Assay Detail

CHEMBL2215510

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Functional

Antiproliferative activity against human NCI-H1975 cells overexpressing EGFR after 48 hrs by BrdU labeling assay

ChEMBL ↗

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Target

NCI-H1975 (CHEMBL614348) ↗

Open DB target context

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NCI-H1975 (CHEMBL614348) is the working anchor for this assay review. Loading the live Open DB target snapshot…

Primary target NCI-H1975

CHEMBL614348

Anchored from Assay target.

Protein identity NCI-H1975

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	Functional
Organism	Homo sapiens
Cell Type	NCI-H1975
Confidence	1 — Organism
Curated By	Autocuration

Target

NCI-H1975 (CHEMBL614348) ↗

Type	CELL-LINE
Organism	Homo sapiens

Publication

Discovery of XL888: a novel tropane-derived small molecule inhibitor of HSP90.

Bussenius J, Blazey CM, Aay N, Anand NK, Arcalas A, Baik T, Bowles OJ, Buhr CA, Costanzo S, Curtis JK, DeFina SC, Dubenko L, Heuer TS, Huang P, Jaeger C, Joshi A, Kennedy AR, Kim AI, Lara K, Lee J, Li J, Lougheed JC, Ma S, Malek S, Manalo JC, Martini JF, McGrath G, Nicoll M, Nuss JM, Pack M, Peto CJ, Tsang TH, Wang L, Womble SW, Yakes M, Zhang W, Rice KD.
Bioorg Med Chem Lett (2012) 22 : 5396 -5404
PubMed 22877636 · DOI

Activity Statistics

Type	Count	Avg pChEMBL	Best pChEMBL
IC50	1	9.15	9.15

Compounds Tested

Compound	Name	Phase	Activities	Best pChEMBL
CHEMBL2204502	—	—	1	9.15

Activity Data

Compound	Name	Type	Rel.	Value	Units	pChEMBL
CHEMBL2204502	—	IC50	=	0.7	nM	9.15