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Assay Detail

CHEMBL5709461

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

Binding
Inhibition of Ca2+ channel L, diltiazem site (unknown origin)
ChEMBL ↗
1
Total Activities
1
Compounds Tested
1
Activity Types
2
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545) ↗
Type UNCHECKED

Publication

(R)-PFI-2 is a potent and selective inhibitor of SETD7 methyltransferase activity in cells.
Barsyte-Lovejoy D, Li F, Oudhoff MJ, Tatlock JH, Dong A, Zeng H, Wu H, Freeman SA, Schapira M, Senisterra GA, Kuznetsova E, Marcellus R, Allali-Hassani A, Kennedy S, Lambert JP, Couzens AL, Aman A, Gingras AC, Al-Awar R, Fish PV, Gerstenberger BS, Roberts L, Benn CL, Grimley RL, Braam MJ, Rossi FM, Sudol M, Brown PJ, Bunnage ME, Owen DR, Zaph C, Vedadi M, Arrowsmith CH.
Proc Natl Acad Sci U S A (2014) 111 : 12853 -12858
PubMed 25136132 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 4.85 4.85

Assay Parameters

Parameter Type Value Units Text
EFO_ID EFO_ID - — MONDO:0004992
EFO_TERM EFO_TERM - — cancer

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3414622 — — 1 4.85

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3414622 — IC50 = 14000.0 nM 4.85