Assay Detail

CHEMBL4767229

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Functional

Antimigratory activity against human T cells assessed as inhibition of S1P-induced T cell migration preincubated for 10 mins followed by addition of S1P measured after 120 mins by calcein-AM dye based fluorescence analysis

ChEMBL ↗

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Target

Unchecked (CHEMBL612545) ↗

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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	Functional
Organism	Homo sapiens
Cell Type	T cell
Confidence	0 — Uncurated / Unknown
Curated By	Autocuration

Target

Unchecked (CHEMBL612545) ↗

Type

UNCHECKED

Publication

Identification and Preclinical Pharmacology of ((1 R,3 S)-1-Amino-3-(( S)-6-(2-methoxyphenethyl)-5,6,7,8-tetrahydronaphthalen-2-yl)cyclopentyl)methanol (BMS-986166): A Differentiated Sphingosine-1-phosphate Receptor 1 (S1P) Modulator Advanced into Clinical Trials.

Gilmore JL,Xiao HY,Dhar TGM,Yang MG,Xiao Z,Xie J,Lehman-McKeeman LD,Gong L,Sun H,Lecureux L,Chen C,Wu DR,Dabros M,Yang X,Taylor TL,Zhou XD,Heimrich EM,Thomas R,McIntyre KW,Borowski V,Warrack BM,Li Y,Shi H,Levesque PC,Yang Z,Marino AM,Cornelius G,D'Arienzo CJ,Mathur A,Rampulla R,Gupta A,Pragalathan B,Shen DR,Cvijic ME,Salter-Cid LM,Carter PH,Dyckman AJ
J Med Chem (2019) 62 : 2265 -2285
PubMed 30785748 · DOI

Activity Statistics

Type	Count	Avg pChEMBL	Best pChEMBL
IC50	3	8.91	9.22

Compounds Tested

Compound	Name	Phase	Activities	Best pChEMBL
CHEMBL4637401	—	—	1	9.22
CHEMBL366208	FTY720-P	-1.0	1	8.92
CHEMBL3806205	—	—	1	8.60

Activity Data

Compound	Name	Type	Rel.	Value	Units	pChEMBL
CHEMBL4637401	—	IC50	=	0.6	nM	9.22
CHEMBL366208	FTY720-P	IC50	=	1.2	nM	8.92
CHEMBL3806205	—	IC50	=	2.5	nM	8.60