DC8348TG6-10-1
TG6-10-1 is an EP2 antagonist, shows low-nanomolar antagonist activity against only EP2, >300-fold selectivity over human EP3, EP4, and IP receptors, 100-fold selectivity over EP1 receptors.
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DC8348TG6-10-1 is an EP2 antagonist, shows low-nanomolar antagonist activity against only EP2, >300-fold selectivity over human EP3, EP4, and IP receptors, 100-fold selectivity over EP1 receptors.
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DC8335Bimiralisib is a potent, brain-penetrant, orally bioavailable, pan-class I PI3K/mTOR inhibitor with IC50s of 33 nM, 451 nM, 661 nM, 708 nM and 89 nM for PI3Kα, PI3Kδ, PI3Kβ, PI3Kγ and mTOR, respectively. Bimiralisib is…
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DC9274YM-90709 is a novel antagonist which inhibits the binding of interleukin-5 to interleukin-5 receptor.
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DC8169Solcitinib is an orally active, competitive, potent, selective JAK1 inhibitor, with an IC50 of 9.8 nM, and 11-, 55- and 23-fold selectivity over JAK2, JAK3 and TYK2, respectively; Solcitinib is used in the research of…
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DC8080WHI-P258, a quinazoline compound, binds to the active site of JAK3 with an estimated Ki of 72 µM. WHI-P258 does not inhibit JAK3 and does not affect the thrombin-induced aggregation of platelets even at 100 μM[1][2].
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DC9259DAA1106 is a potent and selective ligand for peripheral benzodiazepine receptor (PBR), as a potent and selective agonist at the peripheral benzodiazepine receptor.Target:PBRin vitro: DAA1106 binding to PBR was…
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DC8852SW044248 is a non-canonical topoisomerase I inhibitor, and selectively toxic for certain non-small cell lung cancer (NSCLC) cell lines.
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DC5905SN-38 is an active metabolite of the Topoisomerase I inhibitor Irinotecan. SN-38 inhibits DNA and RNA synthesis with IC50s of 0.077 and 1.3 μM, respectively.
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DC9669Fluoroclebopride is useful chemical for PET image study. [18F]fluoroclebopride had been used for PET imaging of dopamine D2 receptors in monkeys
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DC9271JNJ-63533054 is a potent and selective agonist of hGPR139 with an EC50 = 16 nM.IC50 value: 16 nM (EC50)Target: hGPR139in vitro: JNJ-63533054 is a selective small-molecule agonist. JNJ-63533054 specifically activates…
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DC7867AMG 837 is a potent GPR40 agonist(EC50=13 nM) with a superior pharmacokinetic profile and robust glucose-dependent stimulation of insulin secretion in rodents.AMG 837 displayed the expected two-fold increase in potency…
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DC2046Cobicistat is a potent, and selective inhibitor of cytochrome P450 3A (CYP3A) enzymes with IC50 of 30-285 nM.
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DC9182Vardenafil is a PDE5 inhibitor used for treating erectile dysfunction.Vardenafil specifically inhibited the hydrolysis of cGMP by PDE5 with an IC50 of 0.7 nM (6.6 nM). In contrast, the IC50 of vardenafil for PDE1 was…
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DC10477CPI-637 is a potent and selective CBP/EP300 bromodomains inhibitor with IC50 of 0.03±0.01μM and 11.0±0.6 μM for CBP/EP300 and BRD4, respectively.IC50:0.03±0.01μM (CBP/EP300)[1]IC50:11.0±0.6 μM(BRD4)[1]CPI-637, which…
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DC8795Pimavanserin is a selective inverse agonist of the 5-HT2A receptor with pIC50 and pKd of 8.73 and 9.3, respectively.
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DC8794NVP-ACC789 is an inhibitor of human VEGFR-1, VEGFR-2 (mouse VEGFR-2), VEGFR-3 and PDGFR-β with IC50s of 0.38, 0.02 (0.23), 0.18, 1.4 μM, respectively.
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DC1013Fostamatinib Disodium (R788 Disodium), a prodrug of the active metabolite R406, is a potent Syk inhibitor with IC50 of 41 nM.
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DC10503GW806742X is a Mixed Lineage Kinase Domain-Like (MLKL) inhibitor which binds the MLKL pseudokinase domain with a Kd value of 9.3 μM and anti-necroptosis activity. GW806742X has activity against VEGFR2[1][2].
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DC9677AL 082D06 is a selective, nonsteroidal glucocorticoid receptor (GR) antagonist with Ki of 210 nM.
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DCAPI1374Cyclovirobuxine D (CVB-D) is the main active component of the traditional Chinese medicine Buxus microphylla. Cyclovirobuxine D induces autophagy and attenuates the phosphorylation of Akt and mTOR[1]. Cyclovirobuxine D…
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DC9276KM11060 is a novel corrector of the F508del-CFTR trafficking defect.Target: CFTRin vitro: Small-molecule correctors such as KM11060 may serve as useful pharmacological tools in studies of the F508del-CFTR processing…
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DC10158Fluralaner (INN) is a systemic insecticide and acaricide Fluralaner through potent blockage of GABA and L-glutamate gated chloride channels.
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DC7455Lonafarnib is an orally bioavailable farnesyl protein transferase (FPTase) inhibitor for H-ras, K-ras and N-ras with IC50 of 1.9 nM, 5.2 nM and 2.8 nM, respectively.
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DC5107Ispinesib is a specific inhibitor of KSP, with a Ki app of 1.7 nM.
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DC8810GW 5074 is a potent and selective c-Raf inhibitor with IC50 of 9 nM, and has no effect on the activities of JNK1/2/3, MEK1, MKK6/7, CDK1/2, c-Src, p38 MAP, VEGFR2 or c-Fms.
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DC9994ML346 is an activator of Hsp70 expression and HSF-1 activity, with an EC50 of 4.6 μM for Hsp70. ML346 restores protein folding in conformational disease models, without significant cytotoxicity or lack of specificity.…
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DC7221P 22077 is a cell-permeable ubiquitin-specific protease 7 (USP7) inhibitor with an EC50 of 8.01 μM. It also inhibits USP47 with an EC50 of 8.74 μM.
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DC9987RAF709 is a potent, selective, and efficacious RAF inhibitor with IC50s of 0.4 nM and 0.5 nM for BRAF and CRAF, respectively[1]. Antitumor efficacy[1].
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DC8083NS11394 is a potent and subtype-selective GABA(A) receptor-positive modulator; possesses a functional efficacy selectivity profile of alpha(5) > alpha(3) > alpha(2) > alpha(1) at GABA(A) alpha subunit-containing…
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DC7396DAPT is a γ-secretase inhibitor with IC50s of 115 and 200 nM for total Aβ and Aβ42, respectively.
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DC9827Epetraborole hydrochloride is a novel leucyl-tRNA synthetase (LeuRS) inhibitor, which inhibits protein synthesis by binding "to the terminal adenosine ribose (A76) of leucyl-tRNA synthetase". It is intended for the…
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DC10441Relebactam is a diazabicyclooctane inhibitor with activity against a wide spectrum of β-lactamases, including class A (extended-spectrum β-lactamases [ESBLs] and KPC) and class C (AmpC) enzymes.Target:…
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DC8534α-Amyloid Precursor Protein Modulator(TPPB) is a cell-permeable benzolactam-derived protein kinase C (PKC) activator with a Ki of 11.9 nM.
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DC8614Rolapitant (SCH619734) is a potent, selective and orally active neurokinin NK1 receptor antagonist with a Ki of 0.66 nM.
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DC10113Pipequaline (PK 8165) is a non-selective GABAA receptor partial agonist with anxiolytic activity.
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DC3118Torin 1 is a potent inhibitor of mTOR with an IC50 of 3 nM. Torin 1 inhibits both mTORC1/2 complexes with IC50 values between 2 and 10 nM.
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DC8350Selective HDAC3, HDAC6 and HDAC8 inhibitor (IC50 values are 16.9, 2.47 and 1.46 μM for HDAC3, 6 and 8 respectively). Induces apoptosis. Shows antitumor effects in vivo. For the detailed information of Droxinostat, the…
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DC10474GBT 440 (Voxelotor) is an orally bioavailable modulator of sickle cell hemoglobin.
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DC8461Mc-Val-Cit-PABC-PNP is a cathepsin cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs).
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DC10104VX-222 (VCH-222) is a novel, potent and selective inhibitor of HCV polymerase with IC50 of 0.94-1.2 μM, 15.3-fold less effective for mutant M423T, and 108-fold less effective for mutant I482L.VX-222 is a small molecule…
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DC8530SAR131675 is a potent and selective VEGFR3 inhibitor with an IC50 of 23 nM.
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DC20016Naloxegol (NKTR-118; AZ-13337019) is an opioid-receptor antagonist[1].
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DC10544MKC3946 is a potent and soluble IRE1α inhibitor, used for cancer research.
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DC8342Vactosertib (EW-7197) is an ATP-competitive inhibitor of ALK5 with an IC50 of 12.9 nM. It also inhibits ALK2 and ALK4 at nanomolar concentrations.
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DC40320H-D-Phe-Pip-Arg-pNA hydrochloride, a chromogenic substrate, is patterned after the N-terminal portion of the A alpha chain of fibrinogen, which is the natural substrate of thrombin. H-D-Phe-Pip-Arg-pNA hydrochloride is…
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DC9255VU0357017 hydrochloride is a highly selective M1 agonists that appear to act at an allosteric site to activate the receptor (EC50 = 477 ± 172 nM; pEC50 = 6.37 ± 0.15).
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DC9873Selonsertib is an apoptosis signal-regulating kinase 1 (ASK1) inhibitor with a pIC50 of 8.3±0.07.
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DC5893A novel stearoyl-CoA desaturase1 (SCD1) inhibitor.The compound exhibited robust in vivo activity with dose-dependent desaturation index lowering effects. For the detailed information of SCD1 inhibitor, the solubility…
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