|
T13099 |
TC ASK 10
|
|
ASK
,
MAPK
|
|
|
|
T2086 |
ELN-441958
|
ELN 441958 |
Bradykinin Receptor
|
|
ELN-441958 is a potent, neutral antagonist of B1 receptor, inhibits the binding of the B1 agonist ligand [3H]DAKD to IMR-90 cells with Ki of 0.26 nM. ELN-441958(ELN 441958) is highly selective for B1 over B2 receptors. |
|
T1770 |
GNE-9605
|
|
LRRK2
|
|
GNE-9605 is a highly effective, specifical, and brain-penetrant LRRK2 inhibitor (IC50: 19 nM). |
|
T10606 |
BRD0705
|
|
GSK-3
|
|
BRD0705 is a potent, paralog selective and orally active GSK3α inhibitor (IC50: 66 nM; Kd: 4.8 μM). BRD0705 displays increased selectivity for GSK3α (8-fold) versus GSK3β (IC50: 515 nM). |
|
TQ0239 |
PF-06291874
|
Glucagon receptor antagonists-4 |
Glucagon Receptor
|
|
PF-06291874 (Glucagon receptor antagonists-4) (Glucagon receptor antagonists-4) is a highly effective and orally active antagonist of the glucagon receptor. |
|
T24493 |
Monoelaidin
|
|
|
|
Monoelaidin is a poorly water-soluble drug enhancer of solubility and oral bioavailability. |
|
T69757 |
PDDC inhibitor
|
|
|
|
PDDC is the first nSMase2 inhibitor that possesses both favorable pharmacodynamics and pharmacokinetic (PK) parameters, including substantial oral bioavailability, brain penetration, and significant inhibition of exosome... |
|
T19609 |
HP-β-CD
|
Hydroxypropyl-β-cyclodextrin,Hydroxypropyl betadex |
Others
|
|
HP-β-CD (HP-β-CD) is a widely used drug delivery vehicle to improve stability and bioavailability. |
|
T9173 |
HM-30181 mesylate monohydrate
|
|
P-gp
|
|
HM-30181 mesylate monohydrate is an oral P-glycoprotein (P-gp) inhibitor, used to enhance the oral bioavailability of P-gp substrate drugs. |
|
T15409 |
GNF179
|
|
Parasite
|
|
GNF179 is an optimized 8,8-dimethyl IP analog. It exhibited the potency(4.8 nM against the multidrug resistant strain W2) in vitro metabolic stability and in vivo oral bioavailability. |
|
T7614 |
Eniluracil
|
GW776C85,5-Ethynyluracil |
Others
|
|
Eniluracil (GW776C85) is an orally activedihydropyrimidine dehydrogenase (DPD) inhibitor,increases the oral bioavailability of 5-FU to 100%, facilitating uniform absorption and predictable toxicity. |
|
T8850 |
Sbp-7455
|
|
Autophagy
|
|
SBP-7455 potently inhibited ULK1/2 enzymatic activity in vitro and in cells, reduced the viability of TNBC cells and had oral bioavailability in mice. |
|
TQ0039 |
(±)-Zanubrutinib
|
(±)-BGB-3111 |
BTK
|
|
(±)-Zanubrutinib ((±)-BGB-3111) is a potent and orally available Bruton's tyrosine kinase (Btk) inhibitor that demonstrates superior oral bioavailability, achieving higher exposure and more complete target inhibi. |
|
T7897 |
PK150
|
|
Others
,
Antibacterial
|
|
PK150 shows oral bioavailability and antibacterial activity against several pathogenic strains at submicromolar concentrations. |
|
T26863 |
BMS-929075
|
BMS 929075,BMS929075 |
HCV Protease
|
|
BMS-929075 is an orally active HCV NS5B replicase (HCV NS5B replicase) palm site variant inhibitor with potency, high oral bioavailability and pharmacokinetic parameters.BMS-929075 shows cytotoxicity. |
|
T9692 |
Paltusotine
|
|
Somatostatin
|
|
Paltusotine is a nonpeptide, small molecule somatostatin type 2 (SST2) receptor agonist with high oral bioavailability. Paltusotine maintains GH and IGF-1 levels in acromegaly patients |
|
T16143 |
MRTX-1257
|
|
Ras
|
|
MRTX-1257 is a selective, irreversible, and covalent inhibitor of KRAS G12C. It has an IC50 of 900 pM for KRAS dependent ERK phosphorylation in H358 cells. MRTX1257 demonstrated 31% bioavailability in the mouse, with fre... |
|
T24480 |
MK-8325
|
MK 8325,MK8325 |
HCV Protease
|
|
MK-8325 is a potent and orally available HCV NS5A inhibitor with replicative activity against a wide range of genotypes.MK-8325 has demonstrated bioavailability in in vitro and in vivo assays and has a favorable overall ... |
|
T3312 |
AM-2394
|
AM2394 |
Glucokinase
|
|
AM-2394 is an effective and specific Glucokinase agonist (GKA, EC50: 60 nM), which catalyzes the phosphorylation of glucose to glucose-6-phosphate. AM-2394(AM2394) increases the affinity of GK for glucose by approximatel... |
|
T14091 |
AC-73
|
|
Autophagy
|
|
AC-73 is an orally available Cluster of Differentiation 147 (CD147) inhibitor with high bioavailability that selectively disrupts the dimerization of CD147 (the binding site is in the N-terminal IgC2 domain of CD147 incl... |
|
T64133L |
Laniquidar TFA
|
Laniquidar TFA(197509-46-9 Free base),R101933 |
P-gp
|
|
Laniquidar TFA (R101933) is a novel orally available non-competitive P-glycoprotein (P-gp) inhibitor with an IC50 value of 0.51 μM.Laniquidar has limited bioavailability and can be used to modulate the multidrug resistan... |
|
T60538 |
SARS-CoV-2-IN-14
|
3',5-Dichlorosalicylanilide |
SARS-CoV
|
|
SARS-CoV-2-IN-14 is a potent and oral inhibitor of SARS-CoV-2 (IC50:0.39 μM), which is an analogue of niclosamide. SARS-CoV-2-IN-14 was more stable than niclosamide in the determination of human plasma and liver S9 enzym... |
|
T72077 |
Imidacloprid-urea
|
|
|
|
Imidacloprid-urea is a secondary metabolite of imidacloprid. Imidacloprid is a potent and widely used neonicotinoid with inhibitory effects on pests of cereals, vegetables, tea and cotton. imidacloprid-urea can occupy or... |
|
T60919 |
SARS-CoV-2-IN-13
|
|
SARS-CoV
|
|
SARS-CoV-2-IN-13 (compound 5) is an analogue of niclosamide. SARS-CoV-2-IN-13 is more stable than niclosamide in human plasma and liver S9 enzymes assay. SARS-CoV-2-IN-13 can improve bioavailability and half-life when ad... |
|
T73447 |
NP10679
|
|
|
|
NP10679 is a selective, pH dependent GluN2B subunit -specific N-methyl-D-aspartate ( NMDA ) receptor inhibitor with high oral bioavailability and good brain penetration. NP10679 inhibits GluN2B with IC 50 s of 23 and 142... |
|
T26690 |
AVN-101
|
|
5-HT Receptor
,
Adrenergic Receptor
,
Histamine Receptor
|
|
AVN-101 is a potent 5-HT7 receptor antagonist. |
|
T32286 |
JE-2178
|
JE2178 |
|
|
JE-2178 is compound with high bioavailability . |
|
T32005 |
GSK1842799
|
GSK 1842799 |
|
|
GSK1842799 is a selective S1P1 receptor agonist with good oral bioavailability. |
|
T24853 |
ZINC05626394
|
ZINC-05626394,ZINC 05626394 |
|
|
ZINC05626394 is a Cytochrome b5 reductase 3 inhibitor that acts by increasing NO bioavailability. |
|
T10448 |
Bacampicillin
|
|
Others
|
|
Bacampicillin is an improved oral bioavailability penicillin antibiotic which is a prodrug of ampicillin. |
|
T10448L |
Bacampicillin hydrochloride
|
|
Others
|
|
Bacampicillin hydrochloride is an improved oral bioavailability penicillin antibiotic which is a prodrug of ampicillin. |
|
T33291 |
Meproscillarin
|
KY-18,Rambufaside,Clift,KY 18,KY18 |
|
|
Meproscillarin is a glycoside with high bioavailability (about 70%) and an elimination independent of renal function. |
|
T16755 |
RIPK-IN-4
|
|
TNF
|
|
RIPK-IN-4 is an effective and selective inhibitor of RIPK2. It also has excellent oral bioavailability (IC50: 3 nM). |
|
T70166 |
Indinavir monohydrate
|
|
|
|
Indinavir monohydrate is a potent and specific HIV protease inhibitor that appears to have good oral bioavailability. |
|
T14500 |
BAY-1316957
|
|
Prostaglandin Receptor
|
|
BAY-1316957 is a highly potent and selective EP4 receptor antagonist. With an IC50 of 15.3 nM. Good oral bioavailability[1]. |
|
T33763 |
NVP CXCR2 20
|
NVP-CXCR2 20,NVP CXCR2-20,NVP CXCR220 |
|
|
NVP CXCR2 20 is an effective selective CXCR2 antagonist (IC50 = 40 nM) with oral bioavailability. |
|
T39935 |
TRPA1-IN-1
|
TRPA1-IN-1 |
|
|
TRPA1-IN-1 is a potent, selective antagonist of the TRPA1 channel, demonstrating significant oral bioavailability as a small molecule. |
|
T16424 |
P38 MAPK-IN-1
|
|
p38 MAPK
|
|
p38 MAPK-IN-1 displays sustained levels, low clearance, and good bioavailability. p38 MAPK-IN-1 is a novel effective and selective inhibitor of p38 MAPK (IC50: 68 nM). |
|
T70179 |
THIQ-40
|
|
|
|
THIQ-40 is a novel potent erα antagonist and selective estrogen receptor degrader (serd), exhibiting good oral bioavailability, antitumor efficacy, and serd activity in vivo |
|
T27373 |
FR-181157
|
FR-181157 Free Base |
|
|
FR-181157, a novel prostaglandin (PG) mimetic, shows high potency and agonist efficacy at the IP receptor and has good bioavailability. |
|
T38990 |
MGS0274
|
|
|
|
MGS0274, an ester-based lipophilic prodrug of the metabotropic glutamate (mGlu)2 and mGlu3 receptor agonist MGS0008, demonstrates enhanced oral bioavailability and holds promise for schizophrenia research applications. |
|
T27374 |
FR-181877
|
FR181877,FR 181877 |
|
|
FR-181877, a nonprostanoid PGI2 agonist, inhibits ADP-induced aggregation of human platelets with an IC50 value of 0.081 microM and has high oral bioavailability (56%) with a long half-life (4.3 h) in rats. |
|
T29151 |
WAY267464 HCl
|
WAY267464,WAY-267464,WAY 267,464 dihydrochloride,WAY-267,464 dihydrochloride,WAY 267464 dihydrochloride,WAY 267464 |
|
|
WAY267464 is a nonpeptide small-molecule OT agonists with anxiolytic activity. WAY267464 may be used for modulation of potency, selectivity over the structurally similar vasopressin receptors, CNS penetration, and oral b... |
|
T11445 |
GNF179 (Metabolite)
|
GNF179 Metabolite |
Others
|
|
GNF179 Metabolite, the derivative of GNF179—an optimized 8,8-dimethyl IP analog—demonstrates significant potency (4.8 nM against the multidrug-resistant W2 strain) alongside in vitro metabolic stability and in vivo oral ... |
|
T40280 |
JH-XVI-178
|
|
|
|
JH-XVI-178 is a highly potent and selective CDK8/19 inhibitor with favorable pharmacokinetic attributes, including low clearance and moderate oral bioavailability. |
|
T15093 |
Dehydro-ZINC39395747
|
|
Others
|
|
Dehydro-ZINC39395747 is a ZINC39395747 derivative. ZINC39395747 can increase NO bioavailability in vascular cells. ZINC39395747 is a potent cytochrome b5 reductase 3 inhibitor (IC50 : 9.14 μM and Kd: 1.11 μM). |
|
T18652 |
RTC-30
|
|
Others
|
|
RTC-30 is an optimized phenothiazine compound possessing potent anti-cancer properties. It is formulated with a hydroxylated linker (N) which enhances its oral bioavailability[1]. |
|
T15366 |
Gabapentin enacarbil
|
XP-13512 |
Others
,
Calcium Channel
|
|
Gabapentin enacarbil (XP-13512) is a prodrug for the anticonvulsant and analgesic drug gabapentin. Gabapentin enacarbil provides sustained dose-proportional exposure to gabapentin and predictable bioavailability. |
|
T25234 |
CH5447240
|
CH 5447240,CH-5447240 |
|
|
CH5447240 is an effective Human Parathyroid Hormone Receptor 1 (hPTHR1) Agonist for the treatment of Hypoparathyroidism. CH5447240 showed a potent in vitro hPTHR1 agonist effect (EC20: 3.0 nM; EC50: 12 nM). It showed 55%... |
|
T11648 |
INCB 3284
|
|
Others
|
|
INCB 3284, a potent and selective human CCR2 antagonist with an oral bioavailability, is utilized in the study of acute liver failure. It effectively inhibits the binding of monocyte chemoattractant protein-1 (MCP-1) to ... |
