Assay Detail

CHEMBL3993021

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Binding

Inhibition of ALK T1151-L1152 insT mutant (unknown origin) using peptide as substrate measured after 30 mins by fluorescence assay

ChEMBL ↗

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Target

Unchecked (CHEMBL612545) ↗

Open DB target context

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Unchecked (CHEMBL612545) is the working anchor for this assay review. Loading the live Open DB target snapshot…

Primary target Unchecked

CHEMBL612545

Anchored from Assay target.

Protein identity Unchecked

Disease frame Disease evidence pending

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Review focus Open DB context pending

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Total Activities

Compounds Tested

Activity Types

Assay Parameters

Assay Information

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

Target

Unchecked (CHEMBL612545) ↗

Type

UNCHECKED

Publication

Replacing the terminal piperidine in ceritinib with aliphatic amines confers activities against crizotinib-resistant mutants including G1202R.

Mathi GR, Kang CH, Lee HK, Achary R, Lee HY, Lee JY, Ha JD, Ahn S, Park CH, Lee CO, Hwang JY, Yun CS, Jung HJ, Cho SY, Kim HR, Kim P.
Eur J Med Chem (2017) 126 : 536 -549
PubMed 27915169 · DOI

Activity Statistics

Type	Count	Avg pChEMBL	Best pChEMBL
IC50	2	9.20	9.20

Compounds Tested

Compound	Name	Phase	Activities	Best pChEMBL
CHEMBL2403108	CERITINIB	4.0	1	9.20
CHEMBL4099660	—	—	1	9.20

Activity Data

Compound	Name	Type	Rel.	Value	Units	pChEMBL
CHEMBL2403108	CERITINIB	IC50	=	0.63	nM	9.20
CHEMBL4099660	—	IC50	=	0.63	nM	9.20