CHIA

Summary

CHIA (chitinase acidic, HGNC:17432) is a protein-coding gene on chromosome 1p13.2, encoding Acidic mammalian chitinase (Q9BZP6). Degrades chitin and chitotriose.

The protein encoded by this gene degrades chitin, which is found in the cell wall of most fungi as well as in arthropods and some nematodes. The encoded protein can also stimulate interleukin 13 expression, and variations in this gene can lead to asthma susceptibility. Several transcript variants encoding a few different isoforms have been found for this gene.

Source: NCBI Gene 27159 — RefSeq curated summary.

At a glance

• GWAS associations: 4
• Clinical variants (ClinVar): 104 total
• Druggable target: yes — 1 molecules with ChEMBL bioactivity
• MANE Select transcript: NM_201653

Identifiers

Gene identifiers

Field	Value
HGNC ID	HGNC:17432
Approved symbol	CHIA
Name	chitinase acidic
Location	1p13.2
Locus type	gene with protein product
Status	Approved
Aliases	AMCase, TSA1902, CHIT2
Ensembl gene	ENSG00000134216
Ensembl biotype	protein_coding
OMIM	606080
Entrez	27159

Gene structure

Transcript identifiers

Ensembl transcripts: 10 — 8 protein_coding, 1 nonsense_mediated_decay, 1 retained_intron

ENST00000343320, ENST00000352594, ENST00000353665, ENST00000369740, ENST00000422815, ENST00000430615, ENST00000451398, ENST00000477918, ENST00000483391, ENST00000489524

RefSeq mRNA: 8 — MANE Select: NM_201653 NM_001040623, NM_001258001, NM_001258002, NM_001258003, NM_001258004, NM_001258005, NM_021797, NM_201653

CCDS: CCDS41368, CCDS58017, CCDS832

Canonical transcript exons

ENST00000369740 — 12 exons

Exon	Start	End
ENSE00001068650	111312190	111312391
ENSE00001450758	111310400	111310492
ENSE00001450759	111290851	111290950
ENSE00003460735	111315270	111315435
ENSE00003504952	111317986	111318109
ENSE00003505793	111318493	111318678
ENSE00003519558	111319120	111319239
ENSE00003592290	111317681	111317805
ENSE00003611810	111319327	111319468
ENSE00003613513	111311689	111311718
ENSE00003668302	111314540	111314596
ENSE00003842174	111320213	111320563

Expression profiles

Bgee: expression breadth ubiquitous, 107 present calls, max score 86.31.

FANTOM5 (CAGE): breadth tissue_specific, TPM avg 0.0161 / max 3.6619, expressed in 15 samples.

FANTOM5 promoters (1 alternative TSS)

Promoter ID	TPM avg	Samples expressed
4620	0.0161	15

Top tissues by expression

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

Tissue	Anatomy ID	Expression score	Quality
cardia of stomach	UBERON:0001162	86.31	gold quality
body of stomach	UBERON:0001161	82.64	gold quality
fundus of stomach	UBERON:0001160	77.56	gold quality
stomach	UBERON:0000945	77.20	gold quality
lower lobe of lung	UBERON:0008949	75.24	gold quality
upper lobe of lung	UBERON:0008948	65.22	gold quality
upper lobe of left lung	UBERON:0008952	64.47	gold quality
lung	UBERON:0002048	64.10	gold quality
skeletal muscle tissue of rectus abdominis	UBERON:0004511	62.19	gold quality
oocyte	CL:0000023	62.04	gold quality
right lung	UBERON:0002167	59.59	gold quality
adenohypophysis	UBERON:0002196	58.83	gold quality
diaphragm	UBERON:0001103	58.39	gold quality
esophagus squamous epithelium	UBERON:0006920	57.96	silver quality
parotid gland	UBERON:0001831	57.83	gold quality
epithelium of esophagus	UBERON:0001976	57.28	silver quality
myocardium	UBERON:0002349	56.70	gold quality
pituitary gland	UBERON:0000007	56.63	gold quality
tendon of biceps brachii	UBERON:0008188	55.84	gold quality
visceral pleura	UBERON:0002401	55.45	gold quality
decidua	UBERON:0002450	55.18	gold quality
skeletal muscle tissue of biceps brachii	UBERON:0004502	54.67	gold quality
endometrium	UBERON:0001295	54.60	gold quality
lateral globus pallidus	UBERON:0002476	54.08	gold quality
trabecular bone tissue	UBERON:0002483	53.83	gold quality
male germ cell	CL:0000015	53.47	gold quality
sperm	CL:0000019	53.46	gold quality
deltoid	UBERON:0001476	52.90	gold quality
quadriceps femoris	UBERON:0001377	52.87	gold quality
pancreatic ductal cell	CL:0002079	52.84	silver quality

Single-cell (SCXA)

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

Experiment	Marker?	Max mean expression
E-ANND-3	yes	7.69

Regulation

Is transcription factor: no

miRNA regulators (miRDB)

19 targeting CHIA, 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-32-5P	99.98	75.21	1964
HSA-MIR-92A-3P	99.98	75.21	1960
HSA-MIR-92B-3P	99.98	75.25	1955
HSA-MIR-25-3P	99.98	74.60	1817
HSA-MIR-363-3P	99.98	74.72	1821
HSA-MIR-367-3P	99.98	74.83	1819
HSA-MIR-548P	99.98	72.25	3784
HSA-MIR-10527-5P	99.91	72.28	3754
HSA-MIR-2052	99.79	69.37	2031
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-4688	99.48	64.68	828
HSA-MIR-6743-5P	99.48	63.60	721
HSA-MIR-1286	99.09	66.23	1046
HSA-MIR-676-3P	97.86	65.70	668
HSA-MIR-3059-3P	96.71	67.08	606
HSA-MIR-4680-5P	96.43	67.15	893

Literature-anchored findings (GeneRIF, showing 25)

• expressed in exaggerated quantities in human asthma (PMID:15192232)
• human AMCase has only one pH optimum for k(cat)/K(m) between pH 4 and 5. Steady state kinetics shows that human AMCase has “low” intrinsic transglycosidase activity, which leads to the observation of apparent substrate inhibition. (PMID:16584180)
• results establish a significant association of CHIA with atopic asthma and serum total IgE levels in the Indian population (PMID:18602573)
• lung epithelial cells secrete AMCase via an EGFR-dependent pathway that is activated by ADAM17 and mediates its effects via Ras. (PMID:18824549)
• The three-dimensional (3D) model of the human acidic mammalian chitinase (hAMCase) was constructed based on the crystal structure of the human chitotriosidase (EC 3.2.1.44, PDB code 1HKK) by using InsightII/Homology module. (PMID:19085022)
• Results showed the presence of CHIT1 and AMCase mRNA in gastric mucosa and the correlation with the presence of H. pylori was significant only for CHIT1 but not for AMCase expression. (PMID:19242357)
• secreted AMCase feeds back in an autocrine and/or paracrine manner to protect pulmonary epithelial cells from growth factor withdrawal- and Fas ligand-induced apoptosis (PMID:19342690)
• The abundant biopolymer chitin appears to be recognized by a yet uncharacterized receptor on sinonasal epithelial cells. Chitin stimulates production of AMCase and eotaxin-3, two pro-Th2 effector proteins. (PMID:19379605)
• Genetic association analyses of AMCase haplotypes for asthma revealed significant protective associations between the variant haplotype in several asthma cohorts. (PMID:19435888)
• novel asthma susceptibility genes; review of genetic and fuctional studies (PMID:19644363)
• Our study found no associations between single nucleotide polymorphisms in the genes CHIT1, CHIA, and CHI3L1 and asthma, changes in lung physiology, or allergy-related phenotypes in subjects with mild-to-moderate asthma (PMID:20226308)
• The levels of expression of AMCase and chitotriosidase mRNAs and proteins were increased in allergic turbinate mucosa compared with normal turbinate mucosa. (PMID:20422678)
• Environmental exposure to fungi does not modify the effect of CHIA SNPs on severe asthma exacerbations (PMID:20538957)
• Report increased CSF chitinase levels in patients with neuromyelitis optica and relapsing remitting multiple sclerosis. (PMID:21159721)
• AMCase and eotaxin-3 may be important mediators in the pathogenesis of nasal polyps. The increased AMCase and eotaxin-3 might lead to nasal polyp formation and growth. (PMID:21303604)
• A ten base pair insertion in the second exon in the 5’UTR region of the AMCase gene may modify the gene expression and thus may affect the severity of asthma. (PMID:21511453)
• increased chitinolytic activity in nasal polyps (PMID:21711963)
• study demonstrated genetic associations between chitinase gene variants and lung function level and rate of decline in chronic obstructive pulmonary disease patients from the Lung Health Study; also functional effect of the rs3818822 polymorphism on AMCase levels and activity was demonstrated (PMID:22200767)
• results showed that the expression of AMCase and CHIT-1 were differently modulated in monocyte macrophages at different stage of maturation. The behavior of these two active chitinase suggests that in the immune response their role is complementary. (PMID:23129258)
• loss of acidic chitinase expression is a promising marker for corpus atrophy (PMID:24119614)
• These data provide the experimental evidence that telomere shortening and related inflammatory proteins are associated with human IgAN, and it could be a new direction for the disease progression study. (PMID:24903994)
• we showed that M at the position 61 is highly conserved in the many mammals other than orangutan and humans. In addition, introduction of M61R and M61I to WT mouse AMCase lead to a significant reduction of its chitinolytic activity. Taken together, our present and previous data by Seibold et al. (2009) indicate that G339T (R61M) in humans is associated with asthma protection in the fashion of gain of function (PMID:27702777)
• This is the first report on the association between low-frequency and common variants in the chitinases-related genes CHIA and CHI3L1 with the intensity of specific IgE to ABA-1 in a population naturally exposed to Ascaris and with Bet v 1 in a Swedish population. (PMID:27977724)
• rs10494132 polymorphism of CHIA might be a risk factor for asthma. (PMID:29233108)
• AMCase expression was significantly higher in helminths-infected patients than the noninfected, or protozoa infected. (PMID:30117166)

Cross-species orthologs

44 orthologs

Organism	Symbol	Gene ID
mus_musculus	Chil6	ENSMUSG00000027902
mus_musculus	Chil3	ENSMUSG00000040809
mus_musculus	Chil5	ENSMUSG00000043873
mus_musculus	Chia1	ENSMUSG00000062778
mus_musculus	Chil4	ENSMUSG00000063779
rattus_norvegicus	Chial1	ENSRNOG00000017574
rattus_norvegicus	Chia	ENSRNOG00000033162
rattus_norvegicus	Chi3l3	ENSRNOG00000037115
drosophila_melanogaster	Idgf6	FBGN0013763
drosophila_melanogaster	Idgf3	FBGN0020414
drosophila_melanogaster	Idgf2	FBGN0020415
drosophila_melanogaster	Idgf1	FBGN0020416
drosophila_melanogaster	Idgf4	FBGN0026415
drosophila_melanogaster	Cht7	FBGN0035398
drosophila_melanogaster	Cda4	FBGN0052499
drosophila_melanogaster	Idgf5	FBGN0064237
caenorhabditis_elegans		WBGENE00000503
caenorhabditis_elegans		WBGENE00007465
caenorhabditis_elegans		WBGENE00007466
caenorhabditis_elegans		WBGENE00007467
caenorhabditis_elegans		WBGENE00007469
caenorhabditis_elegans		WBGENE00007470
caenorhabditis_elegans		WBGENE00007471
caenorhabditis_elegans		WBGENE00007472
caenorhabditis_elegans		WBGENE00007473
caenorhabditis_elegans		WBGENE00010799
caenorhabditis_elegans		WBGENE00010945
caenorhabditis_elegans		WBGENE00011157
caenorhabditis_elegans		WBGENE00011158
caenorhabditis_elegans		WBGENE00011159
caenorhabditis_elegans		WBGENE00011161
caenorhabditis_elegans		WBGENE00011162
caenorhabditis_elegans		WBGENE00011164
caenorhabditis_elegans		WBGENE00011166
caenorhabditis_elegans		WBGENE00011167
caenorhabditis_elegans		WBGENE00011170
caenorhabditis_elegans		WBGENE00011846
caenorhabditis_elegans		WBGENE00014162
caenorhabditis_elegans		WBGENE00016665
caenorhabditis_elegans		WBGENE00017233
caenorhabditis_elegans		WBGENE00020141
caenorhabditis_elegans		WBGENE00020407
caenorhabditis_elegans		WBGENE00044546
caenorhabditis_elegans		WBGENE00044807

Paralogs (6): CHI3L2 (ENSG00000064886), OVGP1 (ENSG00000085465), CTBS (ENSG00000117151), CHI3L1 (ENSG00000133048), CHIT1 (ENSG00000133063), CHID1 (ENSG00000177830)

Protein

Protein identifiers

Acidic mammalian chitinase — Q9BZP6 (reviewed: Q9BZP6)

Alternative names: Lung-specific protein TSA1902

All UniProt accessions (4): E9PLJ2, Q9BZP6, H7BXH6, Q5VUV5

UniProt curated annotations — full annotation on UniProt →

Function. Degrades chitin and chitotriose. May participate in the defense against nematodes, fungi and other pathogens. Plays a role in T-helper cell type 2 (Th2) immune response. Contributes to the response to IL-13 and inflammation in response to IL-13. Stimulates chemokine production by pulmonary epithelial cells. Protects lung epithelial cells against apoptosis and promotes phosphorylation of AKT1. Its function in the inflammatory response and in protecting cells against apoptosis is inhibited by allosamidin, suggesting that the function of this protein depends on carbohydrate binding.

Subunit / interactions. Interacts with EGFR.

Subcellular location. Secreted Cytoplasm Cytoplasm.

Tissue specificity. Detected in lung epithelial cells from asthma patients (at protein level). Highly expressed in stomach. Detected at lower levels in lung.

Induction. Up-regulated in lung epithelial cells from asthma patients.

Similarity. Belongs to the glycosyl hydrolase 18 family. Chitinase class II subfamily.

Isoforms (3)

UniProt ID	Names	Canonical?
Q9BZP6-1	1	yes
Q9BZP6-2	2, TSA1902-L
Q9BZP6-3	3, TSA1902-S

RefSeq proteins (8): NP_001035713, NP_001244930, NP_001244931, NP_001244932, NP_001244933, NP_001244934, NP_068569, NP_970615* (*=MANE)

Domains & families (InterPro)

ID	Name	Type
IPR001223	Glyco_hydro18_cat	Domain
IPR001579	Glyco_hydro_18_chit_AS	Active_site
IPR002557	Chitin-bd_dom	Domain
IPR011583	Chitinase_II/V-like_cat	Domain
IPR017853	GH_hydrolase_sf	Homologous_superfamily
IPR029070	Chitinase_insertion_sf	Homologous_superfamily
IPR036508	Chitin-bd_dom_sf	Homologous_superfamily
IPR050314	Glycosyl_Hydrlase_18	Family

Pfam: PF00704, PF01607

Enzyme classification (BRENDA):

• EC 3.2.1.14 — chitinase (BRENDA: 265 organisms, 959 substrates, 432 inhibitors, 204 Km, 181 kcat entries)

Substrate kinetics (BRENDA)

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

Substrate	Km (mM)	Measurements
4-NITROPHENYL BETA-N,N’-DIACETYLCHITOBIOSIDE	0.03–12.7	14
4-METHYLUMBELLIFERYL BETA-N,N’,N’’-TRIACETYLCHIT	0.0042–1.13	9
4-METHYLUMBELLIFERYL-N,N’-DIACETYLCHITOBIOSE	0.0077–0.042	8
CHITOHEXAOSE	0.163–0.218	8
N,N’,N’’,N’’’,N’’’’-PENTAACETYLCHITOPENTAOSE	0.014–0.16	7
4-METHYLUMBELLIFERYL 2-ACETAMIDO-4-O-(2-ACETAMID	0.03–0.171	6
4-NITROPHENYL N,N’-DIACETYL-BETA-D-CHITOBIOSIDE	0.127–3.9	6
COLLOIDAL CHITIN	0.019–9.66	6
P-NITROPHENYL-N,N’-DIACETYLCHITOBIOSE	0.062–0.315	6
4-METHYLUMBELLIFERYL-N,N’,N’’-TRIACETYLCHITOTRIO	0.0014–1.1	5
4-NITROPHENYL-BETA-1,4-N,N’-DIACETYL-CHITOBIOSE	0.101–0.555	5
CHITIN	2–54.29	5
4-METHYLUMBELLIFERYL BETA-D-N,N’-DIACETYLCHITOBI	0.0022–0.0155	4
P-NITROPHENYL BETA-D-N,N’-DIACETYLCHITOBIOSE	0.537–54.7	4
4-METHYLUMBELLIFERYL-BETA-D-N,N’,N’’-TRIACETYL-C	0.0035–0.174	3

UniProt features (66 total): helix 20, strand 15, sequence variant 10, binding site 5, turn 4, disulfide bond 3, splice variant 2, domain 2, signal peptide 1, chain 1, mutagenesis site 1, sequence conflict 1, active site 1

Structure

Experimental structures (PDB)

8 structures.

PDB	Method	Resolution (Å)
3FY1	X-RAY DIFFRACTION	1.7
3RM8	X-RAY DIFFRACTION	1.8
3RME	X-RAY DIFFRACTION	1.8
3RM4	X-RAY DIFFRACTION	1.9
3FXY	X-RAY DIFFRACTION	2
3RM9	X-RAY DIFFRACTION	2.1
2YBT	X-RAY DIFFRACTION	2.22
2YBU	X-RAY DIFFRACTION	2.25

Predicted structure (AlphaFold)

Model	pLDDT	Fraction very-high
AF-Q9BZP6-F1	92.65	0.85

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): 140 (proton donor)

Ligand- & substrate-binding residues (5): 70–71; 97–100; 141; 210–213; 360

Disulfide bonds (3): 26–51, 49–394, 307–372

Mutagenesis-validated functional residues (1):

Position	Phenotype
138	loss of chitinase activity. no effect on protection against apoptosis or on akt1 activation.

Function

Pathways and Gene Ontology

Reactome pathways

1 pathways

ID	Pathway
R-HSA-189085	Digestion of dietary carbohydrate

MSigDB gene sets: 97 (showing top): GSE45365_NK_CELL_VS_BCELL_DN, GOBP_DIGESTION, LIANG_HEMATOPOIESIS_STEM_CELL_NUMBER_SMALL_VS_HUGE_UP, GOBP_INFLAMMATORY_RESPONSE, REACTOME_DIGESTION_OF_DIETARY_CARBOHYDRATE, GOBP_MACROMOLECULE_CATABOLIC_PROCESS, GOBP_CARBOHYDRATE_DERIVATIVE_CATABOLIC_PROCESS, GOBP_POSITIVE_REGULATION_OF_CYTOKINE_PRODUCTION, GOBP_CARBOHYDRATE_DERIVATIVE_METABOLIC_PROCESS, GOLDRATH_ANTIGEN_RESPONSE, GOBP_POLYSACCHARIDE_CATABOLIC_PROCESS, GOBP_PRODUCTION_OF_MOLECULAR_MEDIATOR_INVOLVED_IN_INFLAMMATORY_RESPONSE, GOBP_CYTOKINE_PRODUCTION, GOBP_AMINOGLYCAN_METABOLIC_PROCESS, GOBP_CARBOHYDRATE_METABOLIC_PROCESS

GO Biological Process (10): polysaccharide catabolic process (GO:0000272), immune system process (GO:0002376), production of molecular mediator involved in inflammatory response (GO:0002532), chitin metabolic process (GO:0006030), chitin catabolic process (GO:0006032), apoptotic process (GO:0006915), positive regulation of chemokine production (GO:0032722), polysaccharide digestion (GO:0044245), carbohydrate metabolic process (GO:0005975), inflammatory response (GO:0006954)

GO Molecular Function (8): chitinase activity (GO:0004568), chitin binding (GO:0008061), endochitinase activity (GO:0008843), kinase binding (GO:0019900), hydrolase activity, hydrolyzing O-glycosyl compounds (GO:0004553), protein binding (GO:0005515), hydrolase activity (GO:0016787), hydrolase activity, acting on glycosyl bonds (GO:0016798)

GO Cellular Component (3): extracellular region (GO:0005576), obsolete extracellular space (GO:0005615), cytoplasm (GO:0005737)

Reactome top-level categories

Rollup of top-1 pathways:

Category	Pathways
Digestion	1

GO top-level categories

Rollup of top GO terms by namespace:

Category	Terms
cellular anatomical structure	2
polysaccharide metabolic process	1
macromolecule catabolic process	1
carbohydrate catabolic process	1
biological_process	1
inflammatory response	1
multicellular organismal process	1
aminoglycan metabolic process	1
amino sugar metabolic process	1
aminoglycan catabolic process	1
chitin metabolic process	1
glucosamine-containing compound catabolic process	1
programmed cell death	1
apoptotic signaling pathway	1
execution phase of apoptosis	1
positive regulation of cytokine production	1
chemokine production	1
regulation of chemokine production	1
digestion	1
primary metabolic process	1
defense response	1
hydrolase activity, hydrolyzing O-glycosyl compounds	1
carbohydrate derivative binding	1
chitinase activity	1
enzyme binding	1
hydrolase activity, acting on glycosyl bonds	1
binding	1
catalytic activity	1
hydrolase activity	1
intracellular anatomical structure	1

Protein interactions and networks

STRING

1636 interactions, top by confidence (×1000):

Protein A	Protein B	Partner UniProt	Score
CHIA	CTCF	P49711	787
CHIA	IL13	P35225	740
CHIA	ARG1	P05089	715
CHIA	MDFIC	Q9P1T7	713
CHIA	IL4	P05112	689
CHIA	CHID1	Q9BWS9	665
CHIA	IL13RA2	Q14627	608
CHIA	IL4R	P24394	598
CHIA	IL33	O95760	592
CHIA	IL13RA1	P78552	583
CHIA	RETNLB	Q9BQ08	582
CHIA	RAD21	O60216	582
CHIA	MRC1	P22897	578
CHIA	CD72	P21854	552
CHIA	TFF1	P04155	522

IntAct

19 interactions, top by confidence:

A	B	Type	Score
PIK3R3	PIK3CD	psi-mi:“MI:0914”(association)	0.800
RBBP8NL	CHIA	psi-mi:“MI:0915”(physical association)	0.560
TBC1D5	CHIA	psi-mi:“MI:0915”(physical association)	0.560
COX20	CHIA	psi-mi:“MI:0915”(physical association)	0.560
CHIA	EGFR	psi-mi:“MI:0915”(physical association)	0.400
CHIA	H1-4	psi-mi:“MI:0915”(physical association)	0.400
CHIA	TPP2	psi-mi:“MI:0914”(association)	0.350
CHIA	AP1G2	psi-mi:“MI:0914”(association)	0.350
CHIA	SLC25A16	psi-mi:“MI:0914”(association)	0.350
CPA4	IGF1R	psi-mi:“MI:0914”(association)	0.350
FGG	ACOT7	psi-mi:“MI:0914”(association)	0.350
CHIA	RBBP8NL	psi-mi:“MI:0915”(physical association)	0.000
CHIA	TBC1D5	psi-mi:“MI:0915”(physical association)	0.000
CHIA	COX20	psi-mi:“MI:0915”(physical association)	0.000

BioGRID (60): UBR4 (Affinity Capture-MS), FAM63A (Affinity Capture-MS), RIC8B (Affinity Capture-MS), BIRC6 (Affinity Capture-MS), GNAL (Affinity Capture-MS), UBAC1 (Affinity Capture-MS), TPP2 (Affinity Capture-MS), HELZ (Affinity Capture-MS), RNF123 (Affinity Capture-MS), HPS3 (Affinity Capture-MS), NDE1 (Affinity Capture-MS), MOCOS (Affinity Capture-MS), NPRL3 (Affinity Capture-MS), GNB2 (Affinity Capture-MS), KCMF1 (Affinity Capture-MS)

ESM2 similar proteins: A0A2U7QU15, A1CX14, A1D4Q5, A1DCV5, A2QFV7, A2RAR6, A6N6J0, B0XN12, B0Y6E0, B0YB65, B7SIW2, C5J411, C5P230, E9ERT9, E9QRF2, G4MTF8, G4NI45, G5EAZ3, I1S3T9, O14456, O59859, P0C1B3, P0C1B4, P0CB51, P23360, P30292, P32470, P33559, P46239, P48827, Q00177, Q02905, Q02906, Q0CBM8, Q0H904, Q12713, Q1E3R8, Q2PGV8, Q4JHP5, Q4WGT3

Diamond homologs: A0A072UR65, A0A072VEP0, A0A1B1J8Z2, A6N6J0, E9ERT9, O35744, O81862, P29030, P36222, P36362, P36718, P48827, Q12889, Q13231, Q15782, Q28042, Q28542, Q28990, Q29411, Q5RBP6, Q62010, Q6RY07, Q91XA9, Q91Z98, Q95M17, Q9BZP6, Q9W092, Q9W5U2, U5N4E3, O14456, P20533, P30922, P36909, Q60557, Q6TMG6, Q8SPQ0, A0A0A2JVV3, C5P230, E9QRF2, G5EAZ3

SIGNOR signaling

0 interactions.

Disease & clinical

Clinical variants and AI predictions

ClinVar

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

Classification	Count (floor)
Pathogenic	0
Likely pathogenic	0
Uncertain significance	89
Likely benign	6
Benign	7

Top pathogenic / likely-pathogenic (0)

SpliceAI

1373 predictions. Top by Δscore:

Variant	Effect	Δscore
1:111314530:T:TA	acceptor_gain	1.0000
1:111314535:TACA:T	acceptor_loss	1.0000
1:111314536:ACAG:A	acceptor_gain	1.0000
1:111314537:C:G	acceptor_gain	1.0000
1:111314538:A:AG	acceptor_gain	1.0000
1:111314538:AG:A	acceptor_gain	1.0000
1:111314539:G:GC	acceptor_loss	1.0000
1:111314539:G:GT	acceptor_gain	1.0000
1:111314539:GG:G	acceptor_gain	1.0000
1:111314539:GGA:G	acceptor_gain	1.0000
1:111314539:GGAA:G	acceptor_gain	1.0000
1:111314539:GGAAC:G	acceptor_gain	1.0000
1:111314592:GCCCC:G	donor_gain	1.0000
1:111314593:CCCC:C	donor_gain	1.0000
1:111314594:CCC:C	donor_gain	1.0000
1:111314595:CC:C	donor_gain	1.0000
1:111314595:CCGTA:C	donor_loss	1.0000
1:111314596:CG:C	donor_loss	1.0000
1:111314597:G:GG	donor_gain	1.0000
1:111314597:GTAAG:G	donor_loss	1.0000
1:111314598:T:A	donor_loss	1.0000
1:111315268:A:AG	acceptor_gain	1.0000
1:111315269:G:GG	acceptor_gain	1.0000
1:111315372:G:GT	donor_gain	1.0000
1:111315372:G:T	donor_gain	1.0000
1:111315406:G:GT	donor_gain	1.0000
1:111315445:G:GT	donor_gain	1.0000
1:111317680:GGAA:G	acceptor_gain	1.0000
1:111317803:ACAG:A	donor_loss	1.0000
1:111317804:CA:C	donor_gain	1.0000

AlphaMissense

3149 scored. Top likely-pathogenic:

Variant	Protein change	am_pathogenicity
1:111318056:A:C	S226R	0.994
1:111318058:C:A	S226R	0.994
1:111318058:C:G	S226R	0.994
1:111319239:G:C	K345N	0.994
1:111319239:G:T	K345N	0.994
1:111319225:A:C	S341R	0.992
1:111319227:C:A	S341R	0.992
1:111319227:C:G	S341R	0.992
1:111318542:T:C	L260P	0.989
1:111319201:T:A	W333R	0.988
1:111319201:T:C	W333R	0.988
1:111312287:T:G	C51W	0.987
1:111318542:T:A	L260H	0.987
1:111319384:G:C	D365H	0.987
1:111312285:T:A	C51S	0.985
1:111312286:G:C	C51S	0.985
1:111319203:G:C	W333C	0.984
1:111319203:G:T	W333C	0.984
1:111312285:T:C	C51R	0.983
1:111312286:G:A	C51Y	0.982
1:111318550:G:A	G263R	0.979
1:111318550:G:C	G263R	0.979
1:111319387:G:C	D366H	0.979
1:111318551:G:A	G263E	0.978
1:111318006:T:A	V209D	0.977
1:111318574:T:C	F271L	0.977
1:111318576:C:A	F271L	0.977
1:111318576:C:G	F271L	0.977
1:111319337:T:C	L349P	0.977
1:111319390:T:C	F367L	0.977

dbSNP variants (sampled 300 via entrez): RS1000104226 (1:111317165 G>A), RS1000235593 (1:111314814 T>C,G), RS1000329787 (1:111296716 G>C), RS1000360502 (1:111320111 C>T), RS1000427008 (1:111291684 TA>T,TAA), RS1000505902 (1:111301450 A>T), RS1000575908 (1:111315986 G>A), RS1000788839 (1:111301298 C>G,T), RS1000903412 (1:111315788 C>A,G), RS1000947374 (1:111299817 T>C), RS1000992099 (1:111311154 C>T), RS1001132125 (1:111306892 C>A,T), RS1001141105 (1:111305203 A>G), RS1001282003 (1:111316908 C>T), RS1001294782 (1:111311905 G>A)

Disease associations

OMIM: gene MIM:606080 | disease phenotypes:

GenCC curated gene-disease

Mondo (0):

Orphanet (0):

HPO phenotypes

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

GWAS associations

4 associations (top):

Study	Trait	p-value
GCST002666_6	Interferon alpha levels in systemic lupus erythematosus	3.000000e-06
GCST007726_1	Anti-Toxoplasma gondii IgG seropositivity	5.000000e-06
GCST009391_1500	Metabolite levels	6.000000e-06
GCST009391_91	Metabolite levels	9.000000e-06

EFO canonical traits (3, from GWAS)

EFO ID	Trait name
EFO:0006517	interferon alpha measurement
EFO:0007047	Toxoplasma gondii seropositivity
EFO:0010416	triacylglycerol 52:4 measurement

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (1): CHEMBL1293197 (SINGLE PROTEIN)

Molecules with ChEMBL bioactivity

1 molecules (phase ≥1), by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 206 (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
CHEMBL4788866	5-(4-((2S,5S)-5-(4-CHLOROBENZYL)-2-METHYLMORPHOLINO)PIPERIDIN-1-YL)-1H-1,2,4-TRIAZOL-3-AMINE	2	206

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

PharmGKB clinical annotations

1 annotations.

Variant	Type	Level	Drugs	Phenotypes
rs3818822	Toxicity	3	aspirin	Aspirin-induced asthma

PharmGKB variants

1 variants.

Variant	Genes	Level	Score	#Clin annots	Drugs
rs3818822	CHIA	3	3.00	1	aspirin

GtoPdb / IUPHAR curated pharmacology

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

Target class: enzyme — Chitinases

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

Ligand	Action	Affinity	Parameter
GLPG4716	Inhibition	8.05	pIC50
compound 7f [PMID: 29283260]	Inhibition	7.85	pIC50

Binding affinities (BindingDB)

51 measured of 88 human assays (88 total across all organisms); most potent 50 below. Values come from heterogeneous assays and are not directly comparable.

Ligand	Measure	Value	Patent
(6R)-1′-(5-amino-4H-1,2,4-triazol-3-yl)-6-(4-chlorobenzyl)-[1,4′-bipiperidine]-3-carboxylic acid	IC50	550 nM	US-10208020: Substituted amino triazoles useful as human chitinase inhibitors
5-((2S,4S)-2-(4-chlorobenzyl)-4-methoxy-[1,4′-bipiperidin]-1′-yl)-4H-1,2,4-triazol-3-amine	IC50	550 nM	US-10208020: Substituted amino triazoles useful as human chitinase inhibitors
5-(4-((2S,3S)-2-(4-chlorobenzyl)-3-methoxyazetidin-1-yl)piperidin-1-yl)-4H-1,2,4-triazol-3-amine	IC50	550 nM	US-10208020: Substituted amino triazoles useful as human chitinase inhibitors
(S)-5-(4-(2-(4-chlorobenzyl)piperazin-1-yl)piperidin-1-yl)-4H-1,2,4-triazol-3-amine	IC50	550 nM	US-10208020: Substituted amino triazoles useful as human chitinase inhibitors
(S)-5-(4-(2-(4-chlorobenzyl)-4-methylpiperazin-1-yl)piperidin-1-yl)-4H-1,2,4-triazol-3-amine	IC50	550 nM	US-10208020: Substituted amino triazoles useful as human chitinase inhibitors
(S)-5-(4-(2-(4-chlorobenzyl)-4-isobutylpiperazin-1-yl)piperidin-1-yl)-4H-1,2,4-triazol-3-amine	IC50	550 nM	US-10208020: Substituted amino triazoles useful as human chitinase inhibitors
((2R,5S)-4-(1-(5-amino-4H-1,2,4-triazol-3-yl)piperidin-4-yl)-5-(4-chlorobenzyl)-1-methylpiperazin-2-yl)methanol	IC50	550 nM	US-10208020: Substituted amino triazoles useful as human chitinase inhibitors
methyl 2-[(2S,5S)-4-[1-(5-amino-1H-1,2,4-triazol-3-yl)piperidin-4-yl]-5-[(4-chlorophenyl)methyl]-2-methylpiperazin-1-yl]acetate	IC50	550 nM	US-10208020: Substituted amino triazoles useful as human chitinase inhibitors
(S)-4-(1-(5-amino-4H-1,2,4-triazol-3-yl)piperidin-4-yl)-3-(4-chlorobenzyl)thiomorpholine 1,1-dioxide	IC50	550 nM	US-10208020: Substituted amino triazoles useful as human chitinase inhibitors
5-(4-((2R,5S)-5-(4-chlorobenzyl)-2-methylmorpholino)piperidin-1-yl)-4H-1,2,4-triazol-3-amine	IC50	550 nM	US-10208020: Substituted amino triazoles useful as human chitinase inhibitors
(5S)-1-(1-(5-amino-4H-1,2,4-triazol-3-yl)piperidin-4-yl)-5-(4-chlorobenzyl)-3-methylpyrrolidin-3-ol	IC50	550 nM	US-10208020: Substituted amino triazoles useful as human chitinase inhibitors
3-((3S,4S)-4-((2S,5S)-5-(4-chlorobenzyl)-2-methylmorpholino)-3-methoxypiperidin-1-yl)-1H-1,2,4-triazol-5-amine	IC50	550 nM	US-10208020: Substituted amino triazoles useful as human chitinase inhibitors
(S)-5-(4-(3-(4-chlorobenzyl)-6-methylene-1,4-oxazepan-4-yl)piperidin-1-yl)-4H-1,2,4-triazol-3-amine	IC50	550 nM	US-10208020: Substituted amino triazoles useful as human chitinase inhibitors
(S)-5-(4-(3-(4-chlorobenzyl)-1-methyl-2,3-dihydro-1H-benzo[e][1,4]diazepin-4(5H)-yl)piperidin-1-yl)-4H-1,2,4-triazol-3-amine	IC50	550 nM	US-10208020: Substituted amino triazoles useful as human chitinase inhibitors
(S)-5-(4-(7-chloro-3-(4-chlorobenzyl)-1-methyl-2,3-dihydro-1H-benzo[e][1,4]diazepin-4(5H)-yl)piperidin-1-yl)-4H-1,2,4-triazol-3-amine	IC50	550 nM	US-10208020: Substituted amino triazoles useful as human chitinase inhibitors
(S)-5-(4-(3-(4-chlorobenzyl)-2,3-dihydrobenzo[f][1,4]oxazepin-4(5H)-yl)piperidin-1-yl)-4H-1,2,4-triazol-3-amine	IC50	550 nM	US-10208020: Substituted amino triazoles useful as human chitinase inhibitors
(S)-5-(4-(3-(4-chlorobenzyl)-7-fluoro-2,3-dihydrobenzo[f][1,4]oxazepin-4(5H)-yl)piperidin-1-yl)-4H-1,2,4-triazol-3-amine	IC50	550 nM	US-10208020: Substituted amino triazoles useful as human chitinase inhibitors
3-[4-[2-[(4-chlorophenyl)methyl]piperazin-1-yl]piperidin-1-yl]-1H-1,2,4-triazol-5-amine	IC50	550 nM	US-9944624: Substituted amino triazoles useful as human chitinase inhibitors
3-[4-[2-[(4-chlorophenyl)methyl]-4-methylpiperazin-1-yl]piperidin-1-yl]-1H-1,2,4-triazol-5-amine	IC50	550 nM	US-9944624: Substituted amino triazoles useful as human chitinase inhibitors
3-[4-[2-[(4-chlorophenyl)methyl]-4-(2-methylpropyl)piperazin-1-yl]piperidin-1-yl]-1H-1,2,4-triazol-5-amine	IC50	550 nM	US-9944624: Substituted amino triazoles useful as human chitinase inhibitors
[(2R)-4-[1-(5-amino-1H-1,2,4-triazol-3-yl)piperidin-4-yl]-5-[(4-chlorophenyl)methyl]-1-methylpiperazin-2-yl]methanol	IC50	550 nM	US-9944624: Substituted amino triazoles useful as human chitinase inhibitors
3-[4-[3-[(4-chlorophenyl)methyl]-1,1-dioxo-1,4-thiazinan-4-yl]piperidin-1-yl]-1H-1,2,4-triazol-5-amine	IC50	550 nM	US-9944624: Substituted amino triazoles useful as human chitinase inhibitors
3-[4-[(2R)-5-[(4-chlorophenyl)methyl]-2-methylmorpholin-4-yl]piperidin-1-yl]-1H-1,2,4-triazol-5-amine	IC50	550 nM	US-9944624: Substituted amino triazoles useful as human chitinase inhibitors
3-[(3S)-4-[(2S)-5-[(4-chlorophenyl)methyl]-2-methylmorpholin-4-yl]-3-methoxypiperidin-1-yl]-1H-1,2,4-triazol-5-amine	IC50	550 nM	US-9944624: Substituted amino triazoles useful as human chitinase inhibitors
(2S,5S)-4-(1-(5-amino-4H-1,2,4-triazol-3-yl)piperidin-4-yl)-5-(4-chlorobenzyl)morpholine-2-carboxamide	IC50	5500 nM	US-10208020: Substituted amino triazoles useful as human chitinase inhibitors
(6R)-1′-(5-amino-4H-1,2,4-triazol-3-yl)-6-(4-chlorobenzyl)-3-methyl-[1,4′-bipiperidine]-3-carboxylic acid	IC50	5500 nM	US-10208020: Substituted amino triazoles useful as human chitinase inhibitors
5-((2S,4R)-2-(4-chlorobenzyl)-4-methoxy-[1,4′-bipiperidin]-1′-yl)-4H-1,2,4-triazol-3-amine	IC50	5500 nM	US-10208020: Substituted amino triazoles useful as human chitinase inhibitors
(S)-4-(1-(5-amino-4H-1,2,4-triazol-3-yl)piperidin-4-yl)-5-(4-chlorobenzyl)piperazin-2-one	IC50	5500 nM	US-10208020: Substituted amino triazoles useful as human chitinase inhibitors
(S)-5-(4-(2-(4-chlorobenzyl)-4-(methylsulfonyl)piperazin-1-yl)piperidin-1-yl)-4H-1,2,4-triazol-3-amine	IC50	5500 nM	US-10208020: Substituted amino triazoles useful as human chitinase inhibitors
(S)-5-(4-(2-(4-chlorobenzyl)-4-tosylpiperazin-1-yl)piperidin-1-yl)-4H-1,2,4-triazol-3-amine	IC50	5500 nM	US-10208020: Substituted amino triazoles useful as human chitinase inhibitors
5-(4-((2S,5S)-2-(4-chlorobenzyl)-5-methyl-4-(methylsulfonyl)piperazin-1-yl)piperidin-1-yl)-4H-1,2,4-triazol-3-amine	IC50	5500 nM	US-10208020: Substituted amino triazoles useful as human chitinase inhibitors
(S)-4-(1-(5-amino-4H-1,2,4-triazol-3-yl)piperidin-4-yl)-3-(4-chlorobenzyl)piperazin-2-one	IC50	5500 nM	US-10208020: Substituted amino triazoles useful as human chitinase inhibitors
5-(4-((3S,6S)-3-(4-chlorobenzyl)-2,2,6-trimethylmorpholino)piperidin-1-yl)-4H-1,2,4-triazol-3-amine	IC50	5500 nM	US-10208020: Substituted amino triazoles useful as human chitinase inhibitors
(S)-5-(4-(7-chloro-3-(4-chlorobenzyl)-2,3-dihydrobenzo[f][1,4]oxazepin-4(5H)-yl)piperidin-1-yl)-4H-1,2,4-triazol-3-amine	IC50	5500 nM	US-10208020: Substituted amino triazoles useful as human chitinase inhibitors
(S)-5-(4-(3-(4-chlorobenzyl)-2,3-dihydropyrido[4,3-f][1,4]oxazepin-4(5H)-yl)piperidin-1-yl)-4H-1,2,4-triazol-3-amine	IC50	5500 nM	US-10208020: Substituted amino triazoles useful as human chitinase inhibitors
3-[4-[2-[(4-chlorophenyl)methyl]-4-methylsulfonylpiperazin-1-yl]piperidin-1-yl]-1H-1,2,4-triazol-5-amine	IC50	5500 nM	US-9944624: Substituted amino triazoles useful as human chitinase inhibitors
3-[4-[2-[(4-chlorophenyl)methyl]-4-(4-methylphenyl)sulfonylpiperazin-1-yl]piperidin-1-yl]-1H-1,2,4-triazol-5-amine	IC50	5500 nM	US-9944624: Substituted amino triazoles useful as human chitinase inhibitors
3-[4-[(5S)-2-[(4-chlorophenyl)methyl]-5-methyl-4-methylsulfonylpiperazin-1-yl]piperidin-1-yl]-1H-1,2,4-triazol-5-amine	IC50	5500 nM	US-9944624: Substituted amino triazoles useful as human chitinase inhibitors
methyl (2S)-4-[1-(5-amino-1H-1,2,4-triazol-3-yl)piperidin-4-yl]-5-[(4-chlorophenyl)methyl]-2-methylpiperazine-1-carboxylate	IC50	5500 nM	US-9944624: Substituted amino triazoles useful as human chitinase inhibitors
4-[1-(5-amino-1H-1,2,4-triazol-3-yl)piperidin-4-yl]-3-[(4-chlorophenyl)methyl]piperazin-2-one	IC50	5500 nM	US-9944624: Substituted amino triazoles useful as human chitinase inhibitors
3-[4-[(6S)-3-[(4-chlorophenyl)methyl]-2,2,6-trimethylmorpholin-4-yl]piperidin-1-yl]-1H-1,2,4-triazol-5-amine	IC50	5500 nM	US-9944624: Substituted amino triazoles useful as human chitinase inhibitors
(1′-(5-amino-4H-1,2,4-triazol-3-yl)-[1,4′-bipiperidin]-2-yl)(4-chlorophenyl)methanol	IC50	55000 nM	US-10208020: Substituted amino triazoles useful as human chitinase inhibitors
5-(4-((2S,3R)-2-(4-chlorobenzyl)-3-fluoroazetidin-1-yl)piperidin-1-yl)-4H-1,2,4-triazol-3-amine	IC50	55000 nM	US-10208020: Substituted amino triazoles useful as human chitinase inhibitors
5-(4-((2S,5S)-2,5-bis(4-chlorobenzyl)-4-(methyl sulfonyl)piperazin-1-yl)piperidin-1-yl)-4H-1,2,4-triazol-3-amine	IC50	55000 nM	US-10208020: Substituted amino triazoles useful as human chitinase inhibitors
1-((2S,5S)-4-(1-(5-amino-4H-1,2,4-triazol-3-yl)piperidin-4-yl)-5-(4-chlorobenzyl)-2-methylpiperazin-1-yl)ethanone	IC50	55000 nM	US-10208020: Substituted amino triazoles useful as human chitinase inhibitors
methyl (2S,5S)-4-[1-(5-amino-1H-1,2,4-triazol-3-yl)piperidin-4-yl]-5-[(4-chlorophenyl)methyl]-2-methylpiperazine-1-carboxylate	IC50	55000 nM	US-10208020: Substituted amino triazoles useful as human chitinase inhibitors
(S)-5-(4-(3-(4-chlorobenzyl)-2,2-dimethylmorpholino)piperidin-1-yl)-4H-1,2,4-triazol-3-amine	IC50	55000 nM	US-10208020: Substituted amino triazoles useful as human chitinase inhibitors
(S)-5-(4-(7,9-dichloro-3-(4-chlorobenzyl)-2,3-dihydrobenzo[f][1,4]oxazepin-4(5H)-yl)piperidin-1-yl)-4H-1,2,4-triazol-3-amine	IC50	55000 nM	US-10208020: Substituted amino triazoles useful as human chitinase inhibitors
3-[4-[(5S)-2,5-bis[(4-chlorophenyl)methyl]-4-methylsulfonylpiperazin-1-yl]piperidin-1-yl]-1H-1,2,4-triazol-5-amine	IC50	55000 nM	US-9944624: Substituted amino triazoles useful as human chitinase inhibitors
1-[(2S)-4-[1-(5-amino-1H-1,2,4-triazol-3-yl)piperidin-4-yl]-5-[(4-chlorophenyl)methyl]-2-methylpiperazin-1-yl]ethanone	IC50	55000 nM	US-9944624: Substituted amino triazoles useful as human chitinase inhibitors

ChEMBL bioactivities

186 potent at pChembl≥5 of 214 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).

pChembl	Type	Value	Unit	Molecule
9.15	IC50	0.7	nM	CHEMBL4643001
8.85	IC50	1.4	nM	CHEMBL4635305
8.80	IC50	1.6	nM	CHEMBL4756869
8.70	IC50	2	nM	CHEMBL4637417
8.70	IC50	2	nM	CHEMBL4634943
8.52	IC50	3	nM	CHEMBL4077644
8.47	IC50	3.4	nM	CHEMBL4084573
8.47	IC50	3.4	nM	CHEMBL4794014
8.46	IC50	3.5	nM	CHEMBL4077644
8.40	IC50	4	nM	CHEMBL4646309
8.32	Ki	4.8	nM	5-(4-((2S,5S)-5-(4-CHLOROBENZYL)-2-METHYLMORPHOLINO)PIPERIDIN-1-YL)-1H-1,2,4-TRIAZOL-3-AMINE
8.30	IC50	5	nM	CHEMBL4077482
8.30	IC50	5	nM	CHEMBL4632547
8.30	IC50	5	nM	CHEMBL4646247
8.27	IC50	5.4	nM	CHEMBL4077482
8.22	IC50	6	nM	CHEMBL4649081
8.17	IC50	6.8	nM	CHEMBL4789376
8.15	IC50	7	nM	CHEMBL4640857
8.15	IC50	7	nM	CHEMBL4648962
8.15	IC50	7	nM	CHEMBL4764430
8.10	IC50	8	nM	CHEMBL4638897
8.06	IC50	8.7	nM	CHEMBL4082060
8.06	IC50	8.7	nM	CHEMBL4068944
8.05	IC50	9	nM	5-(4-((2S,5S)-5-(4-CHLOROBENZYL)-2-METHYLMORPHOLINO)PIPERIDIN-1-YL)-1H-1,2,4-TRIAZOL-3-AMINE
8.05	IC50	8.9	nM	CHEMBL4755139
7.92	IC50	12	nM	CHEMBL4642053
7.92	IC50	12	nM	CHEMBL4644319
7.87	Ki	13.5	nM	CHEMBL4076989
7.85	IC50	14.2	nM	CHEMBL4076989
7.82	IC50	15	nM	CHEMBL4076989
7.82	IC50	15	nM	CHEMBL4637250
7.72	IC50	19	nM	CHEMBL4537828
7.68	IC50	21	nM	CHEMBL4541831
7.66	IC50	22	nM	CHEMBL4461925
7.64	IC50	23	nM	CHEMBL4580568
7.62	IC50	24	nM	CHEMBL4749391
7.58	IC50	26	nM	CHEMBL4470253
7.55	IC50	28	nM	CHEMBL4546929
7.55	IC50	28	nM	CHEMBL4453964
7.52	IC50	30	nM	CHEMBL4648998
7.43	IC50	37	nM	CHEMBL4457342
7.41	IC50	39	nM	CHEMBL4442663
7.40	IC50	40	nM	CHEMBL4446970
7.40	IC50	40	nM	ALLOSAMIDIN
7.31	IC50	49	nM	CHEMBL4647895
7.30	IC50	50	nM	CHEMBL4547227
7.27	IC50	54	nM	CHEMBL4776610
7.26	IC50	55	nM	CHEMBL4648162
7.17	IC50	68	nM	CHEMBL4464754
7.17	IC50	68	nM	CHEMBL4637576

PubChem BioAssay actives

128 with measured affinity, of 213 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
3-[4-[(3S)-7-chloro-3-[(4-chlorophenyl)methyl]-1-methyl-3,5-dihydro-2H-1,4-benzodiazepin-4-yl]piperidin-1-yl]-1H-1,2,4-triazol-5-amine	1658488: Inhibition of full length recombinant C-terminal His-tagged human acidic mammalian chitinase expressed in CHOK1 cells assessed as reduction in chitinolytic activity using 4-methylumbelliferyl-beta-D-N,N-diacetylchitobioside hydrate as substrate incubated for 60 mins under shaking condition by microplate fluorometry analysis	ic50	0.0007	uM
3-[4-[(3S)-3-[(4-chlorophenyl)methyl]-1-methyl-3,5-dihydro-2H-1,4-benzodiazepin-4-yl]piperidin-1-yl]-1H-1,2,4-triazol-5-amine	1658488: Inhibition of full length recombinant C-terminal His-tagged human acidic mammalian chitinase expressed in CHOK1 cells assessed as reduction in chitinolytic activity using 4-methylumbelliferyl-beta-D-N,N-diacetylchitobioside hydrate as substrate incubated for 60 mins under shaking condition by microplate fluorometry analysis	ic50	0.0014	uM
3-[4-[(2S,5S)-5-[(4-chlorophenyl)methyl]-2-(2-methylpropyl)morpholin-4-yl]piperidin-1-yl]-1H-1,2,4-triazol-5-amine	1699195: Inhibition of full-length C-terminal his-tagged human AMCase expressed in CHO-K1 cells assessed as reduction in chitinolytic activity using 4-methylumbelliferyl-beta-D-N,N-diacetylchitobioside hydrate as substrate after 60 mins by fluorometric assay	ic50	0.0016	uM
2-[[[1-(5-amino-1H-1,2,4-triazol-3-yl)piperidin-4-yl]-[2-(4-chlorophenyl)ethyl]amino]methyl]phenol	1658488: Inhibition of full length recombinant C-terminal His-tagged human acidic mammalian chitinase expressed in CHOK1 cells assessed as reduction in chitinolytic activity using 4-methylumbelliferyl-beta-D-N,N-diacetylchitobioside hydrate as substrate incubated for 60 mins under shaking condition by microplate fluorometry analysis	ic50	0.0020	uM
3-[[[1-(5-amino-1H-1,2,4-triazol-3-yl)piperidin-4-yl]-[2-(4-chlorophenyl)ethyl]amino]methyl]phenol	1658488: Inhibition of full length recombinant C-terminal His-tagged human acidic mammalian chitinase expressed in CHOK1 cells assessed as reduction in chitinolytic activity using 4-methylumbelliferyl-beta-D-N,N-diacetylchitobioside hydrate as substrate incubated for 60 mins under shaking condition by microplate fluorometry analysis	ic50	0.0020	uM
1-(5-amino-1H-1,2,4-triazol-3-yl)-N-[2-(4-chlorophenyl)ethyl]-N-[(2-chlorophenyl)methyl]piperidin-4-amine	1658488: Inhibition of full length recombinant C-terminal His-tagged human acidic mammalian chitinase expressed in CHOK1 cells assessed as reduction in chitinolytic activity using 4-methylumbelliferyl-beta-D-N,N-diacetylchitobioside hydrate as substrate incubated for 60 mins under shaking condition by microplate fluorometry analysis	ic50	0.0030	uM
1-(5-amino-1H-1,2,4-triazol-3-yl)-N-[2-(4-chlorophenyl)ethyl]-N-(naphthalen-1-ylmethyl)piperidin-4-amine	1468013: Inhibition of human recombinant full length C-terminal His-tagged acidic mammalian chitinase expressed in CHO-K1 cells using 4-methylumbelliferyl-beta-D-N,N’-diacetylchitobioside hydrate as substrate after 60 mins by fluorescence assay	ic50	0.0034	uM
3-[4-[(2S,5S)-5-[(4-chlorophenyl)methyl]-2-propan-2-ylmorpholin-4-yl]piperidin-1-yl]-1H-1,2,4-triazol-5-amine	1699195: Inhibition of full-length C-terminal his-tagged human AMCase expressed in CHO-K1 cells assessed as reduction in chitinolytic activity using 4-methylumbelliferyl-beta-D-N,N-diacetylchitobioside hydrate as substrate after 60 mins by fluorometric assay	ic50	0.0034	uM
1-(5-amino-1H-1,2,4-triazol-3-yl)-N-[2-(4-chlorophenyl)ethyl]-N-[(4-chlorophenyl)methyl]piperidin-4-amine	1658488: Inhibition of full length recombinant C-terminal His-tagged human acidic mammalian chitinase expressed in CHOK1 cells assessed as reduction in chitinolytic activity using 4-methylumbelliferyl-beta-D-N,N-diacetylchitobioside hydrate as substrate incubated for 60 mins under shaking condition by microplate fluorometry analysis	ic50	0.0040	uM
3-[4-[(2S,5S)-5-[(4-chlorophenyl)methyl]-2-methylmorpholin-4-yl]piperidin-1-yl]-1H-1,2,4-triazol-5-amine	1699195: Inhibition of full-length C-terminal his-tagged human AMCase expressed in CHO-K1 cells assessed as reduction in chitinolytic activity using 4-methylumbelliferyl-beta-D-N,N-diacetylchitobioside hydrate as substrate after 60 mins by fluorometric assay	ki	0.0048	uM
1-(5-amino-1H-1,2,4-triazol-3-yl)-N-benzyl-N-[2-(4-chlorophenyl)ethyl]piperidin-4-amine	1658488: Inhibition of full length recombinant C-terminal His-tagged human acidic mammalian chitinase expressed in CHOK1 cells assessed as reduction in chitinolytic activity using 4-methylumbelliferyl-beta-D-N,N-diacetylchitobioside hydrate as substrate incubated for 60 mins under shaking condition by microplate fluorometry analysis	ic50	0.0050	uM
1-(5-amino-1H-1,2,4-triazol-3-yl)-N-[(2-chloro-4-fluorophenyl)methyl]-N-[2-(4-chlorophenyl)ethyl]piperidin-4-amine	1658488: Inhibition of full length recombinant C-terminal His-tagged human acidic mammalian chitinase expressed in CHOK1 cells assessed as reduction in chitinolytic activity using 4-methylumbelliferyl-beta-D-N,N-diacetylchitobioside hydrate as substrate incubated for 60 mins under shaking condition by microplate fluorometry analysis	ic50	0.0050	uM
1-(5-amino-1H-1,2,4-triazol-3-yl)-N-[2-(4-chlorophenyl)ethyl]-N-[(2,5-difluorophenyl)methyl]piperidin-4-amine	1658488: Inhibition of full length recombinant C-terminal His-tagged human acidic mammalian chitinase expressed in CHOK1 cells assessed as reduction in chitinolytic activity using 4-methylumbelliferyl-beta-D-N,N-diacetylchitobioside hydrate as substrate incubated for 60 mins under shaking condition by microplate fluorometry analysis	ic50	0.0050	uM
1-(5-amino-1H-1,2,4-triazol-3-yl)-N-[2-(4-chlorophenyl)ethyl]-N-[(3-chlorophenyl)methyl]piperidin-4-amine	1658488: Inhibition of full length recombinant C-terminal His-tagged human acidic mammalian chitinase expressed in CHOK1 cells assessed as reduction in chitinolytic activity using 4-methylumbelliferyl-beta-D-N,N-diacetylchitobioside hydrate as substrate incubated for 60 mins under shaking condition by microplate fluorometry analysis	ic50	0.0060	uM
[(2R,5S)-4-[1-(5-amino-1H-1,2,4-triazol-3-yl)piperidin-4-yl]-5-[(4-chlorophenyl)methyl]morpholin-2-yl]methanol	1699195: Inhibition of full-length C-terminal his-tagged human AMCase expressed in CHO-K1 cells assessed as reduction in chitinolytic activity using 4-methylumbelliferyl-beta-D-N,N-diacetylchitobioside hydrate as substrate after 60 mins by fluorometric assay	ic50	0.0068	uM
2-[(2R,5S)-4-[1-(5-amino-1H-1,2,4-triazol-3-yl)piperidin-4-yl]-5-[(4-chlorophenyl)methyl]morpholin-2-yl]propan-2-ol	1699195: Inhibition of full-length C-terminal his-tagged human AMCase expressed in CHO-K1 cells assessed as reduction in chitinolytic activity using 4-methylumbelliferyl-beta-D-N,N-diacetylchitobioside hydrate as substrate after 60 mins by fluorometric assay	ic50	0.0070	uM
3-[4-[(3S)-3-[(4-chlorophenyl)methyl]-3,5-dihydro-2H-1,4-benzoxazepin-4-yl]piperidin-1-yl]-1H-1,2,4-triazol-5-amine	1658488: Inhibition of full length recombinant C-terminal His-tagged human acidic mammalian chitinase expressed in CHOK1 cells assessed as reduction in chitinolytic activity using 4-methylumbelliferyl-beta-D-N,N-diacetylchitobioside hydrate as substrate incubated for 60 mins under shaking condition by microplate fluorometry analysis	ic50	0.0070	uM
3-[4-[(3S)-3-[(4-chlorophenyl)methyl]-7-fluoro-3,5-dihydro-2H-1,4-benzoxazepin-4-yl]piperidin-1-yl]-1H-1,2,4-triazol-5-amine	1658488: Inhibition of full length recombinant C-terminal His-tagged human acidic mammalian chitinase expressed in CHOK1 cells assessed as reduction in chitinolytic activity using 4-methylumbelliferyl-beta-D-N,N-diacetylchitobioside hydrate as substrate incubated for 60 mins under shaking condition by microplate fluorometry analysis	ic50	0.0070	uM
3-[4-[(3S)-7-chloro-3-[(4-chlorophenyl)methyl]-3,5-dihydro-2H-1,4-benzoxazepin-4-yl]piperidin-1-yl]-1H-1,2,4-triazol-5-amine	1658488: Inhibition of full length recombinant C-terminal His-tagged human acidic mammalian chitinase expressed in CHOK1 cells assessed as reduction in chitinolytic activity using 4-methylumbelliferyl-beta-D-N,N-diacetylchitobioside hydrate as substrate incubated for 60 mins under shaking condition by microplate fluorometry analysis	ic50	0.0080	uM
1-(5-amino-1H-1,2,4-triazol-3-yl)-N-[2-(4-bromophenyl)ethyl]-N-(2-methylpropyl)piperidin-4-amine	1468013: Inhibition of human recombinant full length C-terminal His-tagged acidic mammalian chitinase expressed in CHO-K1 cells using 4-methylumbelliferyl-beta-D-N,N’-diacetylchitobioside hydrate as substrate after 60 mins by fluorescence assay	ic50	0.0087	uM
1-(5-amino-1H-1,2,4-triazol-3-yl)-N-[2-(4-chlorophenyl)ethyl]-N-(cyclohexylmethyl)piperidin-4-amine	1468013: Inhibition of human recombinant full length C-terminal His-tagged acidic mammalian chitinase expressed in CHO-K1 cells using 4-methylumbelliferyl-beta-D-N,N’-diacetylchitobioside hydrate as substrate after 60 mins by fluorescence assay	ic50	0.0087	uM
3-[4-[(2R,5S)-5-[(4-chlorophenyl)methyl]-2-(methoxymethyl)morpholin-4-yl]piperidin-1-yl]-1H-1,2,4-triazol-5-amine	1699195: Inhibition of full-length C-terminal his-tagged human AMCase expressed in CHO-K1 cells assessed as reduction in chitinolytic activity using 4-methylumbelliferyl-beta-D-N,N-diacetylchitobioside hydrate as substrate after 60 mins by fluorometric assay	ic50	0.0089	uM
1-(5-amino-1H-1,2,4-triazol-3-yl)-N-[2-(4-chlorophenyl)ethyl]-N-[[3-(trifluoromethyl)phenyl]methyl]piperidin-4-amine	1658488: Inhibition of full length recombinant C-terminal His-tagged human acidic mammalian chitinase expressed in CHOK1 cells assessed as reduction in chitinolytic activity using 4-methylumbelliferyl-beta-D-N,N-diacetylchitobioside hydrate as substrate incubated for 60 mins under shaking condition by microplate fluorometry analysis	ic50	0.0120	uM
3-[4-[(3S)-3-[(4-chlorophenyl)methyl]-6-methylidene-1,4-oxazepan-4-yl]piperidin-1-yl]-1H-1,2,4-triazol-5-amine	1658488: Inhibition of full length recombinant C-terminal His-tagged human acidic mammalian chitinase expressed in CHOK1 cells assessed as reduction in chitinolytic activity using 4-methylumbelliferyl-beta-D-N,N-diacetylchitobioside hydrate as substrate incubated for 60 mins under shaking condition by microplate fluorometry analysis	ic50	0.0120	uM
1-(5-amino-1H-1,2,4-triazol-3-yl)-N-[2-(4-chlorophenyl)ethyl]-N-(2-methylpropyl)piperidin-4-amine	1468017: Inhibition of human recombinant full length C-terminal His-tagged acidic mammalian chitinase expressed in CHO-K1 cells using 4-methylumbelliferyl-beta-D-N,N’-diacetylchitobioside hydrate as substrate after 60 mins by Lineweaver-Burk plot analysis	ki	0.0135	uM
1-(5-amino-1H-1,2,4-triazol-3-yl)-N-[2-(4-chlorophenyl)ethyl]-N-[(3-chloro-4-pyridinyl)methyl]piperidin-4-amine	1658488: Inhibition of full length recombinant C-terminal His-tagged human acidic mammalian chitinase expressed in CHOK1 cells assessed as reduction in chitinolytic activity using 4-methylumbelliferyl-beta-D-N,N-diacetylchitobioside hydrate as substrate incubated for 60 mins under shaking condition by microplate fluorometry analysis	ic50	0.0150	uM
3-[4-[(2S,4S)-2-[(4-chlorophenyl)methyl]-4-methoxypyrrolidin-1-yl]piperidin-1-yl]-1H-1,2,4-triazol-5-amine	1516422: Inhibition of full-length C-terminal his-tagged human acidic mammalian chitinase expressed in CHOK1 cells assessed as reduction in chitinolytic activity using 4-methylumbelliferyl-beta-D-N,N-diacetylchitobioside hydrate as substrate after 60 mins by fluorometric assay	ic50	0.0190	uM
1-(5-amino-1H-1,2,4-triazol-3-yl)-N-[2-(4-chlorophenyl)ethyl]-N-(oxolan-2-ylmethyl)piperidin-4-amine	1516422: Inhibition of full-length C-terminal his-tagged human acidic mammalian chitinase expressed in CHOK1 cells assessed as reduction in chitinolytic activity using 4-methylumbelliferyl-beta-D-N,N-diacetylchitobioside hydrate as substrate after 60 mins by fluorometric assay	ic50	0.0210	uM
3-[4-[(3S)-3-[(4-chlorophenyl)methyl]morpholin-4-yl]piperidin-1-yl]-1H-1,2,4-triazol-5-amine	1516422: Inhibition of full-length C-terminal his-tagged human acidic mammalian chitinase expressed in CHOK1 cells assessed as reduction in chitinolytic activity using 4-methylumbelliferyl-beta-D-N,N-diacetylchitobioside hydrate as substrate after 60 mins by fluorometric assay	ic50	0.0220	uM
3-[4-[(2R)-2-[(4-chlorophenyl)methyl]piperidin-1-yl]piperidin-1-yl]-1H-1,2,4-triazol-5-amine	1516422: Inhibition of full-length C-terminal his-tagged human acidic mammalian chitinase expressed in CHOK1 cells assessed as reduction in chitinolytic activity using 4-methylumbelliferyl-beta-D-N,N-diacetylchitobioside hydrate as substrate after 60 mins by fluorometric assay	ic50	0.0230	uM
(2R,5S)-4-[1-(5-amino-1H-1,2,4-triazol-3-yl)piperidin-4-yl]-5-[(4-chlorophenyl)methyl]-N-methylmorpholine-2-carboxamide	1699195: Inhibition of full-length C-terminal his-tagged human AMCase expressed in CHO-K1 cells assessed as reduction in chitinolytic activity using 4-methylumbelliferyl-beta-D-N,N-diacetylchitobioside hydrate as substrate after 60 mins by fluorometric assay	ic50	0.0240	uM
3-[4-[(2S,4R)-2-[(4-chlorophenyl)methyl]-4-methoxypyrrolidin-1-yl]piperidin-1-yl]-1H-1,2,4-triazol-5-amine	1516422: Inhibition of full-length C-terminal his-tagged human acidic mammalian chitinase expressed in CHOK1 cells assessed as reduction in chitinolytic activity using 4-methylumbelliferyl-beta-D-N,N-diacetylchitobioside hydrate as substrate after 60 mins by fluorometric assay	ic50	0.0260	uM
2-[[1-(5-amino-1H-1,2,4-triazol-3-yl)piperidin-4-yl]-[2-(4-chlorophenyl)ethyl]amino]-N-methylethanesulfonamide	1516422: Inhibition of full-length C-terminal his-tagged human acidic mammalian chitinase expressed in CHOK1 cells assessed as reduction in chitinolytic activity using 4-methylumbelliferyl-beta-D-N,N-diacetylchitobioside hydrate as substrate after 60 mins by fluorometric assay	ic50	0.0280	uM
1-(5-amino-1H-1,2,4-triazol-3-yl)-N-[2-(4-chlorophenyl)ethyl]-N-(2-methoxy-2-methylpropyl)piperidin-4-amine	1516422: Inhibition of full-length C-terminal his-tagged human acidic mammalian chitinase expressed in CHOK1 cells assessed as reduction in chitinolytic activity using 4-methylumbelliferyl-beta-D-N,N-diacetylchitobioside hydrate as substrate after 60 mins by fluorometric assay	ic50	0.0280	uM
3-[4-[(3S)-3-[(4-chlorophenyl)methyl]-3,5-dihydro-2H-pyrido[3,2-f][1,4]oxazepin-4-yl]piperidin-1-yl]-1H-1,2,4-triazol-5-amine	1658488: Inhibition of full length recombinant C-terminal His-tagged human acidic mammalian chitinase expressed in CHOK1 cells assessed as reduction in chitinolytic activity using 4-methylumbelliferyl-beta-D-N,N-diacetylchitobioside hydrate as substrate incubated for 60 mins under shaking condition by microplate fluorometry analysis	ic50	0.0300	uM
N-[2-[[1-(5-amino-1H-1,2,4-triazol-3-yl)piperidin-4-yl]-[2-(4-chlorophenyl)ethyl]amino]ethyl]methanesulfonamide	1516422: Inhibition of full-length C-terminal his-tagged human acidic mammalian chitinase expressed in CHOK1 cells assessed as reduction in chitinolytic activity using 4-methylumbelliferyl-beta-D-N,N-diacetylchitobioside hydrate as substrate after 60 mins by fluorometric assay	ic50	0.0370	uM
(3S,5S)-1-[1-(5-amino-1H-1,2,4-triazol-3-yl)piperidin-4-yl]-5-[(4-chlorophenyl)methyl]pyrrolidin-3-ol	1516422: Inhibition of full-length C-terminal his-tagged human acidic mammalian chitinase expressed in CHOK1 cells assessed as reduction in chitinolytic activity using 4-methylumbelliferyl-beta-D-N,N-diacetylchitobioside hydrate as substrate after 60 mins by fluorometric assay	ic50	0.0390	uM
N-[(2S,3R,4S,5S,6R)-2-[(2R,3S,4S,5R,6R)-6-[[(3aR,4R,5R,6S,6aS)-2-(dimethylamino)-4-hydroxy-6-(hydroxymethyl)-4,5,6,6a-tetrahydro-3aH-cyclopenta[d][1,3]oxazol-5-yl]oxy]-5-acetamido-4-hydroxy-2-(hydroxymethyl)oxan-3-yl]oxy-4,5-dihydroxy-6-(hydroxymethyl)oxan-3-yl]acetamide	539003: Inhibition of human chitinase	ic50	0.0400	uM
1-[[1-(5-amino-1H-1,2,4-triazol-3-yl)piperidin-4-yl]-[2-(4-chlorophenyl)ethyl]amino]-2-methylpropan-2-ol	1516422: Inhibition of full-length C-terminal his-tagged human acidic mammalian chitinase expressed in CHOK1 cells assessed as reduction in chitinolytic activity using 4-methylumbelliferyl-beta-D-N,N-diacetylchitobioside hydrate as substrate after 60 mins by fluorometric assay	ic50	0.0400	uM
(3S)-4-[1-(5-amino-1H-1,2,4-triazol-3-yl)piperidin-4-yl]-3-[(4-chlorophenyl)methyl]-3,5-dihydro-2H-1,4-benzoxazepine-7-carbonitrile	1658488: Inhibition of full length recombinant C-terminal His-tagged human acidic mammalian chitinase expressed in CHOK1 cells assessed as reduction in chitinolytic activity using 4-methylumbelliferyl-beta-D-N,N-diacetylchitobioside hydrate as substrate incubated for 60 mins under shaking condition by microplate fluorometry analysis	ic50	0.0490	uM
(3R,5S)-1-[1-(5-amino-1H-1,2,4-triazol-3-yl)piperidin-4-yl]-5-[(4-chlorophenyl)methyl]pyrrolidin-3-ol	1516422: Inhibition of full-length C-terminal his-tagged human acidic mammalian chitinase expressed in CHOK1 cells assessed as reduction in chitinolytic activity using 4-methylumbelliferyl-beta-D-N,N-diacetylchitobioside hydrate as substrate after 60 mins by fluorometric assay	ic50	0.0500	uM
3-[4-[(2S,5S)-5-[(4-chlorophenyl)methyl]-2-ethylmorpholin-4-yl]piperidin-1-yl]-1H-1,2,4-triazol-5-amine	1699195: Inhibition of full-length C-terminal his-tagged human AMCase expressed in CHO-K1 cells assessed as reduction in chitinolytic activity using 4-methylumbelliferyl-beta-D-N,N-diacetylchitobioside hydrate as substrate after 60 mins by fluorometric assay	ic50	0.0540	uM
3-[4-[(3S)-3-[(4-chlorophenyl)methyl]-3,5-dihydro-2H-pyrido[4,3-f][1,4]oxazepin-4-yl]piperidin-1-yl]-1H-1,2,4-triazol-5-amine	1658488: Inhibition of full length recombinant C-terminal His-tagged human acidic mammalian chitinase expressed in CHOK1 cells assessed as reduction in chitinolytic activity using 4-methylumbelliferyl-beta-D-N,N-diacetylchitobioside hydrate as substrate incubated for 60 mins under shaking condition by microplate fluorometry analysis	ic50	0.0550	uM
3-[4-[(3S)-7,9-dichloro-3-[(4-chlorophenyl)methyl]-3,5-dihydro-2H-1,4-benzoxazepin-4-yl]piperidin-1-yl]-1H-1,2,4-triazol-5-amine	1658488: Inhibition of full length recombinant C-terminal His-tagged human acidic mammalian chitinase expressed in CHOK1 cells assessed as reduction in chitinolytic activity using 4-methylumbelliferyl-beta-D-N,N-diacetylchitobioside hydrate as substrate incubated for 60 mins under shaking condition by microplate fluorometry analysis	ic50	0.0680	uM
1-(5-amino-1H-1,2,4-triazol-3-yl)-N-[2-(4-chlorophenyl)ethyl]-N-(oxan-2-ylmethyl)piperidin-4-amine	1516422: Inhibition of full-length C-terminal his-tagged human acidic mammalian chitinase expressed in CHOK1 cells assessed as reduction in chitinolytic activity using 4-methylumbelliferyl-beta-D-N,N-diacetylchitobioside hydrate as substrate after 60 mins by fluorometric assay	ic50	0.0680	uM
(2S,5S)-5-[(4-chlorophenyl)methyl]-4-[1-(4-fluoro-2-pyridinyl)piperidin-4-yl]-2-methylmorpholine	2090843: Inhibition of human C-terminal His tagged AMCase expressed in CHO-K1 cells using 4-methylumbelliferyl beta-D-N,N’-diacetylchitobioside hydrate as substrate incubated for 60 mins by fluorometric assay	ic50	0.0700	uM
1-(5-amino-1H-1,2,4-triazol-3-yl)-N-[2-(4-bromophenyl)ethyl]-N-ethylpiperidin-4-amine	1468013: Inhibition of human recombinant full length C-terminal His-tagged acidic mammalian chitinase expressed in CHO-K1 cells using 4-methylumbelliferyl-beta-D-N,N’-diacetylchitobioside hydrate as substrate after 60 mins by fluorescence assay	ic50	0.0730	uM
3-[4-[(2R)-2-[(4-chlorophenyl)methyl]pyrrolidin-1-yl]piperidin-1-yl]-1H-1,2,4-triazol-5-amine	1516422: Inhibition of full-length C-terminal his-tagged human acidic mammalian chitinase expressed in CHOK1 cells assessed as reduction in chitinolytic activity using 4-methylumbelliferyl-beta-D-N,N-diacetylchitobioside hydrate as substrate after 60 mins by fluorometric assay	ic50	0.0730	uM
1-(5-amino-1H-1,2,4-triazol-3-yl)-N-[2-(4-chlorophenyl)ethyl]-N-(oxetan-3-yl)piperidin-4-amine	1516422: Inhibition of full-length C-terminal his-tagged human acidic mammalian chitinase expressed in CHOK1 cells assessed as reduction in chitinolytic activity using 4-methylumbelliferyl-beta-D-N,N-diacetylchitobioside hydrate as substrate after 60 mins by fluorometric assay	ic50	0.0830	uM
3-[4-[(2S,5S)-2-[(4-chlorophenyl)methyl]-5-methyl-4-(2-methylpropyl)piperazin-1-yl]piperidin-1-yl]-1H-1,2,4-triazol-5-amine	1699195: Inhibition of full-length C-terminal his-tagged human AMCase expressed in CHO-K1 cells assessed as reduction in chitinolytic activity using 4-methylumbelliferyl-beta-D-N,N-diacetylchitobioside hydrate as substrate after 60 mins by fluorometric assay	ic50	0.0840	uM

CTD chemical–gene interactions

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

Chemical	Actions (top 5)	PubMed papers
Aflatoxin B1	increases methylation	2
CGP 52608	affects binding, increases reaction	1
Arsenic Trioxide	increases expression	1
Benzo(a)pyrene	affects methylation	1
Tobacco Smoke Pollution	increases methylation	1
Valproic Acid	decreases methylation	1
Okadaic Acid	decreases expression	1

ChEMBL screening assays

23 unique, capped per target: 23 binding

Representative assays (with source publication via chembl_document):

Assay ID	Type	Description	Source paper
CHEMBL1041581	Binding	Inhibition of human acidic mammalian chitinase	Molecular modeling of human acidic mammalian chitinase in complex with the natural-product cyclopentapeptide chitinase inhibitor argifin. — Bioorg Med Chem

Clinical trials (associated diseases)

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