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Assay Detail

CHEMBL4830154

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Functional
Antiproliferative activity against human A-375 cells assessed as reduction in cell viability after 96 hrs by alamar blue assay
23
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type A-375
Confidence 1 — Organism
Curated By Autocuration

Target

A-375 (CHEMBL613859)
Type CELL-LINE
Organism Homo sapiens

Publication

Discovery of ASTX029, A Clinical Candidate Which Modulates the Phosphorylation and Catalytic Activity of ERK1/2.
Heightman TD, Berdini V, Bevan L, Buck IM, Carr MG, Courtin A, Coyle JE, Day JEH, East C, Fazal L, Griffiths-Jones CM, Howard S, Kucia-Tran J, Martins V, Muench S, Munck JM, Norton D, O'Reilly M, Palmer N, Pathuri P, Peakman TM, Reader M, Rees DC, Rich SJ, Shah A, Wallis NG, Walton H, Wilsher NE, Woolford AJ, Cooke M, Cousin D, Onions S, Shannon J, Watts J, Murray CW.
J Med Chem (2021) 64 : 12286 -12303
PubMed 34387469 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 23 7.71 8.54

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4861945 1 8.54
CHEMBL4847260 BEROTERKIB ANHYDROUS 2.0 1 8.47
CHEMBL4869086 1 8.40
CHEMBL4212211 1 8.31
CHEMBL4847212 1 8.28
CHEMBL4871302 1 8.23
CHEMBL4870176 1 7.96
CHEMBL4869800 1 7.96
CHEMBL4867689 1 7.92
CHEMBL4873400 1 7.92
CHEMBL4856124 1 7.92
CHEMBL4878876 1 7.82
CHEMBL4857389 1 7.75
CHEMBL4866448 1 7.75
CHEMBL4849148 1 7.70
CHEMBL4873851 1 7.68
CHEMBL4870129 1 7.54
CHEMBL4868536 1 7.50
CHEMBL4865318 1 7.42
CHEMBL4213466 1 7.35
CHEMBL4849535 1 6.92
CHEMBL4847468 1 6.48
CHEMBL4850133 1 5.60

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4861945 IC50 = 2.9 nM 8.54
CHEMBL4847260 BEROTERKIB ANHYDROUS IC50 = 3.4 nM 8.47
CHEMBL4869086 IC50 = 4.0 nM 8.40
CHEMBL4212211 IC50 = 4.9 nM 8.31
CHEMBL4847212 IC50 = 5.3 nM 8.28
CHEMBL4871302 IC50 = 5.9 nM 8.23
CHEMBL4870176 IC50 = 11.0 nM 7.96
CHEMBL4869800 IC50 = 11.0 nM 7.96
CHEMBL4867689 IC50 = 12.0 nM 7.92
CHEMBL4873400 IC50 = 12.0 nM 7.92
CHEMBL4856124 IC50 = 12.0 nM 7.92
CHEMBL4878876 IC50 = 15.0 nM 7.82
CHEMBL4857389 IC50 = 18.0 nM 7.75
CHEMBL4866448 IC50 = 18.0 nM 7.75
CHEMBL4849148 IC50 = 20.0 nM 7.70
CHEMBL4873851 IC50 = 21.0 nM 7.68
CHEMBL4870129 IC50 = 29.0 nM 7.54
CHEMBL4868536 IC50 = 32.0 nM 7.50
CHEMBL4865318 IC50 = 38.0 nM 7.42
CHEMBL4213466 IC50 = 45.0 nM 7.35
CHEMBL4849535 IC50 = 120.0 nM 6.92
CHEMBL4847468 IC50 = 330.0 nM 6.48
CHEMBL4850133 IC50 = 2500.0 nM 5.60