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TG6-10-1 chemical structureDC8348

TG6-10-1

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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PQR-309(Bimiralisib) chemical structureDC8335

PQR-309(Bimiralisib)

Bimiralisib 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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Solcitinib(GLPG0778) chemical structureDC8169

Solcitinib(GLPG0778)

Solcitinib 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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WHI-P258 chemical structureDC8080

WHI-P258

WHI-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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DAA1106 chemical structureDC9259

DAA1106

DAA1106 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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SW-044248 chemical structureDC8852

SW-044248

SW044248 is a non-canonical topoisomerase I inhibitor, and selectively toxic for certain non-small cell lung cancer (NSCLC) cell lines.

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SN-38(NK-012) chemical structureDC5905

SN-38(NK-012)

SN-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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JNJ-63533054 chemical structureDC9271

JNJ-63533054

JNJ-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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AMG-837 chemical structureDC7867

AMG-837

AMG 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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CPI-637 chemical structureDC10477

CPI-637

CPI-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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NVP-ACC-789 chemical structureDC8794

NVP-ACC-789

NVP-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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GW806742X chemical structureDC10503

GW806742X

GW806742X 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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Cyclovirobuxin D(Bebuxine) chemical structureDCAPI1374

Cyclovirobuxin D(Bebuxine)

Cyclovirobuxine 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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KM 11060 chemical structureDC9276

KM 11060

KM11060 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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Fluralaner chemical structureDC10158

Fluralaner

Fluralaner (INN) is a systemic insecticide and acaricide Fluralaner through potent blockage of GABA and L-glutamate gated chloride channels.

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Lonafarnib chemical structureDC7455

Lonafarnib

Lonafarnib 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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GW-5074 chemical structureDC8810

GW-5074

GW 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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ML-346 chemical structureDC9994

ML-346

ML346 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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P22077 chemical structureDC7221

P22077

P 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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RAF709 chemical structureDC9987

RAF709

RAF709 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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NS11394 chemical structureDC8083

NS11394

NS11394 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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DAPT chemical structureDC7396

DAPT

DAPT is a γ-secretase inhibitor with IC50s of 115 and 200 nM for total Aβ and Aβ42, respectively.

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AN3365(Epetraborole) chemical structureDC9827

AN3365(Epetraborole)

Epetraborole 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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Relebactam chemical structureDC10441

Relebactam

Relebactam 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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Torin1 chemical structureDC3118

Torin1

Torin 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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Droxinostat chemical structureDC8350

Droxinostat

Selective 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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VX222(Lomibuvir) chemical structureDC10104

VX222(Lomibuvir)

VX-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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EW-7197 chemical structureDC8342

EW-7197

Vactosertib (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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VU0357017 chemical structureDC9255

VU0357017

VU0357017 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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SCD1 inhibitor chemical structureDC5893

SCD1 inhibitor

A 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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