BMP2K

Summary

BMP2K (BMP2 inducible kinase, HGNC:18041) is a protein-coding gene on chromosome 4q21.21, encoding BMP-2-inducible protein kinase (Q9NSY1). May be involved in osteoblast differentiation.

This gene is the human homolog of mouse BMP-2-inducible kinase. Bone morphogenic proteins (BMPs) play a key role in skeletal development and patterning. Expression of the mouse gene is increased during BMP-2 induced differentiation and the gene product is a putative serine/threonine protein kinase containing a nuclear localization signal. Therefore, the protein encoded by this human homolog is thought to be a protein kinase with a putative regulatory role in attenuating the program of osteoblast differentiation. Two transcript variants encoding different isoforms have been found for this gene.

Source: NCBI Gene 55589 — RefSeq curated summary.

At a glance

• GWAS associations: 22
• Clinical variants (ClinVar): 122 total
• Druggable target: yes — 60 molecules with ChEMBL bioactivity
• MANE Select transcript: NM_198892

Identifiers

Gene identifiers

Field	Value
HGNC ID	HGNC:18041
Approved symbol	BMP2K
Name	BMP2 inducible kinase
Location	4q21.21
Locus type	gene with protein product
Status	Approved
Aliases	DKFZp434K0614, BIKe
Ensembl gene	ENSG00000138756
Ensembl biotype	protein_coding
OMIM	617648
Entrez	55589

Gene structure

Transcript identifiers

Ensembl transcripts: 7 — 3 protein_coding, 3 retained_intron, 1 nonsense_mediated_decay

ENST00000389010, ENST00000502613, ENST00000502871, ENST00000505725, ENST00000507670, ENST00000515075, ENST00000858772

RefSeq mRNA: 4 — MANE Select: NM_198892 NM_001419799, NM_001419800, NM_017593, NM_198892

CCDS: CCDS34019, CCDS47083

Canonical transcript exons

ENST00000502613 — 16 exons

Exon	Start	End
ENSE00001123554	78850924	78851056
ENSE00001485759	78887174	78887284
ENSE00001485761	78878734	78878891
ENSE00001594445	78844928	78845049
ENSE00001669530	78833582	78833687
ENSE00001676256	78847188	78847269
ENSE00001793790	78826037	78826155
ENSE00001804583	78842385	78842527
ENSE00002026633	78910610	78916365
ENSE00003481842	78870783	78871060
ENSE00003512574	78865557	78865720
ENSE00003513318	78872614	78872798
ENSE00003614292	78861389	78861468
ENSE00003662345	78871850	78871948
ENSE00003687199	78859584	78859687
ENSE00003904404	78776350	78776721

Expression profiles

Bgee: expression breadth ubiquitous, 287 present calls, max score 93.03.

FANTOM5 (CAGE): breadth ubiquitous, TPM avg 24.2600 / max 868.3864, expressed in 1807 samples.

FANTOM5 promoters (9 alternative TSS)

Promoter ID	TPM avg	Samples expressed
48468	18.7238	1789
48478	1.7799	470
48469	1.4747	626
48463	1.2232	853
48467	0.4062	184
48473	0.2824	106
48466	0.1689	45
48465	0.1016	39
48464	0.0993	27

Top tissues by expression

292 total, by Bgee expression score (0-100, higher = more expressed):

Tissue	Anatomy ID	Expression score	Quality
adrenal tissue	UBERON:0018303	93.03	gold quality
secondary oocyte	CL:0000655	92.58	gold quality
trabecular bone tissue	UBERON:0002483	92.36	gold quality
sural nerve	UBERON:0015488	91.47	gold quality
oocyte	CL:0000023	91.34	gold quality
rectum	UBERON:0001052	89.79	gold quality
monocyte	CL:0000576	89.42	gold quality
mononuclear cell	CL:0000842	89.30	gold quality
leukocyte	CL:0000738	89.10	gold quality
amniotic fluid	UBERON:0000173	88.94	gold quality
lymph node	UBERON:0000029	88.45	gold quality
vermiform appendix	UBERON:0001154	88.17	gold quality
calcaneal tendon	UBERON:0003701	87.92	gold quality
stromal cell of endometrium	CL:0002255	87.90	gold quality
bone marrow cell	CL:0002092	87.78	gold quality
tonsil	UBERON:0002372	87.77	gold quality
blood	UBERON:0000178	87.70	gold quality
bone marrow	UBERON:0002371	87.59	gold quality
tibial nerve	UBERON:0001323	87.34	gold quality
medial globus pallidus	UBERON:0002477	87.16	gold quality
caecum	UBERON:0001153	86.62	gold quality
cervix squamous epithelium	UBERON:0006922	86.17	gold quality
corpus callosum	UBERON:0002336	85.98	gold quality
C1 segment of cervical spinal cord	UBERON:0006469	85.98	gold quality
tendon	UBERON:0000043	85.91	gold quality
male germ line stem cell (sensu Vertebrata) in testis	CL:0000089 ∩ UBERON:0000473	85.75	gold quality
globus pallidus	UBERON:0001875	85.69	gold quality
spinal cord	UBERON:0002240	85.42	gold quality
ventricular zone	UBERON:0003053	85.31	gold quality
spleen	UBERON:0002106	85.30	gold quality

Single-cell (SCXA)

Detected in 8 experiment(s), a significant marker in 5.

Experiment	Marker?	Max mean expression
E-MTAB-6701	yes	42.89
E-HCAD-35	yes	42.22
E-HCAD-25	yes	14.46
E-ANND-3	yes	9.19
E-MTAB-9801	yes	5.91
E-MTAB-6386	no	498.13
E-GEOD-124858	no	154.64
E-MTAB-7303	no	148.94

Regulation

Is transcription factor: no

miRNA regulators (miRDB)

63 targeting BMP2K, top 30 by miRDB confidence (max_score; target_count = how many genes the miRNA targets in total — lower means more specific):

miRNA	Max score	Avg score	miRNA target_count
HSA-MIR-4262	100.00	73.26	3931
HSA-MIR-4776-3P	100.00	68.73	1340
HSA-MIR-3924	100.00	72.09	2394
HSA-MIR-9-5P	100.00	72.28	2361
HSA-MIR-574-5P	100.00	66.01	989
HSA-MIR-186-5P	99.99	70.83	3707
HSA-MIR-181A-5P	99.99	72.96	2995
HSA-MIR-181B-5P	99.99	72.97	2996
HSA-MIR-181C-5P	99.99	72.95	2996
HSA-MIR-181D-5P	99.99	73.04	2997
HSA-MIR-4803	99.98	71.99	3117
HSA-MIR-3617-3P	99.98	67.86	918
HSA-MIR-4482-3P	99.98	72.50	3147
HSA-MIR-302C-5P	99.97	72.56	3642
HSA-MIR-1468-3P	99.96	72.74	3797
HSA-MIR-1250-3P	99.96	70.04	4038
HSA-MIR-3910	99.95	71.13	2227
HSA-MIR-3143	99.93	71.96	3104
HSA-MIR-1305	99.91	71.43	3443
HSA-MIR-8063	99.91	69.76	3146
HSA-MIR-124-3P	99.89	73.74	3043
HSA-MIR-506-3P	99.89	73.55	3057
HSA-MIR-8080	99.82	67.52	1342
HSA-MIR-4658	99.77	64.94	514
HSA-MIR-6790-5P	99.77	65.24	505
HSA-MIR-3714	99.71	70.74	2671
HSA-MIR-494-3P	99.70	71.45	2795
HSA-MIR-1303	99.65	69.77	1662
HSA-MIR-651-5P	99.64	68.49	1104
HSA-MIR-587	99.64	70.86	2611

Literature-anchored findings (GeneRIF, showing 7)

• PGE2 produced by COX-2 increased BMP-2 expression via binding the EP4 receptor. (PMID:15254968)
• The association of the BMP-2 gene polymorphisms Ser37Ala and Arg190Ser with osteoporosis in 6353 men and women from the Rotterdam Study was studied. (PMID:16753015)
• BMP2K gene 1379 G/A variant is strongly correlated with high myopia and may contribute to a genetic risk factor for high degrees of myopic pathogenesis. (PMID:19927351)
• Results present the first structures of AAK1 and BIKE which reveal that all members of the Numb-associated kinase family share unusual activation segment architecture. (PMID:26853940)
• Regulation of BMP2K in AP2M1-mediated EGFR internalization during the development of gallbladder cancer. (PMID:32792513)
• Splicing variation of BMP2K balances abundance of COPII assemblies and autophagic degradation in erythroid cells. (PMID:32795391)
• The cargo adapter protein CLINT1 is phosphorylated by the Numb-associated kinase BIKE and mediates dengue virus infection. (PMID:35452674)

Cross-species orthologs

3 orthologs

Organism	Symbol	Gene ID
danio_rerio	bmp2k	ENSDARG00000020009
mus_musculus	Bmp2k	ENSMUSG00000034663
rattus_norvegicus	Bmp2k	ENSRNOG00000002040

Paralogs (2): STK16 (ENSG00000115661), AAK1 (ENSG00000115977)

Protein

Protein identifiers

BMP-2-inducible protein kinase — Q9NSY1 (reviewed: Q9NSY1)

All UniProt accessions (3): Q9NSY1, H0Y9P1, K4DI97

UniProt curated annotations — full annotation on UniProt →

Function. May be involved in osteoblast differentiation.

Subcellular location. Nucleus.

Post-translational modifications. Autophosphorylated.

Similarity. Belongs to the protein kinase superfamily. Ser/Thr protein kinase family.

Isoforms (3)

UniProt ID	Names	Canonical?
Q9NSY1-1	1	yes
Q9NSY1-2	2
Q9NSY1-3	3

RefSeq proteins (4): NP_001406728, NP_001406729, NP_060063, NP_942595* (*=MANE)

Domains & families (InterPro)

ID	Name	Type
IPR000719	Prot_kinase_dom	Domain
IPR008271	Ser/Thr_kinase_AS	Active_site
IPR011009	Kinase-like_dom_sf	Homologous_superfamily
IPR028182	BMP2K_C	Domain
IPR051744	AP2_assoc_SerThr_kinase	Family

Pfam: PF00069, PF15282

Catalyzed reactions (Rhea), 2 shown:

• L-seryl-[protein] + ATP = O-phospho-L-seryl-[protein] + ADP + H(+) (RHEA:17989)
• L-threonyl-[protein] + ATP = O-phospho-L-threonyl-[protein] + ADP + H(+) (RHEA:46608)

UniProt features (76 total): modified residue 15, helix 14, compositionally biased region 11, strand 10, region of interest 7, sequence variant 6, splice variant 3, sequence conflict 3, binding site 2, turn 2, chain 1, domain 1, active site 1

Structure

Experimental structures (PDB)

5 structures.

PDB	Method	Resolution (Å)
4W9W	X-RAY DIFFRACTION	1.72
4W9X	X-RAY DIFFRACTION	2.14
5I3O	X-RAY DIFFRACTION	2.4
5I3R	X-RAY DIFFRACTION	2.4
5IKW	X-RAY DIFFRACTION	2.41

Predicted structure (AlphaFold)

Model	pLDDT	Fraction very-high
AF-Q9NSY1-F1	55.52	0.26

Functional residue map

Curated UniProt residues grouped by drug-discovery relevance — catalytic, ligand-binding, modification, and mutation-validated positions. Source: UniProtKB sequence features.

Catalytic / active sites (1): 180 (proton acceptor)

Ligand- & substrate-binding residues (2): 57–65; 79

Post-translational modifications (15): 14, 689, 742, 817, 818, 834, 928, 1029, 1031, 1032, 1039, 1041, 1076, 1107, 1111

Function

Pathways and Gene Ontology

Reactome pathways

0 pathways

MSigDB gene sets: 303 (showing top): CREL_01, HALMOS_CEBPA_TARGETS_UP, GOBP_POSITIVE_REGULATION_OF_NOTCH_SIGNALING_PATHWAY, IVANOVA_HEMATOPOIESIS_LATE_PROGENITOR, IVANOVA_HEMATOPOIESIS_MATURE_CELL, GOBP_VESICLE_MEDIATED_TRANSPORT, USF_C, BOHN_PRIMARY_IMMUNODEFICIENCY_SYNDROM_DN, GOBP_REGULATION_OF_VESICLE_MEDIATED_TRANSPORT, LINDGREN_BLADDER_CANCER_CLUSTER_2A_DN, GARGALOVIC_RESPONSE_TO_OXIDIZED_PHOSPHOLIPIDS_BLUE_DN, GOBP_BONE_MINERALIZATION, GOBP_REGULATION_OF_RECEPTOR_MEDIATED_ENDOCYTOSIS, BLALOCK_ALZHEIMERS_DISEASE_UP, SCHAEFFER_PROSTATE_DEVELOPMENT_48HR_DN

GO Biological Process (4): regulation of bone mineralization (GO:0030500), positive regulation of Notch signaling pathway (GO:0045747), regulation of clathrin-dependent endocytosis (GO:2000369), protein phosphorylation (GO:0006468)

GO Molecular Function (10): protein serine/threonine kinase activity (GO:0004674), ATP binding (GO:0005524), phosphatase regulator activity (GO:0019208), AP-2 adaptor complex binding (GO:0035612), protein serine kinase activity (GO:0106310), nucleotide binding (GO:0000166), protein kinase activity (GO:0004672), protein binding (GO:0005515), kinase activity (GO:0016301), transferase activity (GO:0016740)

GO Cellular Component (3): nucleus (GO:0005634), cytoplasm (GO:0005737), nuclear speck (GO:0016607)

GO top-level categories

Rollup of top GO terms by namespace:

Category	Terms
protein kinase activity	2
regulation of ossification	1
bone mineralization	1
regulation of biomineral tissue development	1
Notch signaling pathway	1
regulation of Notch signaling pathway	1
positive regulation of signal transduction	1
regulation of receptor-mediated endocytosis	1
clathrin-dependent endocytosis	1
phosphorylation	1
protein modification process	1
adenyl ribonucleotide binding	1
purine ribonucleoside triphosphate binding	1
phosphatase activity	1
phosphatase binding	1
enzyme regulator activity	1
protein-containing complex binding	1
nucleoside phosphate binding	1
heterocyclic compound binding	1
kinase activity	1
phosphotransferase activity, alcohol group as acceptor	1
catalytic activity, acting on a protein	1
binding	1
transferase activity, transferring phosphorus-containing groups	1
catalytic activity	1
intracellular membrane-bounded organelle	1
intracellular anatomical structure	1
cellular anatomical structure	1
nuclear ribonucleoprotein granule	1

Protein interactions and networks

STRING

880 interactions, top by confidence (×1000):

Protein A	Protein B	Partner UniProt	Score
BMP2K	NUMB	P49757	656
BMP2K	NUMBL	Q9Y6R0	647
BMP2K	GAK	O14976	599
BMP2K	NEIL3	Q8TAT5	456
BMP2K	CD33	P20138	433
BMP2K	SYNRG	Q9UMZ2	430
BMP2K	FCHO2	Q0JRZ9	418
BMP2K	AURKA	O14965	413
BMP2K	LIMK1	P53667	410
BMP2K	FCGR3A	P08637	407
BMP2K	FCGR3B	O75015	397
BMP2K	CD19	P15391	396
BMP2K	BMPER	Q8N8U9	374
BMP2K	CYP24A1	Q07973	371
BMP2K	NAB2	Q15742	368

IntAct

190 interactions, top by confidence:

A	B	Type	Score
STAMBP	PIK3C2A	psi-mi:“MI:0914”(association)	0.730
BMP2K	CLINT1	psi-mi:“MI:0915”(physical association)	0.710
BMP2K	CLINT1	psi-mi:“MI:0217”(phosphorylation reaction)	0.710
BMP2K	STAMBP	psi-mi:“MI:0915”(physical association)	0.660
STAMBPL1	PIK3C2A	psi-mi:“MI:0914”(association)	0.640
AP2S1	AP2A2	psi-mi:“MI:0914”(association)	0.640
RALBP1	JUN	psi-mi:“MI:0914”(association)	0.640
BMP2K	RUNDC3A	psi-mi:“MI:0915”(physical association)	0.550
SLC25A41	NUDT19	psi-mi:“MI:0914”(association)	0.530
LIMS1	TYMS	psi-mi:“MI:0914”(association)	0.530
AP2B1	AP2A2	psi-mi:“MI:0914”(association)	0.530
NECAP2	AP2A2	psi-mi:“MI:0914”(association)	0.530
FHL2	CNOT1	psi-mi:“MI:0914”(association)	0.530
CLINT1	PIK3C2A	psi-mi:“MI:0914”(association)	0.530
PICALM	PIK3C2A	psi-mi:“MI:0914”(association)	0.530
RNF166	MPDZ	psi-mi:“MI:0914”(association)	0.530
REPS1	AP2B1	psi-mi:“MI:0914”(association)	0.530
DAB2	FCHO2	psi-mi:“MI:0914”(association)	0.530
RALBP1	AP2B1	psi-mi:“MI:0914”(association)	0.530
PIP	TBKBP1	psi-mi:“MI:0914”(association)	0.530
BMP2K	DAZAP1	psi-mi:“MI:0915”(physical association)	0.490
BMP2K	BAAT	psi-mi:“MI:0915”(physical association)	0.490

BioGRID (150): BMP2K (Affinity Capture-MS), BMP2K (Affinity Capture-MS), BMP2K (Affinity Capture-MS), BMP2K (Affinity Capture-MS), BMP2K (Affinity Capture-MS), BMP2K (Affinity Capture-MS), BMP2K (Affinity Capture-MS), BMP2K (Affinity Capture-MS), BMP2K (Affinity Capture-MS), BMP2K (Affinity Capture-MS), BMP2K (Affinity Capture-MS), BMP2K (Affinity Capture-MS), BMP2K (Affinity Capture-MS), BMP2K (Affinity Capture-MS), BMP2K (Affinity Capture-MS)

ESM2 similar proteins: A0A140LFM6, A0A1L8H8C0, A0A1L8HFX9, A0A2R6X6S3, A0JM08, A2ARZ3, A2RUV4, A5WUN7, A6QP06, D4AEC2, E9Q309, O76039, P51960, Q03898, Q05935, Q06190, Q08AD1, Q08D57, Q0WPH8, Q3KQW7, Q3UTQ8, Q498L0, Q5RAU1, Q5SW79, Q5T0W9, Q5T5U3, Q5VT06, Q62770, Q66J90, Q69Z38, Q6A065, Q6DFG0, Q6DFV3, Q6IRN6, Q71M21, Q80TN7, Q8AV28, Q8C1B1, Q8IVL0, Q8IZ21

Diamond homologs: A2X6X1, A5A7I8, A8WRV1, F1MH24, F1SPM8, F4I4F2, G5ECQ3, O13839, O14976, O34507, O43066, O75716, O77676, O88697, P00516, P00517, P05130, P05132, P0C1X8, P0C605, P17157, P17612, P17948, P25321, P31374, P32023, P33981, P34100, P34331, P35761, P35916, P35917, P35969, P38070, P38080, P40494, P53767, P53974, P54119, P57760

SIGNOR signaling

0 interactions.

Enriched among interaction partners

Reactome pathways and GO biological processes over-represented among this gene’s 181 IntAct physical interaction partners (hypergeometric vs the genome-wide background, BH-FDR, gene-set size 15–500, ranked by fold). A functional readout of the neighbourhood — distinct from this gene’s own memberships above, and biased toward well-studied / hub proteins, so read it as themes rather than proof.

Reactome pathways:

Pathway	Partners	Fold	FDR
WNT5A-dependent internalization of FZD4	8	51.2×	1e-10
VLDLR internalisation and degradation	8	48.0×	2e-10
Nef-mediates down modulation of cell surface receptors by recruiting them to clathrin adapters	7	37.3×	3e-08
The role of Nef in HIV-1 replication and disease pathogenesis	7	37.3×	3e-08
LDL clearance	7	32.0×	6e-08
Trafficking of GluR2-containing AMPA receptors	5	28.2×	2e-05
Plasma lipoprotein clearance	6	24.0×	4e-06
Host Interactions of HIV factors	7	19.8×	2e-06

GO biological processes:

GO term	Partners	Fold	FDR
clathrin coat assembly	13	74.4×	6e-20
clathrin-dependent endocytosis	13	48.7×	7e-17
negative regulation of protein localization to plasma membrane	7	28.2×	8e-07
synaptic vesicle endocytosis	10	27.9×	6e-10
receptor-mediated endocytosis	6	8.6×	7e-03
endocytosis	12	7.4×	2e-05
protein localization to plasma membrane	8	5.6×	7e-03
vesicle-mediated transport	9	5.6×	4e-03

Disease & clinical

Clinical variants and AI predictions

ClinVar

122 variants total. Per-class counts are floors (≥ shown; pagination cap):

Classification	Count (floor)
Pathogenic	0
Likely pathogenic	0
Uncertain significance	96
Likely benign	2
Benign	1

Top pathogenic / likely-pathogenic (0)

SpliceAI

2663 predictions. Top by Δscore:

Variant	Effect	Δscore
4:78826032:TCTA:T	acceptor_loss	1.0000
4:78826033:CTAG:C	acceptor_loss	1.0000
4:78826035:A:AG	acceptor_gain	1.0000
4:78826035:A:C	acceptor_loss	1.0000
4:78826035:AGGT:A	acceptor_gain	1.0000
4:78826035:AGGTG:A	acceptor_gain	1.0000
4:78826036:G:A	acceptor_loss	1.0000
4:78826036:G:GA	acceptor_gain	1.0000
4:78826036:GGT:G	acceptor_gain	1.0000
4:78826036:GGTG:G	acceptor_gain	1.0000
4:78826036:GGTGG:G	acceptor_gain	1.0000
4:78826152:TATGG:T	donor_loss	1.0000
4:78826154:TGGT:T	donor_loss	1.0000
4:78826155:GGTA:G	donor_loss	1.0000
4:78826156:G:T	donor_loss	1.0000
4:78826157:T:A	donor_loss	1.0000
4:78833576:TTCCA:T	acceptor_loss	1.0000
4:78833579:CAG:C	acceptor_loss	1.0000
4:78833580:A:AG	acceptor_gain	1.0000
4:78833581:G:GG	acceptor_gain	1.0000
4:78833581:GAA:G	acceptor_gain	1.0000
4:78833581:GAAA:G	acceptor_gain	1.0000
4:78833684:CGAGG:C	donor_loss	1.0000
4:78833685:GAG:G	donor_gain	1.0000
4:78833686:AG:A	donor_gain	1.0000
4:78833687:GG:G	donor_gain	1.0000
4:78833687:GGT:G	donor_loss	1.0000
4:78833688:G:GA	donor_loss	1.0000
4:78833688:G:GG	donor_gain	1.0000
4:78833689:TAA:T	donor_loss	1.0000

AlphaMissense

0 scored. Top likely-pathogenic:

dbSNP variants (sampled 300 via entrez): RS1000008704 (4:78784129 A>G), RS1000066012 (4:78831199 A>T), RS1000075556 (4:78790661 C>T), RS1000091559 (4:78808565 C>T), RS1000096492 (4:78831538 T>A), RS1000114491 (4:78808524 C>A), RS1000169956 (4:78778478 T>C), RS1000179194 (4:78902216 T>C), RS1000181712 (4:78844685 T>A,C), RS1000204360 (4:78793644 C>G,T), RS1000236413 (4:78850196 T>A,C), RS1000237370 (4:78897084 T>A), RS1000248260 (4:78865399 C>T), RS1000292252 (4:78889704 G>T), RS1000315916 (4:78882921 C>T)

Disease associations

OMIM: gene MIM:617648 | disease phenotypes:

GenCC curated gene-disease

Mondo (0):

Orphanet (0):

HPO phenotypes

0 total (0 of 0 shown, HPO-id order):

GWAS associations

22 associations (top):

Study	Trait	p-value
GCST005184_11	Common carotid intima-media thickness in HIV infection	4.000000e-06
GCST005184_4	Common carotid intima-media thickness in HIV infection	2.000000e-06
GCST005987_32	Albumin-globulin ratio	5.000000e-59
GCST005988_3	Serum albumin levels	2.000000e-17
GCST005989_9	Serum total protein levels	8.000000e-13
GCST005990_2	Non-albumin protein levels	8.000000e-47
GCST005993_4	Mean corpuscular hemoglobin	2.000000e-09
GCST005999_8	Aspartate aminotransferase levels	2.000000e-08
GCST010002_9	Refractive error	2.000000e-65
GCST011494_12	Daytime nap	1.000000e-16
GCST90002385_250	High light scatter reticulocyte count	5.000000e-13
GCST90002385_251	High light scatter reticulocyte count	6.000000e-11
GCST90002386_579	High light scatter reticulocyte percentage of red cells	2.000000e-10
GCST90002386_580	High light scatter reticulocyte percentage of red cells	5.000000e-11
GCST90002387_92	Immature fraction of reticulocytes	3.000000e-10
GCST90002390_214	Mean corpuscular hemoglobin	2.000000e-17
GCST90002397_11	Mean spheric corpuscular volume	7.000000e-13
GCST90002401_146	Platelet distribution width	3.000000e-11
GCST90002404_80	Red cell distribution width	8.000000e-11
GCST90002404_81	Red cell distribution width	1.000000e-11
GCST90002405_37	Reticulocyte count	2.000000e-12
GCST90002406_89	Reticulocyte fraction of red cells	3.000000e-09

EFO canonical traits (7, from GWAS)

EFO ID	Trait name
EFO:0005128	albumin:globulin ratio measurement
EFO:0004527	mean corpuscular hemoglobin
EFO:0004736	aspartate aminotransferase measurement
EFO:0007828	daytime rest measurement
EFO:0007986	reticulocyte count
EFO:0007984	platelet component distribution width
EFO:0009188	Red cell distribution width

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (1): CHEMBL4522 (SINGLE PROTEIN)

Molecules with ChEMBL bioactivity

60 molecules (phase ≥1), by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 337,470 (via chembl_molecule»patent_compound — counts attach to the compound, not the gene–compound relationship, so off-target/promiscuous molecules can dominate).

Molecule	Name	Phase	Patents
CHEMBL1078178	MOMELOTINIB	4	3,481
CHEMBL1287853	FEDRATINIB	4	3,554
CHEMBL1289926	AXITINIB	4	15,732
CHEMBL1614701	SELUMETINIB	4	10,221
CHEMBL1789941	RUXOLITINIB	4	11,547
CHEMBL189963	PALBOCICLIB	4	13,102
CHEMBL2035187	PACRITINIB	4	3,345
CHEMBL2103743	TOFACITINIB CITRATE	4	1,672
CHEMBL2105759	BARICITINIB	4	6,741
CHEMBL221959	TOFACITINIB	4	10,408
CHEMBL288441	BOSUTINIB	4	12,255
CHEMBL3301607	FILGOTINIB	4	2,905
CHEMBL3301610	ABEMACICLIB	4	7,045
CHEMBL3301622	GILTERITINIB	4	2,395
CHEMBL477772	PAZOPANIB	4	15,540
CHEMBL502835	NINTEDANIB	4	8,545
CHEMBL535	SUNITINIB	4	79,020
CHEMBL553	ERLOTINIB	4	108,300
CHEMBL601719	CRIZOTINIB	4	14,403
CHEMBL608533	MIDOSTAURIN	4	7,259
CHEMBL2105728	CRENOLANIB	3
CHEMBL274654	ORANTINIB	3
CHEMBL300138	ENZASTAURIN	3
CHEMBL31965	CANERTINIB	3
CHEMBL38380	FASUDIL	3
CHEMBL522892	DOVITINIB	3
CHEMBL603469	LESTAURTINIB	3
CHEMBL91829	RUBOXISTAURIN	3
CHEMBL1614713	CC-401	2
CHEMBL1667969	SAR-407899 FREE BASE	2

PharmGKB: 1 entry (VIP=true, CPIC=false)

GtoPdb / IUPHAR curated pharmacology

(IUPHAR/BPS Guide to Pharmacology — expert-curated)

Target class: enzyme — Numb-associated kinase (NAK) family

Most potent curated ligand interactions (3 total), top 3:

Ligand	Action	Affinity	Parameter
compound 6 [PMID: 34333981]	Inhibition	7.42	pIC50
compound 13 [PMID: 34333981]	Inhibition	7.4	pIC50
baricitinib	Inhibition	7.4	pKd

Binding affinities (BindingDB)

12 measured of 12 human assays (12 total across all organisms); most potent 12 below. Values come from heterogeneous assays and are not directly comparable.

Ligand	Measure	Value
Staurosporine	KD	1.7 nM
PKC-412	KD	190 nM
(3Z)-4-amino-5-fluoro-3-[5-(4-methylpiperazino)-1,3-dihydrobenzimidazol-2-ylidene]carbostyril	KD	520 nM
(18S)-18-[(dimethylamino)methyl]-17-oxa-4,14,21-triazahexacyclo[19.6.1.1^{7,14}.0^{2,6}.0^{8,13}.0^{22,27}]nonacosa-1(28),2(6),7(29),8(13),9,11,22(27),23,25-nonaene-3,5-dione	KD	700 nM
N-[4-({4-[(3-methyl-1H-pyrazol-5-yl)amino]-6-(4-methylpiperazin-1-yl)pyrimidin-2-yl}sulfanyl)phenyl]cyclopropanecarboxamide	KD	1100 nM
ERLOTINIB HYDROCHLORIDE	KD	1200 nM
CI-1033	KD	1700 nM
5-[(Z)-(5-fluoranyl-2-oxidanylidene-1H-indol-3-ylidene)methyl]-2,4-dimethyl-N-[(2S)-3-morpholin-4-yl-2-oxidanyl-propyl]-1H-pyrrole-3-carboxamide	KD	2600 nM
5-({4-[(2,3-dimethyl-2H-indazol-6-yl)(methyl)amino]pyrimidin-2-yl}amino)-2-methylbenzene-1-sulfonamide	KD	2900 nM
1-Acyl-1H-[1,2,4]triazole-3,5-diamine Analogue 3b	KD	3100 nM
(E)-N-[4-(3-chloro-4-fluoro-anilino)-3-cyano-7-ethoxy-6-quinolyl]-4-(dimethylamino)but-2-enamide	KD	3500 nM
N-[2-(diethylamino)ethyl]-5-[(Z)-(5-fluoro-2-oxo-1,2-dihydro-3H-indol-3-ylidene)methyl]-2,4-dimethyl-1H-pyrrole-3-carboxamide	KD	3500 nM

ChEMBL bioactivities

184 potent at pChembl≥5 of 191 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).

pChembl	Type	Value	Unit	Molecule
9.66	Kd	0.22	nM	CHEMBL4290597
9.10	Kd	0.8	nM	Cerdulatinib Hydrochloride
9.00	Kd	1	nM	STAUROSPORINE
8.93	Kd	1.187	nM	CHEMBL3752910
8.75	ED50	1.796	nM	CHEMBL3752910
8.66	Kd	2.2	nM	NINTEDANIB
8.43	Kd	3.7	nM	STAUROSPORINE
8.42	Kd	3.8	nM	CHEMBL1077979
8.26	Kd	5.5	nM	SUNITINIB
8.25	Kd	5.6	nM	STAUROSPORINE
8.22	Kd	6	nM	CHEMBL3990456
8.22	IC50	6	nM	CHEMBL5188433
8.15	Kd	7	nM	CYC-116
8.12	Kd	7.5	nM	CHEMBL4284499
8.10	Kd	8	nM	RGB-286638
8.02	Kd	9.6	nM	KW-2449
8.00	IC50	10	nM	CHEMBL5184381
7.89	Kd	13	nM	SAR-407899 FREE BASE
7.89	Ki	13	nM	CHEMBL4516665
7.85	Kd	14	nM	XL-228
7.82	Kd	15	nM	PF-03814735
7.80	Kd	16	nM	LESTAURTINIB
7.77	Ki	17	nM	CHEMBL4534959
7.77	Ki	17	nM	CHEMBL4571548
7.77	Ki	17	nM	CHEMBL4535040
7.77	Ki	17	nM	CHEMBL4452939
7.72	Kd	19	nM	CHEMBL4576489
7.72	Ki	19	nM	CHEMBL4452360
7.70	Kd	20	nM	XL-019
7.70	Ki	20	nM	CHEMBL4531680
7.70	Kd	20	nM	BARICITINIB
7.70	IC50	20	nM	CHEMBL5202142
7.62	Kd	24	nM	CHEMBL4465866
7.60	Kd	25	nM	SP-600125
7.57	Ki	27	nM	CHEMBL4447403
7.57	Kd	27	nM	SU-014813
7.52	Ki	30	nM	CHEMBL4552310
7.52	IC50	30	nM	CHEMBL5205578
7.50	Kd	32	nM	FEDRATINIB
7.48	Ki	33	nM	CHEMBL4582326
7.47	Kd	34	nM	AT-9283
7.44	Ki	36	nM	CHEMBL4470026
7.43	Ki	37	nM	CHEMBL4542463
7.42	Kd	38	nM	SUNITINIB
7.42	IC50	38	nM	CHEMBL5083125
7.41	Kd	39	nM	PACRITINIB
7.40	IC50	40	nM	CHEMBL5079149
7.38	Ki	42	nM	CHEMBL4561238
7.35	Kd	45	nM	KW-2449
7.34	Kd	46	nM	GILTERITINIB

PubChem BioAssay actives

176 with measured affinity, of 602 total; 50 most potent distinct compounds. Largely complementary to BindingDB; screening values are coarse (µM, 4 dp), so sub-nM hits tie at the floor.

Compound	Assay	Type	Value	Unit
3-[(3R)-3-(4,5-dimethoxy-8-oxo-9,14,16-triazatetracyclo[8.7.0.02,7.011,15]heptadeca-1(17),2,4,6,10,12,15-heptaen-9-yl)piperidin-1-yl]-3-oxopropanenitrile	1415050: Binding affinity to DNA-tagged recombinant human BIKE (34 to 329 residues) expressed in bacterial expression system by KINOMEscan assay	kd	0.0002	uM
4-(cyclopropylamino)-2-[4-(4-ethylsulfonylpiperazin-1-yl)anilino]pyrimidine-5-carboxamide;hydrochloride	1424920: Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	kd	0.0008	uM
(2S,3R,4R,6R)-3-methoxy-2-methyl-4-(methylamino)-29-oxa-1,7,17-triazaoctacyclo[12.12.2.12,6.07,28.08,13.015,19.020,27.021,26]nonacosa-8,10,12,14,19,21,23,25,27-nonaen-16-one	1948630: Binding affinity to recombinant BMP2K (unknown origin) assessed as dissociation constant by DSF assay	kd	0.0010	uM
4-methyl-3-[(1-methyl-6-pyridin-3-ylpyrazolo[3,4-d]pyrimidin-4-yl)amino]-N-[3-(trifluoromethyl)phenyl]benzamide	2147948: Binding affinity to human BMP2K incubated for 45 mins by Kinobead based pull down assay	kd	0.0012	uM
methyl 2-hydroxy-3-[N-[4-[methyl-[2-(4-methylpiperazin-1-yl)acetyl]amino]phenyl]-C-phenylcarbonimidoyl]-1H-indole-6-carboxylate	625109: Binding constant for BIKE kinase domain	kd	0.0022	uM
(4S,6Z,9S,10S,12E)-9,10,18-trihydroxy-16-methoxy-4-methyl-3-oxabicyclo[12.4.0]octadeca-1(14),6,12,15,17-pentaene-2,8-dione	1876268: Binding affinity to BIKE (unknown origin) assessed as dissociation constant	kd	0.0038	uM
Sunitinib	435275: Binding constant for BIKE kinase domain	kd	0.0055	uM
methyl N-[4-[6-[(2S)-2-amino-2,4-dimethylpentoxy]-5-chloro-3-pyridinyl]-2-pyridinyl]carbamate	1904665: Inhibition of BIKE (unknown origin)	ic50	0.0060	uM
2-amino-2-cyclohexyl-N-[2-(1-methylpyrazol-4-yl)-9-oxo-3,10,11-triazatricyclo[6.4.1.04,13]trideca-1,4,6,8(13),11-pentaen-6-yl]acetamide	1424920: Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	kd	0.0060	uM
4-methyl-5-[2-(4-morpholin-4-ylanilino)pyrimidin-4-yl]-1,3-thiazol-2-amine	1424920: Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	kd	0.0070	uM
9-(cyclohexylmethyl)-4,5-dimethoxy-9,14,16-triazatetracyclo[8.7.0.02,7.011,15]heptadeca-1(17),2,4,6,10,12,15-heptaen-8-one	1415050: Binding affinity to DNA-tagged recombinant human BIKE (34 to 329 residues) expressed in bacterial expression system by KINOMEscan assay	kd	0.0075	uM
1-[3-[4-[[4-(2-methoxyethyl)piperazin-1-yl]methyl]phenyl]-4-oxo-1H-indeno[2,1-d]pyrazol-5-yl]-3-morpholin-4-ylurea	1424920: Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	kd	0.0080	uM
[4-[(E)-2-(1H-indazol-3-yl)ethenyl]phenyl]-piperazin-1-ylmethanone	625109: Binding constant for BIKE kinase domain	kd	0.0096	uM
methyl N-[4-[6-[(2S)-2-amino-2,4-dimethylpentoxy]-5-methyl-3-pyridinyl]-2-pyridinyl]carbamate	1904665: Inhibition of BIKE (unknown origin)	ic50	0.0100	uM
N-[6-[3-(cyclopropylsulfonylamino)phenyl]-1H-indazol-3-yl]cyclopropanecarboxamide	1547794: Displacement of Alexafluor labelled kinase tracer236 from biotinylated C-terminal Avi-tagged BMP2K kinase domain (38 to 345 residues) (unknown origin) expressed in Escherichia coli measured after 1.5 hrs by TR-FRET assay	ki	0.0130	uM
6-piperidin-4-yloxy-2H-isoquinolin-1-one	1424920: Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	kd	0.0130	uM
4-N-(5-cyclopropyl-1H-pyrazol-3-yl)-6-(4-methylpiperazin-1-yl)-2-N-[(3-propan-2-yl-1,2-oxazol-5-yl)methyl]pyrimidine-2,4-diamine	1424920: Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	kd	0.0140	uM
N-[2-[4-[[4-(cyclobutylamino)-5-(trifluoromethyl)pyrimidin-2-yl]amino]-11-azatricyclo[6.2.1.02,7]undeca-2(7),3,5-trien-11-yl]-2-oxoethyl]acetamide	1424920: Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	kd	0.0150	uM
(15S,16S,18R)-16-hydroxy-16-(hydroxymethyl)-15-methyl-28-oxa-4,14,19-triazaoctacyclo[12.11.2.115,18.02,6.07,27.08,13.019,26.020,25]octacosa-1,6,8,10,12,20,22,24,26-nonaen-3-one	507840: Binding affinity to BIKE	kd	0.0160	uM
N-[6-[3-(diethylsulfamoylamino)phenyl]-1H-indazol-3-yl]cyclopropanecarboxamide	1547794: Displacement of Alexafluor labelled kinase tracer236 from biotinylated C-terminal Avi-tagged BMP2K kinase domain (38 to 345 residues) (unknown origin) expressed in Escherichia coli measured after 1.5 hrs by TR-FRET assay	ki	0.0170	uM
N-[6-[3-(cyclopropylmethylsulfonylamino)phenyl]-1H-indazol-3-yl]cyclopropanecarboxamide	1547794: Displacement of Alexafluor labelled kinase tracer236 from biotinylated C-terminal Avi-tagged BMP2K kinase domain (38 to 345 residues) (unknown origin) expressed in Escherichia coli measured after 1.5 hrs by TR-FRET assay	ki	0.0170	uM
N-[6-[3-(cyclobutylsulfonylamino)phenyl]-1H-indazol-3-yl]cyclopropanecarboxamide	1547794: Displacement of Alexafluor labelled kinase tracer236 from biotinylated C-terminal Avi-tagged BMP2K kinase domain (38 to 345 residues) (unknown origin) expressed in Escherichia coli measured after 1.5 hrs by TR-FRET assay	ki	0.0170	uM
N-[6-[3-(2-methylpropylsulfonylamino)phenyl]-1H-indazol-3-yl]cyclopropanecarboxamide	1547794: Displacement of Alexafluor labelled kinase tracer236 from biotinylated C-terminal Avi-tagged BMP2K kinase domain (38 to 345 residues) (unknown origin) expressed in Escherichia coli measured after 1.5 hrs by TR-FRET assay	ki	0.0170	uM
N-[6-[3-(dimethylsulfamoylamino)phenyl]-1H-indazol-3-yl]cyclopropanecarboxamide	1547794: Displacement of Alexafluor labelled kinase tracer236 from biotinylated C-terminal Avi-tagged BMP2K kinase domain (38 to 345 residues) (unknown origin) expressed in Escherichia coli measured after 1.5 hrs by TR-FRET assay	ki	0.0190	uM
3-(2,2-difluoro-10,12-dimethyl-1-aza-3-azonia-2-boranuidatricyclo[7.3.0.03,7]dodeca-3,5,7,9,11-pentaen-4-yl)-N-[2-[2-[2-[2-[[(2S,3R,4R,6R)-3-methoxy-2-methyl-16-oxo-29-oxa-1,7,17-triazaoctacyclo[12.12.2.12,6.07,28.08,13.015,19.020,27.021,26]nonacosa-8,10,12,14,19,21,23,25,27-nonaen-4-yl]-methylamino]ethoxy]ethoxy]ethoxy]ethyl]propanamide	1526251: Binding affinity to recombinant full-length N-terminal His-FLAG-GST-tagged BMP2K (unknown origin) expressed in baculovirus infected Sf9 insect cells incubated for 1 hr by TR-FRET assay	kd	0.0190	uM
methyl N-[4-[5-[(2S)-2-amino-2,4-dimethylpentoxy]-6-(difluoromethyl)-2-pyridinyl]-2-pyridinyl]carbamate	1904665: Inhibition of BIKE (unknown origin)	ic50	0.0200	uM
N-[6-[3-[[ethyl(methyl)sulfamoyl]amino]phenyl]-1H-indazol-3-yl]cyclopropanecarboxamide	1547794: Displacement of Alexafluor labelled kinase tracer236 from biotinylated C-terminal Avi-tagged BMP2K kinase domain (38 to 345 residues) (unknown origin) expressed in Escherichia coli measured after 1.5 hrs by TR-FRET assay	ki	0.0200	uM
Baricitinib	1769943: Binding affinity to BIKE (unknown origin)	kd	0.0200	uM
N-[4-[2-(4-morpholin-4-ylanilino)pyrimidin-4-yl]phenyl]pyrrolidine-2-carboxamide	1424920: Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	kd	0.0200	uM
3-(2,2-difluoro-10,12-dimethyl-1-aza-3-azonia-2-boranuidatricyclo[7.3.0.03,7]dodeca-3,5,7,9,11-pentaen-4-yl)-N-[2-[2-[2-[2-[[(2S,3R,4R,6R)-3-methoxy-2-methyl-16-oxo-29-oxa-1,7,17-triazaoctacyclo[12.12.2.12,6.07,28.08,13.015,19.020,27.021,26]nonacosa-8,10,12,14,19,21,23,25,27-nonaen-4-yl]amino]ethoxy]ethoxy]ethoxy]ethyl]propanamide	1526251: Binding affinity to recombinant full-length N-terminal His-FLAG-GST-tagged BMP2K (unknown origin) expressed in baculovirus infected Sf9 insect cells incubated for 1 hr by TR-FRET assay	kd	0.0240	uM
14,15-diazatetracyclo[7.6.1.02,7.013,16]hexadeca-1(15),2,4,6,9(16),10,12-heptaen-8-one	256571: Average Binding Constant for BIKE; NA=Not Active at 10 uM	kd	0.0250	uM
5-[(Z)-(5-fluoro-2-oxo-1H-indol-3-ylidene)methyl]-N-[(2S)-2-hydroxy-3-morpholin-4-ylpropyl]-2,4-dimethyl-1H-pyrrole-3-carboxamide	435275: Binding constant for BIKE kinase domain	kd	0.0270	uM
N-[6-[3-[(3,3,3-trifluoropropylsulfonylamino)methyl]phenyl]-1H-indazol-3-yl]cyclopropanecarboxamide	1547794: Displacement of Alexafluor labelled kinase tracer236 from biotinylated C-terminal Avi-tagged BMP2K kinase domain (38 to 345 residues) (unknown origin) expressed in Escherichia coli measured after 1.5 hrs by TR-FRET assay	ki	0.0270	uM
methyl N-[4-[5-[(2S)-2-amino-2,4-dimethylpentoxy]-6-chloro-2-pyridinyl]-2-pyridinyl]carbamate	1904665: Inhibition of BIKE (unknown origin)	ic50	0.0300	uM
N-[6-[3-(propylsulfonylamino)phenyl]-1H-indazol-3-yl]cyclopropanecarboxamide	1547794: Displacement of Alexafluor labelled kinase tracer236 from biotinylated C-terminal Avi-tagged BMP2K kinase domain (38 to 345 residues) (unknown origin) expressed in Escherichia coli measured after 1.5 hrs by TR-FRET assay	ki	0.0300	uM
Fedratinib	625109: Binding constant for BIKE kinase domain	kd	0.0320	uM
N-[6-[3-[(2,2,2-trifluoroethylsulfonylamino)methyl]phenyl]-1H-indazol-3-yl]cyclopropanecarboxamide	1547794: Displacement of Alexafluor labelled kinase tracer236 from biotinylated C-terminal Avi-tagged BMP2K kinase domain (38 to 345 residues) (unknown origin) expressed in Escherichia coli measured after 1.5 hrs by TR-FRET assay	ki	0.0330	uM
1-cyclopropyl-3-[5-[6-(morpholin-4-ylmethyl)-1H-benzimidazol-2-yl]-1H-pyrazol-4-yl]urea	1424920: Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	kd	0.0340	uM
N-[6-[3-[[[ethyl(methyl)sulfamoyl]amino]methyl]phenyl]-1H-indazol-3-yl]cyclopropanecarboxamide	1547794: Displacement of Alexafluor labelled kinase tracer236 from biotinylated C-terminal Avi-tagged BMP2K kinase domain (38 to 345 residues) (unknown origin) expressed in Escherichia coli measured after 1.5 hrs by TR-FRET assay	ki	0.0360	uM
N-[6-[3-[(cyclopropylmethylsulfonylamino)methyl]phenyl]-1H-indazol-3-yl]cyclopropanecarboxamide	1547794: Displacement of Alexafluor labelled kinase tracer236 from biotinylated C-terminal Avi-tagged BMP2K kinase domain (38 to 345 residues) (unknown origin) expressed in Escherichia coli measured after 1.5 hrs by TR-FRET assay	ki	0.0370	uM
4-[[[5-bromo-2-[3-(morpholin-4-ylmethyl)anilino]pyrimidin-4-yl]amino]methyl]benzenesulfonamide	1823780: Inhibition of recombinant human BIKe using peptide as substrate incubated for 120 mins in presence of [gamma-33ATP] by scintillation counting based radiometry assay	ic50	0.0380	uM
Pacritinib	1424920: Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	kd	0.0390	uM
N-[3-[[5-bromo-4-[(4-sulfamoylphenyl)methylamino]pyrimidin-2-yl]amino]phenyl]pyrrolidine-1-carboxamide	1823780: Inhibition of recombinant human BIKe using peptide as substrate incubated for 120 mins in presence of [gamma-33ATP] by scintillation counting based radiometry assay	ic50	0.0400	uM
N-[6-[3-[[[methyl(2,2,2-trifluoroethyl)sulfamoyl]amino]methyl]phenyl]-1H-indazol-3-yl]cyclopropanecarboxamide	1547794: Displacement of Alexafluor labelled kinase tracer236 from biotinylated C-terminal Avi-tagged BMP2K kinase domain (38 to 345 residues) (unknown origin) expressed in Escherichia coli measured after 1.5 hrs by TR-FRET assay	ki	0.0420	uM
Gilteritinib	1424920: Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.	kd	0.0460	uM
(3Z)-5-[(2,6-dichlorophenyl)methylsulfonyl]-3-[[3,5-dimethyl-4-[(2R)-2-(pyrrolidin-1-ylmethyl)pyrrolidine-1-carbonyl]-1H-pyrrol-2-yl]methylidene]-1H-indol-2-one	625109: Binding constant for BIKE kinase domain	kd	0.0470	uM
N-[6-[3-[(2-fluorophenyl)methylsulfonylamino]phenyl]-1H-indazol-3-yl]cyclopropanecarboxamide	1547794: Displacement of Alexafluor labelled kinase tracer236 from biotinylated C-terminal Avi-tagged BMP2K kinase domain (38 to 345 residues) (unknown origin) expressed in Escherichia coli measured after 1.5 hrs by TR-FRET assay	ki	0.0510	uM
N-[6-[3-[(3-fluorophenyl)methylsulfonylamino]phenyl]-1H-indazol-3-yl]cyclopropanecarboxamide	1547794: Displacement of Alexafluor labelled kinase tracer236 from biotinylated C-terminal Avi-tagged BMP2K kinase domain (38 to 345 residues) (unknown origin) expressed in Escherichia coli measured after 1.5 hrs by TR-FRET assay	ki	0.0530	uM
4-amino-5-fluoro-3-[6-(4-methylpiperazin-1-yl)-1H-benzimidazol-2-yl]-1H-quinolin-2-one	435275: Binding constant for BIKE kinase domain	kd	0.0540	uM
N-[6-[3-[(2-methylpropylsulfonylamino)methyl]phenyl]-1H-indazol-3-yl]cyclopropanecarboxamide	1547794: Displacement of Alexafluor labelled kinase tracer236 from biotinylated C-terminal Avi-tagged BMP2K kinase domain (38 to 345 residues) (unknown origin) expressed in Escherichia coli measured after 1.5 hrs by TR-FRET assay	ki	0.0590	uM

CTD chemical–gene interactions

50 total (human), top 30 by PubMed support.

Chemical	Actions (top 5)	PubMed papers
Valproic Acid	increases expression, affects expression, decreases methylation	3
Resveratrol	affects cotreatment, decreases expression, increases expression	2
Benzo(a)pyrene	affects methylation, decreases expression	2
Indomethacin	affects cotreatment, decreases expression	2
Tobacco Smoke Pollution	decreases expression, increases expression	2
Cadmium Chloride	decreases expression, increases abundance, increases expression	2
bisphenol F	affects cotreatment, decreases expression	1
testosterone enanthate	affects expression	1
methylmercuric chloride	decreases expression	1
pirinixic acid	decreases expression, increases activity, affects binding	1
bisphenol A	decreases methylation	1
glycidyl methacrylate	increases expression	1
beta-lapachone	decreases expression	1
tris(1,3-dichloro-2-propyl)phosphate	increases expression	1
potassium chromate(VI)	decreases expression, affects cotreatment	1
coumarin	decreases phosphorylation	1
epigallocatechin gallate	affects cotreatment, decreases expression	1
di-n-butylphosphoric acid	affects expression	1
pentabromodiphenyl ether	decreases expression	1
abrine	increases expression	1
2,2’,4,4’-tetrabromodiphenyl ether	decreases expression	1
jinfukang	affects cotreatment, decreases expression	1
2-amino-7-(4-fluoro-2-(6-methoxypyridin-2-yl)phenyl)-4-methyl-7,8-dihydropyrido(4,3-d)pyrimidin-5(6H)-one	decreases expression, increases activity	1
Sunitinib	increases expression	1
Amiodarone	increases expression	1
Cadmium	decreases expression, increases abundance	1
Caffeine	decreases phosphorylation	1
Carbamazepine	affects expression	1
Cisplatin	affects cotreatment, decreases expression	1
Dexamethasone	affects cotreatment, decreases expression	1

ChEMBL screening assays

172 unique, capped per target: 172 binding

Representative assays (with source publication via chembl_document):

Assay ID	Type	Description	Source paper
CHEMBL1017876	Binding	Inhibition of BIKE assessed as enzyme activity relative to control	Examining the chirality, conformation and selective kinase inhibition of 3-((3R,4R)-4-methyl-3-(methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino)piperidin-1-yl)-3-oxopropanenitrile (CP-690,550). — J Med Chem

Cellosaurus cell lines

3 cell lines: 3 cancer cell line

First 10 cell lines (id-ordered, not curated):

Cellosaurus	Name	Category	Sex
CVCL_B1LD	Abcam HeLa BMP2K KO	Cancer cell line	Female
CVCL_SF34	HAP1 BMP2K (-) 1	Cancer cell line	Male
CVCL_SF35	HAP1 BMP2K (-) 2	Cancer cell line	Male

Clinical trials (associated diseases)

0 trials via MONDO — disease-level, not drug-specific.