Assay Detail

CHEMBL5685498

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

Binding

Inhibition of N-terminal 6His-tagged wild type TRKA (486 to 786 residues) (unknown origin) expressed in Escherichia coli incubated for 60 mins by [gamma-33P]-ATP based TopCount NXT liquid scintillation assay

ChEMBL ↗

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Target

High affinity nerve growth factor receptor (CHEMBL2815) ↗

Open DB target context

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High affinity nerve growth factor receptor (CHEMBL2815) is the working anchor for this assay review. Loading the live Open DB target snapshot…

Primary target High affinity nerve growth factor receptor

CHEMBL2815

Anchored from Assay target.

Protein identity High affinity nerve growth factor receptor

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	9 — Direct single protein target
Curated By	Autocuration

Target

High affinity nerve growth factor receptor (CHEMBL2815) ↗

Type	SINGLE PROTEIN
Organism	Homo sapiens

Publication

A Next-Generation TRK Kinase Inhibitor Overcomes Acquired Resistance to Prior TRK Kinase Inhibition in Patients with TRK Fusion-Positive Solid Tumors.

Drilon A, Nagasubramanian R, Blake JF, Ku N, Tuch BB, Ebata K, Smith S, Lauriault V, Kolakowski GR, Brandhuber BJ, Larsen PD, Bouhana KS, Winski SL, Hamor R, Wu WI, Parker A, Morales TH, Sullivan FX, DeWolf WE, Wollenberg LA, Gordon PR, Douglas-Lindsay DN, Scaltriti M, Benayed R, Raj S, Hanusch B, Schram AM, Jonsson P, Berger MF, Hechtman JF, Taylor BS, Andrews S, Rothenberg SM, Hyman DM.
Cancer Discov (2017) 7 : 963 -972
PubMed 28578312 · DOI

Activity Statistics

Type	Count	Avg pChEMBL	Best pChEMBL
IC50	2	9.14	9.22

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
CHEMBL4297627	SELITRECTINIB	2.0	1	9.22
CHEMBL3889654	LAROTRECTINIB	4.0	1	9.05

Activity Data

Compound	Name	Type	Rel.	Value	Units	pChEMBL
CHEMBL4297627	SELITRECTINIB	IC50	=	0.6	nM	9.22
CHEMBL3889654	LAROTRECTINIB	IC50	=	0.9	nM	9.05