Gene and Protein Information
Species	TM	AA	Chromosomal Location	Gene Symbol	Gene Name	Reference
Human	-	1085	2q13	BUB1	BUB1 mitotic checkpoint serine/threonine kinase
Mouse	-	1058	2 62.1 cM	Bub1	BUB1, mitotic checkpoint serine/threonine kinase
Rat	-	1059	3q36	Bub1	BUB1 mitotic checkpoint serine/threonine kinase

Previous and Unofficial Names

BUB1A | BUB1L | BUB1, mitotic checkpoint serine/threonine kinase | BUB1

Database Links
Alphafold	O43683 (Hs), O08901 (Mm)
BRENDA	2.7.11.1
CATH/Gene3D	1.25.40.10
ChEMBL Target	CHEMBL1772932 (Hs)
Ensembl Gene	ENSG00000169679 (Hs), ENSMUSG00000027379 (Mm), ENSRNOG00000032778 (Rn)
Entrez Gene	699 (Hs), 12235 (Mm), 296137 (Rn)
Human Protein Atlas	ENSG00000169679 (Hs)
KEGG Enzyme	2.7.11.1
KEGG Gene	hsa:699 (Hs), mmu:12235 (Mm), rno:296137 (Rn)
OMIM	602452 (Hs)
Orphanet	ORPHA367084 (Hs)
Pharos	O43683 (Hs)
RefSeq Nucleotide	NM_004336 (Hs), NM_001113179 (Mm), NM_001106507 (Rn)
RefSeq Protein	NP_004327 (Hs), NP_001106650 (Mm), NP_001099977 (Rn)
UniProtKB	O43683 (Hs), O08901 (Mm)
Wikipedia	BUB1 (Hs)

Selected 3D Structures
	Description:  Structure and Substrate Recruitment of the Human Spindle Checkpoint Kinase Bub PDB Id:  3E7E Resolution:  2.31Å Species:  Human References:  5

Enzyme Reaction
EC Number: 2.7.11.1

Download all structure-activity data for this target as a CSV file

Inhibitors
Key to terms and symbols	View all chemical structures	Click column headers to sort
Ligand Sp. Action Value Parameter Reference compound 2-1-1 [PMID: 24900824] Hs Inhibition 8.3 pIC50 2 ⤷ pIC50 8.3 (IC50 5x10-9 M) [2] compound 2-3-2 [PMID: 24900824] Hs Inhibition 8.2 pIC50 2 ⤷ pIC50 8.2 (IC50 6x10-9 M) [2] compound 2-3-1 [PMID: 24900824] Hs Inhibition 8.1 pIC50 2 ⤷ pIC50 8.1 (IC50 9x10-9 M) [2] compound 2-13-1 [PMID: 24900824] Hs Inhibition 7.5 pIC50 2 ⤷ pIC50 7.5 (IC50 3x10-8 M) [2] BAY-524 Hs Inhibition 6.3 pIC50 1 ⤷ pIC50 6.3 (IC50 4.5x10-7 M) [1] Description: Measuring inhibition of the recombinant catalytic domain of human Bub1 (amino acids 704–1085). BAY-320 Hs Inhibition 6.2 pIC50 1 ⤷ pIC50 6.2 (IC50 6.8x10-7 M) [1] Description: Measuring inhibition of the recombinant catalytic domain of human Bub1 (amino acids 704–1085).

Clinically-Relevant Mutations and Pathophysiology
Disease:  Mosaic variegated aneuploidy syndrome Orphanet: ORPHA1052

General Comments

Bub1 as a mitotic checkpoint protein playing multiple roles during mitosis [3,6]. Mitotic checkpoint abrogation through pharmacological inhibition of components of the mitotic checkpoint, such as Bub1 kinase, is being investigated by drug development companies as a novel mechanism for the treatment of proliferative disorders, as evidenced by patent submissions claiming Bub1 inhibitory compounds. For example, BAY-320 and BAY-524 are two of the compounds claimed in patent WO2013092512 [4].