|
T15712 |
Laropiprant
|
MK-0524 |
Prostaglandin Receptor
|
|
Laropiprant (MK-0524) is a potent and selective antagonist of prostaglandin D2 (PGD2) receptor (DP) such as and DP/DP1 receptor(Ki = 0.57 nM) and TP Receptor(Ki = 2.95 nM). |
|
T8441 |
Lerisetron
|
|
5-HT Receptor
|
|
Lerisetron is an antagonist of serotonin type 3 (5-HT3) receptor, with antiemetic activity. |
|
T1752 |
NS6180
|
|
Potassium Channel
|
|
NS6180 is a potent and selective KCa3.1 channel inhibitor(IC50= 9 nM). It prevents T-cell activation and inflammation. |
|
T7121 |
Sulfaclozine
|
Sulfachloropyrazine,Sulfachloropyrazine sodium |
Antibacterial
,
Antibiotic
,
Parasite
|
|
Sulfachloropyrazine sodium(Sulfachloropyrazine) is an antiprotozoal,with antibacterial and anticoccidial effects |
|
T0096 |
Vardenafil
|
Vivanza,Levitra,Vardenafil hydrochloride |
PDE
|
|
|
|
T8405 |
Vardenafil hydrochloride
|
|
PDE
|
|
Vardenafil hydrochloride is a New Phosphodiesterase Type 5(PDE5) Inhibitor, in the Treatment of Erectile Dysfunction in Men With Diabetes |
|
T4097 |
Vardenafil hydrochloride trihydrate
|
Vardenafil HCl Trihydrate,BAY38-9456 |
PDE
|
|
Vardenafil hydrochloride trihydrate (BAY38-9456) is a new type PDE inhibitor with IC50 of 0.7 and 180 nM for PDE5 and PDE1, respectively. |
|
T4480 |
Vardenafil dihydrochloride
|
Levitra,Vardenafil Hydrochloride |
PDE
|
|
Vardenafil dihydrochloride (Levitra) is a new type PDE inhibitor with IC50 of 0.7 and 180 nM for PDE5 and PDE1, respectively. |
|
T22249 |
1588-A4
|
ARS-1620 Intermediate |
Ras
|
|
1588-A4 (ARS-1620 Intermediate) is an intermediate of ARS-1620 which is an atropisomeric selective KRASG12C inhibitor with desirable pharmacokinetics. |
|
T25824 |
ML400
|
ML 400,CID-73050863,ML-400,CID73050863,CID 73050863 |
Phosphatase
|
|
ML400 (CID73050863) is an allosteric inhibitor of LMPTP with an EC50 of 1μM. ML400 displays good cell-based activity and rodent pharmacokinetics. |
|
T2006 |
Omecamtiv mecarbil
|
CK-1827452 |
ATPase
,
Myosin
|
|
Omecamtiv mecarbil (CK-1827452) has been used in trials studying the treatment and basic science of Heart Failure, Echocardiogram, Pharmacokinetics, Chronic Heart Failure, and History of Chronic Heart Failure, among othe... |
|
T6705 |
TIC10 Isomer
|
ONC201 isomer,TIC10 Analogue |
Others
|
|
TIC10 Isomer (ONC201 isomer) is an isomer of TIC10, which inactivates Akt and ERK to induce TRAIL through Foxo3a, possesses superior drug properties: delivery across the blood-brain barrier, superior stability and improv... |
|
T7001 |
TIC10
|
ONC-201 |
Apoptosis
,
TNF
|
|
TIC10 (ONC-201) inactivates Akt and ERK to induce TRAIL through Foxo3a, possesses superior drug properties: delivery across the blood-brain barrier, superior stability and improved pharmacokinetics. Phase 1/2. |
|
T20570 |
Labetalol
|
Apo-Labetalol,Albetol,Trandate,Dilevalol,Normodyne |
Adrenergic Receptor
|
|
Labetalol (Apo-Labetalol) is a mixed alpha/beta-adrenergic antagonist.It is used to treat high blood pressure. It can be given by mouth for long term hypertension management or intravenously in severe hypertensive situat... |
|
T8947 |
Dasiglucagon acetate
|
dasiglucagon acetate(1544300-84-6 free base) |
Others
|
|
Dasiglucagon acetate is a novel glucagon analog for diabetic hypoglycemia therapy. Dasiglucagon acetate has demonstrated established solubility and stability in an aqueous formulation. Pharmacokinetics studies have shown... |
|
T36520 |
COR659
|
|
Cannabinoid Receptor
,
GABA Receptor
|
|
COR659 is a GABAB positive allosteric modulator (PAM) . COR659 suppresses alcohol and chocolate self-administration in rats[1].
COR659 apparently exerts its effects via a composite mechanism, including positive allosteri... |
|
T39124 |
BAY 1217224
|
|
|
|
BAY 1217224 is a neutral, non-prodrug Thrombin inhibitor with good oral pharmacokinetics. |
|
T30514 |
BMS-344577
|
U259PQB19A,UNII-U259PQB19A,CHEMBL570867,BMS 344577 |
|
|
BMS-344577, a lactam derivative based on arylguanidine, is a potent oral active FXA inhibitor with excellent susceptibility in vitro, good pharmacokinetics, and pharmacodynamics in animal models. |
|
T39502 |
Lipid 5
|
|
|
|
Lipid 5 is an amino lipid compound that demonstrates proficient mRNA delivery in rodent and primate models, displaying favorable pharmacokinetics and minimal toxicity. |
|
T28067 |
ML372
|
ML 372,ML-372 |
|
|
ML372 is a potent and selective SMN Modulator (EC50 = 12 nM, 325% increase inSMN2) with good potency, pharmacokinetics, tolerance, and CNS penetration. |
|
T27383 |
FR-221647
|
|
|
|
FR-221647 is a non-nucleoside adenosine deaminase inhibitor, it has moderate activity and good pharmacokinetics compared with the known inhibitors EHNA and pentostatin. |
|
T33392 |
MIP-1095 I-123
|
123-I-MIP-1095,(123I)MIP 1095 |
|
|
MIP-1095 I-123, as a radiotracer, is under investigation in clinical trial NCT00712829 (Evaluating the Safety, Pharmacokinetics, Tissue Distribution, Metabolism and Dosimetry of Two Prostate Cancer Imaging Agents). |
|
T78070 |
Despropylene gatifloxacin
|
|
|
|
Despropylene gatifloxacin, a metabolite of AM-1155, exhibits potent antibacterial activity and has favorable pharmacokinetics [1]. |
|
T37638 |
Tofacitinib metabolite-1
|
|
|
|
Tofacitinib metabolite-1, a derivative of Tofacitinib, which is a JAK inhibitor, is employed in studies focused on the pharmacokinetics and metabolism of tofacitinib[1][2]. |
|
T70930 |
GSK SYK inhibitor
|
|
|
|
The immunoregulator spleen tyrosine kinase (SYK) is upregulated in cutaneous lupus erythematosus (CLE). This double-blind, multicentre, Phase Ib study evaluated the safety, tolerability, pharmacokinetics, pharmacodynamic... |
|
T61663 |
SBI-581
|
|
|
|
SBI-581 is an orally active, potent selective inhibitor of serine-threonine kinase TAO3, with an IC 50 of 42 nM. It effectively promotes the accumulation of TKS5α at RAB11-positive vesicles and inhibits the formation of ... |
|
T37463 |
CAY10704
|
|
|
|
CAY10704 is a potent inhibitor of hepatitis C virus (HCV) infection (EC50 = 17 nM) that displays low cytotoxicity of virally-infected human hepatoma Huh7.5.1 cells (CC50 = 21.3 μM). It displays good pharmacokinetics in m... |
|
T62605 |
CDK4/6-IN-13
|
|
|
|
Compounds 10B and 10C, functioning as cdk4/6 inhibitors, demonstrated low nanomolar activity, optimal antiproliferative effects, excellent metabolic properties, and acceptable pharmacokinetics targeting cdk4/6. |
|
T69983 |
Ixazomib citrate EtOH
|
|
|
|
Ixazomib citrate, also known as MLN9708, is a prodrug of Ixazomib (MMLN-2238). MLN9708 is an orally bioavailable second generation proteasome inhibitor (PI) with potential antineoplastic activity. MLN9708, after hydrol... |
|
T81382 |
PROTAC BRD9 Degrader-7
|
|
PROTACs
|
|
PROTAC BRD9 Degrader-7 is a selective and orally active BRD9 degrader with a DC50 of 1.02 nM and demonstrates superior pharmacokinetics, evidenced by a Cmax of 3436.95 ng/mL [1]. |
|
T79513 |
ABCG2-IN-1
|
|
BCRP
|
|
ABCG2-IN-1 (compound K2), an analog of Ko143, constitutes an orally active inhibitor targeting ABCG2 with an inhibitory concentration (IC50) of 0.13 μM. Demonstrating favorable oral pharmacokinetics in mice, ABCG2-IN-1 s... |
|
T74380 |
XY-06-007
|
|
|
|
XY-06-007, a potent and selective bump-and-hole (B&H) PROTAC BRD4 BD1 L94V degrader, exhibits a DC50, 6 h of 10 nM specifically against BRD4 BD1 L94V without degrading off-targets. It also demonstrates favorable pharmaco... |
|
T39035 |
FXIa-IN-6
|
|
|
|
FXIa-IN-6 is a potent FXIa inhibitor with selectivity against most of the relevant serine proteases ( K i = 0.3 nM). FXIa-IN-6 also demonstrated excellent pharmacokinetics (PK) profile (high oral bioavailability and low ... |
|
T72125 |
Cap-dependent endonuclease-IN-9
|
|
Influenza Virus
|
|
Cap-dependent endonuclease-IN-9 is a potent (CEN) inhibitor with notable efficacy against the influenza virus and exhibits minimal cytotoxicity, enhanced in vivo pharmacokinetics, and robust pharmacodynamics. It effectiv... |
|
T63396 |
HCV-IN-38
|
|
|
|
HCV-IN-38 is a selective, potent, orally active hepatitis C virus (HCV) inhibitor with an EC50 value of 15 nM and an SI value of 431. HCV-IN-38 has a good safety profile and oral pharmacokinetics, exhibiting high anti-HC... |
|
T78815 |
MOZ-IN-3
|
|
Histone Acetyltransferase
|
|
MOZ-IN-3 (Compound 6j), a potent KAT6A (MOZ) acetyltransferase inhibitor with an IC50 of 30 nM, exhibits antitumor activity against multiple myeloid leukemia cell lines, including HL-60, U937, SKNO-1, and K562. This comp... |
|
T71757 |
SC-10914
|
|
|
|
SC10914 is a highly potent PARP inhibitor (PARP1 IC50 = 7.87 nM) with potent anti-proliferative activity against human BRCA deficient tumor cells (MDA-MB-436, BRCA1 deficient, IC50 = 4.03 nM, Capan-1 BRCA2 deficient, IC5... |
|
T77139 |
Pavurutamab
|
|
|
|
Pavurutamab (AMG-701) is a bispecific T-cell engager that targets CD3 and B-cell maturation antigens (BCMA), based on the extended half-life derived from Pacanalotamab. Its Fc region is engineered for improved pharmacoki... |
|
T70247 |
Clemizole sulfate
|
|
|
|
Clemizole sulfate is a drug in clinical development for the treatment of hepatitis C virus (HCV) infection. Clemizole is a novel inhibitor of TRPC5 channels. Clemizole is an H1 antagonist. Clemizole, an antihistamine dru... |
|
T60699 |
Aditoprime
|
|
|
|
Aditoprime (Aditoprim) is a selective inhibitor of bacterial dihydrofolate reductase (DHFR) that inhibits the transformation of dihydrofolic acid to tetrahydrofolic acid. Aditoprime shows good antibacterial activity and ... |
|
T61936 |
AChE-IN-7
|
|
|
|
AChE-IN-7 (Compound 16) is a selective and effective acetylcholinesterase inhibitor with IC50 of 0.045 μM and 19.68 μ M for eeAChE and eeBuChE, respectively. AChE-IN-7 has high permeability of blood-brain barrier. AChE-I... |
|
T37627 |
Latanoprost ethyl amide
|
|
|
|
Latanoprost ethyl amide (Lat-NEt) is a latanoprost analog in which the C-1 carboxyl group has been modified to an N-ethyl amide. Prostaglandin esters have been shown to have ocular hypotensive activity. Prostaglandin N-e... |
|
T79455 |
SARS-CoV-2 Mpro-IN-9
|
|
SARS-CoV
|
|
SARS-CoV-2 Mpro-IN-9 (compound c7), a nonpeptidic, noncovalent inhibitor of SARS-CoV-2 main protease (Mpro), exhibits potent inhibitory action (IC50 = 0.085 μM) and improved physicochemical and drug metabolism and pharma... |
|
T60439 |
CAY10789
|
|
|
|
CAY10789 (compound 6) is a potent CysLT1R (cysteinyl leukotriene receptor 1) antagonist with an IC50 of 2.80 μM. CAY10789 is also a GPBAR1 (G-protein-coupled bile acid receptor 1) agonist with an EC50 of 3 μM. CAY10789 s... |
|
T81661 |
NNMT-IN-4
|
|
|
|
NNMT-IN-4 (compound 38) is a selective, uncompetitive inhibitor of nicotinamide N-methyltransferase (NNMT) with in vitro biochemical and cell-based assay IC50 values of 42 nM and 38 nM, respectively. It demonstrates favo... |
|
T37939 |
N-Desethyl Bimatoprost
|
17-phenyl trinor Prostaglandin F2α amide |
|
|
N-Desethyl Bimatoprost (17-phenyl trinor PGF2α amide) is an F-series PG analog in which the C-1 carboxyl group has been modified to an unsubstituted amide. PG esters have been shown to have ocular hypotensive activity. P... |
|
T35645 |
4-oxo Cyclophosphamide
|
|
|
|
4-oxo Cyclophosphamide is an inactive metabolite of the alkylating agent cyclophosphamide .1,2It is formed from cyclophosphamide through a 4-hydroxycyclophosphamide intermediate by aldehyde dehydrogenases.2
1.Struck, R.F... |
|
T38266 |
Nirogacestat dihydrobromide
|
|
|
|
Potent γ-secretase inhibitor (IC50 values are 1.2 and 6.2 nM in whole cell and cell-free assays, respectively). Reduces Aβ in brain, CSF and plasma in mice and guinea pigs.
Lanz et al (2010) Pharmacodynamics and pharmaco... |
|
T36969 |
ARN24139
|
|
|
|
ARN24139 is a topoisomerase II poison (IC50= 7.3 μM in a topoisomerase II decatenation assay).1It inhibits proliferation of DU145, HeLa, and A549 cells (IC50s = 4.7, 3.8, and 3.1 μM, respectively).
1.Arencibia, J.M., Bri... |
|
T35720 |
4’-hydroxy Atomoxetine Glucuronide (hydrate)
|
|
|
|
4’-hydroxy Atomoxetine glucuronide is a metabolite of the norepinephrine transporter (NET) inhibitor atomoxetine .1It is formed from atomoxetine by glucuronidation of the intermediate metabolite 4-hydroxy atomoxetine.2
1... |
