CPA2

Summary

CPA2 (carboxypeptidase A2, HGNC:2297) is a protein-coding gene on chromosome 7q32.2, encoding Carboxypeptidase A2 (P48052). Carboxypeptidase that catalyzes the release of a C-terminal amino acid, with a preference for large aromatic C-terminal residues.

Three different forms of human pancreatic procarboxypeptidase A have been isolated. The encoded protein represents the A2 form, which is a monomeric protein with different biochemical properties from the A1 and A3 forms. The A2 form of pancreatic procarboxypeptidase acts on aromatic C-terminal residues and is a secreted protein.

Source: NCBI Gene 1358 — RefSeq curated summary.

At a glance

• GWAS associations: 1
• Clinical variants (ClinVar): 63 total
• Druggable target: yes
• MANE Select transcript: NM_001869

Identifiers

Gene identifiers

Field	Value
HGNC ID	HGNC:2297
Approved symbol	CPA2
Name	carboxypeptidase A2
Location	7q32.2
Locus type	gene with protein product
Status	Approved
Ensembl gene	ENSG00000158516
Ensembl biotype	protein_coding
OMIM	600688
Entrez	1358

Gene structure

Transcript identifiers

Ensembl transcripts: 4 — 2 retained_intron, 1 protein_coding, 1 nonsense_mediated_decay

ENST00000222481, ENST00000416698, ENST00000480781, ENST00000487259

RefSeq mRNA: 1 — MANE Select: NM_001869 NM_001869

CCDS: CCDS5817

Canonical transcript exons

ENST00000222481 — 11 exons

Exon	Start	End
ENSE00000723221	130277826	130277916
ENSE00000723222	130279463	130279662
ENSE00000723223	130282104	130282188
ENSE00001871689	130266863	130266952
ENSE00001930985	130289560	130289798
ENSE00003498710	130269669	130269803
ENSE00003529526	130275149	130275247
ENSE00003534882	130276628	130276738
ENSE00003609982	130268929	130269010
ENSE00003617091	130273076	130273177
ENSE00003668417	130270693	130270788

Expression profiles

Bgee: expression breadth ubiquitous, 162 present calls, max score 99.95.

FANTOM5 (CAGE): breadth tissue_specific, TPM avg 24.8123 / max 38237.9180, expressed in 26 samples.

FANTOM5 promoters (3 alternative TSS)

Promoter ID	TPM avg	Samples expressed
81058	24.1727	22
81056	0.3953	13
81057	0.2443	11

Top tissues by expression

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

Tissue	Anatomy ID	Expression score	Quality
body of pancreas	UBERON:0001150	99.95	gold quality
islet of Langerhans	UBERON:0000006	99.24	gold quality
pancreas	UBERON:0001264	99.23	gold quality
epithelial cell of pancreas	CL:0000083	92.35	gold quality
body of stomach	UBERON:0001161	88.23	gold quality
type B pancreatic cell	CL:0000169	88.19	gold quality
stomach	UBERON:0000945	86.22	gold quality
duodenum	UBERON:0002114	82.80	gold quality
male germ line stem cell (sensu Vertebrata) in testis	CL:0000089 ∩ UBERON:0000473	82.26	gold quality
pancreatic ductal cell	CL:0002079	82.15	silver quality
C1 segment of cervical spinal cord	UBERON:0006469	81.66	gold quality
fundus of stomach	UBERON:0001160	80.67	gold quality
jejunal mucosa	UBERON:0000399	78.79	gold quality
spinal cord	UBERON:0002240	78.09	gold quality
cardia of stomach	UBERON:0001162	75.94	gold quality
ileal mucosa	UBERON:0000331	74.61	gold quality
tibialis anterior	UBERON:0001385	74.22	silver quality
primordial germ cell in gonad	CL:0000670 ∩ UBERON:0000991	71.66	gold quality
small intestine	UBERON:0002108	70.21	gold quality
buccal mucosa cell	CL:0002336	70.05	gold quality
small intestine Peyer’s patch	UBERON:0003454	69.55	gold quality
ectocervix	UBERON:0012249	68.60	gold quality
right coronary artery	UBERON:0001625	67.68	gold quality
right adrenal gland	UBERON:0001233	67.65	gold quality
right lobe of liver	UBERON:0001114	66.76	gold quality
left uterine tube	UBERON:0001303	66.02	gold quality
right adrenal gland cortex	UBERON:0035827	65.78	gold quality
cervix squamous epithelium	UBERON:0006922	65.74	gold quality
endocervix	UBERON:0000458	65.66	gold quality
left adrenal gland	UBERON:0001234	65.30	gold quality

Single-cell (SCXA)

Detected in 6 experiment(s), a significant marker in 6.

Experiment	Marker?	Max mean expression
E-GEOD-81547	yes	10224.42
E-MTAB-5061	yes	6910.58
E-ENAD-27	yes	3655.66
E-GEOD-83139	yes	3085.90
E-HCAD-31	yes	2708.91
E-ANND-3	no	0.00

Regulation

Is transcription factor: no

Literature-anchored findings (GeneRIF, showing 8)

• changes in zinc ligation promote remodeling of the active site in the zinc hydrolase superfamily (PMID:11743734)
• NMR structure of the activation domain (PMID:12538893)
• The high-resolution crystal structure and solution NMR structure of AYEdesign show that the experimentally determined backbone and side-chains conformations are effectively superimposable with the computational model at atomic resolution. (PMID:17196978)
• we have used one of the best-characterized models for folding and misfolding, the activation domain of procarboxypeptidase A2. The wild type (WT) and three mutants affecting the kinetics of aggregation have been studied by IR from the folded state (PMID:19817500)
• Chymotrypsin C is a co-activator of human pancreatic procarboxypeptidases A1 and A2. (PMID:21098023)
• CPMG RD data analysis thus allowed a detailed structural characterization of the ADA2h denatured state under folding conditions not previously achieved for this protein. (PMID:26115097)
• This study showed that CPA2 and CPB1 variants are not associated with chronic pancreatitis. (PMID:26316592)
• Complex Formation of Human Proelastases with Procarboxypeptidases A1 and A2. (PMID:27358403)

Cross-species orthologs

21 orthologs

Organism	Symbol	Gene ID
danio_rerio	cpa2	ENSDARG00000010146
danio_rerio	cpa4	ENSDARG00000043722
mus_musculus	Cpa2	ENSMUSG00000071553
rattus_norvegicus	Cpa4	ENSRNOG00000010463
drosophila_melanogaster	CG18585	FBGN0031929
drosophila_melanogaster	CG7025	FBGN0031930
drosophila_melanogaster	CG4017	FBGN0032143
drosophila_melanogaster	CG17633	FBGN0032144
drosophila_melanogaster	CG2915	FBGN0033241
drosophila_melanogaster	CG12374	FBGN0033774
drosophila_melanogaster	CG14820	FBGN0035718
drosophila_melanogaster	CG8562	FBGN0035779
drosophila_melanogaster	CG18417	FBGN0035780
drosophila_melanogaster	CG8560	FBGN0035781
drosophila_melanogaster	CG8539	FBGN0035791
drosophila_melanogaster	CG4408	FBGN0039073
drosophila_melanogaster	CG32379	FBGN0052379
drosophila_melanogaster	CG42264	FBGN0259149
caenorhabditis_elegans		WBGENE00004747
caenorhabditis_elegans	T06A4.1	WBGENE00020281
caenorhabditis_elegans	Y47G6A.19	WBGENE00021645

Paralogs (8): CPB2 (ENSG00000080618), CPA1 (ENSG00000091704), CPA4 (ENSG00000128510), CPO (ENSG00000144410), CPB1 (ENSG00000153002), CPA5 (ENSG00000158525), CPA3 (ENSG00000163751), CPA6 (ENSG00000165078)

Protein

Protein identifiers

Carboxypeptidase A2 — P48052 (reviewed: P48052)

All UniProt accessions (2): P48052, J3QT58

UniProt curated annotations — full annotation on UniProt →

Function. Carboxypeptidase that catalyzes the release of a C-terminal amino acid, with a preference for large aromatic C-terminal residues.

Subcellular location. Secreted.

Cofactor. Binds 1 zinc ion per subunit.

Similarity. Belongs to the peptidase M14 family.

RefSeq proteins (1): NP_001860* (*=MANE)

Domains & families (InterPro)

ID	Name	Type
IPR000834	Peptidase_M14	Domain
IPR003146	M14A_act_pep	Domain
IPR034248	CPA_M14_CPD	Domain
IPR036990	M14A-like_propep	Homologous_superfamily
IPR057246	CARBOXYPEPT_ZN_1	Binding_site
IPR057247	CARBOXYPEPT_ZN_2	Binding_site

Pfam: PF00246, PF02244

Enzyme classification (BRENDA):

• EC 3.4.17.15 — carboxypeptidase A2 (BRENDA: 4 organisms, 17 substrates, 4 inhibitors, 16 Km, 14 kcat entries)

Substrate kinetics (BRENDA)

11 substrates with measured Km, best-characterized 11. Km ranges are aggregated across organisms/conditions.

Substrate	Km (mM)	Measurements
BENZYLOXYCARBONYL-GLY-TRP	0.127–2.028	3
BENZYLOXYCARBONYL-GLY-GLY-LEU	5.3–6.53	2
BENZYLOXYCARBONYL-GLY-GLY-PHE	0.314–0.372	2
BENZYLOXYCARBONYL-GLY-TYR	0.145–0.175	2
ANGIOTENSIN II	0.191	1
BENZYLOXYCARBONYL-GLY-GLY-TRP	0.146	1
BENZYLOXYCARBONYL-GLY-GLY-TYR	0.125	1
BENZYLOXYCARBONYL-GLY-PHE	2.27	1
HIPPURYL-L-PHENYLALANINE	0.49	1
METHOTREXATE-ALPHA-(1-NAPHTHYL)ALANINE	0.016	1
METHOTREXATE-ALPHA-PHENYLALANINE	0.056	1

UniProt features (57 total): strand 18, helix 16, binding site 8, turn 4, sequence conflict 3, disulfide bond 2, signal peptide 1, propeptide 1, sequence variant 1, chain 1, domain 1, active site 1

Structure

Experimental structures (PDB)

3 structures.

PDB	Method	Resolution (Å)
1DTD	X-RAY DIFFRACTION	1.65
1AYE	X-RAY DIFFRACTION	1.8
1O6X	SOLUTION NMR

Predicted structure (AlphaFold)

Model	pLDDT	Fraction very-high
AF-P48052-F1	95.00	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 (1): 380 (proton donor/acceptor)

Ligand- & substrate-binding residues (8): 306; 307–308; 358; 179–182; 179; 182; 237; 254–255

Disulfide bonds (2): 248–271, 320–354

Function

Pathways and Gene Ontology

Reactome pathways

3 pathways

ID	Pathway
R-HSA-9925561	Developmental Lineage of Pancreatic Acinar Cells
R-HSA-1266738	Developmental Biology
R-HSA-9734767	Developmental Cell Lineages

MSigDB gene sets: 74 (showing top): GOMF_METALLOPEPTIDASE_ACTIVITY, GOBP_MACROMOLECULE_CATABOLIC_PROCESS, RACCACAR_AML_Q6, chr7q32, AACTTT_UNKNOWN, RYTTCCTG_ETS2_B, VECCHI_GASTRIC_CANCER_EARLY_DN, DR3_Q4, GOBP_PROTEIN_CATABOLIC_PROCESS, FOXO4_02, DEURIG_T_CELL_PROLYMPHOCYTIC_LEUKEMIA_UP, TGGAAA_NFAT_Q4_01, RAAGNYNNCTTY_UNKNOWN, GOBP_PROTEOLYSIS, OSF2_Q6

GO Biological Process (2): proteolysis (GO:0006508), protein catabolic process in the vacuole (GO:0007039)

GO Molecular Function (7): carboxypeptidase activity (GO:0004180), metallocarboxypeptidase activity (GO:0004181), zinc ion binding (GO:0008270), peptidase activity (GO:0008233), metallopeptidase activity (GO:0008237), hydrolase activity (GO:0016787), metal ion binding (GO:0046872)

GO Cellular Component (3): extracellular region (GO:0005576), obsolete extracellular space (GO:0005615), vacuole (GO:0005773)

Reactome top-level categories

Rollup of top-2 pathways:

Category	Pathways
Developmental Cell Lineages of the Exocrine Pancreas	1
Developmental Biology	1

GO top-level categories

Rollup of top GO terms by namespace:

Category	Terms
protein metabolic process	1
vacuole	1
protein catabolic process	1
exopeptidase activity	1
carboxypeptidase activity	1
metalloexopeptidase activity	1
transition metal ion 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
cytoplasm	1
intracellular membrane-bounded organelle	1

Protein interactions and networks

STRING

788 interactions, top by confidence (×1000):

Protein A	Protein B	Partner UniProt	Score
CPA2	LXN	Q9BS40	809
CPA2	CELA3A	P09093	640
CPA2	CELA2A	P08217	638
CPA2	SLC9B2	Q86UD5	594
CPA2	SLC9B1	Q4ZJI4	585
CPA2	PRSS2	P07478	552
CPA2	CELA3B	P08861	542
CPA2	RBPJL	Q9UBG7	528
CPA2	CTRC	Q99895	523
CPA2	PNLIPRP1	P54315	470
CPA2	ACD	Q96AP0	464
CPA2	PRSS1	P07477	460
CPA2	CELA1	Q9UNI1	460
CPA2	CTRB1	P17538	434
CPA2	TSGA13	Q96PP4	420

IntAct

6 interactions, top by confidence:

A	B	Type	Score
CPA2		psi-mi:“MI:0407”(direct interaction)	0.440
CPA2	NME4	psi-mi:“MI:0914”(association)	0.350
BMI1	MEIS3P1	psi-mi:“MI:0914”(association)	0.350
CPA2	MPZL1	psi-mi:“MI:0914”(association)	0.350
CPA2	GAS6	psi-mi:“MI:0914”(association)	0.350

BioGRID (12): RBM14-RBM4 (Affinity Capture-MS), GAS6 (Affinity Capture-MS), MPZL1 (Affinity Capture-MS), ITGA4 (Affinity Capture-MS), HSPA5 (Affinity Capture-MS), INHBE (Affinity Capture-MS), NME4 (Affinity Capture-MS), MPZL1 (Affinity Capture-MS), RBM14-RBM4 (Affinity Capture-MS), HSPA5 (Affinity Capture-MS), GAS6 (Affinity Capture-MS), CPA4 (Affinity Capture-MS)

ESM2 similar proteins: A0A1S4F020, A6XGK3, B6V865, B8JLQ9, B8XGR3, C5FH26, C5FVN6, D4AS12, D4B5N0, D4D675, D4DL57, O02350, O17754, O97397, P00730, P00731, P00732, P09954, P09955, P15085, P15086, P15088, P15089, P16406, P19222, P19223, P21961, P37892, P38836, P42787, P48052, P54969, P55261, Q0II73, Q29NC4, Q2KIG3, Q2KJ83, Q3T905, Q4R7R2, Q504N0

Diamond homologs: A0A1S4F020, A6XGK3, B6H233, B6Q972, B6V865, B8JLQ9, B8XGR3, C5FH26, C5FVN6, D4AS12, D4DL57, O02350, P00730, P00731, P00732, P04069, P09954, P09955, P15085, P15086, P18143, P19222, P19223, P29068, P38836, P42788, P48052, P55261, Q0C9B4, Q0II73, Q29NC4, Q3T905, Q504N0, Q5U901, Q7TPZ8, Q8IVL8, Q8N4T0, Q9VL86, A1CSU3, A1DGH9

SIGNOR signaling

0 interactions.

Disease & clinical

Clinical variants and AI predictions

ClinVar

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

Classification	Count (floor)
Pathogenic	0
Likely pathogenic	0
Uncertain significance	57
Likely benign	0
Benign	3

Top pathogenic / likely-pathogenic (0)

SpliceAI

1831 predictions. Top by Δscore:

Variant	Effect	Δscore
7:130266948:GTGGG:G	donor_gain	1.0000
7:130266950:GGG:G	donor_gain	1.0000
7:130266951:GGG:G	donor_gain	1.0000
7:130266953:G:GA	donor_loss	1.0000
7:130266954:T:A	donor_loss	1.0000
7:130274996:GA:G	donor_gain	1.0000
7:130276739:G:GG	donor_gain	1.0000
7:130277799:A:AG	acceptor_gain	1.0000
7:130277799:AT:A	acceptor_gain	1.0000
7:130277799:ATGT:A	acceptor_gain	1.0000
7:130277800:T:G	acceptor_gain	1.0000
7:130277809:T:A	acceptor_gain	1.0000
7:130279659:GCTG:G	donor_gain	1.0000
7:130280254:C:G	donor_gain	1.0000
7:130266951:GG:G	donor_gain	0.9900
7:130266952:GG:G	donor_gain	0.9900
7:130266953:G:GG	donor_gain	0.9900
7:130268927:A:AG	acceptor_gain	0.9900
7:130268928:G:GG	acceptor_gain	0.9900
7:130269665:TCA:T	acceptor_loss	0.9900
7:130269666:CA:C	acceptor_loss	0.9900
7:130269667:A:AG	acceptor_gain	0.9900
7:130269667:AG:A	acceptor_loss	0.9900
7:130269667:AGCTT:A	acceptor_gain	0.9900
7:130269668:G:GA	acceptor_gain	0.9900
7:130269668:GC:G	acceptor_gain	0.9900
7:130269668:GCT:G	acceptor_gain	0.9900
7:130269668:GCTT:G	acceptor_gain	0.9900
7:130269668:GCTTG:G	acceptor_gain	0.9900
7:130269799:TGCAG:T	donor_loss	0.9900

AlphaMissense

2764 scored. Top likely-pathogenic:

Variant	Protein change	am_pathogenicity
7:130277893:G:C	R255P	0.998
7:130289652:T:C	F389L	0.998
7:130289654:C:A	F389L	0.998
7:130289654:C:G	F389L	0.998
7:130277897:C:A	N256K	0.997
7:130277897:C:G	N256K	0.997
7:130277910:T:C	F261L	0.997
7:130277912:T:A	F261L	0.997
7:130277912:T:G	F261L	0.997
7:130275207:A:T	E182V	0.996
7:130276708:C:A	N222K	0.996
7:130276708:C:G	N222K	0.996
7:130277837:G:C	W236C	0.996
7:130277837:G:T	W236C	0.996
7:130277839:G:C	R237P	0.996
7:130277891:C:A	N254K	0.996
7:130277891:C:G	N254K	0.996
7:130277898:T:A	W257R	0.996
7:130277898:T:C	W257R	0.996
7:130279505:G:A	G277E	0.996
7:130275197:C:G	H179D	0.995
7:130275204:G:C	R181P	0.995
7:130275211:G:C	W183C	0.995
7:130275211:G:T	W183C	0.995
7:130277835:T:A	W236R	0.995
7:130277835:T:C	W236R	0.995
7:130277884:A:G	D252G	0.995
7:130277900:G:C	W257C	0.995
7:130277900:G:T	W257C	0.995
7:130279594:A:C	S307R	0.995

dbSNP variants (sampled 300 via entrez): RS1000100332 (7:130279871 A>G), RS1000162820 (7:130272961 C>G,T), RS1000186947 (7:130286473 C>G), RS1000368920 (7:130281004 G>A), RS1000407638 (7:130266427 G>T), RS1000408643 (7:130266917 T>A,C), RS1000443117 (7:130286535 C>T), RS1000461247 (7:130274305 C>A), RS1000803673 (7:130280567 A>G), RS1001106021 (7:130279130 A>G), RS1001250286 (7:130288324 G>A), RS1001397961 (7:130282124 T>C), RS1001617187 (7:130287577 C>T), RS1001684992 (7:130281140 C>T), RS1001916632 (7:130289212 T>TAG)

Disease associations

OMIM: gene MIM:600688 | disease phenotypes:

GenCC curated gene-disease

Mondo (0):

Orphanet (0):

HPO phenotypes

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

GWAS associations

1 associations (top):

Study	Trait	p-value
GCST003501_2	Asparaginase-induced acute pancreatitis in acute lymphoblastic leukemia (onset time)	2.000000e-08

EFO canonical traits (1, from GWAS)

EFO ID	Trait name
EFO:1001507	asparaginase-induced acute pancreatitis

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (1): CHEMBL4939 (SINGLE PROTEIN)

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

PharmGKB clinical annotations

1 annotations.

Variant	Type	Level	Drugs	Phenotypes
rs199695765	Toxicity	3	asparaginase	Acute lymphoblastic leukemia;Pancreatitis

PharmGKB variants

1 variants.

Variant	Genes	Level	Score	#Clin annots	Drugs
rs199695765	CPA2	3	3.00	1	asparaginase

GtoPdb / IUPHAR curated pharmacology

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

Target class: enzyme — M14: Carboxypeptidase A

ChEMBL bioactivities

11 potent at pChembl≥5 of 11 total, top 11 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).

pChembl	Type	Value	Unit	Molecule
9.70	Ki	0.2	nM	CHEMBL4436298
9.15	Ki	0.7	nM	CHEMBL4528407
9.00	Ki	1	nM	CHEMBL4460840
8.77	Ki	1.7	nM	CHEMBL4483485
8.62	Ki	2.4	nM	CHEMBL4532731
8.49	Ki	3.2	nM	CHEMBL4453900
8.34	Ki	4.6	nM	CHEMBL4448096
8.28	Ki	5.3	nM	CHEMBL4445882
8.24	Ki	5.7	nM	CHEMBL4454162
8.11	Ki	7.8	nM	CHEMBL4513310
7.86	Ki	13.8	nM	CHEMBL4440735

PubChem BioAssay actives

11 with measured affinity, of 11 total; 11 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-[[[(1R)-1-[[(2S)-2-acetamido-4-methylpentanoyl]amino]-2-phenylethyl]-hydroxyphosphoryl]methyl]-4-phenylbutanoic acid	1614546: Inhibition of human CPA2 using AAFP as substrate preincubated for 45 mins to 2 hrs measured at 30 sec intervals for 15 mins by UV/vis-spectrophotometry	ki	0.0002	uM
(2S)-2-[[[(1R)-1-[[(2S)-2-acetamido-4-methylpentanoyl]amino]ethyl]-hydroxyphosphoryl]methyl]-4-phenylbutanoic acid	1614546: Inhibition of human CPA2 using AAFP as substrate preincubated for 45 mins to 2 hrs measured at 30 sec intervals for 15 mins by UV/vis-spectrophotometry	ki	0.0007	uM
(2S)-2-[[[(1R)-1-[[(2S)-2-acetamido-4-methylpentanoyl]amino]-2-phenylethyl]-hydroxyphosphoryl]methyl]-3-phenylpropanoic acid	1614546: Inhibition of human CPA2 using AAFP as substrate preincubated for 45 mins to 2 hrs measured at 30 sec intervals for 15 mins by UV/vis-spectrophotometry	ki	0.0010	uM
(2S)-2-[[[(1R)-1-[[(2S)-2-acetamido-3-(4-hydroxyphenyl)propanoyl]amino]ethyl]-hydroxyphosphoryl]methyl]-4-phenylbutanoic acid	1614546: Inhibition of human CPA2 using AAFP as substrate preincubated for 45 mins to 2 hrs measured at 30 sec intervals for 15 mins by UV/vis-spectrophotometry	ki	0.0017	uM
(2S)-2-[[[(1R)-1-[[(2S)-2-acetamido-6-aminohexanoyl]amino]ethyl]-hydroxyphosphoryl]methyl]-4-phenylbutanoic acid	1614546: Inhibition of human CPA2 using AAFP as substrate preincubated for 45 mins to 2 hrs measured at 30 sec intervals for 15 mins by UV/vis-spectrophotometry	ki	0.0024	uM
(2S)-2-[[[(1R)-1-[[(2S)-1-acetylpyrrolidine-2-carbonyl]amino]ethyl]-hydroxyphosphoryl]methyl]-4-phenylbutanoic acid	1614546: Inhibition of human CPA2 using AAFP as substrate preincubated for 45 mins to 2 hrs measured at 30 sec intervals for 15 mins by UV/vis-spectrophotometry	ki	0.0032	uM
(4S)-4-acetamido-5-[[(1R)-1-[[(2S)-2-carboxy-4-phenylbutyl]-hydroxyphosphoryl]ethyl]amino]-5-oxopentanoic acid	1614546: Inhibition of human CPA2 using AAFP as substrate preincubated for 45 mins to 2 hrs measured at 30 sec intervals for 15 mins by UV/vis-spectrophotometry	ki	0.0046	uM
(2E)-2-[(2Z,4E)-3-[4-[3-[2-[2-[2-[3-[2-[2-[2-[[(2S)-1-[[(1R)-1-[[(2S)-2-carboxy-4-phenylbutyl]-hydroxyphosphoryl]ethyl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-2-oxoethoxy]ethoxy]ethylamino]-3-oxopropoxy]ethoxy]ethoxy]ethylamino]-3-oxopropyl]phenyl]-5-[1,1-dimethyl-6,8-disulfo-3-(4-sulfobutyl)benzo[e]indol-3-ium-2-yl]penta-2,4-dienylidene]-1,1-dimethyl-8-sulfo-3-(4-sulfobutyl)benzo[e]indole-6-sulfonate	1614546: Inhibition of human CPA2 using AAFP as substrate preincubated for 45 mins to 2 hrs measured at 30 sec intervals for 15 mins by UV/vis-spectrophotometry	ki	0.0053	uM
(2S)-2-[[[(1R)-1-[[(2S)-2-[[2-[2-(2-acetamidoethoxy)ethoxy]acetyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]ethyl]-hydroxyphosphoryl]methyl]-4-phenylbutanoic acid	1614546: Inhibition of human CPA2 using AAFP as substrate preincubated for 45 mins to 2 hrs measured at 30 sec intervals for 15 mins by UV/vis-spectrophotometry	ki	0.0057	uM
(2S)-2-[[[(1R)-1-[[(2S)-2-[[2-[2-(2-aminoethoxy)ethoxy]acetyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]ethyl]-hydroxyphosphoryl]methyl]-4-phenylbutanoic acid	1614546: Inhibition of human CPA2 using AAFP as substrate preincubated for 45 mins to 2 hrs measured at 30 sec intervals for 15 mins by UV/vis-spectrophotometry	ki	0.0078	uM
(2S)-2-[[[(1R)-1-[[(2S)-2-acetamido-3-hydroxypropanoyl]amino]ethyl]-hydroxyphosphoryl]methyl]-4-phenylbutanoic acid	1614546: Inhibition of human CPA2 using AAFP as substrate preincubated for 45 mins to 2 hrs measured at 30 sec intervals for 15 mins by UV/vis-spectrophotometry	ki	0.0138	uM

CTD chemical–gene interactions

7 total (human), top 7 by PubMed support.

Chemical	Actions (top 5)	PubMed papers
Aflatoxin B1	decreases methylation, increases methylation	2
sodium arsenite	affects acetylation, affects methylation	1
benzo(e)pyrene	decreases methylation	1
aflatoxin B2	decreases methylation	1
monomethylarsonous acid	affects acetylation, affects methylation	1
abrine	increases expression	1
Methapyrilene	decreases methylation	1

ChEMBL screening assays

1 unique, capped per target: 1 binding

Representative assays (with source publication via chembl_document):

Assay ID	Type	Description	Source paper
CHEMBL4413959	Binding	Inhibition of human CPA2 using AAFP as substrate preincubated for 45 mins to 2 hrs measured at 30 sec intervals for 15 mins by UV/vis-spectrophotometry	Synthesis and Structural/Functional Characterization of Selective M14 Metallocarboxypeptidase Inhibitors Based on Phosphinic Pseudopeptide Scaffold: Implications on the Design of Specific Optical Probes. — J Med Chem

Clinical trials (associated diseases)

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