Assay Detail

CHEMBL1016954

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Binding

Inhibition of JAK1

ChEMBL ↗

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Target

Tyrosine-protein kinase JAK1 (CHEMBL2835) ↗

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Tyrosine-protein kinase JAK1 (CHEMBL2835) is the working anchor for this assay review. Loading the live Open DB target snapshot…

Primary target Tyrosine-protein kinase JAK1

CHEMBL2835

Anchored from Assay target.

Protein identity Tyrosine-protein kinase JAK1

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
Confidence	8 — Homologous single protein target
Curated By	Intermediate

Target

Tyrosine-protein kinase JAK1 (CHEMBL2835) ↗

Type	SINGLE PROTEIN
Organism	Homo sapiens

Publication

Prevention of organ allograft rejection by a specific Janus kinase 3 inhibitor.

Changelian PS, Flanagan ME, Ball DJ, Kent CR, Magnuson KS, Martin WH, Rizzuti BJ, Sawyer PS, Perry BD, Brissette WH, McCurdy SP, Kudlacz EM, Conklyn MJ, Elliott EA, Koslov ER, Fisher MB, Strelevitz TJ, Yoon K, Whipple DA, Sun J, Munchhof MJ, Doty JL, Casavant JM, Blumenkopf TA, Hines M, Brown MF, Lillie BM, Subramanyam C, Shang-Poa C, Milici AJ, Beckius GE, Moyer JD, Su C, Woodworth TG, Gaweco AS, Beals CR, Littman BH, Fisher DA, Smith JF, Zagouras P, Magna HA, Saltarelli MJ, Johnson KS, Nelms LF, Des Etages SG, Hayes LS, Kawabata TT, Finco-Kent D, Baker DL, Larson M, Si MS, Paniagua R, Higgins J, Holm B, Reitz B, Zhou YJ, Morris RE, O'Shea JJ, Borie DC.
Science (2003) 302 : 875 -878
PubMed 14593182 · DOI

Activity Statistics

Type	Count	Avg pChEMBL	Best pChEMBL
IC50	4	6.21	6.95

Compounds Tested

Compound	Name	Phase	Activities	Best pChEMBL
CHEMBL221959	TOFACITINIB	4.0	1	6.95
CHEMBL56543	—	—	1	5.47
CHEMBL405130	WHI-P131	1.0	1	-
CHEMBL473773	—	—	1	-

Activity Data

Compound	Name	Type	Rel.	Value	Units	pChEMBL
CHEMBL221959	TOFACITINIB	IC50	=	112.0	nM	6.95
CHEMBL56543	—	IC50	=	3380.0	nM	5.47
CHEMBL405130	WHI-P131	IC50	>	10000.0	nM	-
CHEMBL473773	—	IC50	>	10000.0	nM	-