065187:CCTT:C	donor_gain	1.0000
10:100069710:CTA:C	donor_loss	1.0000
10:100069712:ACC:A	donor_loss	1.0000
10:100069713:CCTGA:C	donor_gain	1.0000
10:100069865:GGGCC:G	acceptor_gain	1.0000
10:100069867:GCC:G	acceptor_gain	1.0000
10:100069867:GCCCT:G	acceptor_loss	1.0000
10:100069868:CC:C	acceptor_gain	1.0000
10:100069868:CCC:C	acceptor_gain	1.0000
10:100069869:CC:C	acceptor_gain	1.0000
10:100069870:C:CC	acceptor_gain	1.0000
10:100069870:CTAA:C	acceptor_loss	1.0000
10:100069871:T:C	acceptor_loss	1.0000
10:100069880:A:AC	acceptor_gain	1.0000
10:100069880:A:C	acceptor_gain	1.0000

AlphaMissense

3021 scored. Top likely-pathogenic:

Variant	Protein change	am_pathogenicity
10:100069808:C:G	R161P	0.999
10:100057143:T:A	D294V	0.998
10:100057143:T:G	D294A	0.998
10:100057144:C:G	D294H	0.998
10:100063641:C:A	G282W	0.998
10:100063721:G:T	A255D	0.998
10:100048855:C:G	R378P	0.997
10:100063630:C:A	W285C	0.997
10:100063630:C:G	W285C	0.997
10:100065282:G:T	A222D	0.997
10:100069801:G:C	F163L	0.997
10:100069801:G:T	F163L	0.997
10:100069803:A:G	F163L	0.997
10:100057143:T:C	D294G	0.996
10:100063632:A:G	W285R	0.996
10:100063632:A:T	W285R	0.996
10:100069802:A:C	F163C	0.996
10:100075941:G:C	N130K	0.996
10:100075941:G:T	N130K	0.996
10:100063640:C:T	G282E	0.995
10:100063652:C:A	G278V	0.995
10:100063652:C:T	G278D	0.995
10:100063722:C:G	A255P	0.995
10:100065273:G:T	P225Q	0.995
10:100065313:A:G	S212P	0.995
10:100069802:A:G	F163S	0.995
10:100069810:G:C	N160K	0.995
10:100069810:G:T	N160K	0.995
10:100057100:T:A	E308D	0.994
10:100057100:T:G	E308D	0.994

dbSNP variants (sampled 300 via entrez): RS1000097102 (10:100079848 G>C), RS1000151001 (10:100079436 A>G), RS1000219033 (10:100078049 CT>C,CTT), RS1000319597 (10:100073158 A>T), RS1000400247 (10:100058960 G>A,C), RS1000553241 (10:100078268 T>C,G), RS1000559077 (10:100066588 G>C), RS1000606909 (10:100074609 G>C), RS1000623045 (10:100079775 G>C), RS1000656596 (10:100071813 G>A), RS1000675309 (10:100073296 C>T), RS1000748558 (10:100067790 T>A), RS1000871017 (10:100054531 T>C), RS1000908432 (10:100046474 A>G), RS1000939069 (10:100046664 T>G)

Disease associations

OMIM: gene MIM:603103 | disease phenotypes: MIM:212070

GenCC curated gene-disease

Disease	Classification	Inheritance
carboxypeptidase N deficiency	Limited	Autosomal recessive

Mondo (2): carboxypeptidase N deficiency (MONDO:0008910), hereditary angioedema with normal C1Inh (MONDO:0100567)

Orphanet (1): Hereditary angioedema with normal C1Inh (Orphanet:528647)

HPO phenotypes

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

GWAS associations

10 associations (top):

Study	Trait	p-value
GCST000248_3	Liver enzyme levels	2.000000e-08
GCST000817_153	Height	2.000000e-13
GCST001275_4	Liver enzyme levels (alanine transaminase)	4.000000e-09
GCST003522_3	Dermatomyositis	9.000000e-07
GCST006014_33	Creatine kinase levels	6.000000e-17
GCST006269_706	General cognitive ability	1.000000e-09
GCST006979_600	Heel bone mineral density	4.000000e-11
GCST007691_33	Femoral neck bone mineral density	9.000000e-10
GCST009159_9	Blood protein levels	4.000000e-08
GCST90002396_492	Mean reticulocyte volume	4.000000e-09

EFO canonical traits (6, from GWAS)

EFO ID	Trait name
EFO:0004534	creatine kinase measurement
EFO:0004337	intelligence
EFO:0009270	heel bone mineral density
EFO:0007785	femoral neck bone mineral density
EFO:0004747	protein measurement
EFO:0010701	mean reticulocyte volume

MeSH disease descriptors (1)

Descriptor	Name	Tree numbers
C562876	Carboxypeptidase N Deficiency (supp.)

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (1): CHEMBL4713 (SINGLE PROTEIN)

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

GtoPdb / IUPHAR curated pharmacology

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

Target class: enzyme — M14: Carboxypeptidase A

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

Ligand	Action	Affinity	Parameter
SQ-24,798	Inhibition	8.7	pKi
compound 3 [PMID: 14640538]	Inhibition	7.77	pIC50

ChEMBL bioactivities

19 potent at pChembl≥5 of 21 total, top 19 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).

pChembl	Type	Value	Unit	Molecule
8.70	Ki	2	nM	CHEMBL236822
8.70	IC50	2	nM	CHEMBL236822
8.52	IC50	3	nM	CHEMBL245787
8.22	IC50	6	nM	CHEMBL245787
8.15	IC50	7	nM	CHEMBL245985
8.10	IC50	8	nM	CHEMBL245787
7.42	IC50	38	nM	CHEMBL245589
7.24	IC50	58	nM	CHEMBL245589
7.22	IC50	60	nM	CHEMBL246978
7.21	IC50	61	nM	CHEMBL391595
6.45	IC50	357	nM	CHEMBL246595
6.38	IC50	420	nM	CHEMBL395661
6.00	IC50	1000	nM	CHEMBL394951
5.76	IC50	1750	nM	CHEMBL245591
5.57	IC50	2700	nM	ANABAENOPEPTIN F
5.51	IC50	3100	nM	CHEMBL245593
5.30	IC50	4950	nM	CHEMBL245786
5.27	IC50	5400	nM	ANABAENOPEPTIN B
5.24	IC50	5700	nM	CHEMBL3577334

PubChem BioAssay actives

19 with measured affinity, of 37 total; 15 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
5-(diaminomethylideneamino)-2-(sulfanylmethyl)pentanoic acid	304052: Inhibition of human plasma carboxypeptidase N	ki	0.0020	uM
2-[3-(diaminomethylideneamino)phenyl]-3-sulfanylpropanoic acid	305880: Inhibition of human carboxypeptidase N	ic50	0.0030	uM
2-[2-chloro-5-(diaminomethylideneamino)phenyl]-3-sulfanylpropanoic acid	305880: Inhibition of human carboxypeptidase N	ic50	0.0070	uM
2-(1-carbamimidoylpiperidin-3-yl)-3-sulfanylpropanoic acid	305880: Inhibition of human carboxypeptidase N	ic50	0.0380	uM
2-piperidin-4-yl-3-sulfanylpropanoic acid	305880: Inhibition of human carboxypeptidase N	ic50	0.0600	uM
2-(piperidin-4-ylmethyl)-3-sulfanylpropanoic acid	305880: Inhibition of human carboxypeptidase N	ic50	0.0610	uM
2-(3-aminophenyl)-3-sulfanylpropanoic acid	305880: Inhibition of human carboxypeptidase N	ic50	0.3570	uM
2-(piperidin-3-ylmethyl)-3-sulfanylpropanoic acid	305880: Inhibition of human carboxypeptidase N	ic50	0.4200	uM
2-(4-carbamimidoylphenyl)-3-sulfanylpropanoic acid	305880: Inhibition of human carboxypeptidase N	ic50	1.0000	uM
2-piperidin-3-yl-3-sulfanylpropanoic acid	305880: Inhibition of human carboxypeptidase N	ic50	1.7500	uM
(2S)-2-[[(3S,6S,9S,12S,15R)-3-benzyl-12-[(2S)-butan-2-yl]-9-[2-(4-hydroxyphenyl)ethyl]-6,7-dimethyl-2,5,8,11,14-pentaoxo-1,4,7,10,13-pentazacyclononadec-15-yl]carbamoylamino]-5-(diaminomethylideneamino)pentanoic acid	1227129: Inhibition of CPN (unknown origin)	ic50	2.7000	uM
2-(1-carbamimidoylpiperidin-4-yl)-3-sulfanylpropanoic acid	305880: Inhibition of human carboxypeptidase N	ic50	3.1000	uM
2-[1-(2-aminoacetyl)piperidin-4-yl]-3-sulfanylpropanoic acid	305880: Inhibition of human carboxypeptidase N	ic50	4.9500	uM
(2S)-2-[[(3S,6S,9S,12S,15R)-3-benzyl-9-[2-(4-hydroxyphenyl)ethyl]-6,7-dimethyl-2,5,8,11,14-pentaoxo-12-propan-2-yl-1,4,7,10,13-pentazacyclononadec-15-yl]carbamoylamino]-5-(diaminomethylideneamino)pentanoic acid	1227129: Inhibition of CPN (unknown origin)	ic50	5.4000	uM
(2S)-6-amino-2-[[(3S,6S,9S,12S,15R)-3-benzyl-9-[2-(4-hydroxyphenyl)ethyl]-6,7-dimethyl-2,5,8,11,14-pentaoxo-12-propan-2-yl-1,4,7,10,13-pentazacyclononadec-15-yl]carbamoylamino]hexanoic acid	1227129: Inhibition of CPN (unknown origin)	ic50	5.7000	uM

CTD chemical–gene interactions

29 total (human), top 29 by PubMed support.

Chemical	Actions (top 5)	PubMed papers
Benzo(a)pyrene	affects methylation, decreases expression	2
Tetrachlorodibenzodioxin	affects expression, decreases expression	2
Valproic Acid	affects expression, decreases expression, decreases methylation	2
Cyclosporine	decreases expression	2
methyleugenol	decreases expression	1
propionaldehyde	decreases expression	1
pirinixic acid	decreases expression, increases activity, affects binding	1
butyraldehyde	decreases expression	1
benazol P	affects expression	1
pentanal	decreases expression	1
perfluoro-n-nonanoic acid	decreases expression	1
Rosiglitazone	decreases expression	1
Resveratrol	affects cotreatment, decreases expression	1
Troglitazone	decreases expression	1
Air Pollutants	decreases expression	1
Aldehydes	decreases expression	1
Cadmium	decreases expression	1
N-Nitrosopyrrolidine	decreases expression	1
Nickel	affects binding	1
Phthalic Acids	increases methylation	1
Plant Extracts	affects cotreatment, decreases expression	1
Quercetin	decreases expression	1
Silicon Dioxide	decreases expression	1
Smoke	increases expression	1
Zinc	affects binding	1
Aflatoxin B1	decreases expression	1
Okadaic Acid	decreases expression	1
Copper Sulfate	decreases expression	1
Magnetite Nanoparticles	increases expression	1

ChEMBL screening assays

8 unique, capped per target: 6 binding, 2 admet

Representative assays (with source publication via chembl_document):

Assay ID	Type	Description	Source paper
CHEMBL3243354	Binding	Inhibition of carboxypeptidase N (unknown origin)	Design and synthesis of conformationally restricted inhibitors of active thrombin activatable fibrinolysis inhibitor (TAFIa). — Bioorg Med Chem
CHEMBL4124566	ADMET	Inhibition of human carboxypeptidase N preincubated for 10 mins followed by hippuryl-lysine substrate addition measured after 30 mins in presence of DTT	Structural basis for the selective inhibition of activated thrombin-activatable fibrinolysis inhibitor (TAFIa) by a selenium-containing inhibitor with chloro-aminopyridine as a basic group. — Bioorg Med Chem Lett

Cellosaurus cell lines

1 cell lines: 1 transformed cell line

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

Cellosaurus	Name	Category	Sex
CVCL_IW08	GM09276	Transformed cell line	Male

Clinical trials (associated diseases)

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