gastrointestinal drug

A drug used for its effects on the gastrointestinal system, e.g. controlling gastric acidity, regulating gastrointestinal motility and water flow, and improving digestion.

ChEBI ID: 55324

Members (17)

Member	Definition	Class
16,16-dimethylprostaglandin e2	A prostanoid that is prostaglandin E2 in which both of the hydrogens at position 16 have been replaced by methyl groups. A synthetic analogue of prostaglandin E2, it is a potent inhibitor of pancreatic function and growth of experimental tumors. It also protects the gastric mucosa, prevents ulceration, and promotes the healing of peptic ulcers.	16,16-dimethylprostaglandin E2
alosetron	A pyrido[4,3-b]indole compound having a 5-methyl-1H-imidazol-4-ylmethyl group at the 2-position.	alosetron
alpha-methylene gamma-butyrolactone	A butan-4-olide having a methylene group at the 3-position.	alpha-methylene gamma-butyrolactone
aurapten	A member of the class of coumarins that is umbelliferone in which the phenolic hydrogen has been replaced by a geranyl group. Ii is isolated from several edible fruits and vegetables and exhibits a variety of therapeutic properties.	auraptene
betazole	Pyrazole in which a hydrogen adjacent to one of the nitrogen atoms is substituted by a 2-aminoethyl group. It is a histamine H2-receptor agonist used clinically to test gastric secretory function.	betazole
ceruletide	A decapeptide comprising 5-oxoprolyl, glutamyl, aspartyl, O-sulfotyrosyl, threonyl, glycyl, tryptopyl, methionyl, aspartyl and phenylalaninamide residues in sequence. Found in the skins of certain Australian amphibians, it is an analogue of the gastrointestinal peptide hormone cholecystokinin and stimulates gastric, biliary, and pancreatic secretion. It is used in cases of paralysis of the intestine (paralytic ileus) and as a diagnostic aid in pancreatic malfunction.	ceruletide
ceruletide diethylamine	The diethylamine salt of ceruletide.	ceruletide diethylamine
cyproheptadine	The product resulting from the formal oxidative coupling of position 5 of 5H-dibenzo[a,d]cycloheptene with position 4 of 1-methylpiperidine resulting in the formation of a double bond between the two fragments. It is a sedating antihistamine with antimuscarinic and calcium-channel blocking actions. It is used (particularly as the hydrochloride sesquihydrate) for the relief of allergic conditions including rhinitis, conjunctivitis due to inhalant allergens and foods, urticaria and angioedema, and in pruritic skin disorders. Unlike other antihistamines, it is also a seratonin receptor antagonist, making it useful in conditions such as vascular headache and anorexia.	cyproheptadine
dehydrocholic acid	An oxo-5beta-cholanic acid in which three oxo substituents are located at positions 3, 7 and 12 on the cholanic acid skeleton.	3,7,12-trioxo-5beta-cholanic acid
devazepide	An indolecarboxamide obtained by formal condensation of the carboxy group of indole-2-carboxylic acid with the exocyclic amino group of (3S)-3-amino-1-methyl-5-phenyl-1,3-dihydro-1,4-benzodiazepin-2-one. A cholecystokinin antagonist used for treatment of gastrointestinal disorders.	devazepide
eluxadoline	An amino acid amide obtained by the formal condensation of the carboxy group of 4-carbamoyl-2,6-dimethyl-L-phenylalanine with the secondary amino group of 2-methoxy-5-({[(1S)-1-(4-phenylimidazol-2-yl)ethyl]amino}methyl)benzoic acid. It has mixed opioid receptor activity and is used for treatment of irritable bowel syndrome with diarrhoea.	eluxadoline
lactulose	A synthetic galactosylfructose disaccharide used in the treatment of constipation and hepatic encephalopathy.	lactulose
metoclopramide	A member of the class of benzamides resulting from the formal condensation of 4-amino-5-chloro-2-methoxybenzoic acid with the primary amino group of N,N-diethylethane-1,2-diamine.	metoclopramide
proglumide	A racemate composed of equal amounts of (R)- and (S)-proglumide. A non-selective CCK antagonist that was used primarily for treatment of stomach ulcers, but has been replaced by newer drugs.	N(2)-benzoyl-N,N-dipropyl-alpha-glutamine; proglumide
rifaximin	A semisynthetic member of the class of rifamycins and non-systemic gastrointestinal site-specific broad spectrum antibiotic. Used in the treatment of traveller's diarrhoea, hepatic encephalopathy and irritable bowel syndrome.	rifaximin
sofalcone	A member of the class of chalcones that is benzene in which the hydrogens at positions 1,2 and 5 are replaced by carboxymethoxy, (1E)-1-{4-[(3-methylbut-2-en-1-yl)oxy]phenyl}-3-oxoprop-1-en-3-yl, and (3-methylbut-2-en-1-yl)oxy groups, respectively. It is a gastrointestinal drug currently used for treatment of gastritis and gastric ulcers in Japan and South Korea.	sofalcone
tegaserod		tegaserod

Research

Studies (12,791)

Timeframe	Studies, Drugs with This Role(%)	All Drugs %
pre-1990	5,595 (43.74)	18.7374
1990's	3,175 (24.82)	18.2507
2000's	1,974 (15.43)	29.6817
2010's	1,538 (12.02)	24.3611
2020's	509 (3.98)	2.80

Study Types

Publication Type	Studies, Drugs with this Role (%)	All Drugs (%)
Trials	1,847 (13.05%)	5.53%
Reviews	849 (6.00%)	6.00%
Case Studies	832 (5.88%)	4.05%
Observational	18 (0.13%)	0.25%
Other	10,602 (74.94%)	84.16%

Protein Targets (291)

Potency Measurements

Protein	Taxonomy	Measurement	Average (mM)	Bioassay(s)	Drugs
15-hydroxyprostaglandin dehydrogenase [NAD(+)] isoform 1	Homo sapiens (human)	Potency	26.1081	1	3
acetylcholinesterase	Homo sapiens (human)	Potency	27.9397	2	3
acid sphingomyelinase	Homo sapiens (human)	Potency	31.6228	1	1
activating transcription factor 6	Homo sapiens (human)	Potency	22.7129	2	5
aldehyde dehydrogenase 1 family, member A1	Homo sapiens (human)	Potency	33.8620	1	5
alpha-galactosidase	Homo sapiens (human)	Potency	14.1254	1	1
apical membrane antigen 1, AMA1	Plasmodium falciparum 3D7	Potency	15.8489	1	1
AR protein	Homo sapiens (human)	Potency	17.8426	8	16
aryl hydrocarbon receptor	Homo sapiens (human)	Potency	10.4375	2	2
ATAD5 protein, partial	Homo sapiens (human)	Potency	23.0999	1	1
Ataxin-2	Homo sapiens (human)	Potency	15.9179	2	2
ATPase family AAA domain-containing protein 5	Homo sapiens (human)	Potency	12.1156	2	2
atrial natriuretic peptide receptor 2 precursor	Homo sapiens (human)	Potency	11.6681	1	1
Bloom syndrome protein isoform 1	Homo sapiens (human)	Potency	26.0932	2	2
bromodomain adjacent to zinc finger domain 2B	Homo sapiens (human)	Potency	28.4326	1	2
caspase 7, apoptosis-related cysteine protease	Homo sapiens (human)	Potency	11.8832	1	1
caspase-3	Cricetulus griseus (Chinese hamster)	Potency	23.7101	1	1
caspase-3	Homo sapiens (human)	Potency	11.8832	1	1
Caspase-7	Cricetulus griseus (Chinese hamster)	Potency	23.7101	1	1
Cellular tumor antigen p53	Homo sapiens (human)	Potency	19.5959	2	6
cellular tumor antigen p53 isoform a	Homo sapiens (human)	Potency	12.5893	1	1
Chain A, 2-oxoglutarate Oxygenase	Homo sapiens (human)	Potency	31.8326	1	2
Chain A, Beta-lactamase	Escherichia coli K-12	Potency	7.9433	1	1
Chain A, Cruzipain	Trypanosoma cruzi	Potency	22.0243	2	3
Chain A, HADH2 protein	Homo sapiens (human)	Potency	25.7877	2	2
Chain A, JmjC domain-containing histone demethylation protein 3A	Homo sapiens (human)	Potency	56.2341	1	2
Chain A, TYROSYL-DNA PHOSPHODIESTERASE	Homo sapiens (human)	Potency	47.9634	1	3
Chain B, HADH2 protein	Homo sapiens (human)	Potency	25.7877	2	2
chaperonin GroEL	Methanococcus maripaludis S2	Potency	100.0000	1	1
chromobox protein homolog 1	Homo sapiens (human)	Potency	60.0366	2	4
cytochrome P450 2C19 precursor	Homo sapiens (human)	Potency	12.5893	1	2
cytochrome P450 2C9, partial	Homo sapiens (human)	Potency	18.7165	1	3
cytochrome P450 2D6	Homo sapiens (human)	Potency	12.1986	1	4
cytochrome P450 2D6 isoform 1	Homo sapiens (human)	Potency	8.2482	1	5
cytochrome P450 3A4 isoform 1	Homo sapiens (human)	Potency	39.8107	2	2
cytochrome P450 family 3 subfamily A polypeptide 4	Homo sapiens (human)	Potency	19.9032	2	3
cytochrome P450, family 19, subfamily A, polypeptide 1, isoform CRA_a	Homo sapiens (human)	Potency	17.9025	1	2
D(1A) dopamine receptor	Homo sapiens (human)	Potency	4.4974	2	4
Disintegrin and metalloproteinase domain-containing protein 17	Homo sapiens (human)	Potency	5.0119	1	1
DNA polymerase eta isoform 1	Homo sapiens (human)	Potency	94.5626	1	2
DNA polymerase iota isoform a (long)	Homo sapiens (human)	Potency	45.1920	1	2
DNA polymerase kappa isoform 1	Homo sapiens (human)	Potency	35.4813	1	1
endonuclease IV	Escherichia coli	Potency	14.1254	1	1
estrogen nuclear receptor alpha	Homo sapiens (human)	Potency	14.6288	8	17
estrogen receptor 2 (ER beta)	Homo sapiens (human)	Potency	21.9360	3	6
estrogen-related nuclear receptor alpha	Homo sapiens (human)	Potency	16.4168	6	18
euchromatic histone-lysine N-methyltransferase 2	Homo sapiens (human)	Potency	24.2548	1	4
EWS/FLI fusion protein	Homo sapiens (human)	Potency	17.0288	4	4
farnesoid X nuclear receptor	Homo sapiens (human)	Potency	22.7455	3	8
Fumarate hydratase	Homo sapiens (human)	Potency	28.4306	1	3
G	Vesicular stomatitis virus	Potency	18.7165	1	3
GABA theta subunit	Rattus norvegicus (Norway rat)	Potency	39.8107	1	1
Gamma-aminobutyric acid receptor subunit alpha-1	Rattus norvegicus (Norway rat)	Potency	39.8107	1	1
Gamma-aminobutyric acid receptor subunit alpha-2	Rattus norvegicus (Norway rat)	Potency	39.8107	1	1
Gamma-aminobutyric acid receptor subunit alpha-3	Rattus norvegicus (Norway rat)	Potency	39.8107	1	1
Gamma-aminobutyric acid receptor subunit alpha-4	Rattus norvegicus (Norway rat)	Potency	39.8107	1	1
Gamma-aminobutyric acid receptor subunit alpha-5	Rattus norvegicus (Norway rat)	Potency	39.8107	1	1
Gamma-aminobutyric acid receptor subunit alpha-6	Rattus norvegicus (Norway rat)	Potency	39.8107	1	1
Gamma-aminobutyric acid receptor subunit beta-1	Rattus norvegicus (Norway rat)	Potency	39.8107	1	1
Gamma-aminobutyric acid receptor subunit beta-2	Rattus norvegicus (Norway rat)	Potency	39.8107	1	1
Gamma-aminobutyric acid receptor subunit beta-3	Rattus norvegicus (Norway rat)	Potency	39.8107	1	1
Gamma-aminobutyric acid receptor subunit delta	Rattus norvegicus (Norway rat)	Potency	39.8107	1	1
Gamma-aminobutyric acid receptor subunit epsilon	Rattus norvegicus (Norway rat)	Potency	39.8107	1	1
Gamma-aminobutyric acid receptor subunit gamma-1	Rattus norvegicus (Norway rat)	Potency	39.8107	1	1
Gamma-aminobutyric acid receptor subunit gamma-2	Rattus norvegicus (Norway rat)	Potency	39.8107	1	1
Gamma-aminobutyric acid receptor subunit gamma-3	Rattus norvegicus (Norway rat)	Potency	39.8107	1	1
Gamma-aminobutyric acid receptor subunit pi	Rattus norvegicus (Norway rat)	Potency	39.8107	1	1
geminin	Homo sapiens (human)	Potency	8.0639	2	6
GLI family zinc finger 3	Homo sapiens (human)	Potency	2.7577	2	5
glp-1 receptor, partial	Homo sapiens (human)	Potency	19.9526	1	1
glucocerebrosidase	Homo sapiens (human)	Potency	31.6228	1	1
glucocorticoid receptor [Homo sapiens]	Homo sapiens (human)	Potency	16.2216	2	7
Glutamate receptor 2	Rattus norvegicus (Norway rat)	Potency	17.3731	1	3
heat shock protein beta-1	Homo sapiens (human)	Potency	22.7759	2	6
Histamine H2 receptor	Cavia porcellus (domestic guinea pig)	Potency	16.6498	1	10
histone acetyltransferase KAT2A isoform 1	Homo sapiens (human)	Potency	24.9054	1	2
histone deacetylase 9 isoform 3	Homo sapiens (human)	Potency	0.0596	1	1
Histone H2A.x	Cricetulus griseus (Chinese hamster)	Potency	55.5628	2	2
HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)	Potency	18.7165	1	3
huntingtin isoform 2	Homo sapiens (human)	Potency	35.4813	1	1
hypoxia-inducible factor 1 alpha subunit	Homo sapiens (human)	Potency	26.8325	2	4
Inositol hexakisphosphate kinase 1	Homo sapiens (human)	Potency	18.7165	1	6
Interferon beta	Homo sapiens (human)	Potency	14.1130	3	10
lamin isoform A-delta10	Homo sapiens (human)	Potency	9.9815	1	5
lethal factor (plasmid)	Bacillus anthracis str. A2012	Potency	8.1712	1	3
lethal(3)malignant brain tumor-like protein 1 isoform I	Homo sapiens (human)	Potency	31.6228	1	1
Luciferase	Photinus pyralis (common eastern firefly)	Potency	35.0649	2	2
Microtubule-associated protein tau	Homo sapiens (human)	Potency	9.8344	1	2
mitogen-activated protein kinase 1	Homo sapiens (human)	Potency	39.8107	1	1
muscarinic acetylcholine receptor M1	Rattus norvegicus (Norway rat)	Potency	0.0298	2	3
nuclear factor erythroid 2-related factor 2 isoform 1	Homo sapiens (human)	Potency	11.6625	2	5
nuclear factor of kappa light polypeptide gene enhancer in B-cells 1 (p105), isoform CRA_a	Homo sapiens (human)	Potency	23.5854	2	4
nuclear receptor ROR-gamma isoform 1	Mus musculus (house mouse)	Potency	10.6025	2	2
nuclear receptor subfamily 1, group I, member 3	Homo sapiens (human)	Potency	18.4486	3	7
parathyroid hormone/parathyroid hormone-related peptide receptor precursor	Homo sapiens (human)	Potency	79.4328	1	1
Parkin	Homo sapiens (human)	Potency	44.6684	1	1
peripheral myelin protein 22	Rattus norvegicus (Norway rat)	Potency	16.6469	2	6
peroxisome proliferator activated receptor gamma	Homo sapiens (human)	Potency	10.7893	3	7
peroxisome proliferator-activated receptor delta	Homo sapiens (human)	Potency	29.6539	3	7
phosphopantetheinyl transferase	Bacillus subtilis	Potency	57.7640	2	4
PINK1	Homo sapiens (human)	Potency	44.6684	1	1
polyprotein	Zika virus	Potency	28.4306	1	3
Polyunsaturated fatty acid lipoxygenase ALOX15B	Homo sapiens (human)	Potency	16.6498	1	5
potassium voltage-gated channel subfamily H member 2 isoform d	Homo sapiens (human)	Potency	10.6937	1	3
PPM1D protein	Homo sapiens (human)	Potency	10.6622	1	4
pregnane X nuclear receptor	Homo sapiens (human)	Potency	16.7985	2	3
progesterone receptor	Homo sapiens (human)	Potency	24.4127	2	3
RAR-related orphan receptor gamma	Mus musculus (house mouse)	Potency	23.2637	2	5
regulator of G-protein signaling 4	Homo sapiens (human)	Potency	3.1763	1	3
retinoic acid nuclear receptor alpha variant 1	Homo sapiens (human)	Potency	17.3887	3	6
retinoid X nuclear receptor alpha	Homo sapiens (human)	Potency	10.2357	2	4
serine-protein kinase ATM isoform a	Homo sapiens (human)	Potency	22.3872	1	1
serine/threonine-protein kinase mTOR isoform 1	Homo sapiens (human)	Potency	26.1216	1	1
SMAD family member 2	Homo sapiens (human)	Potency	27.6510	3	4
SMAD family member 3	Homo sapiens (human)	Potency	27.6510	3	4
Smad3	Homo sapiens (human)	Potency	35.4813	1	1
Spike glycoprotein	Severe acute respiratory syndrome-related coronavirus	Potency	29.3592	2	2
TAR DNA-binding protein 43	Homo sapiens (human)	Potency	10.0000	1	1
TDP1 protein	Homo sapiens (human)	Potency	22.5145	2	8
thioredoxin reductase	Rattus norvegicus (Norway rat)	Potency	70.7946	1	1
thyroid hormone receptor beta isoform 2	Rattus norvegicus (Norway rat)	Potency	14.1566	2	7
thyroid stimulating hormone receptor	Homo sapiens (human)	Potency	15.6720	4	6
ubiquitin carboxyl-terminal hydrolase 2 isoform a	Homo sapiens (human)	Potency	5.0119	1	1
USP1 protein, partial	Homo sapiens (human)	Potency	67.8334	1	2
v-jun sarcoma virus 17 oncogene homolog (avian)	Homo sapiens (human)	Potency	15.7748	2	5
vitamin D (1,25- dihydroxyvitamin D3) receptor	Homo sapiens (human)	Potency	18.6813	1	2
vitamin D3 receptor isoform VDRA	Homo sapiens (human)	Potency	40.3973	1	2
Voltage-dependent calcium channel gamma-2 subunit	Mus musculus (house mouse)	Potency	17.3731	1	3

Inhibition Measurements

Protein	Taxonomy	Measurement	Average (mM)	Bioassay(s)	Drugs
5-hydroxytryptamine receptor 1A	Rattus norvegicus (Norway rat)	IC50	3.9610	2	2
5-hydroxytryptamine receptor 1A	Rattus norvegicus (Norway rat)	Ki	0.0700	1	1
5-hydroxytryptamine receptor 1B	Rattus norvegicus (Norway rat)	IC50	3.9610	2	2
5-hydroxytryptamine receptor 1B	Rattus norvegicus (Norway rat)	Ki	0.0700	1	1
5-hydroxytryptamine receptor 1D	Rattus norvegicus (Norway rat)	IC50	7.8000	1	1
5-hydroxytryptamine receptor 1D	Homo sapiens (human)	Ki	0.1000	1	1
5-hydroxytryptamine receptor 1F	Rattus norvegicus (Norway rat)	IC50	7.8000	1	1
5-hydroxytryptamine receptor 2A	Homo sapiens (human)	IC50	1.8380	1	2
5-hydroxytryptamine receptor 2A	Rattus norvegicus (Norway rat)	IC50	6.6016	2	2
5-hydroxytryptamine receptor 2A	Homo sapiens (human)	Ki	0.1926	5	6
5-hydroxytryptamine receptor 2A	Rattus norvegicus (Norway rat)	Ki	0.0016	1	1
5-hydroxytryptamine receptor 2B	Homo sapiens (human)	IC50	0.2465	1	3
5-hydroxytryptamine receptor 2B	Rattus norvegicus (Norway rat)	IC50	6.6016	2	2
5-hydroxytryptamine receptor 2B	Homo sapiens (human)	Ki	0.1183	2	4
5-hydroxytryptamine receptor 2C	Homo sapiens (human)	IC50	1.1927	1	2
5-hydroxytryptamine receptor 2C	Rattus norvegicus (Norway rat)	IC50	6.6016	2	2
5-hydroxytryptamine receptor 2C	Homo sapiens (human)	Ki	0.3401	3	4
5-hydroxytryptamine receptor 2C	Mus musculus (house mouse)	Ki	0.0110	1	1
5-hydroxytryptamine receptor 3A	Rattus norvegicus (Norway rat)	IC50	0.8800	2	2
5-hydroxytryptamine receptor 3A	Homo sapiens (human)	Ki	2.5027	5	5
5-hydroxytryptamine receptor 3A	Mus musculus (house mouse)	Ki	0.2000	1	2
5-hydroxytryptamine receptor 3A	Rattus norvegicus (Norway rat)	Ki	0.4224	7	8
5-hydroxytryptamine receptor 3B	Rattus norvegicus (Norway rat)	IC50	0.8800	2	2
5-hydroxytryptamine receptor 3B	Mus musculus (house mouse)	Ki	0.2000	1	2
5-hydroxytryptamine receptor 3B	Rattus norvegicus (Norway rat)	Ki	0.4224	7	8
5-hydroxytryptamine receptor 4	Cavia porcellus (domestic guinea pig)	IC50	1.1927	1	2
5-hydroxytryptamine receptor 4	Cavia porcellus (domestic guinea pig)	Ki	3.7498	2	3
5-hydroxytryptamine receptor 4	Homo sapiens (human)	Ki	0.0094	5	5
5-hydroxytryptamine receptor 4	Rattus norvegicus (Norway rat)	Ki	0.0800	1	1
5-hydroxytryptamine receptor 6	Homo sapiens (human)	IC50	0.2810	1	1
5-hydroxytryptamine receptor 6	Homo sapiens (human)	Ki	0.1300	1	1
5-hydroxytryptamine receptor 7	Cavia porcellus (domestic guinea pig)	IC50	94.8000	1	2
5-hydroxytryptamine receptor 7	Homo sapiens (human)	Ki	0.0920	3	3
5-hydroxytryptamine receptor 7	Rattus norvegicus (Norway rat)	Ki	0.0501	1	1
6-phosphogluconate dehydrogenase, decarboxylating	Homo sapiens (human)	Ki	2,111.3000	1	1
Acetylcholinesterase	Homo sapiens (human)	IC50	20.0000	1	1
Acyl carrier protein, mitochondrial	Homo sapiens (human)	IC50	14.5000	2	2
Aldo-keto reductase family 1 member B1	Rattus norvegicus (Norway rat)	IC50	0.5640	1	1
Aldo-keto reductase family 1 member B1	Rattus norvegicus (Norway rat)	Ki	0.5590	1	1
Alpha-1A adrenergic receptor	Rattus norvegicus (Norway rat)	IC50	20.3000	2	2
Alpha-1B adrenergic receptor	Rattus norvegicus (Norway rat)	IC50	20.3000	2	2
Alpha-1D adrenergic receptor	Homo sapiens (human)	IC50	0.1070	1	1
Alpha-1D adrenergic receptor	Rattus norvegicus (Norway rat)	IC50	20.3000	2	2
Alpha-1D adrenergic receptor	Homo sapiens (human)	Ki	0.0530	1	1
Alpha-2A adrenergic receptor	Homo sapiens (human)	IC50	1.5020	1	2
Alpha-2A adrenergic receptor	Rattus norvegicus (Norway rat)	IC50	7.7000	1	1
Alpha-2A adrenergic receptor	Homo sapiens (human)	Ki	0.5630	1	2
Alpha-2B adrenergic receptor	Homo sapiens (human)	IC50	0.0380	1	1
Alpha-2B adrenergic receptor	Rattus norvegicus (Norway rat)	IC50	7.7000	1	1
Alpha-2B adrenergic receptor	Homo sapiens (human)	Ki	0.0170	1	1
Alpha-2C adrenergic receptor	Homo sapiens (human)	IC50	1.2750	1	1
Alpha-2C adrenergic receptor	Rattus norvegicus (Norway rat)	IC50	7.7000	1	1
Alpha-2C adrenergic receptor	Homo sapiens (human)	Ki	0.1850	1	1
Amine oxidase [flavin-containing] A	Mus musculus (house mouse)	IC50	0.0000	1	1
Amine oxidase [flavin-containing] B	Mus musculus (house mouse)	IC50	0.3000	2	2
Angiotensin-converting enzyme	Oryctolagus cuniculus (rabbit)	IC50	17.0491	1	1
Angiotensin-converting enzyme	Oryctolagus cuniculus (rabbit)	Ki	13.9679	1	1
ATP-binding cassette sub-family C member 3	Homo sapiens (human)	IC50	99.0000	1	2
Beta-secretase 1	Homo sapiens (human)	IC50	345.1000	1	1
Bile salt export pump	Homo sapiens (human)	IC50	80.0000	3	4
Canalicular multispecific organic anion transporter 1	Homo sapiens (human)	IC50	74.2000	1	2
Cholecystokinin receptor type A	Cavia porcellus (domestic guinea pig)	IC50	400.1350	1	2
Cholecystokinin receptor type A	Homo sapiens (human)	IC50	0.0002	3	3
Cholecystokinin receptor type A	Rattus norvegicus (Norway rat)	IC50	19.2316	12	13
Cholecystokinin receptor type A	Homo sapiens (human)	Ki	0.0009	2	2
Cholecystokinin receptor type A	Rattus norvegicus (Norway rat)	Ki	0.0004	2	2
Collagenase 3	Homo sapiens (human)	Ki	0.0018	1	1
Complex I intermediate-associated protein 30, mitochondrial	Homo sapiens (human)	IC50	14.5000	2	2
Cytochrome c oxidase subunit NDUFA4	Homo sapiens (human)	IC50	14.5000	2	2
Cytochrome P450 1A2	Homo sapiens (human)	IC50	5.3024	2	2
Cytochrome P450 2B6	Homo sapiens (human)	IC50	10.0000	1	1
Cytochrome P450 2C19	Homo sapiens (human)	IC50	10.0000	1	1
Cytochrome P450 2C9	Homo sapiens (human)	IC50	10.0000	1	1
Cytochrome P450 2D6	Homo sapiens (human)	IC50	5.4000	2	2
Cytochrome P450 2D6	Homo sapiens (human)	Ki	0.9600	1	1
Cytochrome P450 3A4	Homo sapiens (human)	IC50	0.6000	3	3
Cytochrome P450 3A4	Homo sapiens (human)	Ki	0.0550	1	1
D	Rattus norvegicus (Norway rat)	Ki	0.1737	2	3
D(1A) dopamine receptor	Homo sapiens (human)	IC50	0.1580	1	1
D(1A) dopamine receptor	Homo sapiens (human)	Ki	0.0790	1	1
D(1B) dopamine receptor	Rattus norvegicus (Norway rat)	Ki	0.1737	2	3
D(2) dopamine receptor	Homo sapiens (human)	IC50	0.1455	1	2
D(2) dopamine receptor	Rattus norvegicus (Norway rat)	IC50	0.5270	5	5
D(2) dopamine receptor	Bos taurus (cattle)	Ki	0.0800	1	1
D(2) dopamine receptor	Homo sapiens (human)	Ki	0.0697	2	3
D(2) dopamine receptor	Mus musculus (house mouse)	Ki	0.1120	1	1
D(2) dopamine receptor	Rattus norvegicus (Norway rat)	Ki	0.1622	4	6
D(3) dopamine receptor	Homo sapiens (human)	IC50	0.1240	1	2
D(3) dopamine receptor	Homo sapiens (human)	Ki	0.0370	2	3
D(3) dopamine receptor	Rattus norvegicus (Norway rat)	Ki	0.1737	2	3
D(4) dopamine receptor	Rattus norvegicus (Norway rat)	Ki	0.1737	2	3
Delta-type opioid receptor	Rattus norvegicus (Norway rat)	Ki	0.0013	1	1
Endothelin receptor type B	Homo sapiens (human)	Ki	0.0501	2	2
Endothelin receptor type B	Rattus norvegicus (Norway rat)	Ki	0.0501	1	1
Gastrin/cholecystokinin type B receptor	Homo sapiens (human)	IC50	0.2450	1	1
Gastrin/cholecystokinin type B receptor	Rattus norvegicus (Norway rat)	IC50	0.0008	1	1
Gastrin/cholecystokinin type B receptor	Homo sapiens (human)	Ki	0.0560	3	3
Gastrin/cholecystokinin type B receptor	Rattus norvegicus (Norway rat)	Ki	0.2692	1	1
Glycogen phosphorylase, brain form	Homo sapiens (human)	Ki	0.0040	1	1
Glycogen phosphorylase, muscle form	Homo sapiens (human)	Ki	0.0040	1	1
Histamine H1 receptor	Homo sapiens (human)	IC50	0.0037	1	1
Histamine H1 receptor	Homo sapiens (human)	Ki	0.0004	1	1
Histamine H2 receptor	Homo sapiens (human)	IC50	0.1980	1	1
Histamine H2 receptor	Rattus norvegicus (Norway rat)	IC50	2,500.0000	1	1
Histamine H2 receptor	Homo sapiens (human)	Ki	0.1950	1	1
Histone-lysine N-methyltransferase SETD7	Homo sapiens (human)	IC50	8.1333	3	3
Histone-lysine N-methyltransferase SETD7	Homo sapiens (human)	Ki	15.0000	1	1
Kappa-type opioid receptor	Cavia porcellus (domestic guinea pig)	Ki	0.0550	1	1
Lactoperoxidase	Bos taurus (cattle)	IC50	5.0000	1	1
Melatonin receptor type 1A	Homo sapiens (human)	Ki	1.9000	1	1
Mu-type opioid receptor	Rattus norvegicus (Norway rat)	Ki	0.0009	1	1
Multidrug resistance-associated protein 4	Homo sapiens (human)	IC50	81.6000	1	2
Muscarinic acetylcholine receptor M1	Homo sapiens (human)	IC50	0.0160	1	1
Muscarinic acetylcholine receptor M1	Homo sapiens (human)	Ki	0.0040	2	2
Muscarinic acetylcholine receptor M1	Rattus norvegicus (Norway rat)	Ki	0.0040	1	1
Muscarinic acetylcholine receptor M2	Homo sapiens (human)	IC50	0.0350	1	1
Muscarinic acetylcholine receptor M2	Homo sapiens (human)	Ki	0.0080	2	2
Muscarinic acetylcholine receptor M2	Rattus norvegicus (Norway rat)	Ki	0.0040	1	1
Muscarinic acetylcholine receptor M3	Homo sapiens (human)	IC50	0.0460	1	1
Muscarinic acetylcholine receptor M3	Homo sapiens (human)	Ki	0.0068	2	2
Muscarinic acetylcholine receptor M3	Rattus norvegicus (Norway rat)	Ki	0.0040	1	1
Muscarinic acetylcholine receptor M4	Homo sapiens (human)	IC50	0.0160	1	1
Muscarinic acetylcholine receptor M4	Homo sapiens (human)	Ki	0.0031	2	2
Muscarinic acetylcholine receptor M4	Rattus norvegicus (Norway rat)	Ki	0.0040	1	1
Muscarinic acetylcholine receptor M5	Homo sapiens (human)	IC50	0.0038	1	1
Muscarinic acetylcholine receptor M5	Homo sapiens (human)	Ki	0.0034	2	2
Muscarinic acetylcholine receptor M5	Rattus norvegicus (Norway rat)	Ki	0.0040	1	1
Myeloperoxidase	Homo sapiens (human)	IC50	2.6750	2	2
NADH dehydrogenase [ubiquinone] 1 alpha subcomplex assembly factor 2	Homo sapiens (human)	IC50	14.5000	2	2
NADH dehydrogenase [ubiquinone] 1 alpha subcomplex assembly factor 3	Homo sapiens (human)	IC50	14.5000	2	2
NADH dehydrogenase [ubiquinone] 1 alpha subcomplex assembly factor 4	Homo sapiens (human)	IC50	14.5000	2	2
NADH dehydrogenase [ubiquinone] 1 alpha subcomplex subunit 1	Homo sapiens (human)	IC50	14.5000	2	2
NADH dehydrogenase [ubiquinone] 1 alpha subcomplex subunit 10, mitochondrial	Homo sapiens (human)	IC50	14.5000	2	2
NADH dehydrogenase [ubiquinone] 1 alpha subcomplex subunit 11	Homo sapiens (human)	IC50	14.5000	2	2
NADH dehydrogenase [ubiquinone] 1 alpha subcomplex subunit 12	Homo sapiens (human)	IC50	14.5000	2	2
NADH dehydrogenase [ubiquinone] 1 alpha subcomplex subunit 13	Homo sapiens (human)	IC50	14.5000	2	2
NADH dehydrogenase [ubiquinone] 1 alpha subcomplex subunit 2	Homo sapiens (human)	IC50	14.5000	2	2
NADH dehydrogenase [ubiquinone] 1 alpha subcomplex subunit 3	Homo sapiens (human)	IC50	14.5000	2	2
NADH dehydrogenase [ubiquinone] 1 alpha subcomplex subunit 4-like 2	Homo sapiens (human)	IC50	14.5000	2	2
NADH dehydrogenase [ubiquinone] 1 alpha subcomplex subunit 5	Homo sapiens (human)	IC50	14.5000	2	2
NADH dehydrogenase [ubiquinone] 1 alpha subcomplex subunit 6	Homo sapiens (human)	IC50	14.5000	2	2
NADH dehydrogenase [ubiquinone] 1 alpha subcomplex subunit 7	Homo sapiens (human)	IC50	14.5000	2	2
NADH dehydrogenase [ubiquinone] 1 alpha subcomplex subunit 8	Homo sapiens (human)	IC50	14.5000	2	2
NADH dehydrogenase [ubiquinone] 1 alpha subcomplex subunit 9, mitochondrial	Homo sapiens (human)	IC50	14.5000	2	2
NADH dehydrogenase [ubiquinone] 1 beta subcomplex subunit 1	Homo sapiens (human)	IC50	14.5000	2	2
NADH dehydrogenase [ubiquinone] 1 beta subcomplex subunit 10	Homo sapiens (human)	IC50	14.5000	2	2
NADH dehydrogenase [ubiquinone] 1 beta subcomplex subunit 11, mitochondrial	Homo sapiens (human)	IC50	14.5000	2	2
NADH dehydrogenase [ubiquinone] 1 beta subcomplex subunit 2, mitochondrial	Homo sapiens (human)	IC50	14.5000	2	2
NADH dehydrogenase [ubiquinone] 1 beta subcomplex subunit 3	Homo sapiens (human)	IC50	14.5000	2	2
NADH dehydrogenase [ubiquinone] 1 beta subcomplex subunit 4	Homo sapiens (human)	IC50	14.5000	2	2
NADH dehydrogenase [ubiquinone] 1 beta subcomplex subunit 5, mitochondrial	Homo sapiens (human)	IC50	14.5000	2	2
NADH dehydrogenase [ubiquinone] 1 beta subcomplex subunit 6	Homo sapiens (human)	IC50	14.5000	2	2
NADH dehydrogenase [ubiquinone] 1 beta subcomplex subunit 7	Homo sapiens (human)	IC50	14.5000	2	2
NADH dehydrogenase [ubiquinone] 1 beta subcomplex subunit 8, mitochondrial	Homo sapiens (human)	IC50	14.5000	2	2
NADH dehydrogenase [ubiquinone] 1 beta subcomplex subunit 9	Homo sapiens (human)	IC50	14.5000	2	2
NADH dehydrogenase [ubiquinone] 1 subunit C1, mitochondrial	Homo sapiens (human)	IC50	14.5000	2	2
NADH dehydrogenase [ubiquinone] 1 subunit C2	Homo sapiens (human)	IC50	14.5000	2	2
NADH dehydrogenase [ubiquinone] flavoprotein 1, mitochondrial	Homo sapiens (human)	IC50	14.5000	2	2
NADH dehydrogenase [ubiquinone] flavoprotein 2, mitochondrial	Homo sapiens (human)	IC50	14.5000	2	2
NADH dehydrogenase [ubiquinone] flavoprotein 3, mitochondrial	Homo sapiens (human)	IC50	14.5000	2	2
NADH dehydrogenase [ubiquinone] iron-sulfur protein 2, mitochondrial	Homo sapiens (human)	IC50	14.5000	2	2
NADH dehydrogenase [ubiquinone] iron-sulfur protein 3, mitochondrial	Homo sapiens (human)	IC50	14.5000	2	2
NADH dehydrogenase [ubiquinone] iron-sulfur protein 4, mitochondrial	Homo sapiens (human)	IC50	14.5000	2	2
NADH dehydrogenase [ubiquinone] iron-sulfur protein 5	Homo sapiens (human)	IC50	14.5000	2	2
NADH dehydrogenase [ubiquinone] iron-sulfur protein 6, mitochondrial	Homo sapiens (human)	IC50	14.5000	2	2
NADH dehydrogenase [ubiquinone] iron-sulfur protein 7, mitochondrial	Homo sapiens (human)	IC50	14.5000	2	2
NADH dehydrogenase [ubiquinone] iron-sulfur protein 8, mitochondrial	Homo sapiens (human)	IC50	14.5000	2	2
NADH-ubiquinone oxidoreductase 75 kDa subunit, mitochondrial	Homo sapiens (human)	IC50	14.5000	2	2
NADH-ubiquinone oxidoreductase chain 1	Homo sapiens (human)	IC50	14.5000	2	2
NADH-ubiquinone oxidoreductase chain 2	Homo sapiens (human)	IC50	14.5000	2	2
NADH-ubiquinone oxidoreductase chain 3	Homo sapiens (human)	IC50	14.5000	2	2
NADH-ubiquinone oxidoreductase chain 4	Homo sapiens (human)	IC50	14.5000	2	2
NADH-ubiquinone oxidoreductase chain 4L	Homo sapiens (human)	IC50	14.5000	2	2
NADH-ubiquinone oxidoreductase chain 5	Homo sapiens (human)	IC50	14.5000	2	2
NADH-ubiquinone oxidoreductase chain 6	Homo sapiens (human)	IC50	14.5000	2	2
Nuclear receptor subfamily 3 group C member 3	Bos taurus (cattle)	IC50	17.0491	1	1
Nuclear receptor subfamily 3 group C member 3	Bos taurus (cattle)	Ki	13.9679	1	1
Polyunsaturated fatty acid lipoxygenase ALOX15	Homo sapiens (human)	IC50	23.9000	1	1
Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)	IC50	5.0653	6	7
Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)	Ki	13.9679	1	1
Prostaglandin G/H synthase 1	Ovis aries (sheep)	Ki	0.0016	1	1
Sodium-dependent noradrenaline transporter	Mus musculus (house mouse)	Ki	0.2900	1	1
Sodium-dependent noradrenaline transporter	Homo sapiens (human)	IC50	0.5640	1	1
Sodium-dependent noradrenaline transporter	Homo sapiens (human)	Ki	0.4245	2	2
Sodium-dependent serotonin transporter	Homo sapiens (human)	Ki	4.1000	1	1
Sodium-dependent serotonin transporter	Mus musculus (house mouse)	Ki	4.1000	1	1
Solute carrier family 22 member 1	Homo sapiens (human)	IC50	94.8000	1	1
Trans-sialidase	Trypanosoma cruzi	IC50	570.0000	1	1
Transporter	Rattus norvegicus (Norway rat)	Ki	0.2900	1	1

Activation Measurements

Protein	Taxonomy	Measurement	Average (mM)	Bioassay(s)	Drugs
5-hydroxytryptamine receptor 3A	Homo sapiens (human)	Kd	0.0501	1	1
5-hydroxytryptamine receptor 3B	Homo sapiens (human)	Kd	0.0501	1	1
5-hydroxytryptamine receptor 3C	Homo sapiens (human)	Kd	0.0501	1	1
5-hydroxytryptamine receptor 3D	Homo sapiens (human)	Kd	0.0501	1	1
5-hydroxytryptamine receptor 3E	Homo sapiens (human)	Kd	0.0501	1	1
5-hydroxytryptamine receptor 4	Cavia porcellus (domestic guinea pig)	EC50	0.0094	2	2
5-hydroxytryptamine receptor 4	Homo sapiens (human)	EC50	0.0048	5	5
Albumin	Rattus norvegicus (Norway rat)	Kd	1,370.0000	1	1
Delta-type opioid receptor	Homo sapiens (human)	EC50	10.0000	1	1
Histamine H1 receptor	Homo sapiens (human)	Kd	5.4000	1	1
Mu-type opioid receptor	Homo sapiens (human)	EC50	0.0010	1	1
Nuclear receptor subfamily 1 group I member 2	Homo sapiens (human)	EC50	9.1200	5	5

Other Measurements

Protein	Taxonomy	Measurement	Average (mM)	Bioassay(s)	Drugs
5-hydroxytryptamine receptor 4	Rattus norvegicus (Norway rat)	ED50	24.1000	1	1
UDP-glucuronosyltransferase 1A3	Homo sapiens (human)	Km	240.0000	1	1
UDP-glucuronosyltransferase 1A4	Homo sapiens (human)	Km	106.0000	2	2

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Activation Measurements

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