|
T1803 |
GNF-5
|
GNF 5 |
SARS-CoV
,
Bcr-Abl
|
|
GNF-5 is a specific non-ATP competitive inhibitor of Bcr-Abl (IC50: 0.22±0.1 uM, Wild-type Abl). It is an analog of GNF-2 with improved pharmacokinetic properties. |
|
T13099 |
TC ASK 10
|
|
ASK
,
MAPK
|
|
|
|
T4989 |
Fosfomycin Tromethamine
|
|
Antibacterial
,
Antibiotic
|
|
An antibiotic produced by Streptomyces fradiae. |
|
T2397 |
Topiroxostat
|
FYX-051 |
P450
,
ROS
,
Xanthine Oxidase
|
|
Topiroxostat (FYX-051) is a selective xanthine oxidase inhibitor developed for treatment and management of hyperuricemia and gout. |
|
T3131 |
Fosfomycin calcium
|
Phosphomycin calcium salt,Fosmicin |
Antibacterial
,
Antibiotic
|
|
Fosfomycin calcium (Phosphomycin calcium salt) is a blood-brain barrier penetrating, broad-spectrum antibiotic by irreversibly inhibiting an early stage in cell wall synthesis. |
|
T9643 |
ZN-c3
|
|
Wee1
|
|
ZN-c3 is a potent and selective Wee1 inhibitor with balanced potency, ADME, and pharmacokinetic properties. |
|
T34705 |
SR4554
|
SR 4554 |
|
|
SR4554 is a fluorine-containing 2-nitroimidazole, designed as a hypoxia marker detectable with 19F magnetic resonance spectroscopy (MRS). SR-4554 has plasma pharmacokinetic and toxicity profiles suitable for use as a hyp... |
|
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... |
|
T37082 |
HS271
|
|
IRAK
|
|
HS271 is a selective, highly potent and orally active IRAK4 inhibitor (IC50= 7.2 μM). HS271 shows excellent enzymatic and cellular activities, as well as excellent pharmacokinetic properties. |
|
T22338 |
2,6-Dichloro-N-(2-(cyclopropanecarboxamido)pyridin-4-yl)benzamide
|
GDC046 |
Others
,
JAK
|
|
2,6-Dichloro-N-(2-(cyclopropanecarboxamido)pyridin-4-yl)benzamide (GDC046), a potent lead analog, has good kinase selectivity, physicochemical properties and pharmacokinetic profile. |
|
T14338 |
Atabecestat
|
JNJ-54861911 |
BACE
|
|
Atabecestat (JNJ-54861911) is a potent brain-penetrant and orally active β-site amyloid precursor protein cleaving enzyme 1 (BACE1) inhibitor, achieves robust and high CSF Aβ reduction and it is tolerated and displays a ... |
|
T19858 |
Brodimoprim
|
|
DHFR
,
Antibacterial
|
|
Brodimoprim is an inhibitor of dihydrofolate reductase(DHFR). Brodimoprim is also a long-acting broad-spectrum antibacterial agent characterized by a good pharmacokinetic profile. |
|
T26252 |
PI3Kδ-IN-3
|
TC KHNS 11 |
PI3K
|
|
PI3Kδ-IN-3 (TC KHNS 11) is a PI3Kδ inhibitor with an IC50 value of 9 nM.PI3Kδ-IN-3 has a favorable pharmacokinetic profile and inhibits B cell function. |
|
T26969 |
CCT365623
|
CCT-365623,CCT 365623 |
Monoamine Oxidase
|
|
CCT365623 is an orally bioavailable Lysyl Oxidase inhibitor with good anti-LOX potency, selectivity, pharmacokinetic properties, as well as anti-metastatic efficacy. |
|
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. |
|
T6100 |
Torin 2
|
|
Apoptosis
,
ATM/ATR
,
DNA-PK
,
mTOR
,
Autophagy
|
|
Torin 2(IC50=0.25 nM), a specific and effective mTOR inhibitor, is the 800-fold greater specific activity for mTOR than PI3K and improves pharmacokinetic properties. The EC50 of Torin 2 for ATM/ATR/DNA-PK inhibition is 2... |
|
T9642 |
ZW4864 free base
|
|
Wnt/beta-catenin
|
|
ZW4864 (free base) is an orally active and selective β catenin/B-Cell lymphoma 9 protein protein interaction ( β catenin/BCL9 PPI ) inhibitor. ZW4864 (free base) inhibits β catenin/BCL9 PPI with a K i value of 0.76 μM an... |
|
T16679 |
Belzutifan
|
PT2977,MK-6482 |
HIF
|
|
Belzutifan (MK-6482) is a potential treatment for clear cell renal cell carcinoma (ccRCC). Belzutifan is an orally active and selective HIF-2α inhibitor (IC50: 9 nM). Belzutifan , as a second-generation HIF-2α inhibitor,... |
|
T63208 |
Aβ-IN-1
|
|
Gamma-secretase
|
|
Aβ-IN-1 is a novel, potent and orally active γ-secretase modulator (GSM). Aβ-IN-1 potently reduced Aβ42 levels with an IC 50 value of 0.091 μM in cultured cells without inhibiting CYP3A4. Aβ-IN-1 shows a sustained pharma... |
|
T64355 |
TDI-10229
|
|
cAMP
|
|
TDI-10229 is a potent and orally available inhibitor of soluble adenylyl cyclase (sAC, ADCY10). TDI-10229 displays nanomolar inhibition of sAC in both biochemical and cellular assays (IC50= 195 nM). TDI-10229 exhibits mo... |
|
T73593 |
PDS-0330
|
|
Others
|
|
PDS-0330 is a claudin-1 small molecule inhibitor inhibitor.PDS-0330 inhibits claudin-1-dependent CRC progression and binds directly and specifically to claudin-1 with micromolar affinity.PDS-0330 exhibits well characteri... |
|
T14835 |
BTRX-335140
|
CYM-53093 |
Opioid Receptor
|
|
BTRX-335140 (CYM-53093) is a potent and selective, orally active κ opioid receptor (KOR) antagonist, has antagonist activity for κOR, μOR and δOR with IC50 values of 0.8 nM, 110 nM, and 6500 nM, respectively. BTRX-335140... |
|
T21537L |
TMC647055 Choline Hydroxide Salt
|
TMC647055 Choline Hydroxide Salt (1204416-97-6 free base) |
HCV Protease
|
|
TMC647055 Choline Hydroxide Salt is a novel and potent non-nucleoside inhibitor of the HCV NS5B polymerase which potentially for the treatment of HCV infection. It has nanomolar cellular potency (EC(50) of 82 nM) with mi... |
|
T24366 |
L 870810
|
L-870,810,L870810,L 870,810,L870,810,L-870810 |
|
|
L 870810 is a small-molecule inhibitor of HIV-1 integrase with potent antiviral activity in cell culture and good pharmacokinetic properties. |
|
T33442 |
MK-8718
|
MK 8718 |
|
|
MK-8718 is an HIV protease inhibitor with a selective orally bioavailable inhibitor with good pharmacokinetic characteristics. |
|
T40092 |
MNK/PIM-IN-1
|
|
|
|
MNK/PIM-IN-1 is a novel dual inhibitor targeting both MNK and PIM pathways, characterized by its favorable pharmacokinetic profile. |
|
T27982 |
MBRI-001
|
MBRI 001,MBRI001. BPI-2358-d,plinabulin-d,NPI-2358-d |
|
|
MBRI-001 is a deuterium-substituted plinabulin derivative and a potent anti-cancer agent with better pharmacokinetic characteristics tand lower toxicity. |
|
T35852 |
FAPI-34
|
|
|
|
FAPI-34, a fibroblast-activating protein (FAP) inhibitor, boasts advantageous pharmacokinetic and biochemical attributes. |
|
T12795 |
(S)-Ceralasertib
|
(S)-AZD6738 |
Others
|
|
(S)-Ceralasertib is a potent and selective inhibitor of sulfoximine morpholinopyrimidine ATR with excellent preclinical physicochemical and pharmacokinetic (PK) characteristics. . |
|
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. |
|
T30303 |
BAY8040
|
BAY 8040,BAY-8040 |
|
|
BAY8040 is a potent selective human neutrophilic elastase inhibitor with excellent potency and selectivity with promising pharmacokinetic characteristics. |
|
T70033 |
NCATS-SM1440
|
|
|
|
NCATS-SM1440 is a Lactate Dehydrogenase Inhibitor with Optimized Cell Activity and Pharmacokinetic Properties. |
|
T32006 |
GSK-2262167 sodium
|
GSK-2262167,GSK2262167,GSK 2262167 |
|
|
GSK-2262167 is a potent S1P1 agonist, as effective as fingolimod in collagen-induced arthritis models, and shows good preclinical pharmacokinetic properties. |
|
T26309 |
Umirolimus
|
Biolimus-A9,TRM-986,TRM 986,TRM986,Biolimus A9 |
|
|
Umirolimus is a sirolimus derivative from a biodegradable polylactic acid polymer. It has enhanced anti-inflammatory and antiproliferative activity with an improved pharmacokinetic profile. |
|
T40238 |
Tenofovir-C3-O-C12-trimethylsilylacetylene ammonium
|
Tenofovir-C3-O-C12-trimethylsilylacetylene ammonium |
|
|
Tenofovir-C3-O-C12-trimethylsilylacetylene (ammonium) displays a prolonged half-life (t1/2) compared to tenofovir in human liver microsomes. Moreover, it demonstrates potent in vitro anti-HIV activity and improves in viv... |
|
T38135 |
3,4-Dehydro Cilostazol
|
|
|
|
3,4-Dehydro Cilostazol (OPC-13015) is an active metabolite of Cilostazol. 3,4-Dehydro Cilostazol is used for pharmacokinetic study[1].
[1]. T R S Satheeshmanikandan, et al. Liquid Chromatography - Tandem Mass Spectromet... |
|
T68826 |
A33903
|
|
|
|
A33903 is a 1,4-benzodiazepine analog that is being studied as a potential inhibitor of respiratory syncytial virus. This molecule was moderately active and demonstrated good pharmacokinetic properties. |
|
T23807 |
BMS-955176 TFA
|
BMS 955176,GSK-3532795,BMS955176,BMS-955176,GSK3532795 |
|
|
GSK3532795 is an orally active inhibitor of HIV-1 maturation. GSK3532795 combines broad coverage of polymorphic viruses (EC50: 15 nM toward a panel of common polymorphisms representative of 96.5% HIV-1 subtype B virus) w... |
|
T25558 |
JNJ-55511118
|
JNJ 55511118 |
|
|
JNJ-55511118 is a selective negative modulator of AMPA receptors containing TARP-γ8 (Ki: 26 nM). It had excellent pharmacokinetic properties. JNJ-55511118 exhibited a dose-dependent inhibition of neurotransmission within... |
|
T11548 |
HCV-IN-7
|
|
Others
|
|
HCV-IN-7 is an orally active and potent pan-genotypic HCV NS5A inhibitor (IC50s: 3-47 pM). It shows a superior pan-genotypic profile and a good pharmacokinetic profile coupled with a favorable liver uptake. |
|
T11548L |
HCV-IN-7 hydrochloride
|
|
Others
|
|
HCV-IN-7 hydrochloride is an orally active and potent pan-genotypic HCV NS5A inhibitor (IC50s: 3-47 pM). It shows a superior pan-genotypic profile and a good pharmacokinetic profile coupled with a favorable liver uptake. |
|
T40239 |
Tenofovir-C3-O-C15-CF3 ammonium
|
Tenofovir-C3-O-C15-CF3 ammonium |
|
|
Tenofovir-C3-O-C15-CF3 (ammonium) demonstrates prolonged half-life values compared to tenofovir in human liver microsomes. It exhibits potent anti-HIV activity in vitro and enhances pharmacokinetic properties in vivo. |
|
T68356 |
AM-3189
|
|
|
|
AM-3189 is a potent and selective GPR40 Agonist with minimal CNS penetration, superior pharmacokinetic properties and in vivo efficacy comparable to AMG 837. AM-3189 maintains the in vivo efficacy of AMG 837 while displa... |
|
T68345 |
GTS511
|
|
|
|
GTS511 is a EAAT2 Activator. Pharmacokinetic profiles (PK) of GTS511 show a >6 h half-life and higher bioavailability in plasma and the brain under all three routes of administration in rats. GTS511 can be further develo... |
|
T14509 |
BAY-707
|
|
Others
|
|
BAY-707, a highly potent and selective substrate-competitive inhibitor of MTH1 (NUDT1) with an IC50 of 2.3 nM, is well-tolerated in mice and exhibits a favorable pharmacokinetic (PK) profile compared to other MTH1 compou... |
|
T14555 |
BI-1230
|
|
HCV Protease
|
|
BI-1230 is a potent inhibitor of HCV NS3 protease, exhibiting efficacy in the low nanomolar range, and notably suppresses viral replication. This compound demonstrates high selectivity, distinguishing effectively between... |
|
T70754 |
NMS-P953
|
|
|
|
NMS-P953 is a JAK2 inhibitor, displaying significant tumor growth inhibition in SET-2 xenograft tumor model. NMS-P953 has a mechanism of action confirmed in vivo by typical modulation of known biomarkers, and with a favo... |
|
T69761 |
ZL0516
|
|
|
|
ZL0516 is a is a chromone derivatives used as orally bioavailable BRD4-selective inhibitor. This BRD4 BD1 inhibitor has demonstrated impressive in vivo efficacy and overall promising pharmacokinetic properties, indicatin... |
|
T61357 |
EP3 antagonist 3
|
|
|
|
EP3 antagonist 3 (compound 2) is a highly effective and specific antagonist of the EP3 receptor. It displays significant oral bioavailability and exhibits a strong pKi value of 8.3. Furthermore, EP3 antagonist 3 possesse... |
|
T71653 |
GS-9256
|
|
HCV Protease
|
|
GS-9256 is a selective inhibitor of the HCV NS3 protease, exhibiting favorable pharmacokinetic properties and antiviral activity [1]. |
