Page last updated: 2024-12-05

phenformin

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Description

Phenformin is a biguanide antidiabetic drug that was withdrawn from the market in the 1970s due to concerns about lactic acidosis. However, it has been studied extensively for its potential therapeutic effects in various diseases. Its mechanism of action involves inhibiting mitochondrial complex I and activating AMP-activated protein kinase (AMPK), which leads to improved insulin sensitivity, reduced hepatic glucose production, and increased glucose uptake in peripheral tissues. Research suggests that phenformin may have potential benefits for treating type 2 diabetes, non-alcoholic fatty liver disease, and even cancer. However, its use is still under investigation due to its safety concerns. Phenformin can be synthesized by reacting guanylurea with 2-chloro-N-methylpropionamide. It is typically administered orally and undergoes extensive metabolism in the liver.'

Phenformin: A biguanide hypoglycemic agent with actions and uses similar to those of METFORMIN. Although it is generally considered to be associated with an unacceptably high incidence of lactic acidosis, often fatal, it is still available in some countries. (From Martindale, The Extra Pharmacopoeia, 30th ed, p290) [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

phenformin : A member of the class of biguanides that is biguanide in which one of the terminal nitrogen atoms is substituted by a 2-phenylethyl group. It was used as an anti-diabetic drug but was later withdrawn from the market due to potential risk of lactic acidosis. [Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Cross-References

ID SourceID
PubMed CID8249
CHEMBL ID170988
CHEBI ID8064
SCHEMBL ID8424
SCHEMBL ID10325620
SCHEMBL ID17300524
MeSH IDM0016508

Synonyms (123)

Synonym
AKOS005567415
BRD-K11399644-003-03-0
n-(2-phenylethyl)imidodicarbonimidic diamide
biguanide, 1-phenethyl-
BPBIO1_000085
BSPBIO_000077
CMAP_000038
PRESTWICK2_000179
PRESTWICK3_000179
ccris 500
phenethyldiguanide
dibiraf
fenformina
debeone
fenformina [inn-spanish]
phenylethylbiguanide
brn 1977317
db comb
pedg
fenfoduron
beta-phenethylbiguanide
glukopostin
phenforminum [inn-latin]
lentobetic
azucaps
w 32
n'-beta-phenethylformamidinylliminourea
n'-beta-fenetilformamidiniliminourea [italian]
db-retard
diabis
retardo
phenformix
nci-c01741
d bretard
glyphen
hsdb 3154
einecs 204-057-4
1-phenethylbiguanide
insoral
phenformine [inn-french]
debinyl
phenformine
feguanide
dibein
fenormin
cronoformin
phenformin [inn:ban]
dibotin
beta-pebg
C07673
114-86-3
phenformin
1-carbamimidoyl-3-phenethyl-guanidine
imidodicarbonimidic diamide, n-(2-phenylethyl)-
DB00914
fenformin
beta-phenethybiguanide
KBIO2_004960
KBIOSS_002397
KBIOGR_002392
KBIO2_007528
KBIO3_002871
KBIO2_002392
SPBIO_001998
PRESTWICK0_000179
PRESTWICK1_000179
NCGC00016543-02
n''''-[(e)-amino(imino)methyl]-n-(2-phenylethyl)guanidine
n-(2-phenylethyl)imidodicarbonimidic diamide(phenformin)
n''''-{amino[(2-phenylethyl)imino]methyl}guanidine
n-amino(imino)methyl-n-phenethyliminomethanediamine(phenformin)
bdbm50240908
D08351
phenformin (ban)
CHEMBL170988 ,
chebi:8064 ,
STK635703
BBL010845
NCGC00016543-03
NCGC00016543-04
NCGC00016543-05
phenformine hcl
phenforminum
dd5k7529ce ,
unii-dd5k7529ce
n'-beta-fenetilformamidiniliminourea
4-12-00-02472 (beilstein handbook reference)
NCGC00016543-08
phenformin [vandf]
phenformin [inn]
phenformin [who-dd]
phenformin [mi]
phenformin [hsdb]
SCHEMBL8424
n-phenethylbiguanide
MLS006011899
smr004703510
SCHEMBL10325620
8cv ,
n'-.beta.-phenethylformamidinylliminourea
.beta.-phenethylbiguanide
dipar (salt/mix)
n-(2-phenylethyl)dicarbonimidic diamide #
.beta.-pebg
n'-.beta.-fenetilformamidiniliminourea
meltrol (salt/mix)
HMS3604G03
bdbm50237608
SCHEMBL17300524
DTXSID1023449
1-carbamimidamido-n-(2-phenylethyl)methanimidamide
SBI-0206879.P001
SY031759
mfcd00242966
2-(n-phenethylcarbamimidoyl)guanidine
114-86-3 (free base)
Q753100
1-(diaminomethylidene)-2-(2-phenylethyl)guanidine
AC3005
CS-11859
nsc-756501
nsc756501
EN300-7418232

Research Excerpts

Overview

Phenformin is a drug in the biguanide class that was previously used to treat type 2 diabetes. Phenformin may prove to be a useful tool for the study of sodium transport in amphibian epithelia.

ExcerptReferenceRelevance
"Phenformin is an antidiabetic drug of the biguanide class."( Cytotoxic effects of Phenformin on ovarian cancer cells: expression of HIF-1α and PDK1 in the hypoxic microenvironment.
Elbe, H; Gunaydin, B; Yigitturk, G,
)
1.17
"Phenformin is a drug in the biguanide class that was previously used to treat type 2 diabetes. "( Phenformin Promotes Keratinocyte Differentiation via the Calcineurin/NFAT Pathway.
Dotto, GP; Huang, M; Kim, SH; Liu, C; Pérez-Lorenzo, R; Wu, X; Zheng, B; Zhou, Q, 2021
)
3.51
"Phenformin is a mitochondrial complex I inhibitor that induces bioenergetic stress."( STAT1 potentiates oxidative stress revealing a targetable vulnerability that increases phenformin efficacy in breast cancer.
Aguilar-Mahecha, A; Ahn, R; Avizonis, D; Basik, M; Cepeda Cañedo, E; Chabot, C; Dankner, M; Goulet, ML; Hébert, S; Im, YK; Kleinman, CL; Kuasne, H; La Selva, R; Lebeau, B; Lewis, K; Lin, R; Martínez, C; Najyb, O; Nguyen, A; Park, M; Petrecca, K; Pollak, M; Sabourin, V; Santos Martínez, N; Savage, P; Siegel, PM; St-Pierre, J; Topisirovic, I; Totten, SP; Ursini-Siegel, J; Witcher, M, 2021
)
1.57
"Phenformin was found to be a more potent growth inhibitor than metformin and both compounds cause acidification of the medium when incubated with colon cancer cells."( Addition of 2-deoxyglucose enhances growth inhibition but reverses acidification in colon cancer cells treated with phenformin.
Bolikal, S; Chacko, J; Chung, R; desbordes, C; Hong, JY; Lea, MA; Ortega, A, 2011
)
1.3
"Phenformin is a biguanide that has been largely used in the past for its anti-diabetic activity. "( Effects of phenformin on the proliferation of human tumor cell lines.
Bianchi, A; Caraci, F; Chiechio, S; Chisari, M; Frasca, G; Pinto, A; Salomone, S; Sortino, MA, 2003
)
2.15
"Phenformin may prove to be a useful tool for the study of sodium transport in amphibian epithelia."( Effects of biguanides on short-circuit current in frog skin.
Saito, T; Yoshida, S, 1984
)
0.99
"Phenformin is a biguanide compound that can modulate glucose metabolism and promote weight loss and is therefore used to treat patients with type-2 diabetes. "( Phenformin suppresses calcium responses to glutamate and protects hippocampal neurons against excitotoxicity.
Chan, SL; Lane, MA; Lee, J; Lu, C; Mattson, MP, 2002
)
3.2

Effects

Phenformin has clinical potential as an antineoplastic agent and should be considered for clinical trials both in ER-positive and triple-negative breast cancer. Phenformin prolongs thrombin time and enhances fibrinolysis.

ExcerptReferenceRelevance
"Phenformin has clinical potential as an antineoplastic agent and should be considered for clinical trials both in ER-positive and triple-negative breast cancer."( Phenformin as prophylaxis and therapy in breast cancer xenografts.
Alessi, DR; Appleyard, MV; Bray, SE; Coates, PJ; Fleming, S; Kernohan, NM; Murray, KE; Thompson, AM; Wullschleger, S, 2012
)
3.26
"Phenformin has shown the characteristic properties of an antifibrinopathic agent in that it prolongs thrombin time and enhances fibrinolysis."( Antifibrin action of phenformin.
Arya, M; Banerjee, RN; Bardhan, J; Kumar, V; Rao, SR; Sahni, AL, 1975
)
1.29

Actions

The phenformin-induced increase in insulin binding to IM-9 cells was related to a time- and dose-dependent decrease in ATP levels. Phenformin was shown to inhibit the rate of the Ehrlich carcinoma cell growth both in solid and ascitic forms.

ExcerptReferenceRelevance
"The phenformin-induced increase in insulin binding to IM-9 cells was related to a time- and dose-dependent decrease in ATP levels."( The effect of phenformin and other adenosine triphosphate (ATP)-lowering agents on insulin binding to IM-9 human cultured lymphocytes.
Goldfine, ID; Maddux, B; Vigneri, R, 1984
)
1.11
"Phenformin was shown to inhibit the rate of the Ehrlich carcinoma cell growth both in solid and ascitic forms of the tumor. "( [Inhibiting effect of phenformin (phenethyl biguanide) on the growth of Ehrlich carcinoma].
Dil'man, VM; Lebedev, KA; Shikhman, AR, 1981
)
2.02

Treatment

Phenformin treatment should be avoided in case of renal and/or liver insufficiency. Co-treatment of phenformin enhances the effect of anti-PD-1 antibody therapy on inhibiting tumor growth in the BRAF V600E/PTEN-null melanoma model.

ExcerptReferenceRelevance
"Phenformin treatment activates the IRE1α and PERK pathways in an AMPK-dependent manner."( Phenformin activates the unfolded protein response in an AMP-activated protein kinase (AMPK)-dependent manner.
Davisson, RL; Qi, L; Sha, H; Yang, L, 2013
)
3.28
"Phenformin treatment inhibited the development of induced tumors in the nervous system and kidneys, significantly decreased the total incidence and multiplicity of these tumors, the incidence of brain and spinal cord tumors and multiplicity of brain tumors."( [Effect of phenformin and succinic acid on the transplacental carcinogenic effect of N-nitroso-N-ethylurea in rats].
Aleksandrov, VA; Bespalov, VG, 1984
)
1.38
"Phenformin-treated rats revealed-a tendency towards a decrease in blood insulin level (radioimmunoassay)."( Inhibition of DMBA-induced carcinogenesis by phenformin in the mammary gland of rats.
Alexandrov, VA; Berstein, LM; Bobrov, JF; Dilman, VM; Pliss, GB; Zabezhinski, MA, 1978
)
1.24
"Phenformin and metformin treatments may be complicated by lactic adidosis. "( Effects of biguanides on the intermediate metabolism of glucose in normal and portal-strictured rats.
Freund, H; Frick, A; Imler, M; Marbach, J; Schlienger, JL, 1979
)
1.7
"Phenformin treatment should be avoided in case of renal and/or liver insufficiency."( Phenformin-induced lactic acidosis in diabetic patients.
Assan, R; Attali, JR; Girard, JR; Heuclin, C; LeMaire, F, 1975
)
2.42
"Phenformin treatment did not affect the disappearance of glucose, nor the insulin levels after intravenous glucose loading."( The effect of phenformin-HCl on patients with diabetes mellitus, studied under strict balance conditions.
Geldermans, CA; Krans, HM; Terpstra, J, 1975
)
1.34
"Pre-treatment with phenformin increased hatching rate, spontaneous movement, heart beat, and larval motor activity, decreased mortality and malformation rate, increased SOD, CAT, and AChE activities, and reduced MDA compared to irradiation-only embryos."( Protective effects of phenformin on zebrafish embryonic neurodevelopmental toxicity induced by X-ray radiation.
Gan, L; Guo, M; Li, H; Liu, Z; Si, J; Wang, F; Yan, J; Zhang, H; Zhang, J; Zhao, J, 2019
)
1.15
"Co-treatment of phenformin enhances the effect of anti-PD-1 antibody therapy on inhibiting tumor growth in the BRAF V600E/PTEN-null melanoma mouse model."( Phenformin Inhibits Myeloid-Derived Suppressor Cells and Enhances the Anti-Tumor Activity of PD-1 Blockade in Melanoma.
Kim, SH; Li, M; Pasca di Magliano, M; Swanson, KD; Trousil, S; Zhang, Y; Zheng, B, 2017
)
2.23
"Treatment with phenformin did not significantly influence food and water consumption, body weight, and temperature when compared with the ad libitum fed controls."( Effects of phentermine and phenformin on biomarkers of aging in rats.
Anikin, IV; Anisimov, VN; Arutjunyan, AV; Bertsein, LM; Ingram, DK; Lane, MA; Popovich, IG; Roth, GS; Ukraintseva, SV; Zabezhinski, MA,
)
0.77
"Treatment with phenformin, decaris and S-methylmethionine was shown to produce a favorable effect on certain stages of catecholamine synthesis and metabolism as well as on immunologic indexes and hemodynamic stability."( [Correction of the function of the sympathoadrenal system in the surgical and combined treatment of patients with cancer of the esophagus and stomach].
Balitskiĭ, KP; Paliukh, AR; Shmal'ko, IuP; Tarutinov, VI; Vinnitskiĭ, VB, 1985
)
0.61

Toxicity

ExcerptReferenceRelevance
"A survey of the literature leads to the conclusion that lactic acidosis should be considered as a side effect of therapy with biguanides."( [The importance of lactate acidosis as a side effect of biguanide therapy].
Förster, H, 1976
)
0.26
" In Sweden, the combined use of spontaneous adverse drug reaction (ADR) reporting data and different registers has yielded much valuable information on safety problems with different drugs."( Regulatory decisions. Emphasis on safety issues.
Strandberg, K; Wiholm, BE, 1986
)
0.27

Pharmacokinetics

Phenformin hydrochloride can slow down the absorption process of puerarin and change the pharmacokinetic process. Cmax were (2.2) after oral administration with pueraria extracts and phenformin Hydrochloride.

ExcerptReferenceRelevance
" The method was applicable to clinical pharmacokinetic study of metformin and rosiglitazone in healthy volunteers following oral administration."( Simultaneous determination and pharmacokinetic study of metformin and rosiglitazone in human plasma by HPLC-ESI-MS.
Chen, L; Ma, A; Shen, M; Zhou, Z, 2011
)
0.37
" After oral administration in the two groups, their bloods were sampled at different time points to determine the drug concentration of puerarin in rat blood and calculate pharmacokinetic parameters."( [Effect of phenformin hydrochloride on pharmacokinetics of puerarin in rats].
Cui, M; Deng, Y; Li, FM; Li, N; Xiong, ZL, 2012
)
0.77
"After oral administration with pueraria extracts and phenformin hydrochloride combined with pueraria extracts, the two groups showed main pharmacokinetic parameters as follows: Cmax were (2."( [Effect of phenformin hydrochloride on pharmacokinetics of puerarin in rats].
Cui, M; Deng, Y; Li, FM; Li, N; Xiong, ZL, 2012
)
1.02
"Phenformin hydrochloride can slow down the absorption process of puerarin and change the pharmacokinetic process of puerarin to some extent."( [Effect of phenformin hydrochloride on pharmacokinetics of puerarin in rats].
Cui, M; Deng, Y; Li, FM; Li, N; Xiong, ZL, 2012
)
2.21

Compound-Compound Interactions

Phenformin shows potential as an effective drug against bladder cancer, either alone or in combination with gefitinib.

ExcerptReferenceRelevance
"The hepatic organic anion transporting polypeptides (OATPs) influence the pharmacokinetics of several drug classes and are involved in many clinical drug-drug interactions."( Classification of inhibitors of hepatic organic anion transporting polypeptides (OATPs): influence of protein expression on drug-drug interactions.
Artursson, P; Haglund, U; Karlgren, M; Kimoto, E; Lai, Y; Norinder, U; Vildhede, A; Wisniewski, JR, 2012
)
0.38
" Additive effects were seen when these molecules were combined with 3PO."( Inhibition of Growth of Bladder Cancer Cells by 3-(3-Pyridinyl)-1-(4-pyridinyl)-2-propen-1-one in Combination with Other Compounds Affecting Glucose Metabolism.
Altayyar, M; desBordes, C; Lea, MA, 2015
)
0.42
" Here we examined whether the metformin analogue phenformin, either used alone or in combination with gefitinib, could inhibit growth of bladder cancer cells."( Phenformin alone or combined with gefitinib inhibits bladder cancer via AMPK and EGFR pathways.
Darko, KO; Deng, J; He, C; Huang, Y; Peng, M; Su, Q; Tao, T; Yang, X; Zhou, S, 2018
)
2.18
"Phenformin shows potential as an effective drug against bladder cancer, either alone or in combination with gefitinib."( Phenformin alone or combined with gefitinib inhibits bladder cancer via AMPK and EGFR pathways.
Darko, KO; Deng, J; He, C; Huang, Y; Peng, M; Su, Q; Tao, T; Yang, X; Zhou, S, 2018
)
3.37
"A rapid and accurate method for the sensitive detection of illegal drug additives including atenolol (ATN), metformin hydrochloride (MET), and phenformin hydrochloride (PHE) in health products using solvent microextraction (SME) combined with surface-enhanced Raman spectroscopy (SERS) was developed."( Highly sensitive detection of an antidiabetic drug as illegal additives in health products using solvent microextraction combined with surface-enhanced Raman spectroscopy.
He, H; Li, P; Lin, D; Yang, L, 2019
)
0.71

Bioavailability

ExcerptReferenceRelevance
" The rate of absorption decreased from the colon to the duodenum (colon greater than ileum greater than jejunum greater than duodenum)."( Intestinal oxalate absorption. I. Absorption in vitro.
Caspary, WF, 1977
)
0.26
" Taken together, our results suggest that inhibition of mitochondrial metabolism by Metformin or Phenformin is associated with increased leukemia cell susceptibility to induction of intrinsic apoptosis, and provide a rationale for clinical studies exploring the efficacy of combining biguanides with the orally bioavailable derivative of ABT-737, Venetoclax."( Biguanides sensitize leukemia cells to ABT-737-induced apoptosis by inhibiting mitochondrial electron transport.
Andreeff, M; Bornmann, W; Duque, JE; Enciso, L; Jaramillo, D; Konopleva, M; Krystal, G; Lee, JT; Lopez, C; Morales, L; Pan, R; Samudio, I; Suarez, M; Velez, J, 2016
)
0.65
"The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs."( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019
)
0.51

Dosage Studied

In diabetic patients treated with sulphonylureas and phenformin at low dosage it was possible to maintain good glycometabolic control. Of the 141 subjects dosed with debrisoquin, 10 proved to be poor oxidizers. The daily dosage of Phenformin and metformin was increased at weekly intervals up to 300 mg. Although the urinary excretion of unchanged phen formin was greater in PM between 2 and 24 hr after dosing than in EM.

ExcerptRelevanceReference
" No consistent relationship was demonstrable between the serum biguanide level, administered dosage and time of administration."( [Biguanide-induced and - associated lactic acidosis: serum and tissue biguanide levels in hyperlactaemia and lactic acidosis (author's transl)].
Irsigler, K; Kaspar, L; Kritz, H; Regal, H, 1979
)
0.26
" Side effects were more common with metformin, particularly in the higher dosage and overall control of the diabetes was achieved in the same proportion of patients (33%)."( A comparison of phenformin and metformin in the treatment of maturity onset diabetes.
Cairns, SA; Hartog, M; Marshall, AJ; Shalet, S, 1977
)
0.6
" In diabetic patients treated with sulphonylureas and phenformin at low dosage (glibenclamide 5 mg and phenformin 50 mg) it was possible to maintain good glycometabolic control using only the sulphonylurea gliclazide (160 mg/die)."( [Efficacy of sulfonylurea and sulfonylurea-benfluorex therapy in patients with type 2 diabetes treated with commercial sulfonylurea-biguanide combinations].
Benzi, L; Cecchetti, P; Ciccarone, AM; Di Cianni, G; Giannarelli, R; Navalesi, R; Penno, G,
)
0.38
" Of the 141 subjects dosed with debrisoquin, 10 proved to be poor oxidizers, and of the 143 subjects dosed with phenformin, 11 were poor oxidizers."( Dissociation of co-regulatory control of debrisoquin/phenformin and sparteine oxidation in Ghanaians.
Eichelbaum, M; Idle, JR; Oates, NS; Smith, RL; Woolhouse, NM, 1985
)
0.73
" The daily dosage of phenformin and metformin was increased at weekly intervals up to 300 mg."( Weight-reducing effect of diguanides in obese non-diabetic women.
Duncan, LJ; MacCuish, AC; Marshall, A; Munro, JF; Wilson, EM, 1969
)
0.57
" Although the urinary excretion of unchanged phenformin was greater in PM between 2 and 24 hr after dosing than in EM, excretion of 4-hydroxy-phenformin could not be detected in most samples collected from PM but was present in every sample from EM."( Influence of oxidation polymorphism on phenformin kinetics and dynamics.
Idle, JR; Oates, NS; Shah, RR; Smith, RL, 1983
)
0.79
"In this article a new non-model-based significance test for detecting dose-response relationship with the incorporation of historical control data is proposed."( On the use of historical control information for trend test in carcinogenesis.
Guo, J; Ma, Y; Shi, NZ; Tang, ML, 2002
)
0.31
"5 hour after dosing were 21."( Liver uptake of biguanides in rats.
Kitamura, A; Komuro, S; Sogame, Y; Yabuki, M, 2011
)
0.37
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (3)

RoleDescription
antineoplastic agentA substance that inhibits or prevents the proliferation of neoplasms.
geroprotectorAny compound that supports healthy aging, slows the biological aging process, or extends lifespan.
hypoglycemic agentA drug which lowers the blood glucose level.
[role information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Drug Classes (1)

ClassDescription
biguanidesA class of oral hypoglycemic drugs used for diabetes mellitus or prediabetes treatment. They have a structure based on the 2-carbamimidoylguanidine skeleton.
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Protein Targets (24)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
USP1 protein, partialHomo sapiens (human)Potency39.81070.031637.5844354.8130AID504865
hypoxia-inducible factor 1, alpha subunit (basic helix-loop-helix transcription factor)Homo sapiens (human)Potency6.30960.00137.762544.6684AID914; AID915
thyroid stimulating hormone receptorHomo sapiens (human)Potency7.94330.001318.074339.8107AID926; AID938
EWS/FLI fusion proteinHomo sapiens (human)Potency16.99560.001310.157742.8575AID1259252; AID1259253; AID1259255; AID1259256
cytochrome P450 2D6 isoform 1Homo sapiens (human)Potency10.00000.00207.533739.8107AID891
nuclear factor erythroid 2-related factor 2 isoform 1Homo sapiens (human)Potency38.57080.000627.21521,122.0200AID651741
peripheral myelin protein 22Rattus norvegicus (Norway rat)Potency13.78940.005612.367736.1254AID624032
lamin isoform A-delta10Homo sapiens (human)Potency0.39810.891312.067628.1838AID1487
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Solute carrier family 22 member 2Homo sapiens (human)IC50 (µMol)65.00000.40003.10009.7000AID680369
Solute carrier family 22 member 1 Homo sapiens (human)IC50 (µMol)10.00000.21005.553710.0000AID680364
ATP-binding cassette sub-family C member 3Homo sapiens (human)IC50 (µMol)133.00000.63154.45319.3000AID1473740
Multidrug resistance-associated protein 4Homo sapiens (human)IC50 (µMol)133.00000.20005.677410.0000AID1473741
Carbonic anhydrase 12Homo sapiens (human)Ki50.00000.00021.10439.9000AID1425990
Bile salt export pumpHomo sapiens (human)IC50 (µMol)422.66670.11007.190310.0000AID1443980; AID1449628; AID1473738
Dihydrofolate reductaseHomo sapiens (human)Ki140.00000.00000.37564.9000AID1660990
Carbonic anhydrase 1Homo sapiens (human)Ki50.00000.00001.372610.0000AID1425987
Carbonic anhydrase 2Homo sapiens (human)Ki50.00000.00000.72369.9200AID1425988
Cytochrome P450 2D26Rattus norvegicus (Norway rat)IC50 (µMol)45.40000.09402.16285.6000AID54564
Cytochrome P450 2D6Homo sapiens (human)IC50 (µMol)36.20000.00002.015110.0000AID54564; AID54570
Carbonic anhydrase 9Homo sapiens (human)Ki50.00000.00010.78749.9000AID1425989
Cytochrome P450 2D4Rattus norvegicus (Norway rat)IC50 (µMol)833.00001.70001.70001.7000AID54566
Canalicular multispecific organic anion transporter 1Homo sapiens (human)IC50 (µMol)133.00002.41006.343310.0000AID1473739
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Other Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Solute carrier family 22 member 1Rattus norvegicus (Norway rat)Km15.60000.27005.695010.0000AID679316
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (119)

Processvia Protein(s)Taxonomy
activation of cysteine-type endopeptidase activity involved in apoptotic processSolute carrier family 22 member 2Homo sapiens (human)
positive regulation of gene expressionSolute carrier family 22 member 2Homo sapiens (human)
organic cation transportSolute carrier family 22 member 2Homo sapiens (human)
monoatomic cation transportSolute carrier family 22 member 2Homo sapiens (human)
neurotransmitter transportSolute carrier family 22 member 2Homo sapiens (human)
serotonin transportSolute carrier family 22 member 2Homo sapiens (human)
body fluid secretionSolute carrier family 22 member 2Homo sapiens (human)
organic cation transportSolute carrier family 22 member 2Homo sapiens (human)
quaternary ammonium group transportSolute carrier family 22 member 2Homo sapiens (human)
prostaglandin transportSolute carrier family 22 member 2Homo sapiens (human)
amine transportSolute carrier family 22 member 2Homo sapiens (human)
putrescine transportSolute carrier family 22 member 2Homo sapiens (human)
spermidine transportSolute carrier family 22 member 2Homo sapiens (human)
acetylcholine transportSolute carrier family 22 member 2Homo sapiens (human)
choline transportSolute carrier family 22 member 2Homo sapiens (human)
dopamine transportSolute carrier family 22 member 2Homo sapiens (human)
norepinephrine transportSolute carrier family 22 member 2Homo sapiens (human)
xenobiotic transportSolute carrier family 22 member 2Homo sapiens (human)
epinephrine transportSolute carrier family 22 member 2Homo sapiens (human)
histamine transportSolute carrier family 22 member 2Homo sapiens (human)
serotonin uptakeSolute carrier family 22 member 2Homo sapiens (human)
histamine uptakeSolute carrier family 22 member 2Homo sapiens (human)
norepinephrine uptakeSolute carrier family 22 member 2Homo sapiens (human)
thiamine transmembrane transportSolute carrier family 22 member 2Homo sapiens (human)
purine-containing compound transmembrane transportSolute carrier family 22 member 2Homo sapiens (human)
amino acid import across plasma membraneSolute carrier family 22 member 2Homo sapiens (human)
dopamine uptakeSolute carrier family 22 member 2Homo sapiens (human)
L-arginine import across plasma membraneSolute carrier family 22 member 2Homo sapiens (human)
export across plasma membraneSolute carrier family 22 member 2Homo sapiens (human)
transport across blood-brain barrierSolute carrier family 22 member 2Homo sapiens (human)
L-alpha-amino acid transmembrane transportSolute carrier family 22 member 2Homo sapiens (human)
spermidine transmembrane transportSolute carrier family 22 member 2Homo sapiens (human)
L-arginine transmembrane transportSolute carrier family 22 member 2Homo sapiens (human)
cellular detoxificationSolute carrier family 22 member 2Homo sapiens (human)
xenobiotic transport across blood-brain barrierSolute carrier family 22 member 2Homo sapiens (human)
xenobiotic metabolic processSolute carrier family 22 member 1 Homo sapiens (human)
neurotransmitter transportSolute carrier family 22 member 1 Homo sapiens (human)
serotonin transportSolute carrier family 22 member 1 Homo sapiens (human)
establishment or maintenance of transmembrane electrochemical gradientSolute carrier family 22 member 1 Homo sapiens (human)
organic cation transportSolute carrier family 22 member 1 Homo sapiens (human)
quaternary ammonium group transportSolute carrier family 22 member 1 Homo sapiens (human)
prostaglandin transportSolute carrier family 22 member 1 Homo sapiens (human)
monoamine transportSolute carrier family 22 member 1 Homo sapiens (human)
putrescine transportSolute carrier family 22 member 1 Homo sapiens (human)
spermidine transportSolute carrier family 22 member 1 Homo sapiens (human)
acetylcholine transportSolute carrier family 22 member 1 Homo sapiens (human)
dopamine transportSolute carrier family 22 member 1 Homo sapiens (human)
norepinephrine transportSolute carrier family 22 member 1 Homo sapiens (human)
thiamine transportSolute carrier family 22 member 1 Homo sapiens (human)
xenobiotic transportSolute carrier family 22 member 1 Homo sapiens (human)
epinephrine transportSolute carrier family 22 member 1 Homo sapiens (human)
serotonin uptakeSolute carrier family 22 member 1 Homo sapiens (human)
norepinephrine uptakeSolute carrier family 22 member 1 Homo sapiens (human)
thiamine transmembrane transportSolute carrier family 22 member 1 Homo sapiens (human)
metanephric proximal tubule developmentSolute carrier family 22 member 1 Homo sapiens (human)
purine-containing compound transmembrane transportSolute carrier family 22 member 1 Homo sapiens (human)
dopamine uptakeSolute carrier family 22 member 1 Homo sapiens (human)
monoatomic cation transmembrane transportSolute carrier family 22 member 1 Homo sapiens (human)
transport across blood-brain barrierSolute carrier family 22 member 1 Homo sapiens (human)
(R)-carnitine transmembrane transportSolute carrier family 22 member 1 Homo sapiens (human)
acyl carnitine transmembrane transportSolute carrier family 22 member 1 Homo sapiens (human)
spermidine transmembrane transportSolute carrier family 22 member 1 Homo sapiens (human)
cellular detoxificationSolute carrier family 22 member 1 Homo sapiens (human)
xenobiotic transport across blood-brain barrierSolute carrier family 22 member 1 Homo sapiens (human)
xenobiotic metabolic processATP-binding cassette sub-family C member 3Homo sapiens (human)
xenobiotic transmembrane transportATP-binding cassette sub-family C member 3Homo sapiens (human)
bile acid and bile salt transportATP-binding cassette sub-family C member 3Homo sapiens (human)
glucuronoside transportATP-binding cassette sub-family C member 3Homo sapiens (human)
xenobiotic transportATP-binding cassette sub-family C member 3Homo sapiens (human)
transmembrane transportATP-binding cassette sub-family C member 3Homo sapiens (human)
leukotriene transportATP-binding cassette sub-family C member 3Homo sapiens (human)
monoatomic anion transmembrane transportATP-binding cassette sub-family C member 3Homo sapiens (human)
transport across blood-brain barrierATP-binding cassette sub-family C member 3Homo sapiens (human)
prostaglandin secretionMultidrug resistance-associated protein 4Homo sapiens (human)
cilium assemblyMultidrug resistance-associated protein 4Homo sapiens (human)
platelet degranulationMultidrug resistance-associated protein 4Homo sapiens (human)
xenobiotic metabolic processMultidrug resistance-associated protein 4Homo sapiens (human)
xenobiotic transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
bile acid and bile salt transportMultidrug resistance-associated protein 4Homo sapiens (human)
prostaglandin transportMultidrug resistance-associated protein 4Homo sapiens (human)
urate transportMultidrug resistance-associated protein 4Homo sapiens (human)
glutathione transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
cAMP transportMultidrug resistance-associated protein 4Homo sapiens (human)
leukotriene transportMultidrug resistance-associated protein 4Homo sapiens (human)
monoatomic anion transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
export across plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
transport across blood-brain barrierMultidrug resistance-associated protein 4Homo sapiens (human)
guanine nucleotide transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
estrous cycleCarbonic anhydrase 12Homo sapiens (human)
chloride ion homeostasisCarbonic anhydrase 12Homo sapiens (human)
one-carbon metabolic processCarbonic anhydrase 12Homo sapiens (human)
fatty acid metabolic processBile salt export pumpHomo sapiens (human)
bile acid biosynthetic processBile salt export pumpHomo sapiens (human)
xenobiotic metabolic processBile salt export pumpHomo sapiens (human)
xenobiotic transmembrane transportBile salt export pumpHomo sapiens (human)
response to oxidative stressBile salt export pumpHomo sapiens (human)
bile acid metabolic processBile salt export pumpHomo sapiens (human)
response to organic cyclic compoundBile salt export pumpHomo sapiens (human)
bile acid and bile salt transportBile salt export pumpHomo sapiens (human)
canalicular bile acid transportBile salt export pumpHomo sapiens (human)
protein ubiquitinationBile salt export pumpHomo sapiens (human)
regulation of fatty acid beta-oxidationBile salt export pumpHomo sapiens (human)
carbohydrate transmembrane transportBile salt export pumpHomo sapiens (human)
bile acid signaling pathwayBile salt export pumpHomo sapiens (human)
cholesterol homeostasisBile salt export pumpHomo sapiens (human)
response to estrogenBile salt export pumpHomo sapiens (human)
response to ethanolBile salt export pumpHomo sapiens (human)
xenobiotic export from cellBile salt export pumpHomo sapiens (human)
lipid homeostasisBile salt export pumpHomo sapiens (human)
phospholipid homeostasisBile salt export pumpHomo sapiens (human)
positive regulation of bile acid secretionBile salt export pumpHomo sapiens (human)
regulation of bile acid metabolic processBile salt export pumpHomo sapiens (human)
transmembrane transportBile salt export pumpHomo sapiens (human)
tetrahydrobiopterin biosynthetic processDihydrofolate reductaseHomo sapiens (human)
one-carbon metabolic processDihydrofolate reductaseHomo sapiens (human)
negative regulation of translationDihydrofolate reductaseHomo sapiens (human)
axon regenerationDihydrofolate reductaseHomo sapiens (human)
response to methotrexateDihydrofolate reductaseHomo sapiens (human)
dihydrofolate metabolic processDihydrofolate reductaseHomo sapiens (human)
tetrahydrofolate metabolic processDihydrofolate reductaseHomo sapiens (human)
tetrahydrofolate biosynthetic processDihydrofolate reductaseHomo sapiens (human)
folic acid metabolic processDihydrofolate reductaseHomo sapiens (human)
positive regulation of nitric-oxide synthase activityDihydrofolate reductaseHomo sapiens (human)
regulation of removal of superoxide radicalsDihydrofolate reductaseHomo sapiens (human)
one-carbon metabolic processCarbonic anhydrase 1Homo sapiens (human)
morphogenesis of an epitheliumCarbonic anhydrase 2Homo sapiens (human)
positive regulation of synaptic transmission, GABAergicCarbonic anhydrase 2Homo sapiens (human)
positive regulation of cellular pH reductionCarbonic anhydrase 2Homo sapiens (human)
angiotensin-activated signaling pathwayCarbonic anhydrase 2Homo sapiens (human)
regulation of monoatomic anion transportCarbonic anhydrase 2Homo sapiens (human)
secretionCarbonic anhydrase 2Homo sapiens (human)
regulation of intracellular pHCarbonic anhydrase 2Homo sapiens (human)
neuron cellular homeostasisCarbonic anhydrase 2Homo sapiens (human)
positive regulation of dipeptide transmembrane transportCarbonic anhydrase 2Homo sapiens (human)
regulation of chloride transportCarbonic anhydrase 2Homo sapiens (human)
carbon dioxide transportCarbonic anhydrase 2Homo sapiens (human)
one-carbon metabolic processCarbonic anhydrase 2Homo sapiens (human)
xenobiotic metabolic processCytochrome P450 2D6Homo sapiens (human)
steroid metabolic processCytochrome P450 2D6Homo sapiens (human)
cholesterol metabolic processCytochrome P450 2D6Homo sapiens (human)
estrogen metabolic processCytochrome P450 2D6Homo sapiens (human)
coumarin metabolic processCytochrome P450 2D6Homo sapiens (human)
alkaloid metabolic processCytochrome P450 2D6Homo sapiens (human)
alkaloid catabolic processCytochrome P450 2D6Homo sapiens (human)
monoterpenoid metabolic processCytochrome P450 2D6Homo sapiens (human)
isoquinoline alkaloid metabolic processCytochrome P450 2D6Homo sapiens (human)
xenobiotic catabolic processCytochrome P450 2D6Homo sapiens (human)
retinol metabolic processCytochrome P450 2D6Homo sapiens (human)
long-chain fatty acid biosynthetic processCytochrome P450 2D6Homo sapiens (human)
negative regulation of bindingCytochrome P450 2D6Homo sapiens (human)
oxidative demethylationCytochrome P450 2D6Homo sapiens (human)
negative regulation of cellular organofluorine metabolic processCytochrome P450 2D6Homo sapiens (human)
arachidonic acid metabolic processCytochrome P450 2D6Homo sapiens (human)
response to hypoxiaCarbonic anhydrase 9Homo sapiens (human)
morphogenesis of an epitheliumCarbonic anhydrase 9Homo sapiens (human)
response to xenobiotic stimulusCarbonic anhydrase 9Homo sapiens (human)
response to testosteroneCarbonic anhydrase 9Homo sapiens (human)
secretionCarbonic anhydrase 9Homo sapiens (human)
one-carbon metabolic processCarbonic anhydrase 9Homo sapiens (human)
xenobiotic metabolic processCanalicular multispecific organic anion transporter 1Homo sapiens (human)
xenobiotic transmembrane transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
negative regulation of gene expressionCanalicular multispecific organic anion transporter 1Homo sapiens (human)
bile acid and bile salt transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
bilirubin transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
heme catabolic processCanalicular multispecific organic anion transporter 1Homo sapiens (human)
xenobiotic export from cellCanalicular multispecific organic anion transporter 1Homo sapiens (human)
transmembrane transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
transepithelial transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
leukotriene transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
monoatomic anion transmembrane transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
transport across blood-brain barrierCanalicular multispecific organic anion transporter 1Homo sapiens (human)
xenobiotic transport across blood-brain barrierCanalicular multispecific organic anion transporter 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (64)

Processvia Protein(s)Taxonomy
amine transmembrane transporter activitySolute carrier family 22 member 2Homo sapiens (human)
acetylcholine transmembrane transporter activitySolute carrier family 22 member 2Homo sapiens (human)
neurotransmitter transmembrane transporter activitySolute carrier family 22 member 2Homo sapiens (human)
monoamine transmembrane transporter activitySolute carrier family 22 member 2Homo sapiens (human)
organic anion transmembrane transporter activitySolute carrier family 22 member 2Homo sapiens (human)
organic cation transmembrane transporter activitySolute carrier family 22 member 2Homo sapiens (human)
prostaglandin transmembrane transporter activitySolute carrier family 22 member 2Homo sapiens (human)
L-amino acid transmembrane transporter activitySolute carrier family 22 member 2Homo sapiens (human)
pyrimidine nucleoside transmembrane transporter activitySolute carrier family 22 member 2Homo sapiens (human)
choline transmembrane transporter activitySolute carrier family 22 member 2Homo sapiens (human)
thiamine transmembrane transporter activitySolute carrier family 22 member 2Homo sapiens (human)
putrescine transmembrane transporter activitySolute carrier family 22 member 2Homo sapiens (human)
efflux transmembrane transporter activitySolute carrier family 22 member 2Homo sapiens (human)
spermidine transmembrane transporter activitySolute carrier family 22 member 2Homo sapiens (human)
quaternary ammonium group transmembrane transporter activitySolute carrier family 22 member 2Homo sapiens (human)
toxin transmembrane transporter activitySolute carrier family 22 member 2Homo sapiens (human)
xenobiotic transmembrane transporter activitySolute carrier family 22 member 2Homo sapiens (human)
L-arginine transmembrane transporter activitySolute carrier family 22 member 2Homo sapiens (human)
acetylcholine transmembrane transporter activitySolute carrier family 22 member 1 Homo sapiens (human)
neurotransmitter transmembrane transporter activitySolute carrier family 22 member 1 Homo sapiens (human)
dopamine:sodium symporter activitySolute carrier family 22 member 1 Homo sapiens (human)
norepinephrine:sodium symporter activitySolute carrier family 22 member 1 Homo sapiens (human)
protein bindingSolute carrier family 22 member 1 Homo sapiens (human)
monoamine transmembrane transporter activitySolute carrier family 22 member 1 Homo sapiens (human)
secondary active organic cation transmembrane transporter activitySolute carrier family 22 member 1 Homo sapiens (human)
organic anion transmembrane transporter activitySolute carrier family 22 member 1 Homo sapiens (human)
organic cation transmembrane transporter activitySolute carrier family 22 member 1 Homo sapiens (human)
prostaglandin transmembrane transporter activitySolute carrier family 22 member 1 Homo sapiens (human)
pyrimidine nucleoside transmembrane transporter activitySolute carrier family 22 member 1 Homo sapiens (human)
thiamine transmembrane transporter activitySolute carrier family 22 member 1 Homo sapiens (human)
putrescine transmembrane transporter activitySolute carrier family 22 member 1 Homo sapiens (human)
spermidine transmembrane transporter activitySolute carrier family 22 member 1 Homo sapiens (human)
quaternary ammonium group transmembrane transporter activitySolute carrier family 22 member 1 Homo sapiens (human)
toxin transmembrane transporter activitySolute carrier family 22 member 1 Homo sapiens (human)
identical protein bindingSolute carrier family 22 member 1 Homo sapiens (human)
xenobiotic transmembrane transporter activitySolute carrier family 22 member 1 Homo sapiens (human)
(R)-carnitine transmembrane transporter activitySolute carrier family 22 member 1 Homo sapiens (human)
ATP bindingATP-binding cassette sub-family C member 3Homo sapiens (human)
ABC-type xenobiotic transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
glucuronoside transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ABC-type glutathione S-conjugate transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ABC-type bile acid transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ATP hydrolysis activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ATPase-coupled transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
xenobiotic transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ATPase-coupled inorganic anion transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
icosanoid transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ABC-type transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
guanine nucleotide transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
protein bindingMultidrug resistance-associated protein 4Homo sapiens (human)
ATP bindingMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type xenobiotic transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
prostaglandin transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
urate transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
purine nucleotide transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type glutathione S-conjugate transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type bile acid transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
efflux transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
15-hydroxyprostaglandin dehydrogenase (NAD+) activityMultidrug resistance-associated protein 4Homo sapiens (human)
ATP hydrolysis activityMultidrug resistance-associated protein 4Homo sapiens (human)
glutathione transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ATPase-coupled transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
xenobiotic transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ATPase-coupled inorganic anion transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
zinc ion bindingCarbonic anhydrase 12Homo sapiens (human)
carbonate dehydratase activityCarbonic anhydrase 12Homo sapiens (human)
protein bindingBile salt export pumpHomo sapiens (human)
ATP bindingBile salt export pumpHomo sapiens (human)
ABC-type xenobiotic transporter activityBile salt export pumpHomo sapiens (human)
bile acid transmembrane transporter activityBile salt export pumpHomo sapiens (human)
canalicular bile acid transmembrane transporter activityBile salt export pumpHomo sapiens (human)
carbohydrate transmembrane transporter activityBile salt export pumpHomo sapiens (human)
ABC-type bile acid transporter activityBile salt export pumpHomo sapiens (human)
ATP hydrolysis activityBile salt export pumpHomo sapiens (human)
mRNA regulatory element binding translation repressor activityDihydrofolate reductaseHomo sapiens (human)
mRNA bindingDihydrofolate reductaseHomo sapiens (human)
dihydrofolate reductase activityDihydrofolate reductaseHomo sapiens (human)
folic acid bindingDihydrofolate reductaseHomo sapiens (human)
NADPH bindingDihydrofolate reductaseHomo sapiens (human)
sequence-specific mRNA bindingDihydrofolate reductaseHomo sapiens (human)
NADP bindingDihydrofolate reductaseHomo sapiens (human)
arylesterase activityCarbonic anhydrase 1Homo sapiens (human)
carbonate dehydratase activityCarbonic anhydrase 1Homo sapiens (human)
protein bindingCarbonic anhydrase 1Homo sapiens (human)
zinc ion bindingCarbonic anhydrase 1Homo sapiens (human)
hydro-lyase activityCarbonic anhydrase 1Homo sapiens (human)
cyanamide hydratase activityCarbonic anhydrase 1Homo sapiens (human)
arylesterase activityCarbonic anhydrase 2Homo sapiens (human)
carbonate dehydratase activityCarbonic anhydrase 2Homo sapiens (human)
protein bindingCarbonic anhydrase 2Homo sapiens (human)
zinc ion bindingCarbonic anhydrase 2Homo sapiens (human)
cyanamide hydratase activityCarbonic anhydrase 2Homo sapiens (human)
monooxygenase activityCytochrome P450 2D6Homo sapiens (human)
iron ion bindingCytochrome P450 2D6Homo sapiens (human)
oxidoreductase activityCytochrome P450 2D6Homo sapiens (human)
oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygenCytochrome P450 2D6Homo sapiens (human)
heme bindingCytochrome P450 2D6Homo sapiens (human)
anandamide 8,9 epoxidase activityCytochrome P450 2D6Homo sapiens (human)
anandamide 11,12 epoxidase activityCytochrome P450 2D6Homo sapiens (human)
anandamide 14,15 epoxidase activityCytochrome P450 2D6Homo sapiens (human)
carbonate dehydratase activityCarbonic anhydrase 9Homo sapiens (human)
protein bindingCarbonic anhydrase 9Homo sapiens (human)
zinc ion bindingCarbonic anhydrase 9Homo sapiens (human)
molecular function activator activityCarbonic anhydrase 9Homo sapiens (human)
protein bindingCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ATP bindingCanalicular multispecific organic anion transporter 1Homo sapiens (human)
organic anion transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ABC-type xenobiotic transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
bilirubin transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ABC-type glutathione S-conjugate transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ATP hydrolysis activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ATPase-coupled transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
xenobiotic transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ATPase-coupled inorganic anion transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ABC-type transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (28)

Processvia Protein(s)Taxonomy
plasma membraneSolute carrier family 22 member 2Homo sapiens (human)
basal plasma membraneSolute carrier family 22 member 2Homo sapiens (human)
membraneSolute carrier family 22 member 2Homo sapiens (human)
basolateral plasma membraneSolute carrier family 22 member 2Homo sapiens (human)
apical plasma membraneSolute carrier family 22 member 2Homo sapiens (human)
extracellular exosomeSolute carrier family 22 member 2Homo sapiens (human)
presynapseSolute carrier family 22 member 2Homo sapiens (human)
plasma membraneSolute carrier family 22 member 1 Homo sapiens (human)
basal plasma membraneSolute carrier family 22 member 1 Homo sapiens (human)
membraneSolute carrier family 22 member 1 Homo sapiens (human)
basolateral plasma membraneSolute carrier family 22 member 1 Homo sapiens (human)
apical plasma membraneSolute carrier family 22 member 1 Homo sapiens (human)
lateral plasma membraneSolute carrier family 22 member 1 Homo sapiens (human)
presynapseSolute carrier family 22 member 1 Homo sapiens (human)
plasma membraneATP-binding cassette sub-family C member 3Homo sapiens (human)
basal plasma membraneATP-binding cassette sub-family C member 3Homo sapiens (human)
basolateral plasma membraneATP-binding cassette sub-family C member 3Homo sapiens (human)
membraneATP-binding cassette sub-family C member 3Homo sapiens (human)
nucleolusMultidrug resistance-associated protein 4Homo sapiens (human)
Golgi apparatusMultidrug resistance-associated protein 4Homo sapiens (human)
plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
membraneMultidrug resistance-associated protein 4Homo sapiens (human)
basolateral plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
apical plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
platelet dense granule membraneMultidrug resistance-associated protein 4Homo sapiens (human)
external side of apical plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
plasma membraneCarbonic anhydrase 12Homo sapiens (human)
membraneCarbonic anhydrase 12Homo sapiens (human)
basolateral plasma membraneCarbonic anhydrase 12Homo sapiens (human)
apical plasma membraneCarbonic anhydrase 12Homo sapiens (human)
plasma membraneCarbonic anhydrase 12Homo sapiens (human)
basolateral plasma membraneBile salt export pumpHomo sapiens (human)
Golgi membraneBile salt export pumpHomo sapiens (human)
endosomeBile salt export pumpHomo sapiens (human)
plasma membraneBile salt export pumpHomo sapiens (human)
cell surfaceBile salt export pumpHomo sapiens (human)
apical plasma membraneBile salt export pumpHomo sapiens (human)
intercellular canaliculusBile salt export pumpHomo sapiens (human)
intracellular canaliculusBile salt export pumpHomo sapiens (human)
recycling endosomeBile salt export pumpHomo sapiens (human)
recycling endosome membraneBile salt export pumpHomo sapiens (human)
extracellular exosomeBile salt export pumpHomo sapiens (human)
membraneBile salt export pumpHomo sapiens (human)
mitochondrionDihydrofolate reductaseHomo sapiens (human)
cytosolDihydrofolate reductaseHomo sapiens (human)
mitochondrionDihydrofolate reductaseHomo sapiens (human)
cytosolCarbonic anhydrase 1Homo sapiens (human)
extracellular exosomeCarbonic anhydrase 1Homo sapiens (human)
cytoplasmCarbonic anhydrase 2Homo sapiens (human)
cytosolCarbonic anhydrase 2Homo sapiens (human)
plasma membraneCarbonic anhydrase 2Homo sapiens (human)
myelin sheathCarbonic anhydrase 2Homo sapiens (human)
apical part of cellCarbonic anhydrase 2Homo sapiens (human)
extracellular exosomeCarbonic anhydrase 2Homo sapiens (human)
cytoplasmCarbonic anhydrase 2Homo sapiens (human)
plasma membraneCarbonic anhydrase 2Homo sapiens (human)
apical part of cellCarbonic anhydrase 2Homo sapiens (human)
mitochondrionCytochrome P450 2D6Homo sapiens (human)
endoplasmic reticulumCytochrome P450 2D6Homo sapiens (human)
endoplasmic reticulum membraneCytochrome P450 2D6Homo sapiens (human)
cytoplasmCytochrome P450 2D6Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 2D6Homo sapiens (human)
nucleolusCarbonic anhydrase 9Homo sapiens (human)
plasma membraneCarbonic anhydrase 9Homo sapiens (human)
membraneCarbonic anhydrase 9Homo sapiens (human)
basolateral plasma membraneCarbonic anhydrase 9Homo sapiens (human)
microvillus membraneCarbonic anhydrase 9Homo sapiens (human)
plasma membraneCarbonic anhydrase 9Homo sapiens (human)
plasma membraneCanalicular multispecific organic anion transporter 1Homo sapiens (human)
cell surfaceCanalicular multispecific organic anion transporter 1Homo sapiens (human)
apical plasma membraneCanalicular multispecific organic anion transporter 1Homo sapiens (human)
intercellular canaliculusCanalicular multispecific organic anion transporter 1Homo sapiens (human)
apical plasma membraneCanalicular multispecific organic anion transporter 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (153)

Assay IDTitleYearJournalArticle
AID504749qHTS profiling for inhibitors of Plasmodium falciparum proliferation2011Science (New York, N.Y.), Aug-05, Volume: 333, Issue:6043
Chemical genomic profiling for antimalarial therapies, response signatures, and molecular targets.
AID352973Antiobesity activity in lean normal BALB/c mouse assessed as change in average daily weight at 0.62 mmol/kg/day administered through diet for 7 days relative to time-matched control2009Journal of medicinal chemistry, Jun-11, Volume: 52, Issue:11
Benzylguanidines and other galegine analogues inducing weight loss in mice.
AID182470Percent inhibition of glucose rise, following 150 mg/kg oral dose in fasted nondiabetic rats1989Journal of medicinal chemistry, Sep, Volume: 32, Issue:9
Carbohydrate biguanides as potential hypoglycemic agents.
AID352976Antidiabetic activity in lean normal BALB/c mouse assessed as effect on blood lactate level at 0.72 mmol/kg/day administered through diet for 7 days relative to time-matched control2009Journal of medicinal chemistry, Jun-11, Volume: 52, Issue:11
Benzylguanidines and other galegine analogues inducing weight loss in mice.
AID699540Inhibition of human liver OATP1B3 expressed in HEK293 Flp-In cells assessed as reduction in [3H]E17-betaG uptake at 20 uM incubated for 5 mins by scintillation counting2012Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
Classification of inhibitors of hepatic organic anion transporting polypeptides (OATPs): influence of protein expression on drug-drug interactions.
AID404304Effect on human MRP2-mediated estradiol-17-beta-glucuronide transport in Sf9 cells inverted membrane vesicles relative to control2008Journal of medicinal chemistry, Jun-12, Volume: 51, Issue:11
Prediction and identification of drug interactions with the human ATP-binding cassette transporter multidrug-resistance associated protein 2 (MRP2; ABCC2).
AID179728Rise in the blood glucose level after 0 min following 100 mg/kg oral dose in fasted nondiabetic rats1989Journal of medicinal chemistry, Sep, Volume: 32, Issue:9
Carbohydrate biguanides as potential hypoglycemic agents.
AID1894460Synergistic antifungal activity against Candida glabrata assessed as fractional inhibitory concentration index in presence of fluconazole incubated for 18 hrs by checkerboard assay2021European journal of medicinal chemistry, Apr-15, Volume: 216Antimicrobial drugs bearing guanidine moieties: A review.
AID496819Antimicrobial activity against Plasmodium falciparum2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID771316Cellular uptake in human HEK293 cells assessed as human OCT2-mediated drug transport at 2.5 uM after 4 mins by LC-MS/MS analysis2013Journal of medicinal chemistry, Sep-26, Volume: 56, Issue:18
Identification of novel substrates and structure-activity relationship of cellular uptake mediated by human organic cation transporters 1 and 2.
AID679316TP_TRANSPORTER: uptake in OCT1-expressing CHO cells2002The Journal of pharmacology and experimental therapeutics, Aug, Volume: 302, Issue:2
Involvement of organic cation transporter 1 in hepatic and intestinal distribution of metformin.
AID197698In vivo increase of plasma insulin in normal rats at a hypoglycemic dose of 2.0 mmol/kg1983Journal of medicinal chemistry, Jul, Volume: 26, Issue:7
Sulfonyliminoimidazolidines. A new class of oral hypoglycemic agents. 2. Mode of action and X-ray structure of 1-[[p-[2-(crotonylamino)ethyl]phenyl]sulfonyl]-3-cyclohexyl-2-iminoimidazolidine.
AID54570Inhibition of MAMC O-dealkylation mediated by human Cytochrome P450 2D6 expressed in human lymphoblastoid cell line2003Journal of medicinal chemistry, Jan-02, Volume: 46, Issue:1
Homology modeling of rat and human cytochrome P450 2D (CYP2D) isoforms and computational rationalization of experimental ligand-binding specificities.
AID1079945Animal toxicity known. [column 'TOXIC' in source]
AID1079934Highest frequency of acute liver toxicity observed during clinical trials, expressed as a percentage. [column '% AIGUE' in source]
AID1426025Effect on mitochondrial respiration in carbonic anhydrase 9 knockdown human HCT116 cells assessed as reduction in oxygen consumption rate at 0.5 mM after 24 hrs under hypoxic condition by Western blot analysis2017European journal of medicinal chemistry, Feb-15, Volume: 127New approach of delivering cytotoxic drugs towards CAIX expressing cells: A concept of dual-target drugs.
AID1079948Times to onset, minimal and maximal, observed in the indexed observations. [column 'DELAI' in source]
AID179886Rise in the blood glucose level at 150 mg/kg oral dose in fasted nondiabetic rats1989Journal of medicinal chemistry, Sep, Volume: 32, Issue:9
Carbohydrate biguanides as potential hypoglycemic agents.
AID188899Percent reduction in blood glucose after perorally administration of compound at 120 mg/kg in non-glucose-primed rat1981Journal of medicinal chemistry, Dec, Volume: 24, Issue:12
Chemistry and hypoglycemic activity of benzimidoylpyrazoles.
AID1124005Hypoglycemic activity in alloxan-induced diabetic albino mouse assessed as decrease in blood glucose level at 1 mmol/kg, po administered 6 days after alloxan injection measured after 1 to 3 hrs by automated glucose oxidase method relative to control1979Journal of medicinal chemistry, Mar, Volume: 22, Issue:3
Preparation and antidiabetic activity of some sulfonylurea derivatives of 3,5-disubstituted pyrazoles.
AID1079947Comments (NB not yet translated). [column 'COMMENTAIRES' in source]
AID352977Antidiabetic activity in lean normal BALB/c mouse assessed as effect on blood lactate level at 0.54 mmol/kg/day administered through diet for 7 days relative to time-matched control2009Journal of medicinal chemistry, Jun-11, Volume: 52, Issue:11
Benzylguanidines and other galegine analogues inducing weight loss in mice.
AID179884Rise in the blood glucose level at 10 mg/kg oral dose in fasted nondiabetic rats1989Journal of medicinal chemistry, Sep, Volume: 32, Issue:9
Carbohydrate biguanides as potential hypoglycemic agents.
AID352962Antiobesity activity in lean normal BALB/c mouse assessed as change in average daily food intake at 0.62 mmol/kg/day administered through diet for 7 days relative to time-matched control2009Journal of medicinal chemistry, Jun-11, Volume: 52, Issue:11
Benzylguanidines and other galegine analogues inducing weight loss in mice.
AID771315Cellular uptake in human HEK293 cells assessed as human OCT1-mediated drug transport at 2.5 uM after 4 mins by LC-MS/MS analysis relative to passive uptake2013Journal of medicinal chemistry, Sep-26, Volume: 56, Issue:18
Identification of novel substrates and structure-activity relationship of cellular uptake mediated by human organic cation transporters 1 and 2.
AID352938Antidiabetic activity in lean normal BALB/c mouse assessed as effect on blood lactate level at 0.57 mmol/kg/day administered through diet for 7 days relative to time-matched control2009Journal of medicinal chemistry, Jun-11, Volume: 52, Issue:11
Benzylguanidines and other galegine analogues inducing weight loss in mice.
AID184645Lethal dose required to produce 50% lethality in male and female carworth farms CF-1 strain mice weighing 16-25 g administered intraperitoneally1982Journal of medicinal chemistry, Apr, Volume: 25, Issue:4
Chemistry and hypoglycemic activity of N-[[(Dialkylamino)alkoxy]phenyl]benzamidines.
AID1124003Hypoglycemic activity in alloxan-induced diabetic albino mouse assessed as decrease in blood glucose level at 1 mmol/kg, po administered 6 days after alloxan injection measured after 2 to 4 hrs by automated glucose oxidase method relative to control1979Journal of medicinal chemistry, Mar, Volume: 22, Issue:3
Preparation and antidiabetic activity of some sulfonylurea derivatives of 3,5-disubstituted pyrazoles.
AID771314Cellular uptake in human HEK293 cells assessed as human OCT2-mediated drug transport at 2.5 uM after 4 mins by LC-MS/MS analysis relative to passive uptake2013Journal of medicinal chemistry, Sep-26, Volume: 56, Issue:18
Identification of novel substrates and structure-activity relationship of cellular uptake mediated by human organic cation transporters 1 and 2.
AID374712Metabolic stability in ob/ob mouse liver microsomes assessed as oxidative hydroxylation at 50 uM after 45 mins by HPLC-MS analysis2009Journal of medicinal chemistry, Jun-11, Volume: 52, Issue:11
Benzylguanidines and other galegine analogues inducing weight loss in mice.
AID179727Rise in the blood glucose level after 0 min following 10 mg/kg oral dose in fasted nondiabetic rats1989Journal of medicinal chemistry, Sep, Volume: 32, Issue:9
Carbohydrate biguanides as potential hypoglycemic agents.
AID1894461Synergistic antifungal activity against Candida glabrata assessed as fractional inhibitory concentration index in presence of voriconazole incubated for 18 hrs by checkerboard assay2021European journal of medicinal chemistry, Apr-15, Volume: 216Antimicrobial drugs bearing guanidine moieties: A review.
AID54564Inhibition of MAMC O-dealkylation mediated by rat Cytochrome P450 2D2 expressed in Saccharomyces cerevisiae2003Journal of medicinal chemistry, Jan-02, Volume: 46, Issue:1
Homology modeling of rat and human cytochrome P450 2D (CYP2D) isoforms and computational rationalization of experimental ligand-binding specificities.
AID193166In vitro inhibition of glucose oxidation determined in normal rats at a hypoglycemic dose of 2.0 mmol/kg1983Journal of medicinal chemistry, Jul, Volume: 26, Issue:7
Sulfonyliminoimidazolidines. A new class of oral hypoglycemic agents. 2. Mode of action and X-ray structure of 1-[[p-[2-(crotonylamino)ethyl]phenyl]sulfonyl]-3-cyclohexyl-2-iminoimidazolidine.
AID54565Inhibition of MAMC O-dealkylation mediated by rat Cytochrome P450 2D3 expressed in Saccharomyces cerevisiae2003Journal of medicinal chemistry, Jan-02, Volume: 46, Issue:1
Homology modeling of rat and human cytochrome P450 2D (CYP2D) isoforms and computational rationalization of experimental ligand-binding specificities.
AID1473740Inhibition of human MRP3 overexpressed in Sf9 insect cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 10 mins by membrane vesicle transport assay2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID126663Evaluated in normal, fasted monkey for the percentage reduction in blood glucose level after 5 hr as compared to pretreatment blood glucose values at a dose of 10 mg of free base / kg body weight administered orally1982Journal of medicinal chemistry, Apr, Volume: 25, Issue:4
Chemistry and hypoglycemic activity of N-[[(Dialkylamino)alkoxy]phenyl]benzamidines.
AID182468Percent inhibition of glucose rise, following 10 mg/kg oral dose in fasted nondiabetic rats1989Journal of medicinal chemistry, Sep, Volume: 32, Issue:9
Carbohydrate biguanides as potential hypoglycemic agents.
AID77195Evaluated in normal, fasted guinea pig for the percentage reduction in blood glucose level after 5 hr as compared to pretreatment blood glucose values at a dose of 25 mg of free base / kg body weight administered orally1982Journal of medicinal chemistry, Apr, Volume: 25, Issue:4
Chemistry and hypoglycemic activity of N-[[(Dialkylamino)alkoxy]phenyl]benzamidines.
AID134583Lethal dose after intraperitoneal administration in mouse1981Journal of medicinal chemistry, Dec, Volume: 24, Issue:12
Chemistry and hypoglycemic activity of benzimidoylpyrazoles.
AID176493Compound evaluated for hypoglycemic activity by lowering blood glucose in normal rats by 50% after oral administration; inactive(less than 10% blood sugar decrease)1983Journal of medicinal chemistry, Jul, Volume: 26, Issue:7
Sulfonyliminoimidazolidines. A new class of oral hypoglycemic agents. 1. 1-[[p-[2-(acylamino)ethyl]phenyl]sulfonyl]-2-iminoimidazolidines.
AID172905Percent change in blood glucose in normal rats at a hypoglycemic dose of 2.0 mmol/kg. against control1983Journal of medicinal chemistry, Jul, Volume: 26, Issue:7
Sulfonyliminoimidazolidines. A new class of oral hypoglycemic agents. 2. Mode of action and X-ray structure of 1-[[p-[2-(crotonylamino)ethyl]phenyl]sulfonyl]-3-cyclohexyl-2-iminoimidazolidine.
AID1894462Synergistic antifungal activity against Candida glabrata assessed as fractional inhibitory concentration index in presence of amphotericin incubated for 18 hrs by checkerboard assay2021European journal of medicinal chemistry, Apr-15, Volume: 216Antimicrobial drugs bearing guanidine moieties: A review.
AID1079937Severe hepatitis, defined as possibly life-threatening liver failure or through clinical observations. Value is number of references indexed. [column 'MASS' in source]
AID1079949Proposed mechanism(s) of liver damage. [column 'MEC' in source]
AID352936Toxicity in lean normal BALB/c mouse assessed as overt signs of behavioural changes at equimolar dose of 0.5 mmol/kg galegine administered daily through diet for 7 days2009Journal of medicinal chemistry, Jun-11, Volume: 52, Issue:11
Benzylguanidines and other galegine analogues inducing weight loss in mice.
AID1473738Inhibition of human BSEP overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-taurocholate in presence of ATP measured after 15 to 20 mins by membrane vesicle transport assay2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID352975Antidiabetic activity in lean normal BALB/c mouse assessed as effect on blood lactate level at 0.60 mmol/kg/day administered through diet for 7 days relative to time-matched control2009Journal of medicinal chemistry, Jun-11, Volume: 52, Issue:11
Benzylguanidines and other galegine analogues inducing weight loss in mice.
AID204499Evaluated for the plasma glucose level in 24 hr fasted Sprauge-Dawley rats at a dose of 200 mg/kg/day in four divided doses administered intraperitoneally1990Journal of medicinal chemistry, May, Volume: 33, Issue:5
Synthesis and antihyperglycemic activity of novel 5-(naphthalenylsulfonyl)-2,4-thiazolidinediones.
AID75532Hypoglycemic activity was given as differences between the mean changes in blood glucose concentration in control group and the treated group after a dose of 25 mg/kg, ip1985Journal of medicinal chemistry, Oct, Volume: 28, Issue:10
Synthesis and hypoglycemic activity of N-alkylated hydrazonopropionic acids.
AID54566Inhibition of MAMC O-dealkylation mediated by rat Cytochrome P450 2D4 expressed in Saccharomyces cerevisiae2003Journal of medicinal chemistry, Jan-02, Volume: 46, Issue:1
Homology modeling of rat and human cytochrome P450 2D (CYP2D) isoforms and computational rationalization of experimental ligand-binding specificities.
AID352957Hypoglycemic activity in lean normal BALB/c mouse assessed as blood glucose level at 0.62 mmol/kg/day administered through diet for 7 days relative to time-matched control2009Journal of medicinal chemistry, Jun-11, Volume: 52, Issue:11
Benzylguanidines and other galegine analogues inducing weight loss in mice.
AID771317Cellular uptake in human HEK293 cells assessed as human OCT1-mediated drug transport at 2.5 uM after 4 mins by LC-MS/MS analysis2013Journal of medicinal chemistry, Sep-26, Volume: 56, Issue:18
Identification of novel substrates and structure-activity relationship of cellular uptake mediated by human organic cation transporters 1 and 2.
AID173794Compound evaluated for hypoglycemic activity by lowering blood glucose in normal rats by 20% after oral administration; highest dose tested;inactive(less than 10% blood sugar decrease)1983Journal of medicinal chemistry, Jul, Volume: 26, Issue:7
Sulfonyliminoimidazolidines. A new class of oral hypoglycemic agents. 1. 1-[[p-[2-(acylamino)ethyl]phenyl]sulfonyl]-2-iminoimidazolidines.
AID179729Rise in the blood glucose level after 0 min following 150 mg/kg oral dose in fasted nondiabetic rats1989Journal of medicinal chemistry, Sep, Volume: 32, Issue:9
Carbohydrate biguanides as potential hypoglycemic agents.
AID352939Antidiabetic activity in lean normal BALB/c mouse assessed as effect on blood lactate level at 0.70 mmol/kg/day administered through diet for 7 days relative to time-matched control2009Journal of medicinal chemistry, Jun-11, Volume: 52, Issue:11
Benzylguanidines and other galegine analogues inducing weight loss in mice.
AID1079941Liver damage due to vascular disease: peliosis hepatitis, hepatic veno-occlusive disease, Budd-Chiari syndrome. Value is number of references indexed. [column 'VASC' in source]
AID680364TP_TRANSPORTER: inhibition of Cimetidine uptake (Cimetidine: 1 uM) in Xenopus laevis oocytes2002Pharmaceutical research, Aug, Volume: 19, Issue:8
Interactions of n-tetraalkylammonium compounds and biguanides with a human renal organic cation transporter (hOCT2).
AID1896222Antiproliferative activity in human UMUC3 cells assessed as cell growth inhibition2022Journal of medicinal chemistry, 10-27, Volume: 65, Issue:20
Targeting Extracellular Signal-Regulated Protein Kinase 1/2 (ERK1/2) in Cancer: An Update on Pharmacological Small-Molecule Inhibitors.
AID1079946Presence of at least one case with successful reintroduction. [column 'REINT' in source]
AID1473741Inhibition of human MRP4 overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 20 mins by membrane vesicle transport assay2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID1425989Binding affinity to recombinant human carbonic anhydrase 9 after 15 mins by stopped-flow CO2 hydration assay2017European journal of medicinal chemistry, Feb-15, Volume: 127New approach of delivering cytotoxic drugs towards CAIX expressing cells: A concept of dual-target drugs.
AID1079938Chronic liver disease either proven histopathologically, or through a chonic elevation of serum amino-transferase activity after 6 months. Value is number of references indexed. [column 'CHRON' in source]
AID204498Evaluated for the blood lactate level in 24 hr fasted Sprague-Dawley rats at a dose of 200 mg/kg/day in four divided doses administered intraperitoneally1990Journal of medicinal chemistry, May, Volume: 33, Issue:5
Synthesis and antihyperglycemic activity of novel 5-(naphthalenylsulfonyl)-2,4-thiazolidinediones.
AID352948Antidiabetic activity in lean normal BALB/c mouse assessed as effect on blood lactate level at 0.40 mmol/kg/day administered through diet for 7 days relative to time-matched control2009Journal of medicinal chemistry, Jun-11, Volume: 52, Issue:11
Benzylguanidines and other galegine analogues inducing weight loss in mice.
AID1449628Inhibition of human BSEP expressed in baculovirus transfected fall armyworm Sf21 cell membranes vesicles assessed as reduction in ATP-dependent [3H]-taurocholate transport into vesicles incubated for 5 mins by Topcount based rapid filtration method2012Drug metabolism and disposition: the biological fate of chemicals, Dec, Volume: 40, Issue:12
Mitigating the inhibition of human bile salt export pump by drugs: opportunities provided by physicochemical property modulation, in silico modeling, and structural modification.
AID179883Rise in the blood glucose level after 30 min following 50 mg/kg oral dose in fasted nondiabetic rats1989Journal of medicinal chemistry, Sep, Volume: 32, Issue:9
Carbohydrate biguanides as potential hypoglycemic agents.
AID1426024Effect on mitochondrial respiration in human HCT116 cells expressing carbonic anhydrase 9 assessed as reduction in oxygen consumption rate at 0.5 mM after 24 hrs under hypoxic condition by Western blot analysis2017European journal of medicinal chemistry, Feb-15, Volume: 127New approach of delivering cytotoxic drugs towards CAIX expressing cells: A concept of dual-target drugs.
AID77203Percent reduction in blood glucose after perorally administration of compound at 25 mg/kg in in normal fasted guinea pig1981Journal of medicinal chemistry, Dec, Volume: 24, Issue:12
Chemistry and hypoglycemic activity of benzimidoylpyrazoles.
AID1079944Benign tumor, proven histopathologically. Value is number of references indexed. [column 'T.BEN' in source]
AID352979Antidiabetic activity in lean normal BALB/c mouse assessed as effect on blood lactate level at 0.5 mmol/kg/day administered through diet for 7 days relative to time-matched control2009Journal of medicinal chemistry, Jun-11, Volume: 52, Issue:11
Benzylguanidines and other galegine analogues inducing weight loss in mice.
AID1864493Substrate activity at human OCT3 overexpressed in HEK293 cells assessed as uptake ratio incubated for 2 mins by LC-MS/MS analysis2022Journal of medicinal chemistry, 09-22, Volume: 65, Issue:18
Substrates and Inhibitors of the Organic Cation Transporter 3 and Comparison with OCT1 and OCT2.
AID54563Inhibition of MAMC O-dealkylation mediated by rat Cytochrome P450 2D1 expressed in Saccharomyces cerevisiae; ND=no data2003Journal of medicinal chemistry, Jan-02, Volume: 46, Issue:1
Homology modeling of rat and human cytochrome P450 2D (CYP2D) isoforms and computational rationalization of experimental ligand-binding specificities.
AID1079931Moderate liver toxicity, defined via clinical-chemistry results: ALT or AST serum activity 6 times the normal upper limit (N) or alkaline phosphatase serum activity of 1.7 N. Value is number of references indexed. [column 'BIOL' in source]
AID1660993Inhibition of Escherichia coli DHFR2020Journal of medicinal chemistry, 08-13, Volume: 63, Issue:15
The Structural Basis for Nonsteroidal Anti-Inflammatory Drug Inhibition of Human Dihydrofolate Reductase.
AID1079939Cirrhosis, proven histopathologically. Value is number of references indexed. [column 'CIRRH' in source]
AID188229Evaluated in alloxanized, diabetic rat for the percentage reduction in blood glucose level after 5 hr as compared to pretreatment blood glucose values at a dose of 100 mg of free base / kg body weight administered orally1982Journal of medicinal chemistry, Apr, Volume: 25, Issue:4
Chemistry and hypoglycemic activity of N-[[(Dialkylamino)alkoxy]phenyl]benzamidines.
AID699539Inhibition of human liver OATP1B1 expressed in HEK293 Flp-In cells assessed as reduction in E17-betaG uptake at 20 uM by scintillation counting2012Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
Classification of inhibitors of hepatic organic anion transporting polypeptides (OATPs): influence of protein expression on drug-drug interactions.
AID182473Percent inhibition of glucose rise, following 50 mg/kg oral dose in fasted nondiabetic rats1989Journal of medicinal chemistry, Sep, Volume: 32, Issue:9
Carbohydrate biguanides as potential hypoglycemic agents.
AID1443980Inhibition of human BSEP expressed in fall armyworm sf9 cell plasma membrane vesicles assessed as reduction in vesicle-associated [3H]-taurocholate transport preincubated for 10 mins prior to ATP addition measured after 15 mins in presence of [3H]-tauroch2010Toxicological sciences : an official journal of the Society of Toxicology, Dec, Volume: 118, Issue:2
Interference with bile salt export pump function is a susceptibility factor for human liver injury in drug development.
AID182472Percent inhibition of glucose rise, following 300 mg/kg oral dose in fasted nondiabetic rats1989Journal of medicinal chemistry, Sep, Volume: 32, Issue:9
Carbohydrate biguanides as potential hypoglycemic agents.
AID188241Evaluated in glucose-primed, fasted rat for the percentage reduction in blood glucose level after 2 hr as compared to control groups at a dose of 100 mg of free base / kg body weight administered orally1982Journal of medicinal chemistry, Apr, Volume: 25, Issue:4
Chemistry and hypoglycemic activity of N-[[(Dialkylamino)alkoxy]phenyl]benzamidines.
AID588213Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in non-rodents2010Chemical research in toxicology, Jan, Volume: 23, Issue:1
Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.
AID1425987Binding affinity to recombinant human carbonic anhydrase 1 after 15 mins by stopped-flow CO2 hydration assay2017European journal of medicinal chemistry, Feb-15, Volume: 127New approach of delivering cytotoxic drugs towards CAIX expressing cells: A concept of dual-target drugs.
AID1079936Choleostatic liver toxicity, either proven histopathologically or where the ratio of maximal ALT or AST activity above normal to that of Alkaline Phosphatase is < 2 (see ACUTE). Value is number of references indexed. [column 'CHOLE' in source]
AID1079940Granulomatous liver disease, proven histopathologically. Value is number of references indexed. [column 'GRAN' in source]
AID179879Rise in the blood glucose level after 30 min following 100 mg/kg oral dose in fasted nondiabetic rats1989Journal of medicinal chemistry, Sep, Volume: 32, Issue:9
Carbohydrate biguanides as potential hypoglycemic agents.
AID352940Antidiabetic activity in lean normal BALB/c mouse assessed as effect on blood lactate level at 0.59 mmol/kg/day administered through diet for 7 days relative to time-matched control2009Journal of medicinal chemistry, Jun-11, Volume: 52, Issue:11
Benzylguanidines and other galegine analogues inducing weight loss in mice.
AID179880Rise in the blood glucose level after 30 min following 150 mg/kg oral dose in fasted nondiabetic rats1989Journal of medicinal chemistry, Sep, Volume: 32, Issue:9
Carbohydrate biguanides as potential hypoglycemic agents.
AID184646Lethal dose required to produce 50% lethality in male and female carworth farms CF-1 strain mice weighing 16-25 g administered orally1982Journal of medicinal chemistry, Apr, Volume: 25, Issue:4
Chemistry and hypoglycemic activity of N-[[(Dialkylamino)alkoxy]phenyl]benzamidines.
AID588212Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in rodents2010Chemical research in toxicology, Jan, Volume: 23, Issue:1
Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.
AID1079942Steatosis, proven histopathologically. Value is number of references indexed. [column 'STEAT' in source]
AID182469Percent inhibition of glucose rise, following 100 mg/kg oral dose in fasted nondiabetic rats1989Journal of medicinal chemistry, Sep, Volume: 32, Issue:9
Carbohydrate biguanides as potential hypoglycemic agents.
AID1473739Inhibition of human MRP2 overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 20 mins by membrane vesicle transport assay2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID1660990Inhibition of human DHFR in presence of DHF and NADPH by UV-vis spectrometry by Lineweaver-Burk plot analysis2020Journal of medicinal chemistry, 08-13, Volume: 63, Issue:15
The Structural Basis for Nonsteroidal Anti-Inflammatory Drug Inhibition of Human Dihydrofolate Reductase.
AID134584Lethal dose after peroral administration in mouse1981Journal of medicinal chemistry, Dec, Volume: 24, Issue:12
Chemistry and hypoglycemic activity of benzimidoylpyrazoles.
AID1079943Malignant tumor, proven histopathologically. Value is number of references indexed. [column 'T.MAL' in source]
AID179889Rise in the blood glucose level at 50 mg/kg oral dose in fasted nondiabetic rats1989Journal of medicinal chemistry, Sep, Volume: 32, Issue:9
Carbohydrate biguanides as potential hypoglycemic agents.
AID188896Percent reduction in blood glucose after perorally administration of compound at 100 mg/kg in glucose-primed rat1981Journal of medicinal chemistry, Dec, Volume: 24, Issue:12
Chemistry and hypoglycemic activity of benzimidoylpyrazoles.
AID1079933Acute liver toxicity defined via clinical observations and clear clinical-chemistry results: serum ALT or AST activity > 6 N or serum alkaline phosphatases activity > 1.7 N. This category includes cytolytic, choleostatic and mixed liver toxicity. Value is
AID588211Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in humans2010Chemical research in toxicology, Jan, Volume: 23, Issue:1
Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.
AID189025Percent reduction in blood glucose after perorally administration of compound at 80 mg/kg in non-glucose-primed rat1981Journal of medicinal chemistry, Dec, Volume: 24, Issue:12
Chemistry and hypoglycemic activity of benzimidoylpyrazoles.
AID352937Antidiabetic activity in lean normal BALB/c mouse assessed as effect on blood lactate level at 0.51 mmol/kg/day administered through diet for 7 days relative to time-matched control2009Journal of medicinal chemistry, Jun-11, Volume: 52, Issue:11
Benzylguanidines and other galegine analogues inducing weight loss in mice.
AID188897Percent reduction in blood glucose after perorally administration of compound at 100 mg/kg in in alloxanized rat1981Journal of medicinal chemistry, Dec, Volume: 24, Issue:12
Chemistry and hypoglycemic activity of benzimidoylpyrazoles.
AID179736In vitro inhibition of glucose oxidation by the compound in isolated rat fat cells1983Journal of medicinal chemistry, Jul, Volume: 26, Issue:7
Sulfonyliminoimidazolidines. A new class of oral hypoglycemic agents. 2. Mode of action and X-ray structure of 1-[[p-[2-(crotonylamino)ethyl]phenyl]sulfonyl]-3-cyclohexyl-2-iminoimidazolidine.
AID680369TP_TRANSPORTER: inhibition of Cimetidine uptake (Cimetidine: 1 uM) in Xenopus laevis oocytes2002Pharmaceutical research, Aug, Volume: 19, Issue:8
Interactions of n-tetraalkylammonium compounds and biguanides with a human renal organic cation transporter (hOCT2).
AID699541Inhibition of human liver OATP2B1 expressed in HEK293 Flp-In cells assessed as reduction in [3H]E3S uptake at 20 uM incubated for 5 mins by scintillation counting2012Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
Classification of inhibitors of hepatic organic anion transporting polypeptides (OATPs): influence of protein expression on drug-drug interactions.
AID1079935Cytolytic liver toxicity, either proven histopathologically or where the ratio of maximal ALT or AST activity above normal to that of Alkaline Phosphatase is > 5 (see ACUTE). Value is number of references indexed. [column 'CYTOL' in source]
AID1425990Binding affinity to recombinant human carbonic anhydrase 12 after 15 mins by stopped-flow CO2 hydration assay2017European journal of medicinal chemistry, Feb-15, Volume: 127New approach of delivering cytotoxic drugs towards CAIX expressing cells: A concept of dual-target drugs.
AID1425988Binding affinity to recombinant human carbonic anhydrase 2 after 15 mins by stopped-flow CO2 hydration assay2017European journal of medicinal chemistry, Feb-15, Volume: 127New approach of delivering cytotoxic drugs towards CAIX expressing cells: A concept of dual-target drugs.
AID179877Rise in the blood glucose level after 0 min following 50 mg/kg oral dose in fasted nondiabetic rats1989Journal of medicinal chemistry, Sep, Volume: 32, Issue:9
Carbohydrate biguanides as potential hypoglycemic agents.
AID179878Rise in the blood glucose level after 30 min following 10 mg/kg oral dose in fasted nondiabetic rats1989Journal of medicinal chemistry, Sep, Volume: 32, Issue:9
Carbohydrate biguanides as potential hypoglycemic agents.
AID1815734Inhibition of mitochondrial complex I in human HepG2 cells assessed as reduction in oxygen consumption rate incubated for 6 hrs by seahorse XF analyser based assay2022Journal of medicinal chemistry, 01-13, Volume: 65, Issue:1
Discovery and Lead Optimization of Benzene-1,4-disulfonamides as Oxidative Phosphorylation Inhibitors.
AID1079932Highest frequency of moderate liver toxicity observed during clinical trials, expressed as a percentage. [column '% BIOL' in source]
AID352941Antidiabetic activity in lean normal BALB/c mouse assessed as effect on blood lactate level at 0.52 mmol/kg/day administered through diet for 7 days relative to time-matched control2009Journal of medicinal chemistry, Jun-11, Volume: 52, Issue:11
Benzylguanidines and other galegine analogues inducing weight loss in mice.
AID173795Compound evaluated for hypoglycemic activity by lowering blood glucose in streptozotocin-diabetic rats by 20% after oral administration1983Journal of medicinal chemistry, Jul, Volume: 26, Issue:7
Sulfonyliminoimidazolidines. A new class of oral hypoglycemic agents. 1. 1-[[p-[2-(acylamino)ethyl]phenyl]sulfonyl]-2-iminoimidazolidines.
AID352978Antidiabetic activity in lean normal BALB/c mouse assessed as effect on blood lactate level at 0.62 mmol/kg/day administered through diet for 7 days relative to time-matched control2009Journal of medicinal chemistry, Jun-11, Volume: 52, Issue:11
Benzylguanidines and other galegine analogues inducing weight loss in mice.
AID179876Rise in the blood glucose level after 0 min following 300 mg/kg oral dose in fasted nondiabetic rats1989Journal of medicinal chemistry, Sep, Volume: 32, Issue:9
Carbohydrate biguanides as potential hypoglycemic agents.
AID179888Rise in the blood glucose level at 300 mg/kg oral dose in fasted nondiabetic rats1989Journal of medicinal chemistry, Sep, Volume: 32, Issue:9
Carbohydrate biguanides as potential hypoglycemic agents.
AID1896221Antiproliferative activity in mouse MB49 cells assessed as cell growth inhibition2022Journal of medicinal chemistry, 10-27, Volume: 65, Issue:20
Targeting Extracellular Signal-Regulated Protein Kinase 1/2 (ERK1/2) in Cancer: An Update on Pharmacological Small-Molecule Inhibitors.
AID179882Rise in the blood glucose level after 30 min following 300 mg/kg oral dose in fasted nondiabetic rats1989Journal of medicinal chemistry, Sep, Volume: 32, Issue:9
Carbohydrate biguanides as potential hypoglycemic agents.
AID179885Rise in the blood glucose level at 100 mg/kg oral dose in fasted nondiabetic rats1989Journal of medicinal chemistry, Sep, Volume: 32, Issue:9
Carbohydrate biguanides as potential hypoglycemic agents.
AID1347083qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347099qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347095qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347097qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1296008Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening2020SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1347094qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347089qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347086qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347096qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347105qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347103qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347093qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1508630Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID1347092qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347082qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347107qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347104qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1346987P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1346986P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1347090qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347101qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347102qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347154Primary screen GU AMC qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347100qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347106qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347098qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347091qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347108qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1745845Primary qHTS for Inhibitors of ATXN expression
AID1347411qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Mechanism Interrogation Plate v5.0 (MIPE) Libary2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID1159607Screen for inhibitors of RMI FANCM (MM2) intereaction2016Journal of biomolecular screening, Jul, Volume: 21, Issue:6
A High-Throughput Screening Strategy to Identify Protein-Protein Interaction Inhibitors That Block the Fanconi Anemia DNA Repair Pathway.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (1,448)

TimeframeStudies, This Drug (%)All Drugs %
pre-19901178 (81.35)18.7374
1990's50 (3.45)18.2507
2000's45 (3.11)29.6817
2010's131 (9.05)24.3611
2020's44 (3.04)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 48.21

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be strong demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index48.21 (24.57)
Research Supply Index7.43 (2.92)
Research Growth Index4.77 (4.65)
Search Engine Demand Index80.04 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (48.21)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials130 (8.39%)5.53%
Reviews87 (5.61%)6.00%
Case Studies95 (6.13%)4.05%
Observational0 (0.00%)0.25%
Other1,238 (79.87%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (4)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
Incretin-based Drugs and the Risk of Heart Failure: A Multi-center Network Observational Study [NCT02456428]1,499,650 participants (Actual)Observational2014-03-31Completed
The Use of Incretin-based Drugs and the Risk of Acute Pancreatitis in Patients With Type 2 Diabetes [NCT02476760]1,417,914 participants (Actual)Observational2014-03-31Completed
Phase I Trial of Phenformin With Patients With Combination BRAF Inhibitor/MEK Inhibitor in Patients With BRAFV600E/K-mutated Melanoma [NCT03026517]Phase 118 participants (Actual)Interventional2017-01-31Active, not recruiting
The Use of Incretin-based Drugs and the Risk of Pancreatic Cancer in Patients With Type 2 Diabetes [NCT02475499]886,172 participants (Actual)Observational2014-03-31Completed
[information is prepared from clinicaltrials.gov, extracted Sep-2024]