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Assay Detail

CHEMBL4200760

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Binding
Inhibition of human ERG by automated patch clamp assay
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Publication

Discovery of Asciminib (ABL001), an Allosteric Inhibitor of the Tyrosine Kinase Activity of BCR-ABL1.
Schoepfer J, Jahnke W, Berellini G, Buonamici S, Cotesta S, Cowan-Jacob SW, Dodd S, Drueckes P, Fabbro D, Gabriel T, Groell JM, Grotzfeld RM, Hassan AQ, Henry C, Iyer V, Jones D, Lombardo F, Loo A, Manley PW, Pellé X, Rummel G, Salem B, Warmuth M, Wylie AA, Zoller T, Marzinzik AL, Furet P.
J Med Chem (2018) 61 : 8120 -8135
PubMed 30137981 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 5.38 5.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4106732 1 5.82
CHEMBL4110570 1 5.75
CHEMBL3954214 1 5.38
CHEMBL4208229 ASCIMINIB 4.0 1 4.58
CHEMBL3898258 1 -
CHEMBL4217559 1 -
CHEMBL4114922 1 -
CHEMBL4213152 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4106732 IC50 = 1500.0 nM 5.82
CHEMBL4110570 IC50 = 1800.0 nM 5.75
CHEMBL3954214 IC50 = 4200.0 nM 5.38
CHEMBL4208229 ASCIMINIB IC50 = 26000.0 nM 4.58
CHEMBL3898258 IC50 > 30000.0 nM -
CHEMBL4217559 IC50 > 30000.0 nM -
CHEMBL4114922 IC50 > 30000.0 nM -
CHEMBL4213152 IC50 > 30000.0 nM -