(R)-LMI (H2N-R-Leu-Met-Ile-COOH) is a tripeptide analogue of corticotropin-releasing factor (CRF) and CRF antagonist targeting the N-domain of CRF1 receptor; (R)-LMI inhibits CRF-stimulated cAMP accumulation with IC50 of 1.7 uM. (R)-LMI inhibits the production of interleukins by adipocytes and the proliferation rate of RAW 264.7 cells.

(–)-IHCH7041 is a potent, selective partial agonist at DRD2/3 and 5-HT1AR, EC50 of 1.38 nM in Gαi1–γ9 dissociation and 2.75 nM in β-arrestin2 recruitment assays, with negligible 5-HT2AR binding (>100-fold selectivity).(–)-IHCH7041 exhibits negligible affinities for a large number of tested GPCRs, ion channels and transporters (Ki>500 nM), good affinities for DRD2 and DRD3 (Ki=14.42 nM), and moderate binding to 5-HT1A (Ki=60.62 nM).(–)-IHCH7041 behaves as a partial agonist in both G-protein signaling and β-arrestin recruitment activities at DRD2, DRD3 and 5-HT1AR.(–)-IHCH7041 displayed potent antipsychotic activity and has antidepressant properties and reverses cognitive impairmentin mice.

GSK598809 (GSK-598809) is a potent, selective, CNS penetrant and orally bioavailable dopamine D3 receptor antagonist with pKi of 8.9.

GSK598809 hydrochloride is a potent, selective, CNS penetrant and orally bioavailable dopamine D3 receptor antagonist with pKi of 8.9.

NSC45586 free base (NCS 45586, NCI45586) is a potent, specific PHLPP2 inhibitor with IC50 of 4 uM, targets the PHLPP2 PP2C domain, suppresses MYC and triggers cell death.

MyoMed-205 is a small moelcule that inhibits MuRF1 (TRIM63) activity and MuRF1/MuRF2 expression.

Flonoltinib maleate is a potent, highly selective, dual JAK2/FLT3 inhibitor with IC50 of 0.8, 1.4, and 15 nM for JAK2, JAK2V617F, and FLT3, respectively.

DS12881479 (DS 12881479) is a novel potent, selective inhibitor of MAPK-interacting kinase 1 (Mnk1) with IC50 of 21 nM, stabilizes the autoinhibited state of Mnk1.

SRI-37264 (SRI 37264) is a small molecule inhibitor of HIV-1 Nef-mediated activation of the myeloid Src-family kinase Hck, blocks HIV-1 replication in macrophages and disrupts MHC-I downregulation.

MEDS433 is a potent DHODH inhibitor with IC50 of 1.2 nM (hDHODH), inhibits in vitro replication of HSV-1 and HSV-2 in the nanomolar range.

WX-UK1 (UKI-1) is a small synthetic serine protease uPA (urokinase-type plasminogen activator) inhibitor that blocks tumor cell invasion, metastasis and primary tumor growth.

GSK3004774 (GSK-3004774) is a potent, nonabsorbable, gastrointestinally-restricted agonist agonist of calcium-sensing receptor (CaSR) with pEC50 of 7.3.

GLPG1972 (Aldumastat, S201086) is a potent and selective small-molecule inhibitor of ADAMTS5 with IC50 of 19 and <23 nM against human and rat ADAMTS5, respectively.

VUF11207 fumarate is a potent CXCR7 (ACKR3) agonist with EC50 of 1.6 nM, inducse recruitment of β-arrestin2 and subsequent internalization of CXCR7 in cells.

GSK 2793660(GSK2793660) is a potent, selective, irreversible and orally bioavailable cathepsin C inhibitor, but not the activity of downstream neutrophil serine proteases, for the treatment of cystic fibrosis, non-cystic fibrosis bronchiectasis, ANCA-associated vasculitis and bronchiectasis..

PRN473 (Atuzabrutinib, SAR 444727, PRN-473) is a potent, selective, covalent reversible BTK inhibitor.

GDC-0339 (GDC0339) is a novel small molecule pan-Pim kinase inhibitor that was discovered as a potential treatment for multiple myeloma.

GSK2973980A is a potent and selective DGAT1 inhibitor with IC50 of 3 nM, exhibits >2,900-fold selectivity over human DGAT2, ACAT1 and ACAT2 (IC50>10 uM).

GSK 2833503A (GSK2833503A, GSK503A) is a potent, and selective inhibitor of TRPC3/6 channels with IC50 of 4 nM/5 nM, respectively.

GSK-2485852 (GSK2485852, GSK5852) is a highly potent, selective HCV NS5B polymerase inhibitor with IC50 of 3.0 and 1.6 nM for HCV genotypes 1a and 1b in replicon assay, respectively.

Pyrotinib (SHR-1258) is a potent and selective EGFR/HER2 dual inhibitor with IC50 of 13/38 nM, respectively.

ABC 294640 (ABC294640, Opaganib) is a is a selective, competitive and orally bioavailable sphingosine kinase-2 (SphK-2) inhibitor with IC50 of 60 uM, Ki of 9.8 uM.

GSK-2324 (GSK2324) is a potent, selective, full FXR agonist with EC50 of 120 nM in FRET assay.

A cathepsin cleavable ADC peptide linker.

THZ-1 hydrochloride is a potent, selective, covalent CDK7 inhibitor with IC50 of 3.2 nM.

PEAQX (NVP-AAM077) is a potent, selective, NR2A-preferring NMDA receptor antagonist with IC50 of 270 nM (NR1A/2A), >100-fold selectivity over NR1A/2B receptor (IC50=29,600 nM).

NSC194598 is a specific small molecule inhibitor that inhibits p53 sequence-specific DNA binding in vitro (IC50=180 nM) and in vivo.

USP7i-1 is a potent, selective USP7 inhibitor..

HS-276 is a potent, highly selective and orally bioavailable TAK1 inhibitor with Ki of 2.5 nM.

2GBI (2-guanidinobenzimidazole) is a guanidine derivative that inhibits voltage-gated proton channel Hv1 by binding to the VSD from its intracellular side..