Ilaprazole (IY-81149) is a proton pump inhibitor; inhibits H+/K+-ATPase with an IC50 of 6.0 μM.

Hypoxia-inducible factor prolyl hydroxylase inhibitor

GAL-021 is a new intravenous BKCa-channel blocker.

FG-4592 is an HIF αprolyl hydroxylase inhibitor, stabilizes HIF-2 and induces EPO production.

Fesoterodine Fumarate is an antimuscarinic agent and is rapidly de-esterified to its active metabolite 5-hydroxymethyl tolterodine that is a muscarinic receptor antagonist.

Ezutromid is a novel Small utrophin's translation modulator with EC50 of 0.4 uM .

Etrasimod (APD334) is a potent, selective and orally available antagonist of the sphingosine-1-phosphate-1(S1P1) receptor with an IC50 value of 1.88 nM in CHO cells.

Emricasan (IDN-6556, PF-03491390) is a potent irreversible pan-caspase inhibitor.

Eluxadoline is an orally active mixed μ opioid receptor (μOR) agonist δ opioid receptor (δOR) antagonist.

E-64D is an inhibitor of cathepsins B and L; also thought to inhibit calpain,showed a potent activity for COVID-19(SARS-COV-2)with EC50: MERS-COV(1.275),SARS-COV(0.760)

Desogestrel(Org-2969) is a third-generation 19-nortestosterone derivative progestogen; is contained in many oral contraceptive preparations, both combined (COCs) to ethinyl-estradiol (EE) or alone in a progestin-only pill (POP).

Daprodustat(GSK1278863) isa HIF-prolyl hydroxylase inhibitor.

Cilofexor (GS-9674, GS9674) is novel specific, non-steroidal farnesoid X receptor (FXR) agonist that reduces liver fibrosis and ameliorates portal hypertension in rat NASH models.

BMS-986020 is an LPA1 antagonist.

PF-04418948 is an orally active, potent, and selective EP2 receptor antagonist (IC50 = 16 nM).

Ranolazine(RS-43285) is an antianginal agent with antiarrhythmic properties that achieves its effects via a novel mechanism of action (inhibition of the late phase of the inward sodium current), without affecting heart rate or blood pressure (BP).

RO5028442 is a highly potent and selective Brain-Penetrant Vasopressin 1a (V1a) receptor antagonist with Kis of 1 nM (hV1a) and 39 nM (mV1a).

SKQ1 prevents amyloid-beta-induced impairment of long-term potentiation in rat hippocampal slices.

TAK-438 is a novel P-CAB (potassium-competitive acid blocker) that reversibly inhibits H+/K+, ATPase with IC50 of 19 nM (pH 6.5), controls gastric acid secretion.

UK-371804 is a potent and selective uPA inhibitor with excellent enzyme potency (Ki 10 nM) and selectivity profile (4000-fold versus tPA and 2700-fold versus plasmin).

Vadadustat is a novel, titratable, oral hypoxia-inducible factor prolyl hydroxylase (HIF-PH) inhibitor in development for the treatment of anemia.

Valbenazine(NBI-98854) is a potent and selective VMAT2 inhibitor..

VX-809 is a CFTR modulator with EC50 of 0.1 μM.

GSK3179106 (GSK-3179106, GSK 3179106) is a potent, selective, first-in-class and gut-restricted with IC50 of 0.4 and 11 nM in the biochemical assay and cellular assay respectively.

Deferasirox (Exjade)

Danicopan (ACH-4471, ACH-0144471) is a highly potent, orally active Factor D inhibitor with Kd of 0.54 nM, inhibits the proteolytic activity of purified Factor D against substrate Factor B in complex with C3b, blocking production of Bb fragment IC50 of 15 nM.

A nontoxic, orally active heat shock protein (HSP) coinducer and potentiator of the heat shock response.

Cavosonstat is a potent, orally bioavailable inhibitor of S-nitrosoglutathione reductase (GSNOR) and CFTR modulator.

Conivaptan(YM 087) is a non-peptide inhibitor of antidiuretic hormone (vasopressin receptor antagonist) with Ki values of 0.48 and 3.04 nM for rat liver V1A receptor and rat kidney V2 receptor respectively.

Silodosin(Rapaflo) is an α1-adrenoceptor antagonist with high uroselectivity. Silodosin causes practically no orthostatic hypotension (in contrast to other α1 blockers). Since Silodosin is a highly selective inhibitor of the α1A adrenergic receptor, it ca