Assay Detail

CHEMBL4022986

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ADMET

Inhibition of recombinant human CB1 receptor expressed in CHO cells

ChEMBL ↗

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Target

Cannabinoid receptor 1 (CHEMBL218) ↗

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Cannabinoid receptor 1 (CHEMBL218) is the working anchor for this assay review. Loading the live Open DB target snapshot…

Primary target Cannabinoid receptor 1

CHEMBL218

Anchored from Assay target.

Protein identity Cannabinoid receptor 1

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	ADMET
Organism	Homo sapiens
Confidence	9 — Direct single protein target
Curated By	Autocuration

Target

Cannabinoid receptor 1 (CHEMBL218) ↗

Type	SINGLE PROTEIN
Organism	Homo sapiens

Publication

Identification of N-{cis-3-[Methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino]cyclobutyl}propane-1-sulfonamide (PF-04965842): A Selective JAK1 Clinical Candidate for the Treatment of Autoimmune Diseases.

Vazquez ML, Kaila N, Strohbach JW, Trzupek JD, Brown MF, Flanagan ME, Mitton-Fry MJ, Johnson TA, TenBrink RE, Arnold EP, Basak A, Heasley SE, Kwon S, Langille J, Parikh MD, Griffin SH, Casavant JM, Duclos BA, Fenwick AE, Harris TM, Han S, Caspers N, Dowty ME, Yang X, Banker ME, Hegen M, Symanowicz PT, Li L, Wang L, Lin TH, Jussif J, Clark JD, Telliez JB, Robinson RP, Unwalla R.
J Med Chem (2018) 61 : 1130 -1152
PubMed 29298069 · DOI

Activity Statistics

Type	Count	Avg pChEMBL	Best pChEMBL
IC50	1	6.92	6.92

Compounds Tested

Compound	Name	Phase	Activities	Best pChEMBL
CHEMBL3658860	—	—	1	6.92

Activity Data

Compound	Name	Type	Rel.	Value	Units	pChEMBL
CHEMBL3658860	—	IC50	=	120.0	nM	6.92