DOTATATE acetate, a DOTA-conjugated peptide, and can be labelled with radionuclides for positron emission tomography (PET) imaging and peptide receptor radionuclide therapy (PRRT).

Indophagolin is a potent, indoline-containing autophagy inhibitor (IC50=140 nM). Indophagolin antagonizes the purinergic receptor P2X4 as well as P2X1 and P2X3 with IC50s of 2.71, 2.40 and 3.49 μM, respectively. Indophagolin also antagonizes the Gq-protein-coupled P2Y4, P2Y6, and P2Y11 receptors (IC50s =3.4~15.4 μM). Indophagolin has a strong antagonistic effect on serotonin receptor 5-HT6 (IC50=1.0 μM) and a moderate effect on receptors 5-HT1B, 5-HT2B, 5-HT4e, and 5-HT7.

TPT-172, also known as R33 (described in Mecozzi et al' s paper), is a thiophene thiourea derivative with molecule weight 172 in free base form. There is no formal name yet, we temporally call this molecule as TPT-172.

MLN-4760 is a potent and selective human ACE2 inhibitor (IC50, 0.44 nM), with excellent selectivity (>5000-fold) versus related enzymes including human testicular ACE (IC50, >100 μM) and bovine carboxypeptidase A (CPDA; IC50, 27 μM).

AM095 is a potent LPA1 receptor antagonist with IC50 values of 0.98 and 0.73 μM for recombinant human or mouse LPA1 respectively.

CNX-500 is a probe consisting of a covalent Btk inhibitor (CC-292) chemically linked to biotin. CNX-500 retains inhibitory activity against Btk (IC50 of 0.5 nM) and the ability to form a covalent bond with Btk. CNX-500 has low inhibitory effects on kinase epidermal growth factor receptor, and upstream Src-family kinases including Syk and Lyn.

Regorafenib hydrochloride (BAY73-4506) is a potent, orally active multikinase inhibitor that potently inhibits endothelial cell kinases in biochemical and cellular kinase phosphorylation assays with nanomolar range (IC50=3-200 nM).

CK1-IN-1, is a casein kinase 1 (CK1) inhibitor. PUN51207 was reported in patent WO2015119579A1, compound 1c, has IC50s of 15 nM, 16 nM, 73 nM for CK1δ, and CK1ε, p38σ MAPK, respectively.

Bivalirudin, a peptide anticoagulant,direct thrombin inhibitor for anticoagulation in the setting of invasive cardiology, particularly percutaneous coronary intervention.

Eprotirome, also known as KB-2115, is a liver-selective thyroid hormone receptor agonist that has been shown to lower plasma LDL cholesterol concentrations in previous phase 1 and 2 studies of patients with dyslipidaemia. KB2115 lowers plasma LDL cholesterol and stimulates bile acid synthesis without cardiac effects in humans.

Nifeviroc is a CCR5 antagonist potentially for treatment of inflammatory responses to HIV type-1 infection

BCI is A small-molecule, allosteric inhibitor of DUSP6 (dual-specificity phosphatase 6) with IC50 of 12.3 uM; also inhibits human DUSP1 with IC50 of 11.5 uM; suppresses the ERK-induced activation of Dusp6 and regulates heart size in zebrafish.

VU0119498 is a pan Gq mAChR M1, M3, M5 positive allosteric modulator (PAM), with EC50s of 6.04, 6.38, and 4.08 μM, respectively. VU0119498 has antidiabetic activity.

A2793 is an efficient TWIK-related acid-sensitive K+ channel (TASK)-1 inhibitor, with an IC50 of 6.8 μM.

FLT3-IN-3 is a potent FLT3 inhibitor with IC50s of 13 and 8 nM for FLT3 WT and FLT3 D835Y, respectively.

BT2 is a BCKDC kinase (BDK) inhibitor with an IC50 of 3.19 μM. BT2 binding to BDK triggers helix movements in the N-terminal domain, resulting in the dissociation of BDK from the branched-chain α-ketoacid dehydrogenase complex (BCKDC)[1]. BT2 (compound 4) is also a potent and selective Mcl-1 inhibitor with a Ki value of 59 μM[2].

(-)-Cotinine is a major metabolite of nicotine in humans, it is a minor alkaloid found in tobacco plants.

AT-1002, a 6-mer synthetic peptide, is a tight junction regulator and absorption enhancer.

Defactinib is a potent, selective, and orally active FAK inhibitor with demonstrated tolerability and preliminary clinical activity working as a single agent as well as in combination with paclitaxel.

Defensamide, also known as MHP and methyl caprooyl tyrosinate, is an activator of sphingosine kinase (SPHK1), and significantly stimulates CAMP mRNA and protein production in KC.

KL001 (KL-001) is a small molecule that specifically interacts with cryptochrome (CRY) and small molecule modulator of the circadian clock.

ERK1/2 inhibitor 2 (Example 1) is a potent dual ERK1/2 inhibitor. ERK1/2 inhibitor 2 has anti-cancer activity.

Caroverine hydrochloride is a potent, competitive and reversible antagonist of NMDA and AMPA glutamate receptor. Caroverine hydrochloride is also an antioxidant and calcium-blocking agent that exhibits vasorelaxant action. Caroverine hydrochloride can be used for the research of inner ear tinnitus.

A-966492 is a novel and potent inhibitor of PARP1 and PARP2 with Ki of 1 nM and 1.5 nM, respectively.

A potent, specific and orally active 5-Lipoxygenase-activating protein (FLAP) inhibitor with IC50 of 1.6 nM in FLAP binding assay.

Derenofylline(SLV320) is a potent and selective adenosine A1 receptor antagonist (Ki values are 1, 200, 398 and 3981 nM at human A1, A3, A2A and A2B receptors respectively).

YKL-5-124 is a novel potent, selective, and covalent CDK7 inhibitor (IC50=53.5 nM), inhibits CDK7/CycH/MAT1 enzymatic activity with IC50 of 9.7 nM.

Desidustat is an inhibitor of HIF hydroxylase.

Desmethyl VS-5584 is a PI3K/mTOR kinase inhibitor

OSW-1 is a natural anti-enterovirus and anti-cancer compound that targets oxysterol-binding protein (OSBP) with Ki of 26 and 54 nM for OSBP and ORP4L, respectively.