TYROSINE-PROTEIN KINASE JAK2

Approval Year

Substance Class	Protein
Protein Type	KINASE
Protein Sub Type	TYROSINE KINASE
Sequence Origin	HUMAN
Sequence Type	COMPLETE
Record UNII	GL209F9TZS
Record Status	`Validated (UNII)`
Record Version

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Name

Type

Language

TYROSINE-PROTEIN KINASE JAK2

Common Name

English

JAK-2

Preferred Name

English

JAK2

Common Name

English

RECEPTOR-ASSOCIATED TYROSINE KINASE (HUMAN GENE JAK2)

Common Name

English

JANUS KINASE 2

Common Name

English

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Code System

Code

Type

Description

CAS

479842-25-6

ALTERNATIVE

FDA UNII

GL209F9TZS

PRIMARY

CAS

391968-59-5

PRIMARY

WIKIPEDIA

JANUS KINASE 2

PRIMARY

UNIPROT

O60674

PRIMARY

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Subunit 0

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Related Record

Type

Details


					2OYE00PC25

RITLECITINIB

NON-INHIBITOR->OFF-TARGET

Qualification:

IC50

Amount:

[>10] MICROMOLAR (average)


					J8AY0Z4CBP

CEP-11981

INHIBITOR -> TARGET

Qualification:

IC50

Amount:

17 NANOMOLAR (average)


					HY5SOV7O0Q

ROPSACITINIB

INHIBITOR->OFF-TARGET

Qualification:

Kd

Amount:

[0.25 to 0.26] NANOMOLAR (average)


					C4UD8F8XJY

AG-490

INHIBITOR -> TARGET

Comments:

Suppressed IL-4- and IL–13- mediated expression and release of monocyte chemoattractant protein-1 (MCP-1) that influences bronchial hyperreactivity and remodeling in asthma.

Qualification:

IC50

Amount:

100 NANOMOLAR (average)


					2ZT81PV5UM

IZENCITINIB

INHIBITOR -> TARGET

Qualification:

IC50

Amount:

0.1 NANOMOLAR (average)

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Structural Modifications

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Modification Type	Location Site	Residue Modified	Fragment Name	Fragment Approval
AMINO ACID SUBSTITUTION	[1_523]	SERINE	DEXFOSFOSERINE	VI4F0K069V
MOIETY			MAGNESIUM CATION	T6V3LHY838
AMINO ACID SUBSTITUTION	[1_119] [1_372] [1_373] [1_813] [1_868] [1_966] [1_972] [1_1007] [1_1008]	TYROSINE	TYROSINE O-PHOSPHATE	2R86C98KDX

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Name	Property Type	Amount	Referenced Substance	Defining	Parameters	References
Molecular Formula	CHEMICAL	ESTIMATED C5848H9106N1582O1735P10S57
MOL_WEIGHT:NUMBER AVERAGE(CALCULATED)	CHEMICAL	NUMBER AVERAGE 130674 DA (average) UNMODIFIED MW

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