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Assay Detail

CHEMBL5141609

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Inhibition of full length Nano-luc fused EPHB3 in human HEK-293T cells incubated for 2 hrs by cell based NanoBRET target engagement assay
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK-293T
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Ephrin type-B receptor 3 (CHEMBL4901)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of an Orally Bioavailable and Selective PKMYT1 Inhibitor, RP-6306.
Szychowski J, Papp R, Dietrich E, Liu B, Vallée F, Leclaire ME, Fourtounis J, Martino G, Perryman AL, Pau V, Yin SY, Mader P, Roulston A, Truchon JF, Marshall CG, Diallo M, Duffy NM, Stocco R, Godbout C, Bonneau-Fortin A, Kryczka R, Bhaskaran V, Mao D, Orlicky S, Beaulieu P, Turcotte P, Kurinov I, Sicheri F, Mamane Y, Gallant M, Black WC.
J Med Chem (2022) 65 : 10251 -10284
PubMed 35880755 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 8.05 8.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3321809 1 8.15
CHEMBL5191665 1 8.15
CHEMBL5203261 1 8.15
CHEMBL5202826 1 7.75

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3321809 IC50 = 7.0 nM 8.15
CHEMBL5191665 IC50 = 7.0 nM 8.15
CHEMBL5203261 IC50 = 7.0 nM 8.15
CHEMBL5202826 IC50 = 18.0 nM 7.75