phenothiazine antipsychotic drug

null

ChEBI ID: 37930

Members (15)

Member	Definition	Class
acepromazine	A member of the class of phenothiazines that is 10H-phenothiazine substituted by an acetyl group at position 2 and a 3-(dimethylamino)propyl group at position 10.	acepromazine
acetophenazine	A member of the class of phenothiazines that is 10H-phenothiazine substituted by a 3-[4-(2-hydroxyethyl)piperazin-1-yl]propyl group at the nitogen atom and an acetyl group at position 2.	acetophenazine
chlorpromazine	A substituted phenothiazine in which the ring nitrogen at position 10 is attached to C-3 of an N,N-dimethylpropanamine moiety.	chlorpromazine
chlorpromazine hydrochloride	The hydrochloride salt of chlorpromazine.	chlorpromazine hydrochloride
fluphenazine	A member of the class of phenothiazines that is 10H-phenothiazine having a trifluoromethyl subsitituent at the 2-position and a 3-[4-(2-hydroxyethyl)piperazin-1-yl]propyl group at the N-10 position.	fluphenazine
fluphenazine depot	The prodrug of fluphenazine, an antipsychotic drug used for the symptomatic management of psychosis in patients with schizophrenia.	fluphenazine decanoate
methotrimeprazine	A member of the class of phenothiazines that is 10H-phenothiazine substituted by a (2R)-3-(dimethylamino)-2-methylpropyl group and a methoxy group at positions 10 and 2 respectively.	methotrimeprazine
perazine	A phenothiazine derivative in which 10H-phenothiazinecarries a 3-(4-methylpiperazin-1-yl)propyl substituent at the N-10 position.	perazine
perphenazine	A phenothiazine derivative in which the phenothiazine tricycle carries a chloro substituent at the 2-position and a 3-[4-(2-hydroxyethyl)piperazin-1-yl]propyl group at N-10.	perphenazine
promazine	A phenothiazine deriative in which the phenothiazine tricycle has a 3-(dimethylaminopropyl) group at the N-10 position.	promazine
propiomazine	A member of the class of phenothiazines that is 10H-phenothiazine substituted by a 2-(dimethylamino)propyl group at nitrogen atom and a propanoyl group at position 2.	propiomazine
thiethylperazine	A member of the class of phenothiazines that is perazine substituted by a ethylsulfanyl group at position 2.	thiethylperazine
thiopropazate	A phenothiazine derivative in which 10H-phenothiazine has a chloro subsitituent at the 2-position and a 3-[4-(2-acetoxyethyl)piperazin-1-yl]propyl group at N-10.	thiopropazate
thioproperazine	A phenothiazine derivative in which the phenothiazine tricycle has a dimethylaminosulfonyl substituent at the 2-position and a 3-(4-methylpiperazin-1-yl)propyl group at N-10.	thioproperazine
trifluoperazine	A member of the class of phenothiazines that is phenothiazine having a trifluoromethyl subsitituent at the 2-position and a 3-(4-methylpiperazin-1-yl)propyl group at the N-10 position.	trifluoperazine

Research

Studies (23,828)

Timeframe	Studies, Drugs with This Role(%)	All Drugs %
pre-1990	18,405 (77.24)	18.7374
1990's	2,378 (9.98)	18.2507
2000's	1,538 (6.45)	29.6817
2010's	1,198 (5.03)	24.3611
2020's	309 (1.30)	2.80

Study Types

Publication Type	Studies, Drugs with this Role (%)	All Drugs (%)
Trials	1,953 (6.74%)	5.53%
Reviews	873 (3.01%)	6.00%
Case Studies	1,503 (5.18%)	4.05%
Observational	13 (0.04%)	0.25%
Other	24,655 (85.03%)	84.16%

Protein Targets (347)

Potency Measurements

Protein	Taxonomy	Measurement	Average (mM)	Bioassay(s)	Drugs
15-lipoxygenase, partial	Homo sapiens (human)	Potency	19.9526	1	1
67.9K protein	Vaccinia virus	Potency	16.5721	2	10
acetylcholinesterase	Homo sapiens (human)	Potency	31.2290	1	4
activating transcription factor 6	Homo sapiens (human)	Potency	21.3138	1	1
aldehyde dehydrogenase 1 family, member A1	Homo sapiens (human)	Potency	39.8107	1	1
Alpha-synuclein	Homo sapiens (human)	Potency	4.4668	1	1
apical membrane antigen 1, AMA1	Plasmodium falciparum 3D7	Potency	21.4215	1	2
AR protein	Homo sapiens (human)	Potency	37.3061	7	20
aryl hydrocarbon receptor	Homo sapiens (human)	Potency	12.0518	2	2
arylsulfatase A	Homo sapiens (human)	Potency	1.8192	1	2
ATAD5 protein, partial	Homo sapiens (human)	Potency	22.2914	2	5
Ataxin-2	Homo sapiens (human)	Potency	14.7633	1	5
ATP-dependent phosphofructokinase	Trypanosoma brucei brucei TREU927	Potency	19.0420	1	2
atrial natriuretic peptide receptor 2 precursor	Homo sapiens (human)	Potency	15.5854	1	4
bromodomain adjacent to zinc finger domain 2B	Homo sapiens (human)	Potency	32.4648	1	2
caspase 7, apoptosis-related cysteine protease	Homo sapiens (human)	Potency	31.9451	1	4
caspase-3	Cricetulus griseus (Chinese hamster)	Potency	42.2660	1	4
caspase-3	Homo sapiens (human)	Potency	31.9451	1	4
Caspase-7	Cricetulus griseus (Chinese hamster)	Potency	42.2660	1	4
Cellular tumor antigen p53	Homo sapiens (human)	Potency	19.8224	2	4
cellular tumor antigen p53 isoform a	Homo sapiens (human)	Potency	14.2631	2	10
Chain A, 2-oxoglutarate Oxygenase	Homo sapiens (human)	Potency	39.8107	1	1
Chain A, ATP-DEPENDENT DNA HELICASE Q1	Homo sapiens (human)	Potency	35.4813	1	1
Chain A, Beta-lactamase	Escherichia coli K-12	Potency	25.2855	1	2
Chain A, HADH2 protein	Homo sapiens (human)	Potency	0.1995	1	1
Chain A, JmjC domain-containing histone demethylation protein 3A	Homo sapiens (human)	Potency	30.6785	1	3
Chain A, MAJOR APURINIC/APYRIMIDINIC ENDONUCLEASE	Homo sapiens (human)	Potency	23.8186	1	3
Chain A, Putative fructose-1,6-bisphosphate aldolase	Giardia intestinalis	Potency	17.7407	1	1
Chain A, TYROSYL-DNA PHOSPHODIESTERASE	Homo sapiens (human)	Potency	24.4175	1	7
Chain B, HADH2 protein	Homo sapiens (human)	Potency	0.1995	1	1
chromobox protein homolog 1	Homo sapiens (human)	Potency	36.4649	2	7
cytochrome P450 2C19 precursor	Homo sapiens (human)	Potency	6.7267	1	5
cytochrome P450 2C9, partial	Homo sapiens (human)	Potency	38.9018	1	1
cytochrome P450 2D6	Homo sapiens (human)	Potency	0.0623	1	3
cytochrome P450 2D6 isoform 1	Homo sapiens (human)	Potency	0.7335	1	12
cytochrome P450 3A4 isoform 1	Homo sapiens (human)	Potency	10.7848	2	14
cytochrome P450 family 3 subfamily A polypeptide 4	Homo sapiens (human)	Potency	10.1845	2	4
cytochrome P450, family 19, subfamily A, polypeptide 1, isoform CRA_a	Homo sapiens (human)	Potency	34.2969	1	3
D(1A) dopamine receptor	Homo sapiens (human)	Potency	3.3480	3	12
D(1A) dopamine receptor	Sus scrofa (pig)	Potency	20.1433	1	4
Disintegrin and metalloproteinase domain-containing protein 17	Homo sapiens (human)	Potency	15.7217	1	4
DNA dC->dU-editing enzyme APOBEC-3G isoform 1	Homo sapiens (human)	Potency	22.3872	1	1
DNA polymerase beta	Homo sapiens (human)	Potency	89.1251	1	1
DNA polymerase eta isoform 1	Homo sapiens (human)	Potency	50.1187	1	1
DNA polymerase iota isoform a (long)	Homo sapiens (human)	Potency	100.0000	1	1
DNA polymerase kappa isoform 1	Homo sapiens (human)	Potency	28.2867	1	2
dopamine D1 receptor	Homo sapiens (human)	Potency	0.0580	1	1
endonuclease IV	Escherichia coli	Potency	3.9472	1	2
estrogen nuclear receptor alpha	Homo sapiens (human)	Potency	47.0771	8	14
estrogen receptor 2 (ER beta)	Homo sapiens (human)	Potency	21.3332	2	5
estrogen-related nuclear receptor alpha	Homo sapiens (human)	Potency	40.0246	8	23
euchromatic histone-lysine N-methyltransferase 2	Homo sapiens (human)	Potency	21.2145	2	17
EWS/FLI fusion protein	Homo sapiens (human)	Potency	22.4392	4	8
farnesoid X nuclear receptor	Homo sapiens (human)	Potency	27.2643	2	4
Fumarate hydratase	Homo sapiens (human)	Potency	27.6279	1	7
G	Vesicular stomatitis virus	Potency	38.9018	1	1
GABA theta subunit	Rattus norvegicus (Norway rat)	Potency	10.4897	1	8
Gamma-aminobutyric acid receptor subunit alpha-1	Rattus norvegicus (Norway rat)	Potency	10.4897	1	8
Gamma-aminobutyric acid receptor subunit alpha-2	Rattus norvegicus (Norway rat)	Potency	10.4897	1	8
Gamma-aminobutyric acid receptor subunit alpha-3	Rattus norvegicus (Norway rat)	Potency	10.4897	1	8
Gamma-aminobutyric acid receptor subunit alpha-4	Rattus norvegicus (Norway rat)	Potency	10.4897	1	8
Gamma-aminobutyric acid receptor subunit alpha-5	Rattus norvegicus (Norway rat)	Potency	10.4897	1	8
Gamma-aminobutyric acid receptor subunit alpha-6	Rattus norvegicus (Norway rat)	Potency	10.4897	1	8
Gamma-aminobutyric acid receptor subunit beta-1	Rattus norvegicus (Norway rat)	Potency	10.4897	1	8
Gamma-aminobutyric acid receptor subunit beta-2	Rattus norvegicus (Norway rat)	Potency	10.4897	1	8
Gamma-aminobutyric acid receptor subunit beta-3	Rattus norvegicus (Norway rat)	Potency	10.4897	1	8
Gamma-aminobutyric acid receptor subunit delta	Rattus norvegicus (Norway rat)	Potency	10.4897	1	8
Gamma-aminobutyric acid receptor subunit epsilon	Rattus norvegicus (Norway rat)	Potency	10.4897	1	8
Gamma-aminobutyric acid receptor subunit gamma-1	Rattus norvegicus (Norway rat)	Potency	10.4897	1	8
Gamma-aminobutyric acid receptor subunit gamma-2	Rattus norvegicus (Norway rat)	Potency	10.4897	1	8
Gamma-aminobutyric acid receptor subunit gamma-3	Rattus norvegicus (Norway rat)	Potency	10.4897	1	8
Gamma-aminobutyric acid receptor subunit pi	Rattus norvegicus (Norway rat)	Potency	10.4897	1	8
geminin	Homo sapiens (human)	Potency	22.9413	4	17
GLI family zinc finger 3	Homo sapiens (human)	Potency	16.1381	3	7
glp-1 receptor, partial	Homo sapiens (human)	Potency	18.5482	1	2
GLS protein	Homo sapiens (human)	Potency	22.4844	2	4
glucocerebrosidase	Homo sapiens (human)	Potency	20.0576	1	6
glucocorticoid receptor [Homo sapiens]	Homo sapiens (human)	Potency	39.0788	3	6
Glutamate receptor 2	Rattus norvegicus (Norway rat)	Potency	68.5896	1	1
Glycoprotein hormones alpha chain	Homo sapiens (human)	Potency	14.1254	1	2
Guanine nucleotide-binding protein G	Homo sapiens (human)	Potency	25.1189	1	1
heat shock 70kDa protein 5 (glucose-regulated protein, 78kDa)	Homo sapiens (human)	Potency	55.2992	1	2
heat shock protein beta-1	Homo sapiens (human)	Potency	44.0218	2	2
Histamine H2 receptor	Cavia porcellus (domestic guinea pig)	Potency	11.9453	1	14
histone acetyltransferase KAT2A isoform 1	Homo sapiens (human)	Potency	31.8234	1	3
histone deacetylase 9 isoform 3	Homo sapiens (human)	Potency	25.8848	1	2
Histone H2A.x	Cricetulus griseus (Chinese hamster)	Potency	92.3364	2	4
HLA class I histocompatibility antigen, B alpha chain	Homo sapiens (human)	Potency	38.9018	1	1
hypoxia-inducible factor 1, alpha subunit (basic helix-loop-helix transcription factor)	Homo sapiens (human)	Potency	15.0654	2	4
IDH1	Homo sapiens (human)	Potency	21.5430	1	3
Inositol hexakisphosphate kinase 1	Homo sapiens (human)	Potency	38.9018	1	2
Inositol monophosphatase 1	Rattus norvegicus (Norway rat)	Potency	5.4992	1	5
Integrin alpha-IIb	Homo sapiens (human)	Potency	17.9008	1	4
Integrin beta-3	Homo sapiens (human)	Potency	17.9008	1	4
Interferon beta	Homo sapiens (human)	Potency	18.5069	2	4
lamin isoform A-delta10	Homo sapiens (human)	Potency	14.1680	2	12
lethal factor (plasmid)	Bacillus anthracis str. A2012	Potency	15.9633	1	9
lysosomal alpha-glucosidase preproprotein	Homo sapiens (human)	Potency	56.2341	2	2
M-phase phosphoprotein 8	Homo sapiens (human)	Potency	31.0988	1	6
Microtubule-associated protein tau	Homo sapiens (human)	Potency	26.4575	1	9
mitogen-activated protein kinase 1	Homo sapiens (human)	Potency	21.9340	2	6
muscarinic acetylcholine receptor M1	Rattus norvegicus (Norway rat)	Potency	7.1703	2	10
Neuronal acetylcholine receptor subunit alpha-4	Rattus norvegicus (Norway rat)	Potency	56.2341	1	1
Neuronal acetylcholine receptor subunit beta-2	Rattus norvegicus (Norway rat)	Potency	56.2341	1	1
neuropeptide S receptor isoform A	Homo sapiens (human)	Potency	18.2068	1	4
NFKB1 protein, partial	Homo sapiens (human)	Potency	20.8592	2	8
NPC intracellular cholesterol transporter 1 precursor	Homo sapiens (human)	Potency	58.0479	1	2
nuclear factor erythroid 2-related factor 2 isoform 1	Homo sapiens (human)	Potency	31.3693	2	6
nuclear factor NF-kappa-B p105 subunit isoform 1	Homo sapiens (human)	Potency	44.6684	1	1
nuclear factor of kappa light polypeptide gene enhancer in B-cells 1 (p105), isoform CRA_a	Homo sapiens (human)	Potency	40.8868	1	2
nuclear receptor ROR-gamma isoform 1	Mus musculus (house mouse)	Potency	15.8489	1	1
nuclear receptor subfamily 1, group I, member 3	Homo sapiens (human)	Potency	40.8918	3	9
peptidyl-prolyl cis-trans isomerase NIMA-interacting 1	Homo sapiens (human)	Potency	100.0000	1	1
peripheral myelin protein 22	Rattus norvegicus (Norway rat)	Potency	22.1554	2	6
peripheral myelin protein 22 isoform 1	Homo sapiens (human)	Potency	45.1582	1	2
peroxisome proliferator activated receptor gamma	Homo sapiens (human)	Potency	21.7276	3	8
peroxisome proliferator-activated receptor delta	Homo sapiens (human)	Potency	23.6077	3	5
phosphopantetheinyl transferase	Bacillus subtilis	Potency	45.4849	1	7
polyprotein	Zika virus	Potency	27.6279	1	7
Polyunsaturated fatty acid lipoxygenase ALOX15B	Homo sapiens (human)	Potency	11.9453	1	7
potassium voltage-gated channel subfamily H member 2 isoform d	Homo sapiens (human)	Potency	5.5524	1	5
PPM1D protein	Homo sapiens (human)	Potency	11.7086	1	2
pregnane X nuclear receptor	Homo sapiens (human)	Potency	21.6796	2	4
pregnane X receptor	Rattus norvegicus (Norway rat)	Potency	35.4813	1	1
progesterone receptor	Homo sapiens (human)	Potency	26.9482	2	5
Rap guanine nucleotide exchange factor 4	Homo sapiens (human)	Potency	35.4813	1	1
RAR-related orphan receptor gamma	Mus musculus (house mouse)	Potency	25.1057	2	8
ras-related protein Rab-9A	Homo sapiens (human)	Potency	74.3752	1	3
regulator of G-protein signaling 4	Homo sapiens (human)	Potency	22.1796	1	4
retinoic acid nuclear receptor alpha variant 1	Homo sapiens (human)	Potency	34.5031	3	12
retinoid X nuclear receptor alpha	Homo sapiens (human)	Potency	13.0889	2	7
serine/threonine-protein kinase mTOR isoform 1	Homo sapiens (human)	Potency	18.6112	4	14
SMAD family member 2	Homo sapiens (human)	Potency	58.2929	2	2
SMAD family member 3	Homo sapiens (human)	Potency	58.2929	2	2
Smad3	Homo sapiens (human)	Potency	32.0272	1	3
Spike glycoprotein	Severe acute respiratory syndrome-related coronavirus	Potency	17.8511	2	9
survival motor neuron protein isoform d	Homo sapiens (human)	Potency	9.3669	1	5
TAR DNA-binding protein 43	Homo sapiens (human)	Potency	35.4813	1	1
TDP1 protein	Homo sapiens (human)	Potency	17.6799	2	26
thioredoxin reductase	Rattus norvegicus (Norway rat)	Potency	39.2666	1	3
Thrombopoietin	Homo sapiens (human)	Potency	16.3991	2	10
thyroid hormone receptor beta isoform 2	Rattus norvegicus (Norway rat)	Potency	12.2149	3	11
thyroid stimulating hormone receptor	Homo sapiens (human)	Potency	30.4785	6	16
transcriptional regulator ERG isoform 3	Homo sapiens (human)	Potency	25.1189	1	1
transient receptor potential cation channel subfamily V member 1	Homo sapiens (human)	Potency	19.9526	1	1
ubiquitin carboxyl-terminal hydrolase 2 isoform a	Homo sapiens (human)	Potency	15.7217	1	4
USP1 protein, partial	Homo sapiens (human)	Potency	47.7984	2	12
v-jun sarcoma virus 17 oncogene homolog (avian)	Homo sapiens (human)	Potency	14.0202	2	8
vitamin D (1,25- dihydroxyvitamin D3) receptor	Homo sapiens (human)	Potency	16.2996	3	3
vitamin D3 receptor isoform VDRA	Homo sapiens (human)	Potency	59.0491	1	3
Voltage-dependent calcium channel gamma-2 subunit	Mus musculus (house mouse)	Potency	68.5896	1	1
Vpr	Human immunodeficiency virus 1	Potency	12.5893	1	1

Inhibition Measurements

Protein	Taxonomy	Measurement	Average (mM)	Bioassay(s)	Drugs
3-beta-hydroxysteroid-Delta(8),Delta(7)-isomerase	Homo sapiens (human)	Ki	0.0080	1	1
5-hydroxytryptamine receptor 1A	Rattus norvegicus (Norway rat)	IC50	3.8337	1	3
5-hydroxytryptamine receptor 1A	Homo sapiens (human)	Ki	0.6730	2	3
5-hydroxytryptamine receptor 1A	Rattus norvegicus (Norway rat)	Ki	2.1903	1	3
5-hydroxytryptamine receptor 1B	Rattus norvegicus (Norway rat)	IC50	3.8337	1	3
5-hydroxytryptamine receptor 1B	Rattus norvegicus (Norway rat)	Ki	2.1903	1	3
5-hydroxytryptamine receptor 2A	Homo sapiens (human)	IC50	0.0088	2	4
5-hydroxytryptamine receptor 2A	Homo sapiens (human)	Ki	0.0056	4	7
5-hydroxytryptamine receptor 2A	Rattus norvegicus (Norway rat)	Ki	0.0024	3	3
5-hydroxytryptamine receptor 2B	Homo sapiens (human)	IC50	0.1707	1	3
5-hydroxytryptamine receptor 2B	Homo sapiens (human)	Ki	0.0836	3	5
5-hydroxytryptamine receptor 2B	Rattus norvegicus (Norway rat)	Ki	0.0024	3	3
5-hydroxytryptamine receptor 2C	Homo sapiens (human)	IC50	0.0571	1	3
5-hydroxytryptamine receptor 2C	Homo sapiens (human)	Ki	0.0310	4	7
5-hydroxytryptamine receptor 2C	Rattus norvegicus (Norway rat)	Ki	0.0024	3	3
5-hydroxytryptamine receptor 4	Cavia porcellus (domestic guinea pig)	IC50	0.0571	1	3
5-hydroxytryptamine receptor 4	Cavia porcellus (domestic guinea pig)	Ki	0.0299	1	3
5-hydroxytryptamine receptor 6	Homo sapiens (human)	IC50	0.1277	1	3
5-hydroxytryptamine receptor 6	Homo sapiens (human)	Ki	0.0502	5	9
5-hydroxytryptamine receptor 7	Cavia porcellus (domestic guinea pig)	IC50	51.4000	1	6
5-hydroxytryptamine receptor 7	Homo sapiens (human)	Ki	0.1028	6	8
5-hydroxytryptamine receptor 7	Rattus norvegicus (Norway rat)	Ki	0.0210	1	1
Adenosine receptor A3	Homo sapiens (human)	IC50	11.9350	1	1
Adenosine receptor A3	Homo sapiens (human)	Ki	6.7460	1	1
Adenylate cyclase type 1	Rattus norvegicus (Norway rat)	IC50	1.3000	1	1
Adenylate cyclase type 1	Rattus norvegicus (Norway rat)	Ki	0.1180	1	1
Adenylate cyclase type 2	Rattus norvegicus (Norway rat)	IC50	1.3000	1	1
Adenylate cyclase type 2	Rattus norvegicus (Norway rat)	Ki	0.1180	1	1
Adenylate cyclase type 3	Rattus norvegicus (Norway rat)	IC50	1.3000	1	1
Adenylate cyclase type 3	Rattus norvegicus (Norway rat)	Ki	0.1180	1	1
Adenylate cyclase type 4	Rattus norvegicus (Norway rat)	IC50	1.3000	1	1
Adenylate cyclase type 4	Rattus norvegicus (Norway rat)	Ki	0.1180	1	1
Adenylate cyclase type 5	Rattus norvegicus (Norway rat)	IC50	1.3000	1	1
Adenylate cyclase type 5	Rattus norvegicus (Norway rat)	Ki	0.1180	1	1
Adenylate cyclase type 6	Rattus norvegicus (Norway rat)	IC50	1.3000	1	1
Adenylate cyclase type 6	Rattus norvegicus (Norway rat)	Ki	0.1180	1	1
Adenylate cyclase type 8	Rattus norvegicus (Norway rat)	IC50	1.3000	1	1
Adenylate cyclase type 8	Rattus norvegicus (Norway rat)	Ki	0.1180	1	1
Adenylyl cyclase 7	Rattus norvegicus (Norway rat)	IC50	1.3000	1	1
Adenylyl cyclase 7	Rattus norvegicus (Norway rat)	Ki	0.1180	1	1
Aldehyde oxidase	Homo sapiens (human)	IC50	0.3015	1	2
Aldehyde oxidase	Homo sapiens (human)	Ki	2.3000	1	1
Aldehyde oxidase 1	Macaca fascicularis (crab-eating macaque)	IC50	3.6000	1	1
Aldehyde oxidase 1	Mus musculus (house mouse)	IC50	6.1000	1	1
Aldehyde oxidase 1	Oryctolagus cuniculus (rabbit)	IC50	20.0000	1	1
Aldehyde oxidase 1	Rattus norvegicus (Norway rat)	IC50	0.7400	1	1
Aldo-keto reductase family 1 member B1	Rattus norvegicus (Norway rat)	IC50	0.6647	1	3
Aldo-keto reductase family 1 member B1	Rattus norvegicus (Norway rat)	Ki	0.6593	1	3
Alpha-1A adrenergic receptor	Rattus norvegicus (Norway rat)	IC50	3.0868	3	4
Alpha-1A adrenergic receptor	Rattus norvegicus (Norway rat)	Ki	3.3780	2	2
Alpha-1B adrenergic receptor	Rattus norvegicus (Norway rat)	IC50	3.0868	3	4
Alpha-1B adrenergic receptor	Rattus norvegicus (Norway rat)	Ki	3.3780	2	2
Alpha-1D adrenergic receptor	Homo sapiens (human)	IC50	0.0167	1	3
Alpha-1D adrenergic receptor	Rattus norvegicus (Norway rat)	IC50	0.1373	2	3
Alpha-1D adrenergic receptor	Homo sapiens (human)	Ki	0.0080	1	3
Alpha-1D adrenergic receptor	Rattus norvegicus (Norway rat)	Ki	0.0100	1	1
Alpha-2A adrenergic receptor	Homo sapiens (human)	IC50	0.3013	1	3
Alpha-2A adrenergic receptor	Rattus norvegicus (Norway rat)	IC50	1.4791	1	1
Alpha-2A adrenergic receptor	Homo sapiens (human)	Ki	0.1127	1	3
Alpha-2A adrenergic receptor	Rattus norvegicus (Norway rat)	Ki	0.1259	1	1
Alpha-2B adrenergic receptor	Homo sapiens (human)	IC50	0.0243	1	3
Alpha-2B adrenergic receptor	Rattus norvegicus (Norway rat)	IC50	1.4791	1	1
Alpha-2B adrenergic receptor	Homo sapiens (human)	Ki	0.0111	1	3
Alpha-2B adrenergic receptor	Rattus norvegicus (Norway rat)	Ki	0.1259	1	1
Alpha-2C adrenergic receptor	Homo sapiens (human)	IC50	0.2603	1	3
Alpha-2C adrenergic receptor	Rattus norvegicus (Norway rat)	IC50	1.4791	1	1
Alpha-2C adrenergic receptor	Homo sapiens (human)	Ki	0.0377	1	3
Alpha-2C adrenergic receptor	Rattus norvegicus (Norway rat)	Ki	0.1259	1	1
Androgen receptor	Rattus norvegicus (Norway rat)	Ki	0.8000	1	2
Angiotensin-converting enzyme	Oryctolagus cuniculus (rabbit)	IC50	5.4938	1	4
Angiotensin-converting enzyme	Oryctolagus cuniculus (rabbit)	Ki	4.5009	1	4
Angiotensin-converting enzyme 2	Homo sapiens (human)	IC50	11.5200	1	4
ATP-binding cassette sub-family C member 3	Homo sapiens (human)	IC50	133.0000	1	2
ATP-dependent translocase ABCB1	Homo sapiens (human)	IC50	7.8333	3	6
ATP-dependent translocase ABCB1	Homo sapiens (human)	Ki	6.4333	2	3
bcl-2-related protein A1	Mus musculus (house mouse)	IC50	20.0000	1	1
Beta-3 adrenergic receptor	Homo sapiens (human)	IC50	29.4880	1	1
Beta-3 adrenergic receptor	Homo sapiens (human)	Ki	22.1160	1	1
Beta-glucuronidase	Rattus norvegicus (Norway rat)	IC50	7.8000	1	1
Bile salt export pump	Homo sapiens (human)	IC50	82.7307	7	14
Bile salt export pump	Rattus norvegicus (Norway rat)	IC50	122.3000	1	1
C-8 sterol isomerase	Saccharomyces cerevisiae S288C	Ki	0.5000	1	1
Calcium-dependent protein kinase 4	Plasmodium falciparum 3D7	Ki	150.0000	1	1
Calmodulin	Bos taurus (cattle)	IC50	2.5000	1	2
Calmodulin-1	Homo sapiens (human)	IC50	8.5200	3	3
Calmodulin-1	Homo sapiens (human)	Ki	19.2800	1	1
Canalicular multispecific organic anion transporter 1	Homo sapiens (human)	IC50	133.0000	1	2
Cruzipain	Trypanosoma cruzi	IC50	236.5000	2	2
Cys-loop ligand-gated ion channel	Dickeya chrysanthemi	IC50	158.0000	1	1
Cytochrome P450 2C9	Homo sapiens (human)	IC50	17.5000	1	2
Cytochrome P450 2D6	Homo sapiens (human)	IC50	0.3000	1	1
Cytochrome P450 2D6	Homo sapiens (human)	Ki	7.0000	1	1
Cytochrome P450 2J2	Homo sapiens (human)	IC50	17.5000	1	2
D	Bos taurus (cattle)	IC50	0.5428	4	5
D	Rattus norvegicus (Norway rat)	IC50	0.2538	9	16
D	Rattus norvegicus (Norway rat)	Ki	0.0337	3	4
D(1A) dopamine receptor	Homo sapiens (human)	IC50	0.9040	1	3
D(1A) dopamine receptor	Homo sapiens (human)	Ki	0.3260	2	5
D(1B) dopamine receptor	Rattus norvegicus (Norway rat)	IC50	0.1842	7	14
D(1B) dopamine receptor	Homo sapiens (human)	Ki	0.0965	1	2
D(1B) dopamine receptor	Rattus norvegicus (Norway rat)	Ki	0.0140	1	1
D(2) dopamine receptor	Bos taurus (cattle)	IC50	0.4657	5	6
D(2) dopamine receptor	Homo sapiens (human)	IC50	0.0722	6	8
D(2) dopamine receptor	Rattus norvegicus (Norway rat)	IC50	0.1410	10	19
D(2) dopamine receptor	Homo sapiens (human)	Ki	0.0174	10	13
D(2) dopamine receptor	Rattus norvegicus (Norway rat)	Ki	0.0055	8	9
D(3) dopamine receptor	Homo sapiens (human)	IC50	0.0725	1	3
D(3) dopamine receptor	Rattus norvegicus (Norway rat)	IC50	0.1842	7	14
D(3) dopamine receptor	Homo sapiens (human)	Ki	0.0101	8	13
D(3) dopamine receptor	Rattus norvegicus (Norway rat)	Ki	0.0140	1	1
D(4) dopamine receptor	Homo sapiens (human)	IC50	3.6210	1	2
D(4) dopamine receptor	Rattus norvegicus (Norway rat)	IC50	0.1842	7	14
D(4) dopamine receptor	Homo sapiens (human)	Ki	0.5253	3	5
D(4) dopamine receptor	Rattus norvegicus (Norway rat)	Ki	0.0140	1	1
Delta-type opioid receptor	Homo sapiens (human)	IC50	22.4650	1	2
Delta-type opioid receptor	Homo sapiens (human)	Ki	7.9190	1	2
DNA-dependent protein kinase catalytic subunit	Homo sapiens (human)	IC50	100.0000	1	1
Emopamil-binding protein-like	Homo sapiens (human)	Ki	0.0039	1	1
Epidermal growth factor receptor	Homo sapiens (human)	IC50	34.4875	1	2
Gastrin/cholecystokinin type B receptor	Mus musculus (house mouse)	Ki	0.0033	1	2
Genome polyprotein		IC50	0.7000	1	1
Glutamate receptor ionotropic, NMDA 1	Homo sapiens (human)	IC50	0.8500	2	2
Glutamate receptor ionotropic, NMDA 1	Rattus norvegicus (Norway rat)	IC50	1.3000	1	1
Glutamate receptor ionotropic, NMDA 2A	Homo sapiens (human)	IC50	0.8500	2	2
Glutamate receptor ionotropic, NMDA 2A	Rattus norvegicus (Norway rat)	IC50	1.3000	1	1
Glutamate receptor ionotropic, NMDA 2B	Homo sapiens (human)	IC50	0.8500	2	2
Glutamate receptor ionotropic, NMDA 2B	Rattus norvegicus (Norway rat)	IC50	1.3000	1	1
Glutamate receptor ionotropic, NMDA 2C	Homo sapiens (human)	IC50	0.8500	2	2
Glutamate receptor ionotropic, NMDA 2C	Rattus norvegicus (Norway rat)	IC50	1.3000	1	1
Glutamate receptor ionotropic, NMDA 2D	Homo sapiens (human)	IC50	0.8500	2	2
Glutamate receptor ionotropic, NMDA 2D	Rattus norvegicus (Norway rat)	IC50	1.3000	1	1
Glutamate receptor ionotropic, NMDA 3A	Homo sapiens (human)	IC50	0.8500	2	2
Glutamate receptor ionotropic, NMDA 3A	Rattus norvegicus (Norway rat)	IC50	1.3000	1	1
Glutamate receptor ionotropic, NMDA 3B	Homo sapiens (human)	IC50	0.8500	2	2
Glutamate receptor ionotropic, NMDA 3B	Rattus norvegicus (Norway rat)	IC50	1.3000	1	1
Histamine H1 receptor	Homo sapiens (human)	IC50	0.5054	3	5
Histamine H1 receptor	Cavia porcellus (domestic guinea pig)	Ki	0.1585	1	1
Histamine H1 receptor	Homo sapiens (human)	Ki	0.0103	2	5
Histamine H2 receptor	Homo sapiens (human)	IC50	2.2367	1	3
Histamine H2 receptor	Homo sapiens (human)	Ki	2.1990	1	3
Histamine H3 receptor	Homo sapiens (human)	Ki	1.0000	1	2
Kappa-type opioid receptor	Homo sapiens (human)	IC50	17.9045	1	2
Kappa-type opioid receptor	Homo sapiens (human)	Ki	7.1620	1	2
Lysozyme C-1	Rattus norvegicus (Norway rat)	IC50	9.0000	1	1
Melanocortin receptor 3	Homo sapiens (human)	IC50	24.3430	1	1
Melanocortin receptor 3	Homo sapiens (human)	Ki	21.2440	1	1
Melanocortin receptor 4	Homo sapiens (human)	IC50	15.2040	1	1
Melanocortin receptor 4	Homo sapiens (human)	Ki	14.6190	1	1
Melanocortin receptor 5	Homo sapiens (human)	IC50	8.5675	1	2
Melanocortin receptor 5	Homo sapiens (human)	Ki	8.0370	1	2
Mu-type opioid receptor	Homo sapiens (human)	IC50	17.5710	1	2
Mu-type opioid receptor	Homo sapiens (human)	Ki	7.1325	1	2
Multidrug resistance-associated protein 4	Homo sapiens (human)	IC50	133.0000	1	2
Muscarinic acetylcholine receptor M1	Homo sapiens (human)	IC50	1.0843	1	3
Muscarinic acetylcholine receptor M1	Homo sapiens (human)	Ki	0.2272	2	4
Muscarinic acetylcholine receptor M1	Rattus norvegicus (Norway rat)	Ki	0.0603	1	1
Muscarinic acetylcholine receptor M2	Homo sapiens (human)	IC50	3.0740	1	3
Muscarinic acetylcholine receptor M2	Homo sapiens (human)	Ki	1.0930	1	3
Muscarinic acetylcholine receptor M2	Rattus norvegicus (Norway rat)	Ki	0.0603	1	1
Muscarinic acetylcholine receptor M3	Homo sapiens (human)	IC50	1.7833	1	3
Muscarinic acetylcholine receptor M3	Homo sapiens (human)	Ki	0.3780	1	3
Muscarinic acetylcholine receptor M3	Rattus norvegicus (Norway rat)	Ki	0.0603	1	1
Muscarinic acetylcholine receptor M4	Homo sapiens (human)	IC50	1.3053	1	3
Muscarinic acetylcholine receptor M4	Homo sapiens (human)	Ki	0.1764	2	4
Muscarinic acetylcholine receptor M4	Rattus norvegicus (Norway rat)	Ki	0.0603	1	1
Muscarinic acetylcholine receptor M5	Homo sapiens (human)	IC50	0.0445	1	2
Muscarinic acetylcholine receptor M5	Homo sapiens (human)	Ki	0.0320	1	2
Muscarinic acetylcholine receptor M5	Rattus norvegicus (Norway rat)	Ki	0.0603	1	1
NADPH oxidase 1	Homo sapiens (human)	IC50	17.0000	1	4
Nuclear receptor subfamily 3 group C member 3	Bos taurus (cattle)	IC50	5.4938	1	4
Nuclear receptor subfamily 3 group C member 3	Bos taurus (cattle)	Ki	4.5009	1	4
Pleiotropic ABC efflux transporter of multiple drugs	Saccharomyces cerevisiae S288C	IC50	4.6000	1	7
Polyunsaturated fatty acid lipoxygenase ALOX15	Oryctolagus cuniculus (rabbit)	IC50	15.9510	1	1
Potassium channel subfamily K member 2	Homo sapiens (human)	IC50	3.7000	1	2
Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)	IC50	2.8158	9	12
Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)	Ki	4.5009	1	4
Procathepsin L	Homo sapiens (human)	IC50	11.5200	1	4
Protein kinase C alpha type	Rattus norvegicus (Norway rat)	IC50	500.0000	1	1
Protein kinase C beta type	Rattus norvegicus (Norway rat)	IC50	500.0000	1	1
Protein kinase C delta type	Rattus norvegicus (Norway rat)	IC50	500.0000	1	1
Protein kinase C epsilon type	Rattus norvegicus (Norway rat)	IC50	500.0000	1	1
Protein kinase C eta type	Rattus norvegicus (Norway rat)	IC50	500.0000	1	1
Protein kinase C gamma type	Rattus norvegicus (Norway rat)	IC50	500.0000	1	1
Protein kinase C theta type	Rattus norvegicus (Norway rat)	IC50	500.0000	1	1
Protein kinase C zeta type	Rattus norvegicus (Norway rat)	IC50	500.0000	1	1
Receptor tyrosine-protein kinase erbB-2	Homo sapiens (human)	IC50	19.4680	1	2
Replicase polyprotein 1a	Severe acute respiratory syndrome-related coronavirus	IC50	11.5200	1	4
Replicase polyprotein 1ab	Betacoronavirus England 1	IC50	11.5200	1	4
Replicase polyprotein 1ab	Human coronavirus 229E	IC50	11.5200	1	4
Replicase polyprotein 1ab	Severe acute respiratory syndrome coronavirus 2	IC50	11.5200	1	4
Replicase polyprotein 1ab	Severe acute respiratory syndrome-related coronavirus	IC50	11.5200	1	4
Retinal dehydrogenase 1	Homo sapiens (human)	IC50	0.5242	1	1
Sarcoplasmic/endoplasmic reticulum calcium ATPase 1	Oryctolagus cuniculus (rabbit)	IC50	27.6667	1	3
Sigma non-opioid intracellular receptor 1	Homo sapiens (human)	IC50	0.2473	1	3
Sigma non-opioid intracellular receptor 1	Homo sapiens (human)	Ki	0.0816	2	4
Sodium channel protein type 1 subunit alpha	Homo sapiens (human)	IC50	4.3000	1	1
Sodium channel protein type 10 subunit alpha	Homo sapiens (human)	IC50	4.3000	1	1
Sodium channel protein type 11 subunit alpha	Homo sapiens (human)	IC50	4.3000	1	1
Sodium channel protein type 2 subunit alpha	Homo sapiens (human)	IC50	4.3000	1	1
Sodium channel protein type 3 subunit alpha	Homo sapiens (human)	IC50	4.3000	1	1
Sodium channel protein type 4 subunit alpha	Homo sapiens (human)	IC50	4.3000	1	1
Sodium channel protein type 5 subunit alpha	Homo sapiens (human)	IC50	4.3000	1	1
Sodium channel protein type 7 subunit alpha	Homo sapiens (human)	IC50	4.3000	1	1
Sodium channel protein type 8 subunit alpha	Homo sapiens (human)	IC50	4.3000	1	1
Sodium channel protein type 9 subunit alpha	Homo sapiens (human)	IC50	4.3000	1	1
Sodium-dependent dopamine transporter	Rattus norvegicus (Norway rat)	IC50	1.4791	1	2
Sodium-dependent dopamine transporter	Rattus norvegicus (Norway rat)	Ki	0.0040	1	1
Sodium-dependent dopamine transporter	Homo sapiens (human)	IC50	2.3480	1	2
Sodium-dependent dopamine transporter	Homo sapiens (human)	Ki	1.8655	1	2
Sodium-dependent noradrenaline transporter	Homo sapiens (human)	IC50	0.6647	1	3
Sodium-dependent noradrenaline transporter	Homo sapiens (human)	Ki	0.6593	1	3
Sodium-dependent serotonin transporter	Homo sapiens (human)	IC50	0.4342	2	4
Sodium-dependent serotonin transporter	Homo sapiens (human)	Ki	0.2308	2	4
Solute carrier family 22 member 1	Homo sapiens (human)	IC50	39.6250	2	4
Sphingomyelin phosphodiesterase	Homo sapiens (human)	IC50	11.0000	1	1
Spike glycoprotein	Betacoronavirus England 1	IC50	11.5200	1	4
Spike glycoprotein	Severe acute respiratory syndrome-related coronavirus	IC50	11.5200	1	4
Substance-K receptor	Homo sapiens (human)	IC50	24.8395	1	2
Substance-K receptor	Homo sapiens (human)	Ki	8.2800	1	2
Transient receptor potential cation channel subfamily V member 1	Rattus norvegicus (Norway rat)	Ki	0.9100	2	2
Transmembrane protease serine 2	Homo sapiens (human)	IC50	11.5200	1	4
Trypanothione reductase	Trypanosoma cruzi	IC50	132.8167	2	6
Trypanothione reductase	Trypanosoma cruzi	Ki	21.3500	3	6
Tyrosine-protein kinase Fyn	Homo sapiens (human)	IC50	8.3350	1	2
Ubiquitin carboxyl-terminal hydrolase 1	Homo sapiens (human)	IC50	8.0000	1	1
ubiquitin-conjugating enzyme E2 N	Homo sapiens (human)	IC50	14.7900	2	2
Voltage-dependent L-type calcium channel subunit alpha-1C	Homo sapiens (human)	IC50	3.4000	1	1
Voltage-dependent L-type calcium channel subunit alpha-1D	Homo sapiens (human)	IC50	3.4000	1	1
Voltage-dependent L-type calcium channel subunit alpha-1F	Homo sapiens (human)	IC50	3.4000	1	1
Voltage-dependent L-type calcium channel subunit alpha-1S	Homo sapiens (human)	IC50	3.4000	1	1
WD repeat-containing protein 48	Homo sapiens (human)	IC50	8.0000	1	1

Activation Measurements

Protein	Taxonomy	Measurement	Average (mM)	Bioassay(s)	Drugs
5-hydroxytryptamine receptor 2A	Rattus norvegicus (Norway rat)	Kd	0.0010	1	1
5-hydroxytryptamine receptor 2B	Rattus norvegicus (Norway rat)	Kd	0.0010	1	1
5-hydroxytryptamine receptor 2C	Rattus norvegicus (Norway rat)	Kd	0.0010	1	1
Albumin	Homo sapiens (human)	Kd	54.9541	1	1
Albumin	Rattus norvegicus (Norway rat)	Kd	12.8500	1	2
Angiotensin-converting enzyme 2	Homo sapiens (human)	EC50	11.0327	1	11
Calmodulin	Bos taurus (cattle)	Kd	3.2500	1	2
Calmodulin-1	Homo sapiens (human)	Kd	1.1200	2	2
Cytochrome P450 1A2	Homo sapiens (human)	EC50	2.0000	1	1
Cytochrome P450 2D6	Homo sapiens (human)	EC50	2.0000	1	1
D(2) dopamine receptor	Rattus norvegicus (Norway rat)	Kd	0.0005	1	1
Major prion protein	Homo sapiens (human)	EC50	4.0000	1	3
Major prion protein	Mus musculus (house mouse)	EC50	2.0000	1	1
Potassium channel subfamily K member 2	Homo sapiens (human)	EC50	4.7000	1	1
Procathepsin L	Homo sapiens (human)	EC50	11.0327	1	11
Proteasome subunit alpha type-6	Homo sapiens (human)	EC50	12.3500	1	2
Replicase polyprotein 1a	Severe acute respiratory syndrome-related coronavirus	EC50	11.0327	1	11
Replicase polyprotein 1ab	Betacoronavirus England 1	EC50	11.0327	1	11
Replicase polyprotein 1ab	Human coronavirus 229E	EC50	11.0327	1	11
Replicase polyprotein 1ab	Severe acute respiratory syndrome coronavirus 2	EC50	11.0327	1	11
Replicase polyprotein 1ab	Severe acute respiratory syndrome-related coronavirus	EC50	11.0327	1	11
Spike glycoprotein	Betacoronavirus England 1	EC50	11.0327	1	11
Spike glycoprotein	Severe acute respiratory syndrome-related coronavirus	EC50	11.0327	1	11
Transmembrane protease serine 2	Homo sapiens (human)	EC50	11.0327	1	11

Other Measurements

Protein	Taxonomy	Measurement	Average (mM)	Bioassay(s)	Drugs
ATP-dependent translocase ABCB1	Homo sapiens (human)	Km	27.4000	1	1
D(1A) dopamine receptor	Homo sapiens (human)	Kb	1.0000	1	1
D(1B) dopamine receptor	Homo sapiens (human)	Kb	1.0000	1	1
D(2) dopamine receptor	Rattus norvegicus (Norway rat)	K0.5	0.0009	2	3
D(2) dopamine receptor	Homo sapiens (human)	Kb	0.3341	3	3
D(3) dopamine receptor	Homo sapiens (human)	Kb	1.0000	1	1
D(4) dopamine receptor	Homo sapiens (human)	Kb	1.0000	1	1
DNA repair protein RAD52 homolog isoform a	Homo sapiens (human)	AC50	13.4700	1	2
Pleiotropic ABC efflux transporter of multiple drugs	Saccharomyces cerevisiae S288C	INH	43.8143	1	7
Proteasome subunit alpha type-1	Homo sapiens (human)	EC200	45.1250	4	4
Proteasome subunit alpha type-2	Homo sapiens (human)	EC200	45.1250	4	4
Proteasome subunit alpha type-3	Homo sapiens (human)	EC200	45.1250	4	4
Proteasome subunit alpha type-4	Homo sapiens (human)	EC200	45.1250	4	4
Proteasome subunit alpha type-5	Homo sapiens (human)	EC200	45.1250	4	4
Proteasome subunit alpha type-6	Homo sapiens (human)	EC200	45.1250	4	4
Proteasome subunit alpha type-7	Homo sapiens (human)	EC200	45.1250	4	4
Proteasome subunit alpha-type 8	Homo sapiens (human)	EC200	45.1250	4	4
Proteasome subunit beta type-1	Homo sapiens (human)	EC200	45.1250	4	4
Proteasome subunit beta type-10	Homo sapiens (human)	EC200	45.1250	4	4
Proteasome subunit beta type-11	Homo sapiens (human)	EC200	45.1250	4	4
Proteasome subunit beta type-2	Homo sapiens (human)	EC200	45.1250	4	4
Proteasome subunit beta type-3	Homo sapiens (human)	EC200	45.1250	4	4
Proteasome subunit beta type-4	Homo sapiens (human)	EC200	45.1250	4	4
Proteasome subunit beta type-5	Homo sapiens (human)	EC200	45.1250	4	4
Proteasome subunit beta type-6	Homo sapiens (human)	EC200	45.1250	4	4
Proteasome subunit beta type-7	Homo sapiens (human)	EC200	45.1250	4	4
Proteasome subunit beta type-8	Homo sapiens (human)	EC200	45.1250	4	4
Proteasome subunit beta type-9	Homo sapiens (human)	EC200	45.1250	4	4
protein AF-9 isoform a	Homo sapiens (human)	AC50	14.3700	1	2
Snq2p	Saccharomyces cerevisiae EC1118	INH	42.1429	1	7
UDP-glucuronosyltransferase 1A4	Homo sapiens (human)	Km	93.0000	1	1