CCNB1
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Summary
CCNB1 (cyclin B1, HGNC:1579) is a protein-coding gene on chromosome 5q13.2, encoding G2/mitotic-specific cyclin-B1 (P14635). Essential for the control of the cell cycle at the G2/M (mitosis) transition. It is a selective cancer dependency (DepMap: 74.0% of cell lines).
The protein encoded by this gene is a regulatory protein involved in mitosis. The gene product complexes with p34(cdc2) to form the maturation-promoting factor (MPF). The encoded protein is necessary for proper control of the G2/M transition phase of the cell cycle.
Source: NCBI Gene 891 — RefSeq curated summary.
At a glance
- Clinical variants (ClinVar): 66 total
- Druggable target: yes — 34 molecules with ChEMBL bioactivity
- Cancer dependency (DepMap): dependent in 74.0% of screened cell lines
- MANE Select transcript:
NM_031966
Identifiers
Gene identifiers
| Field | Value |
|---|---|
| HGNC ID | HGNC:1579 |
| Approved symbol | CCNB1 |
| Name | cyclin B1 |
| Location | 5q13.2 |
| Locus type | gene with protein product |
| Status | Approved |
| Ensembl gene | ENSG00000134057 |
| Ensembl biotype | protein_coding |
| OMIM | 123836 |
| Entrez | 891 |
Gene structure
Transcript identifiers
Ensembl transcripts: 26 — 24 protein_coding, 1 nonsense_mediated_decay, 1 retained_intron
ENST00000256442, ENST00000503507, ENST00000505500, ENST00000506572, ENST00000507798, ENST00000508407, ENST00000513102, ENST00000870642, ENST00000924407, ENST00000924408, ENST00000924409, ENST00000924410, ENST00000924411, ENST00000924412, ENST00000924413, ENST00000924414, ENST00000924415, ENST00000924416, ENST00000924417, ENST00000924418, ENST00000924419, ENST00000924420, ENST00000924421, ENST00000924422, ENST00000924423, ENST00000960692
RefSeq mRNA: 3 — MANE Select: NM_031966
NM_001354844, NM_001354845, NM_031966
CCDS: CCDS3997
Canonical transcript exons
ENST00000256442 — 9 exons
| Exon | Start | End |
|---|---|---|
| ENSE00000972025 | 69174251 | 69174409 |
| ENSE00000972026 | 69174877 | 69175113 |
| ENSE00000972027 | 69175397 | 69175537 |
| ENSE00000972028 | 69177239 | 69177349 |
| ENSE00001821671 | 69167150 | 69167283 |
| ENSE00001938963 | 69177524 | 69178245 |
| ENSE00003557310 | 69168173 | 69168343 |
| ENSE00003614392 | 69167908 | 69168078 |
| ENSE00003639776 | 69171270 | 69171452 |
Expression profiles
Bgee: expression breadth ubiquitous, 224 present calls, max score 99.83.
FANTOM5 (CAGE): breadth ubiquitous, TPM avg 82.8396 / max 1085.8300, expressed in 1759 samples.
FANTOM5 promoters (2 alternative TSS)
| Promoter ID | TPM avg | Samples expressed |
|---|---|---|
| 56833 | 80.8225 | 1758 |
| 56834 | 2.0171 | 863 |
Top tissues by expression
288 total, by Bgee expression score (0-100, higher = more expressed):
| Tissue | Anatomy ID | Expression score | Quality |
|---|---|---|---|
| secondary oocyte | CL:0000655 | 99.83 | gold quality |
| oocyte | CL:0000023 | 99.76 | gold quality |
| ventricular zone | UBERON:0003053 | 99.26 | gold quality |
| primordial germ cell in gonad | CL:0000670 ∩ UBERON:0000991 | 97.47 | gold quality |
| ganglionic eminence | UBERON:0004023 | 97.03 | gold quality |
| endometrium epithelium | UBERON:0004811 | 96.77 | gold quality |
| embryo | UBERON:0000922 | 96.70 | gold quality |
| male germ line stem cell (sensu Vertebrata) in testis | CL:0000089 ∩ UBERON:0000473 | 95.59 | gold quality |
| mucosa of transverse colon | UBERON:0004991 | 93.88 | gold quality |
| stromal cell of endometrium | CL:0002255 | 93.82 | gold quality |
| lower esophagus mucosa | UBERON:0035834 | 92.69 | gold quality |
| left testis | UBERON:0004533 | 92.05 | gold quality |
| esophagus mucosa | UBERON:0002469 | 91.81 | gold quality |
| right testis | UBERON:0004534 | 91.73 | gold quality |
| testis | UBERON:0000473 | 91.36 | gold quality |
| esophagus squamous epithelium | UBERON:0006920 | 91.12 | gold quality |
| rectum | UBERON:0001052 | 90.96 | gold quality |
| sperm | CL:0000019 | 90.89 | gold quality |
| trabecular bone tissue | UBERON:0002483 | 90.66 | gold quality |
| bone marrow | UBERON:0002371 | 90.27 | gold quality |
| vermiform appendix | UBERON:0001154 | 90.25 | gold quality |
| bone element | UBERON:0001474 | 89.50 | gold quality |
| adrenal tissue | UBERON:0018303 | 89.48 | gold quality |
| epithelium of esophagus | UBERON:0001976 | 88.50 | gold quality |
| male germ cell | CL:0000015 | 88.44 | gold quality |
| gingival epithelium | UBERON:0001949 | 88.40 | gold quality |
| oral cavity | UBERON:0000167 | 88.01 | gold quality |
| bone marrow cell | CL:0002092 | 87.16 | gold quality |
| gingiva | UBERON:0001828 | 86.16 | gold quality |
| squamous epithelium | UBERON:0006914 | 85.94 | gold quality |
Single-cell (SCXA)
Detected in 21 experiment(s), a significant marker in 15.
| Experiment | Marker? | Max mean expression |
|---|---|---|
| E-MTAB-10485 | yes | 1406.86 |
| E-GEOD-99795 | yes | 1300.76 |
| E-MTAB-7249 | yes | 1206.46 |
| E-MTAB-11121 | yes | 1166.78 |
| E-MTAB-7052 | yes | 1032.55 |
| E-MTAB-8894 | yes | 1004.14 |
| E-CURD-79 | yes | 941.20 |
| E-MTAB-6505 | yes | 684.64 |
| E-MTAB-10290 | yes | 540.96 |
| E-HCAD-10 | yes | 507.72 |
| E-HCAD-13 | yes | 453.95 |
| E-CURD-114 | yes | 319.14 |
| E-GEOD-100618 | yes | 257.59 |
| E-GEOD-125970 | yes | 228.00 |
| E-MTAB-6911 | no | 1920.57 |
Regulation
Is transcription factor: no
Upstream regulators (CollecTRI, top): AGO1, AR, BRCA1, CEBPA, CREB1, DROSHA, E2F1, E2F3, E2F4, ERG, ESR2, FOXM1, FOXO1, GPER1, HLX, IRF1, IRF4, KLF4, KLF5, MAX, MXI1, MYB, MYBL2, MYC, MYOD1, NCOR2, NFKB1, NFKB, NKX2-1, OLIG2, PPARA, PTTG1, RBCK1, RELA, RPRD1B, SP1, SSRP1, STOX1, TBP, TFAP2A
miRNA regulators (miRDB)
57 targeting CCNB1, 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-3163 | 100.00 | 77.23 | 8605 |
| HSA-MIR-6798-5P | 100.00 | 65.77 | 699 |
| HSA-MIR-513B-5P | 99.99 | 69.96 | 2150 |
| HSA-MIR-4282 | 99.99 | 75.36 | 6408 |
| HSA-MIR-548N | 99.98 | 71.94 | 4170 |
| HSA-MIR-12136 | 99.98 | 72.81 | 5713 |
| HSA-MIR-607 | 99.97 | 73.62 | 5593 |
| HSA-MIR-548AA | 99.96 | 70.64 | 3753 |
| HSA-MIR-548AP-3P | 99.96 | 70.64 | 3753 |
| HSA-MIR-548T-3P | 99.96 | 70.64 | 3753 |
| HSA-MIR-559 | 99.95 | 72.28 | 3609 |
| HSA-MIR-548AB | 99.95 | 71.31 | 3488 |
| HSA-MIR-548A-5P | 99.94 | 71.27 | 3482 |
| HSA-MIR-548AD-5P | 99.94 | 71.23 | 3502 |
| HSA-MIR-548AE-5P | 99.94 | 71.23 | 3502 |
| HSA-MIR-548AK | 99.94 | 71.24 | 3488 |
| HSA-MIR-548AM-5P | 99.94 | 71.24 | 3488 |
| HSA-MIR-548AP-5P | 99.94 | 71.14 | 3489 |
| HSA-MIR-548AQ-5P | 99.94 | 71.34 | 3426 |
| HSA-MIR-548AR-5P | 99.94 | 71.28 | 3515 |
| HSA-MIR-548AS-5P | 99.94 | 71.22 | 3482 |
| HSA-MIR-548AU-5P | 99.94 | 71.24 | 3488 |
| HSA-MIR-548AY-5P | 99.94 | 71.23 | 3502 |
| HSA-MIR-548B-5P | 99.94 | 71.23 | 3502 |
| HSA-MIR-548BB-5P | 99.94 | 71.27 | 3509 |
| HSA-MIR-548C-5P | 99.94 | 71.24 | 3488 |
| HSA-MIR-548D-5P | 99.94 | 71.23 | 3502 |
| HSA-MIR-548H-5P | 99.94 | 71.24 | 3488 |
| HSA-MIR-548I | 99.94 | 71.25 | 3481 |
| HSA-MIR-548J-5P | 99.94 | 71.14 | 3489 |
Functional genomics
DepMap (CRISPR cell-line fitness): dependent in 74.0% of screened cell lines.
Literature-anchored findings (GeneRIF, showing 40)
- Up-regulation of CCNB1 is responsible, at least in part, for radioresistance after fractionated irradiation. (PMID:11260656)
- expression is related to apoptosis in thymus (PMID:11642719)
- Cyclin b1 promoter activity and functional cdk1 complex formation in G1 phase of human breast cancer cells (PMID:11779217)
- cyclin b1 is overexpressed in laryngeal squamous cell carcinoma (PMID:11809526)
- Overexpression of B-type cyclins alters chromosomal segregation (PMID:11960377)
- The human cyclin Bl gene is cell cycle regulated with maximal activity during G(2)/M. We examined the role of histone deacetylation in cyclin Bl regulation using the histone deacetylase inhibitor trichostatin A (TSA). (PMID:12054478)
- Overexpression of cyclin B1 is associated with esophageal disease progression (PMID:12115375)
- H-ras participates in pathways that regulate cyclin B1 expression and therefore controls the G2/M checkpoint in a p53-independent manner. (PMID:12379461)
- Nuclear accumulation is necessary for cyclin B1-dependent apoptosis. This is consistent with the idea that localization of cyclin B1 is among the factors determining the cellular decision to undergo apoptosis in response to DNA damage. (PMID:12424202)
- regulation of subcellular localization by cooperative phosphorylation, including activity of polo-like kinase 1 (PMID:12447691)
- reduction of nuclear level by induction of GADD45 (PMID:12483522)
- The limitation of detecting cyclin B1 is due to its unscheduled expression, rending cyclin B1 being detected at different time-spots in the G(1) phase. (PMID:12515609)
- Cyclin B1 transcription is enhanced by the p300 coactivator and regulated during the cell cycle by a cell cycle genes homology region-dependent repression mechanism. (PMID:12586340)
- increases significantly during colorectal carcinogenesis and during later metastasis to lymph nodes (PMID:12684677)
- in mammalian cells, the majority of cyclin B1 must be destroyed before the cell can enter anaphase (PMID:12865421)
- data suggest the maintenance of Cdk1/cyclin B1 activity in HCMV-infected cells can be explained by 3 mechanisms: accumulation of cyclin B1, inactivation of negative regulatory pathways for Cdk1, accumulation of positive factors that promote Cdk1 activity (PMID:14645578)
- Expression of Cyclin B1 correlated with differentiation and vascular invasion in NSCLC; Cyclin B1 overexpression associated with higher mean values for Ki-67 proliferative index and proliferating cell nuclear antigen labeling index and poorer prognosis. (PMID:14760118)
- exposure to nonrepairable DNA damage leads to nuclear accumulation of inactive cyclin B1-Cdk1 complexes (PMID:15181148)
- role in regulating Fas ligand transcription (PMID:15215233)
- wild-type p53 mediates transcriptional repression of cyclin B1 through the Sp1 transcription factor (PMID:15710382)
- results show that human papillomavirus type 16 E1 E4 does not inhibit the kinase activity of the Cdk1/cyclin B1 complex; instead, 16E1 E4 uses a novel mechanism in which it sequesters Cdk1/cyclin B1 onto the cytokeratin network (PMID:15767402)
- results strongly indicate that in response to genotoxic stress, Cdk5 activator-binding protein C53(C53) serves as an important regulatory component of DNA damage checkpoint through modulating cyclin dependent kinase 1-cyclin B1 function (PMID:15790566)
- Altered expression is associated with therapy failure and death in patients with multiple types of cancer. (PMID:15931389)
- in nasopharyngeal carcinoma cells, SarCNU-induced apoptosis is p53-dependent while SarCNU-induced G2/M arrest is mediated by the cyclin B1-cdc-2 complex (PMID:16142332)
- results indicated that chronic Pim-1 kinase overexpression dysregulates cyclin B1 protein expression, which contributes to the development of polyploidy by delaying cytokinesis (PMID:16221667)
- Cdc2/cyclin B1 interacts with and modulates inositol 1,4,5-trisphosphate receptor (type 1) functions. (PMID:16237118)
- Study demonstrates the independent prognostic value of cyclin B1 in diffuse large B-cell lymphoma. (PMID:16273239)
- Cyclin G1 enhanced radiation sensitivity by overriding radiation-induced G2 arrest through transcriptional upregulation of cyclin B1. (PMID:16322753)
- Increased intratumoral cyclin B1 positivity and aberrant localization of signals within the cytoplasm of tumor cells is positively correlated with tendency towards tumor progression: significant role of cyclin B1 in development and pathogenesis of RCC (PMID:16557593)
- Up-regulation of cyclin B1 expression occurred in cervical cancer and may play an important role in cervical carcinogenesis. (PMID:16614707)
- hCdc14A is differentially expressed in human cancer cells and can interact with both p53 and the Cdk1/cyclin B complex; it may play a role in carcinogenesis (PMID:16784539)
- Cdk1-mediated phosphorylation of S439 stabilizes mature SREBP1 during mitosis, thereby preserving a critical pool of active transcription factors to support lipid synthesis. (PMID:16880739)
- Mip/LIN-9 is required for the expression of B-Myb, and both proteins collaborate in the control of the cell cycle progression via the regulation of S phase and cyclin A, cyclin B, and CDK1 (PMID:17098733)
- Cyclin B1 overexpression was associated with occult cervical lymph node metastases in tongue carcinoma (PMID:17167975)
- ATM regulates G(2)/M checkpoint recovery through inhibitory phosphorylations of Artemis that occur soon after DNA damage, thus setting a molecular switch that, hours later upon completion of DNA repair, allows activation of the Cdk1-cyclin B complex. (PMID:17242184)
- c-Myb protein plays a previously unappreciated role in the G(2)/M cell cycle transition of normal and malignant human hematopoietic cells (PMID:17242210)
- During both meiotic and mitotic exit in Xenopus eggs, recombinant human cyclin B1-associated cdk1 underwent transient inhibitory phosphorylation at tyr-15. Recominant cyclin B1-cdk1 activity fell more rapidly than the cyclin B1 content. (PMID:17327911)
- Results suggest that an onocogenic role of overexpressed cyclin B1 is mainly mediated in nuclei of breast carcinoma cells, and the nuclear translocation is regulated by polo-like kinase 1 and 14-3-3sigma. (PMID:17359284)
- data strongly argue against mutational events of CDK1, cyclinB1 and cyclinA2 to play a role in gangliogliomas or focal cortical dysplasia (PMID:17359356)
- p38 signaling pathway triggering cyclin B1 proteolysis after arsenite exposure may play an important role in connecting G(2) arrest with apoptosis or genome instability. (PMID:17373649)
Cross-species orthologs
15 orthologs
| Organism | Symbol | Gene ID |
|---|---|---|
| danio_rerio | ccnb1 | ENSDARG00000051923 |
| mus_musculus | Ccnb1 | ENSMUSG00000041431 |
| rattus_norvegicus | Ccnb1 | ENSRNOG00000058539 |
| drosophila_melanogaster | CycA | FBGN0000404 |
| drosophila_melanogaster | CycB | FBGN0000405 |
| drosophila_melanogaster | CycD | FBGN0010315 |
| drosophila_melanogaster | CycE | FBGN0010382 |
| caenorhabditis_elegans | WBGENE00000863 | |
| caenorhabditis_elegans | WBGENE00000864 | |
| caenorhabditis_elegans | WBGENE00000865 | |
| caenorhabditis_elegans | WBGENE00000866 | |
| caenorhabditis_elegans | cyb-2.2 | WBGENE00000867 |
| caenorhabditis_elegans | WBGENE00000870 | |
| caenorhabditis_elegans | cye-1 | WBGENE00000871 |
| caenorhabditis_elegans | WBGENE00017259 |
Paralogs (18): CCNE1 (ENSG00000105173), CCNP (ENSG00000105219), CCNJ (ENSG00000107443), CCND1 (ENSG00000110092), CCND3 (ENSG00000112576), CCNG1 (ENSG00000113328), CCNI (ENSG00000118816), CCND2 (ENSG00000118971), CCNA1 (ENSG00000133101), CCNJL (ENSG00000135083), CCNG2 (ENSG00000138764), CCNA2 (ENSG00000145386), CCNB3 (ENSG00000147082), CCNO (ENSG00000152669), CCNB2 (ENSG00000157456), CCNF (ENSG00000162063), CCNE2 (ENSG00000175305), CCNI2 (ENSG00000205089)
Protein
Protein identifiers
G2/mitotic-specific cyclin-B1 — P14635 (reviewed: P14635)
All UniProt accessions (5): P14635, D6RHI0, E9PC90, H0Y9U8, H0YA62
UniProt curated annotations — full annotation on UniProt →
Function. Essential for the control of the cell cycle at the G2/M (mitosis) transition.
Subunit / interactions. Interacts with the CDC2 protein kinase to form a serine/threonine kinase holoenzyme complex also known as maturation promoting factor (MPF). The cyclin subunit imparts substrate specificity to the complex. Binds HEI10. Interacts with catalytically active RALBP1 and CDC2 during mitosis to form an endocytotic complex during interphase. Interacts with CCNF; interaction is required for nuclear localization. Interacts with CDK5RAP3. Interacts with RFPL4A and UBE2A. Interacts with INCA1.
Subcellular location. Cytoplasm. Nucleus. Cytoskeleton. Microtubule organizing center. Centrosome.
Post-translational modifications. Ubiquitinated by the SCF(NIPA) complex during interphase, leading to its destruction. Deubiquitinated by USP22 during G2/M phase. Phosphorylated by PLK1 at Ser-133 on centrosomes during prophase: phosphorylation by PLK1 does not cause nuclear import. Phosphorylation at Ser-147 was also reported to be mediated by PLK1 but Ser-133 seems to be the primary phosphorylation site.
Similarity. Belongs to the cyclin family. Cyclin AB subfamily.
Isoforms (2)
| UniProt ID | Names | Canonical? |
|---|---|---|
| P14635-1 | 1 | yes |
| P14635-2 | 2 |
RefSeq proteins (3): NP_001341773, NP_001341774, NP_114172* (*=MANE)
Domains & families (InterPro)
| ID | Name | Type |
|---|---|---|
| IPR004367 | Cyclin_C-dom | Domain |
| IPR006671 | Cyclin_N | Domain |
| IPR013763 | Cyclin-like_dom | Domain |
| IPR036915 | Cyclin-like_sf | Homologous_superfamily |
| IPR039361 | Cyclin | Family |
| IPR046965 | Cyclin_A/B-like | Family |
| IPR048026 | CCNB1_first_cyclin-box | Domain |
| IPR048258 | Cyclins_cyclin-box | Conserved_site |
Pfam: PF00134, PF02984
UniProt features (41 total): helix 20, modified residue 6, region of interest 4, turn 3, mutagenesis site 2, sequence conflict 2, strand 2, chain 1, splice variant 1
Structure
Experimental structures (PDB)
14 structures.
| PDB | Method | Resolution (Å) |
|---|---|---|
| 6GU2 | X-RAY DIFFRACTION | 2 |
| 5LQF | X-RAY DIFFRACTION | 2.06 |
| 4Y72 | X-RAY DIFFRACTION | 2.3 |
| 5HQ0 | X-RAY DIFFRACTION | 2.3 |
| 9FH9 | ELECTRON MICROSCOPY | 2.5 |
| 6GU3 | X-RAY DIFFRACTION | 2.65 |
| 4YC3 | X-RAY DIFFRACTION | 2.7 |
| 6GU4 | X-RAY DIFFRACTION | 2.73 |
| 2B9R | X-RAY DIFFRACTION | 2.9 |
| 2JGZ | X-RAY DIFFRACTION | 2.9 |
| 9SKQ | ELECTRON MICROSCOPY | 3.4 |
| 8TAU | ELECTRON MICROSCOPY | 3.5 |
| 7NJ0 | ELECTRON MICROSCOPY | 3.6 |
| 8TAR | ELECTRON MICROSCOPY | 4 |
Predicted structure (AlphaFold)
| Model | pLDDT | Fraction very-high |
|---|---|---|
| AF-P14635-F1 | 77.58 | 0.61 |
Functional residue map
Curated UniProt residues grouped by drug-discovery relevance — catalytic, ligand-binding, modification, and mutation-validated positions. Source: UniProtKB sequence features.
Post-translational modifications (6): 321, 73, 126, 128, 133, 147
Mutagenesis-validated functional residues (2):
| Position | Phenotype |
|---|---|
| 133 | strongly impairs phosphorylation by plk1. |
| 147 | does not affect phosphorylation by plk1. |
Function
Pathways and Gene Ontology
Reactome pathways
57 pathways
| ID | Pathway |
|---|---|
| R-HSA-113507 | E2F-enabled inhibition of pre-replication complex formation |
| R-HSA-156711 | Polo-like kinase mediated events |
| R-HSA-162658 | Golgi Cisternae Pericentriolar Stack Reorganization |
| R-HSA-174048 | APC/C:Cdc20 mediated degradation of Cyclin B |
| R-HSA-176408 | Regulation of APC/C activators between G1/S and early anaphase |
| R-HSA-176412 | Phosphorylation of the APC/C |
| R-HSA-176417 | Phosphorylation of Emi1 |
| R-HSA-2299718 | Condensation of Prophase Chromosomes |
| R-HSA-2465910 | MASTL Facilitates Mitotic Progression |
| R-HSA-2500257 | Resolution of Sister Chromatid Cohesion |
| R-HSA-2514853 | Condensation of Prometaphase Chromosomes |
| R-HSA-2565942 | Regulation of PLK1 Activity at G2/M Transition |
| R-HSA-2980767 | Activation of NIMA Kinases NEK9, NEK6, NEK7 |
| R-HSA-2995383 | Initiation of Nuclear Envelope (NE) Reformation |
| R-HSA-3301854 | Nuclear Pore Complex (NPC) Disassembly |
| R-HSA-4419969 | Depolymerization of the Nuclear Lamina |
| R-HSA-6804114 | TP53 Regulates Transcription of Genes Involved in G2 Cell Cycle Arrest |
| R-HSA-68875 | Mitotic Prophase |
| R-HSA-69273 | Cyclin A/B1/B2 associated events during G2/M transition |
| R-HSA-69478 | G2/M DNA replication checkpoint |
| R-HSA-75035 | Chk1/Chk2(Cds1) mediated inactivation of Cyclin B:Cdk1 complex |
| R-HSA-8852276 | The role of GTSE1 in G2/M progression after G2 checkpoint |
| R-HSA-8878166 | Transcriptional regulation by RUNX2 |
| R-HSA-9725371 | Nuclear events stimulated by ALK signaling in cancer |
| R-HSA-9825892 | Regulation of MITF-M-dependent genes involved in cell cycle and proliferation |
| R-HSA-113510 | E2F mediated regulation of DNA replication |
| R-HSA-1266738 | Developmental Biology |
| R-HSA-1640170 | Cell Cycle |
| R-HSA-1643685 | Disease |
| R-HSA-174143 | APC/C-mediated degradation of cell cycle proteins |
MSigDB gene sets: 576 (showing top):
GOBP_CHROMOSOME_ORGANIZATION, WU_APOPTOSIS_BY_CDKN1A_VIA_TP53, MODULE_52, GOBP_ATTACHMENT_OF_SPINDLE_MICROTUBULES_TO_KINETOCHORE, GOBP_REGULATION_OF_CELL_CYCLE_CHECKPOINT, BORCZUK_MALIGNANT_MESOTHELIOMA_UP, RODRIGUES_THYROID_CARCINOMA_ANAPLASTIC_UP, GOBP_EMBRYO_DEVELOPMENT_ENDING_IN_BIRTH_OR_EGG_HATCHING, HORIUCHI_WTAP_TARGETS_DN, MODULE_451, GOBP_MUSCLE_TISSUE_DEVELOPMENT, REACTOME_APC_C_CDC20_MEDIATED_DEGRADATION_OF_CYCLIN_B, SHIPP_DLBCL_VS_FOLLICULAR_LYMPHOMA_UP, HOFFMANN_SMALL_PRE_BII_TO_IMMATURE_B_LYMPHOCYTE_DN, REACTOME_PHOSPHORYLATION_OF_THE_APC_C
GO Biological Process (31): G1/S transition of mitotic cell cycle (GO:0000082), G2/M transition of mitotic cell cycle (GO:0000086), oocyte maturation (GO:0001556), in utero embryonic development (GO:0001701), mitotic spindle organization (GO:0007052), mitotic metaphase chromosome alignment (GO:0007080), spermatogenesis (GO:0007283), response to xenobiotic stimulus (GO:0009410), response to mechanical stimulus (GO:0009612), negative regulation of gene expression (GO:0010629), positive regulation of G2/M transition of mitotic cell cycle (GO:0010971), positive regulation of mRNA 3’-end processing (GO:0031442), tissue regeneration (GO:0042246), positive regulation of mitotic cell cycle (GO:0045931), response to DDT (GO:0046680), positive regulation of fibroblast proliferation (GO:0048146), digestive tract development (GO:0048565), cell division (GO:0051301), positive regulation of attachment of spindle microtubules to kinetochore (GO:0051987), ventricular cardiac muscle cell development (GO:0055015), positive regulation of cardiac muscle cell proliferation (GO:0060045), regulation of chromosome condensation (GO:0060623), protein-containing complex assembly (GO:0065003), cellular response to iron(III) ion (GO:0071283), cellular response to fatty acid (GO:0071398), cellular response to hypoxia (GO:0071456), regulation of mitotic cell cycle spindle assembly checkpoint (GO:0090266), positive regulation of mitochondrial ATP synthesis coupled electron transport (GO:1905448), response to toxic substance (GO:0009636), mitotic cell cycle phase transition (GO:0044772), positive regulation of cell cycle (GO:0045787)
GO Molecular Function (6): patched binding (GO:0005113), cyclin-dependent protein serine/threonine kinase regulator activity (GO:0016538), protein kinase binding (GO:0019901), ubiquitin-like protein ligase binding (GO:0044389), cyclin-dependent protein serine/threonine kinase activator activity (GO:0061575), protein binding (GO:0005515)
GO Cellular Component (12): spindle pole (GO:0000922), outer kinetochore (GO:0000940), nucleus (GO:0005634), nucleoplasm (GO:0005654), cytoplasm (GO:0005737), mitochondrial matrix (GO:0005759), centrosome (GO:0005813), microtubule organizing center (GO:0005815), cytosol (GO:0005829), membrane (GO:0016020), cyclin B1-CDK1 complex (GO:0097125), cytoskeleton (GO:0005856)
Reactome top-level categories
Rollup of top-13 pathways:
| Category | Pathways |
|---|---|
| G2/M Transition | 3 |
| Mitotic Prophase | 3 |
| Nuclear Envelope Breakdown | 3 |
| Mitotic Prometaphase | 2 |
| E2F mediated regulation of DNA replication | 1 |
| APC/C:Cdc20 mediated degradation of mitotic proteins | 1 |
| APC/C-mediated degradation of cell cycle proteins | 1 |
| Activation of APC/C and APC/C:Cdc20 mediated degradation of mitotic proteins | 1 |
| Regulation of APC/C activators between G1/S and early anaphase | 1 |
| Nuclear Envelope (NE) Reassembly | 1 |
| TP53 Regulates Transcription of Cell Cycle Genes | 1 |
| M Phase | 1 |
| G2/M Checkpoints | 1 |
GO top-level categories
Rollup of top GO terms by namespace:
| Category | Terms |
|---|---|
| cellular anatomical structure | 6 |
| mitotic cell cycle | 5 |
| mitotic cell cycle phase transition | 2 |
| developmental process involved in reproduction | 2 |
| cyclin-dependent protein serine/threonine kinase activity | 2 |
| cell cycle G1/S phase transition | 1 |
| cell cycle G2/M phase transition | 1 |
| cell maturation | 1 |
| oocyte development | 1 |
| chordate embryonic development | 1 |
| spindle organization | 1 |
| microtubule cytoskeleton organization involved in mitosis | 1 |
| mitotic sister chromatid segregation | 1 |
| metaphase chromosome alignment | 1 |
| mitotic cell cycle process | 1 |
| male gamete generation | 1 |
| response to chemical | 1 |
| response to external stimulus | 1 |
| response to abiotic stimulus | 1 |
| gene expression | 1 |
| regulation of gene expression | 1 |
| negative regulation of macromolecule biosynthetic process | 1 |
| G2/M transition of mitotic cell cycle | 1 |
| regulation of G2/M transition of mitotic cell cycle | 1 |
| positive regulation of mitotic cell cycle phase transition | 1 |
| positive regulation of cell cycle G2/M phase transition | 1 |
| mRNA 3’-end processing | 1 |
| regulation of mRNA 3’-end processing | 1 |
| positive regulation of mRNA processing | 1 |
| regeneration | 1 |
| developmental growth | 1 |
| regulation of mitotic cell cycle | 1 |
| positive regulation of cell cycle | 1 |
| response to insecticide | 1 |
| positive regulation of cell population proliferation | 1 |
| fibroblast proliferation | 1 |
| regulation of fibroblast proliferation | 1 |
| tube development | 1 |
| digestive system development | 1 |
| cellular process | 1 |
Protein interactions and networks
STRING
5990 interactions, top by confidence (×1000):
| Protein A | Protein B | Partner UniProt | Score |
|---|---|---|---|
| CCNB1 | CDK1 | P06493 | 999 |
| CCNB1 | CDK2 | P24941 | 993 |
| CCNB1 | PLK1 | P53350 | 982 |
| CCNB1 | CDC20 | Q12834 | 970 |
| CCNB1 | BUB1B | O60566 | 967 |
| CCNB1 | CDC25C | P30307 | 951 |
| CCNB1 | H2AX | P16104 | 950 |
| CCNB1 | WEE1 | P30291 | 932 |
| CCNB1 | TOP2A | P11388 | 926 |
| CCNB1 | CKS2 | P33552 | 923 |
| CCNB1 | BCLAF1 | Q9NYF8 | 912 |
| CCNB1 | TP53 | P04637 | 909 |
| CCNB1 | PTCH1 | Q13635 | 909 |
| CCNB1 | CCNL2 | Q96S94 | 909 |
| CCNB1 | CKS1B | P33551 | 902 |
IntAct
173 interactions, top by confidence:
| A | B | Type | Score |
|---|---|---|---|
| CCNB1 | CDK1 | psi-mi:“MI:0217”(phosphorylation reaction) | 0.980 |
| CCNB1 | CDK1 | psi-mi:“MI:0407”(direct interaction) | 0.980 |
| CDK1 | CCNB1 | psi-mi:“MI:0407”(direct interaction) | 0.980 |
| CDK1 | CCNB1 | psi-mi:“MI:0915”(physical association) | 0.980 |
| CCNB1 | CDK1 | psi-mi:“MI:0915”(physical association) | 0.980 |
| CCNB1 | CDK1 | psi-mi:“MI:0570”(protein cleavage) | 0.980 |
| CCNB1 | CDK1 | psi-mi:“MI:0914”(association) | 0.980 |
| CDK2 | CCNE2 | psi-mi:“MI:0914”(association) | 0.940 |
| CKS1B | CDK1 | psi-mi:“MI:0914”(association) | 0.920 |
| ESPL1 | PTTG1 | psi-mi:“MI:0914”(association) | 0.900 |
| CDK2 | CCNB1 | psi-mi:“MI:0914”(association) | 0.890 |
| CDK5 | CCNB1 | psi-mi:“MI:0915”(physical association) | 0.890 |
| CDKN1A | CCNE2 | psi-mi:“MI:0914”(association) | 0.890 |
| PKMYT1 | CCNB1 | psi-mi:“MI:0915”(physical association) | 0.870 |
| CCNB1 | PKMYT1 | psi-mi:“MI:0915”(physical association) | 0.870 |
| PKMYT1 | CCNB1 | psi-mi:“MI:2364”(proximity) | 0.870 |
| CCNB1 | PKMYT1 | psi-mi:“MI:2364”(proximity) | 0.870 |
| CDK2 | CCNB2 | psi-mi:“MI:0914”(association) | 0.860 |
BioGRID (588): CCNB1 (Affinity Capture-Western), CCNB1 (Affinity Capture-Western), CCNB1 (Affinity Capture-MS), CCNB1 (Biochemical Activity), CCNB1 (Biochemical Activity), CCNB1 (Biochemical Activity), CCNB1 (Biochemical Activity), CCNB1 (Biochemical Activity), CCNB1 (Biochemical Activity), CCNB1 (Reconstituted Complex), CCNB1 (Biochemical Activity), CCNB1 (Reconstituted Complex), CCNB1 (Reconstituted Complex), CCNB1 (Reconstituted Complex), CCNB1 (Reconstituted Complex)
ESM2 similar proteins: F1N2W9, F1QDI9, F1QMB9, O77689, O93229, O95067, P07818, P13350, P13351, P13952, P14100, P14635, P15206, P24860, P24862, P29332, P30276, P30277, P37882, P37883, P54750, Q01061, Q01064, Q01065, Q01066, Q08301, Q08J23, Q0VGM9, Q1HFZ0, Q1LZG6, Q3TZI6, Q3ZBL9, Q4R7A8, Q60FX9, Q60FY0, Q61481, Q64395, Q6H1L8, Q8RWV3, Q92162
Diamond homologs: A0MEB5, A2YH60, O48790, O77689, O93229, O95067, P04962, P07818, P10815, P13350, P13351, P13952, P14635, P14785, P15206, P18606, P20248, P20439, P24860, P24861, P24862, P24871, P25010, P25011, P25012, P29332, P30183, P30274, P30276, P30277, P30278, P30284, P34800, P34801, P37881, P37882, P37883, P39963, P42524, P43449
SIGNOR signaling
21 interactions.
| A | Effect | B | Mechanism |
|---|---|---|---|
| PLK1 | “up-regulates activity” | CCNB1 | phosphorylation |
| CDKN1A | down-regulates | CCNB1 | binding |
| 4-(2,6-dichlorobenzamido)-N-(piperidin-4-yl)-pyrazole-3-carboxamide | down-regulates | CCNB1 | “chemical inhibition” |
| 4-[[5-amino-1-[(2,6-difluorophenyl)-oxomethyl]-1,2,4-triazol-3-yl]amino]benzenesulfonamide | down-regulates | CCNB1 | “chemical inhibition” |
| PTCH1 | up-regulates | CCNB1 | binding |
| CCNB1 | “form complex” | CyclinB/CDK1 | binding |
| R547 | down-regulates | CCNB1 | “chemical inhibition” |
| seliciclib | down-regulates | CCNB1 | “chemical inhibition” |
| HLX | “up-regulates quantity by expression” | CCNB1 | “transcriptional regulation” |
| RPRD1B | “up-regulates quantity by expression” | CCNB1 | “transcriptional regulation” |
| MXI1 | “down-regulates quantity by repression” | CCNB1 | “transcriptional regulation” |
| CDC20 | “down-regulates quantity by destabilization” | CCNB1 | binding |
| CDC25C | “up-regulates activity” | CCNB1 | dephosphorylation |
| CDC25A | “up-regulates activity” | CCNB1 | dephosphorylation |
| AURKA | “up-regulates activity” | CCNB1 | phosphorylation |
| NFY | “up-regulates quantity by expression” | CCNB1 | “transcriptional regulation” |
| APC-c | “down-regulates quantity by destabilization” | CCNB1 | ubiquitination |
| RFPL4A | “down-regulates quantity by destabilization” | CCNB1 | ubiquitination |
Enriched among interaction partners
Reactome pathways and GO biological processes over-represented among this gene’s 130 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 |
|---|---|---|---|
| G1/S DNA Damage Checkpoints | 8 | 60.4× | 3e-11 |
| p53-Dependent G1 DNA Damage Response | 7 | 56.1× | 1e-09 |
| p53-Dependent G1/S DNA damage checkpoint | 7 | 56.1× | 1e-09 |
| TP53 Regulates Transcription of Genes Involved in G1 Cell Cycle Arrest | 6 | 48.1× | 6e-08 |
| TP53 Regulates Transcription of Cell Cycle Genes | 7 | 42.8× | 9e-09 |
| G1 Phase | 9 | 39.8× | 6e-11 |
| Cyclin A/B1/B2 associated events during G2/M transition | 11 | 38.1× | 5e-13 |
| Cyclin A:Cdk2-associated events at S phase entry | 12 | 35.8× | 1e-13 |
GO biological processes:
| GO term | Partners | Fold | FDR |
|---|---|---|---|
| positive regulation of DNA replication | 6 | 30.1× | 9e-06 |
| G2/M transition of mitotic cell cycle | 9 | 24.2× | 3e-08 |
| regulation of mitotic cell cycle | 10 | 20.8× | 2e-08 |
| mitotic G2 DNA damage checkpoint signaling | 5 | 19.1× | 8e-04 |
| G1/S transition of mitotic cell cycle | 11 | 19.0× | 7e-09 |
| cell division | 22 | 8.8× | 6e-12 |
| DNA repair | 12 | 6.6× | 5e-05 |
| cilium assembly | 9 | 5.7× | 3e-03 |
Disease & clinical
Clinical variants and AI predictions
ClinVar
66 variants total. Per-class counts are floors (≥ shown; pagination cap):
| Classification | Count (floor) |
|---|---|
| Pathogenic | 0 |
| Likely pathogenic | 0 |
| Uncertain significance | 50 |
| Likely benign | 2 |
| Benign | 0 |
Top pathogenic / likely-pathogenic (0)
SpliceAI
1301 predictions. Top by Δscore:
| Variant | Effect | Δscore |
|---|---|---|
| 5:69167074:G:GT | donor_gain | 1.0000 |
| 5:69167282:GG:G | donor_gain | 1.0000 |
| 5:69167283:GG:G | donor_gain | 1.0000 |
| 5:69167904:TCAGA:T | acceptor_loss | 1.0000 |
| 5:69167905:CAG:C | acceptor_loss | 1.0000 |
| 5:69167906:A:AG | acceptor_gain | 1.0000 |
| 5:69167906:AGA:A | acceptor_loss | 1.0000 |
| 5:69167907:G:GG | acceptor_gain | 1.0000 |
| 5:69167907:GA:G | acceptor_gain | 1.0000 |
| 5:69168075:GAAG:G | donor_gain | 1.0000 |
| 5:69168075:GAAGG:G | donor_loss | 1.0000 |
| 5:69168076:AAGG:A | donor_loss | 1.0000 |
| 5:69168078:GGTAA:G | donor_loss | 1.0000 |
| 5:69168079:G:T | donor_loss | 1.0000 |
| 5:69168080:T:G | donor_loss | 1.0000 |
| 5:69168167:CTACA:C | acceptor_loss | 1.0000 |
| 5:69168168:TACA:T | acceptor_loss | 1.0000 |
| 5:69168170:CA:C | acceptor_loss | 1.0000 |
| 5:69168171:A:AG | acceptor_gain | 1.0000 |
| 5:69168172:G:GG | acceptor_gain | 1.0000 |
| 5:69168172:GGAA:G | acceptor_gain | 1.0000 |
| 5:69168314:G:GT | donor_gain | 1.0000 |
| 5:69168340:TTTG:T | donor_loss | 1.0000 |
| 5:69168343:GGTAA:G | donor_loss | 1.0000 |
| 5:69168344:G:GG | donor_gain | 1.0000 |
| 5:69168344:GT:G | donor_loss | 1.0000 |
| 5:69168345:T:A | donor_loss | 1.0000 |
| 5:69171265:TCAA:T | acceptor_loss | 1.0000 |
| 5:69171266:CAAG:C | acceptor_loss | 1.0000 |
| 5:69171267:A:AG | acceptor_gain | 1.0000 |
AlphaMissense
2841 scored. Top likely-pathogenic:
| Variant | Protein change | am_pathogenicity |
|---|---|---|
| 5:69174318:T:C | L205P | 1.000 |
| 5:69174326:T:A | W208R | 1.000 |
| 5:69174326:T:C | W208R | 1.000 |
| 5:69174327:G:C | W208S | 1.000 |
| 5:69174328:G:C | W208C | 1.000 |
| 5:69174328:G:T | W208C | 1.000 |
| 5:69174330:T:C | L209P | 1.000 |
| 5:69174350:T:C | F216L | 1.000 |
| 5:69174352:C:A | F216L | 1.000 |
| 5:69174352:C:G | F216L | 1.000 |
| 5:69174913:G:C | G248R | 1.000 |
| 5:69174914:G:A | G248D | 1.000 |
| 5:69174922:G:C | A251P | 1.000 |
| 5:69174923:C:A | A251D | 1.000 |
| 5:69174935:C:A | A255E | 1.000 |
| 5:69174937:A:C | S256R | 1.000 |
| 5:69174939:C:A | S256R | 1.000 |
| 5:69174939:C:G | S256R | 1.000 |
| 5:69174941:A:T | K257I | 1.000 |
| 5:69174942:A:C | K257N | 1.000 |
| 5:69174942:A:T | K257N | 1.000 |
| 5:69175028:A:T | E286V | 1.000 |
| 5:69175084:T:C | F305L | 1.000 |
| 5:69175086:C:A | F305L | 1.000 |
| 5:69175086:C:G | F305L | 1.000 |
| 5:69175095:A:C | R308S | 1.000 |
| 5:69175095:A:T | R308S | 1.000 |
| 5:69171439:T:C | L178P | 0.999 |
| 5:69174307:G:A | M201I | 0.999 |
| 5:69174307:G:C | M201I | 0.999 |
dbSNP variants (sampled 300 via entrez): RS1000074608 (5:69177084 C>G), RS1000384479 (5:69166395 A>C,G), RS1000415781 (5:69166739 G>A,C,T), RS1000445690 (5:69169396 T>C), RS1000478296 (5:69169082 A>T), RS1000716331 (5:69174129 A>G,T), RS1000750363 (5:69167878 C>G,T), RS1000780793 (5:69175608 T>C), RS1001265980 (5:69166850 G>A), RS1001305163 (5:69166994 G>A,T), RS1001319017 (5:69177970 T>C), RS1001461992 (5:69172381 C>T), RS1001511565 (5:69176259 A>G), RS1001616563 (5:69169978 T>C), RS1001647904 (5:69172598 T>A,C)
Disease associations
OMIM: gene MIM:123836 | disease phenotypes:
GenCC curated gene-disease
Mondo (0):
Orphanet (0):
HPO phenotypes
0 total (0 of 0 shown, HPO-id order):
GWAS associations
0 associations (top):
Drugs & pharmacology
Drug and pharmacology data
Is drug target: yes
ChEMBL targets (5): CHEMBL1907602 (PROTEIN COMPLEX), CHEMBL2094127 (PROTEIN COMPLEX GROUP), CHEMBL2412 (SINGLE PROTEIN), CHEMBL4523630 (PROTEIN COMPLEX), CHEMBL4680053 (PROTEIN-PROTEIN INTERACTION)
Molecules with ChEMBL bioactivity
34 molecules (phase ≥1), by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 145,768 (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 |
|---|---|---|---|
| CHEMBL189963 | PALBOCICLIB | 4 | 13,102 |
| CHEMBL3301610 | ABEMACICLIB | 4 | 7,045 |
| CHEMBL1096380 | PLINABULIN | 3 | 686 |
| CHEMBL2103840 | DINACICLIB | 3 | 2,257 |
| CHEMBL407874 | 6-O-BENZYLGUANINE | 3 | 6,988 |
| CHEMBL428690 | ALVOCIDIB | 3 | 27,781 |
| CHEMBL50 | QUERCETIN | 3 | 74,559 |
| CHEMBL1230165 | SILMITASERTIB | 2 | 593 |
| CHEMBL1276127 | INDIRUBIN | 2 | 181 |
| CHEMBL14762 | SELICICLIB | 2 | 3,787 |
| CHEMBL1944698 | ZOTIRACICLIB | 2 | 2,915 |
| CHEMBL2347597 | ASNUCICLIB | 2 | 100 |
| CHEMBL3115681 | NARAZACICLIB | 2 | 287 |
| CHEMBL3655762 | CYC-065 | 2 | 388 |
| CHEMBL3905910 | VORUCICLIB | 2 | 856 |
| CHEMBL4442620 | RONICICLIB | 2 | 367 |
| CHEMBL445813 | AT-7519 | 2 | 2,614 |
| CHEMBL4462530 | ZEMIRCICLIB | 2 | 429 |
| CHEMBL5095094 | CULMERCICLIB | 2 | 12 |
| CHEMBL564829 | MILCICLIB | 2 | 821 |
| CHEMBL8260 | BAICALEIN | 2 | |
| CHEMBL151 | LUTEOLIN | 2 | |
| CHEMBL31574 | FISETIN | 2 | |
| CHEMBL3545283 | RIVICICLIB | 2 | |
| CHEMBL1230607 | PHA-793887 | 1 | |
| CHEMBL258805 | SU-9516 | 1 | |
| CHEMBL296468 | BMS-387032 | 1 | |
| CHEMBL3545083 | RGB-286638 | 1 | |
| CHEMBL4169078 | SRA-737 | 1 | |
| CHEMBL4439321 | ATUVECICLIB | 1 |
PharmGKB: 1 entry (VIP=true, CPIC=false)
Binding affinities (BindingDB)
379 measured of 508 human assays (523 total across all organisms); most potent 50 below. Values come from heterogeneous assays and are not directly comparable.
| Ligand | Measure | Value |
|---|---|---|
| 4-{[3-(4-aminophenyl)-1H-pyrazol-5-yl]amino}benzene-1-sulfonamide | IC50 | 0.34 nM |
| (12Z)-12-{[(4-{[2-(2-hydroxyethoxy)ethyl]sulfamoyl}phenyl)amino]methylidene}-3-thia-5,10-diazatricyclo[7.3.0.0^{2,6}]dodeca-1,4,6,8-tetraen-11-one | IC50 | 0.54 nM |
| 5-{[(5-tert-butyl-1,3-oxazol-2-yl)methyl]sulfanyl}-N-(pyrimidin-4-yl)-1,3-thiazol-2-amine | IC50 | 1 nM |
| N-methyl-4-({[(12Z)-11-oxo-3-thia-5,10-diazatricyclo[7.3.0.0^{2,6}]dodeca-1,4,6,8-tetraen-12-ylidene]methyl}amino)-N-(2,5,8,11-tetraoxatridecan-13-yl)benzene-1-sulfonamide | IC50 | 1 nM |
| 4-{2-[(3Z)-4-(2-methylpropyl)-2-oxo-2,3-dihydro-1H-indol-3-ylidene]hydrazin-1-yl}benzene-1-sulfonamide | IC50 | 1.2 nM |
| 1-(2,6-difluorophenyl)-3-{3-[5-(morpholin-4-ylmethyl)-1H-1,3-benzodiazol-2-yl]-1H-pyrazol-4-yl}urea | IC50 | 1.5 nM |
| 4-{2-[(3Z)-4-(2-methylprop-1-en-1-yl)-2-oxo-2,3-dihydro-1H-indol-3-ylidene]hydrazin-1-yl}benzene-1-sulfonamide | IC50 | 1.5 nM |
| 4-({[(3Z)-4-oxo-5,10-diazatricyclo[7.4.0.0^{2,6}]trideca-1,6,8,10,12-pentaen-3-ylidene]methyl}amino)benzene-1-sulfonamide | IC50 | 1.5 nM |
| 4-[N -2-Oxo-2,3-dihydropyrrolo[3,2-f]quinolin-1-ylidene)-hydrazino]benzenesulfonamide | IC50 | 1.6 nM |
| 3-{[4-(Aminosulfonyl)phenyl]hydrazono}-N-(2,6-dimethoxybenzyl)-2-oxo-5-indolinecarboxamide | IC50 | 1.7 nM |
| 4-({[(3Z)-5-(3-methylbutanoyl)-2-oxo-2,3-dihydro-1H-indol-3-ylidene]methyl}amino)benzene-1-sulfonamide | IC50 | 1.9 nM |
| 2-N-(1-methanesulfonylpiperidin-4-yl)-5-[(2,3,4-trifluoro-6-methoxyphenyl)carbonyl]pyrimidine-2,4-diamine | KI | 2 nM |
| N-(2,6-Difluorophenyl)-N-[5-[[[5-tert-butyl-2-oxazolyl]-methyl]thio]-2-thiazolyl]urea | IC50 | 2 nM |
| 5-{[(5-tert-butyl-1,3-oxazol-2-yl)methyl]sulfanyl}-N-(pyridin-2-yl)-1,3-thiazol-2-amine | IC50 | 2 nM |
| N-{4-[(5-{[(5-tert-butyl-1,3-oxazol-2-yl)methyl]sulfanyl}-1,3-thiazol-2-yl)amino]phenyl}-2-hydroxyethane-1-sulfonamido | IC50 | 2 nM |
| 4-[1-(5-Oxazol-5-yl-2-oxo-1,2-dihydro-indol-3-ylidene)-ethylamino]benzenesulfonamide | IC50 | 2 nM |
| 4-[[5-Amino-1-[(3-fluoro-2-thienyl)carbonyl]-1H-1,2,4-triazol-3-yl]amino]-benzenesulfonamide | IC50 | 2.1 nM |
| methyl (3Z)-2-oxo-3-{[(4-sulfamoylphenyl)amino]methylidene}-2,3-dihydro-1H-indole-5-carboxylate | IC50 | 2.1 nM |
| 3-{[4-(Aminosulfonyl)phenyl]hydrazono}-2-oxo-N-(3-pyridinylmethyl)-2,3-dihydro-1H-indole-5-carboxamide | IC50 | 2.1 nM |
| 4-[N -(1-Chloro-7-oxo-6,7-dihydro-3H-pyrrolo[3,2-e]indazol-8-ylidene)-hydrazino]benzenesulfonamide | IC50 | 2.2 nM |
| 4-{2-[(3Z)-5-(1,3-oxazol-5-yl)-2-oxo-2,3-dihydro-1H-indol-3-ylidene]hydrazin-1-yl}benzene-1-sulfonamide | IC50 | 2.3 nM |
| 4-({[(3Z)-5-(1,3-oxazol-5-yl)-2-oxo-2,3-dihydro-1H-indol-3-ylidene]methyl}amino)benzene-1-sulfonamide | IC50 | 2.5 nM |
| 4-[N’-(4-Isopropyl-2-oxo-1,2-dihydro-indol-3-ylidene)-hydrazino]benzenesulfonamide | IC50 | 2.5 nM |
| 1-(2-fluorophenyl)-3-{3-[5-(morpholin-4-ylmethyl)-1H-1,3-benzodiazol-2-yl]-1H-pyrazol-4-yl}urea | IC50 | 2.8 nM |
| 4-({[(12Z)-11-oxo-3-thia-5,10-diazatricyclo[7.3.0.0^{2,6}]dodeca-1,4,6,8-tetraen-12-ylidene]methyl}amino)benzene-1-sulfonamide | IC50 | 2.8 nM |
| 2,4-Diamino-5-ketopyrimidine 39 | KI | 3 nM |
| 4-N-(2,6-difluorobenzene)-3-N-(4-fluorophenyl)-1H-pyrazole-3,4-diamido | IC50 | 3 nM |
| 3-(5-{[(5-tert-butyl-1,3-oxazol-2-yl)methyl]sulfanyl}-1,3-thiazol-2-yl)-1-(2,6-dichlorophenyl)urea | IC50 | 3 nM |
| N-[5-[[[5-tert-Butyl-2-oxazolyl]methyl]thio]-2-thiazolyl]-4-[[[bis(hydroxymethyl)methyl]amino]methyl]benzeneacetamide Hydrochloride Salt | IC50 | 3 nM |
| 5-{[(5-tert-butyl-1,3-oxazol-2-yl)methyl]sulfanyl}-N-(pyridin-3-yl)-1,3-thiazol-2-amine | IC50 | 3 nM |
| 3-[({6-[(5-{[(5-tert-butyl-1,3-oxazol-2-yl)methyl]sulfanyl}-1,3-thiazol-2-yl)amino]pyridin-3-yl}methyl)amino]-2,2-dimethylpropan-1-ol | IC50 | 3 nM |
| Isobutyl 3-{[4-(aminosulfonyl)anilino]methylene}-2-oxo-2,3-dihydro-1H-indole-5-carboxylate | IC50 | 3 nM |
| 4-[[5-Amino-1-(2,3,6-trifluorobenzoyl)-1H-1,2,4-triazol-3-yl]amino]-benzenesulfonamide | IC50 | 3.2 nM |
| 4-({5-amino-1-[(3,5-dimethylthiophen-2-yl)carbonyl]-1H-1,2,4-triazol-3-yl}amino)benzene-1-sulfonamide | IC50 | 3.2 nM |
| 3-amino-N-(2,6-difluorophenyl)-5-[(4-sulfamoylphenyl)amino]-1H-1,2,4-triazole-1-carbothioamide | IC50 | 3.2 nM |
| 8-{[4-({[Amino(imino)methyl]amino}sulfonyl)anilino]-methylene}-7-oxo-7,8-dihydro-6H-[1,3]thiazolo[5,4-e]indole | IC50 | 3.3 nM |
| 4-{2-[(3Z)-2-oxo-4-(propan-2-yloxy)-2,3-dihydro-1H-indol-3-ylidene]hydrazin-1-yl}benzene-1-sulfonamide | IC50 | 3.4 nM |
| N-{3-[5-(morpholin-4-ylmethyl)-1H-1,3-benzodiazol-2-yl]-1H-pyrazol-4-yl}benzamide | IC50 | 3.5 nM |
| N-[2-(1H-imidazol-5-yl)ethyl]-4-({[(12Z)-11-oxo-3-thia-5,10-diazatricyclo[7.3.0.0^{2,6}]dodeca-1,4,6,8-tetraen-12-ylidene]methyl}amino)benzene-1-sulfonamide | IC50 | 3.6 nM |
| 5-Amino-3-[[4-(aminosulfonyl)phenyl]amino]-N-(2,6-difluorophenyl)-1H-1,2,4-triazole-1-carboamide | IC50 | 3.7 nM |
| N-[5-[[[5-(Cyclohexylmethyl)-2-oxazolyl]methyl]thio]-2-thiazolyl]acetamide | IC50 | 4 nM |
| 5-{[(5-tert-butyl-1,3-oxazol-2-yl)methyl]sulfanyl}-N-phenyl-1,3-thiazol-2-amine | IC50 | 4 nM |
| Pyrazolopyrimidone analog, RGB-286331 | IC50 | 4 nM |
| 4-({[(12Z)-11-oxo-3-thia-5,10-diazatricyclo[7.3.0.0^{2,6}]dodeca-1,4,6,8-tetraen-12-ylidene]methyl}amino)-N-phenylbenzene-1-sulfonamide | IC50 | 4.3 nM |
| 4-[[5-Amino-1-(2-thienylcarbonyl)-1H-1,2,4-triazol-3-yl]amino]-benzenesulfonamide | IC50 | 4.5 nM |
| (3Z)-2-oxo-3-[2-(4-sulfamoylphenyl)hydrazin-1-ylidene]-2,3-dihydro-1H-indole-5-carboxamide | IC50 | 4.5 nM |
| 4-({[(12Z)-11-oxo-3-thia-5,10-diazatricyclo[7.3.0.0^{2,6}]dodeca-1,4,6,8-tetraen-12-ylidene]methyl}amino)-N-(2,5,8,11-tetraoxatridecan-13-yl)benzene-1-sulfonamide | IC50 | 4.5 nM |
| 4-[N’-(4-Iodo-2-oxo-1,2-dihydro-indol-3-ylidene)-hydrazino]benzenesulfonamide | IC50 | 4.6 nM |
| 4-{2-[(3Z)-4-methyl-5-nitro-2-oxo-2,3-dihydro-1H-indol-3-ylidene]hydrazin-1-yl}benzene-1-sulfonamide | IC50 | 4.6 nM |
| N,N-dimethyl-4-({[(12Z)-11-oxo-3-thia-5,10-diazatricyclo[7.3.0.0^{2,6}]dodeca-1,4,6,8-tetraen-12-ylidene]methyl}amino)benzene-1-sulfonamide | IC50 | 4.6 nM |
ChEMBL bioactivities
1204 potent at pChembl≥5 of 1487 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).
| pChembl | Type | Value | Unit | Molecule |
|---|---|---|---|---|
| 9.30 | Ki | 0.5 | nM | CHEMBL2348843 |
| 9.22 | IC50 | 0.6 | nM | CHEMBL261720 |
| 9.22 | IC50 | 0.6 | nM | CHEMBL384350 |
| 9.22 | IC50 | 0.6 | nM | CHEMBL426509 |
| 9.15 | IC50 | 0.7 | nM | CHEMBL511394 |
| 9.00 | Ki | 1 | nM | CHEMBL2348844 |
| 9.00 | IC50 | 1 | nM | CHEMBL3897452 |
| 9.00 | IC50 | 1 | nM | CHEMBL212552 |
| 8.89 | IC50 | 1.3 | nM | STAUROSPORINE |
| 8.86 | IC50 | 1.38 | nM | STAUROSPORINE |
| 8.85 | IC50 | 1.42 | nM | STAUROSPORINE |
| 8.85 | IC50 | 1.4 | nM | XYLOCYDINE |
| 8.82 | Ki | 1.5 | nM | CHEMBL2348842 |
| 8.80 | IC50 | 1.6 | nM | STAUROSPORINE |
| 8.79 | IC50 | 1.63 | nM | STAUROSPORINE |
| 8.74 | IC50 | 1.8 | nM | CHEMBL3716786 |
| 8.72 | IC50 | 1.9 | nM | CHEMBL377449 |
| 8.71 | IC50 | 1.97 | nM | STAUROSPORINE |
| 8.70 | Ki | 2 | nM | CHEMBL2348847 |
| 8.70 | IC50 | 2 | nM | RGB-286638 |
| 8.70 | IC50 | 2 | nM | CHEMBL212299 |
| 8.70 | IC50 | 2 | nM | CHEMBL261720 |
| 8.70 | IC50 | 2 | nM | CHEMBL4748292 |
| 8.68 | IC50 | 2.1 | nM | CHEMBL361900 |
| 8.67 | IC50 | 2.16 | nM | STAUROSPORINE |
| 8.64 | IC50 | 2.3 | nM | CHEMBL4589128 |
| 8.62 | IC50 | 2.4 | nM | STAUROSPORINE |
| 8.60 | IC50 | 2.52 | nM | STAUROSPORINE |
| 8.52 | IC50 | 3 | nM | CHEMBL363607 |
| 8.52 | IC50 | 3 | nM | CHEMBL3604469 |
| 8.52 | IC50 | 3 | nM | DINACICLIB |
| 8.52 | IC50 | 3 | nM | CHEMBL212491 |
| 8.52 | Ki | 3 | nM | DINACICLIB |
| 8.52 | IC50 | 3 | nM | CHEMBL1825101 |
| 8.49 | IC50 | 3.2 | nM | CHEMBL425720 |
| 8.49 | IC50 | 3.2 | nM | CHEMBL187395 |
| 8.49 | IC50 | 3.2 | nM | CHEMBL364927 |
| 8.49 | IC50 | 3.2 | nM | STAUROSPORINE |
| 8.49 | IC50 | 3.2 | nM | CHEMBL1684800 |
| 8.48 | IC50 | 3.3 | nM | STAUROSPORINE |
| 8.43 | IC50 | 3.7 | nM | CHEMBL370698 |
| 8.40 | Ki | 4 | nM | CHEMBL2348845 |
| 8.40 | Ki | 4 | nM | ASNUCICLIB |
| 8.40 | IC50 | 4 | nM | CHEMBL3604462 |
| 8.40 | IC50 | 4 | nM | CHEMBL3604468 |
| 8.40 | IC50 | 4 | nM | PURVALANOLA |
| 8.40 | IC50 | 4 | nM | CHEMBL430653 |
| 8.40 | IC50 | 4 | nM | CHEMBL1825100 |
| 8.35 | IC50 | 4.5 | nM | CHEMBL190643 |
| 8.32 | IC50 | 4.8 | nM | CHEMBL363130 |
PubChem BioAssay actives
1524 with measured affinity, of 3345 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 |
|---|---|---|---|---|
| 4-[[4-[2-(methylamino)-4-(trifluoromethyl)-1,3-thiazol-5-yl]pyrimidin-2-yl]amino]benzenesulfonamide | 741494: Inhibition of human recombinant His6 tagged CDK1/Cyclin B expressed in Sf21 insect cells after 40 mins by scintillation counting analysis | ki | 0.0005 | uM |
| N-[2-methyl-4-(2-pyrrolidin-1-ylethyl)phenyl]-4-(1H-pyrrolo[2,3-b]pyridin-3-yl)pyrimidin-2-amine | 270821: Inhibition of CDK1/cyclinB by Flashplate assay | ic50 | 0.0006 | uM |
| 2-[3-methyl-4-[[4-(1H-pyrrolo[2,3-b]pyridin-3-yl)pyrimidin-2-yl]amino]phenyl]ethanol | 270821: Inhibition of CDK1/cyclinB by Flashplate assay | ic50 | 0.0006 | uM |
| 5-amino-N-(2,6-difluorophenyl)-3-(4-sulfamoylanilino)-1,2,4-triazole-1-carbothioamide | 1795974: Kinase Inhibition Assay from Article 10.1021/jm050267e: “1-Acyl-1H-[1,2,4]triazole-3,5-diamine analogues as novel and potent anticancer cyclin-dependent kinase inhibitors: synthesis and evaluation of biological activities.” | ic50 | 0.0006 | uM |
| N-[[5-[3-(6-fluoro-1H-benzimidazol-2-yl)-3H-pyrazolo[3,4-b]pyridin-5-yl]-3-pyridinyl]methyl]ethanamine | 365550: Inhibition of CDK1/cyclinB | ic50 | 0.0007 | uM |
| N-[[5-[3-(4,6-difluoro-1H-benzimidazol-2-yl)-1H-indazol-4-yl]-4-methyl-3-pyridinyl]methyl]ethanamine | 1317305: Inhibition of CDK1/cyclin B (unknown origin) | ic50 | 0.0010 | uM |
| N-[2-methyl-4-(2-piperidin-1-ylethyl)phenyl]-4-(1H-pyrrolo[2,3-b]pyridin-3-yl)pyrimidin-2-amine | 270821: Inhibition of CDK1/cyclinB by Flashplate assay | ic50 | 0.0010 | uM |
| (3Z)-5-(2-chloroacetyl)-3-(1H-imidazol-5-ylmethylidene)-1H-indol-2-one | 606558: Inhibition of human Cdk1/cyclinB using histone H1 as a substrate and [gamma-32P]ATP | ic50 | 0.0010 | uM |
| (3Z)-5-(2-chloroacetyl)-3-[(5-methyl-1H-imidazol-4-yl)methylidene]-1H-indol-2-one | 606558: Inhibition of human Cdk1/cyclinB using histone H1 as a substrate and [gamma-32P]ATP | ic50 | 0.0010 | uM |
| N-[(3Z)-3-(1H-imidazol-5-ylmethylidene)-2-oxo-1H-indol-5-yl]prop-2-ynamide | 606558: Inhibition of human Cdk1/cyclinB using histone H1 as a substrate and [gamma-32P]ATP | ic50 | 0.0010 | uM |
| N-[(3Z)-3-[(5-methyl-1H-imidazol-4-yl)methylidene]-2-oxo-1H-indol-5-yl]prop-2-ynamide | 606558: Inhibition of human Cdk1/cyclinB using histone H1 as a substrate and [gamma-32P]ATP | ic50 | 0.0010 | uM |
| [4-amino-2-[(1-methylsulfonylpiperidin-4-yl)amino]pyrimidin-5-yl]-(2,3-difluoro-6-methoxyphenyl)methanone | 1796919: Homogeneous Time-resolved Fluorescence (HTRF) Assay from Article 10.1021/jm0606138: “Discovery of 4-Amino-2-(1-methanesulfonylpiperidin-4-ylamino)pyrimidin-5-ylmethanone (R547), a potent and selective cyclin-dependent kinase inhibitor with significant in vivo antitumor activity.” | ki | 0.0010 | uM |
| 4-[[4-[2-(methylamino)-1,3-thiazol-5-yl]pyrimidin-2-yl]amino]benzenesulfonamide | 741494: Inhibition of human recombinant His6 tagged CDK1/Cyclin B expressed in Sf21 insect cells after 40 mins by scintillation counting analysis | ki | 0.0010 | 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 | 629267: Inhibition of CDK1/Cyclin B | ic50 | 0.0013 | uM |
| 4-amino-6-bromo-7-[(2S,3S,4S,5S)-3,4-dihydroxy-5-(hydroxymethyl)oxolan-2-yl]pyrrolo[2,3-d]pyrimidine-5-carboxamide | 632963: Inhibition of CDK1/Cyclin B in human HeLa cell extracts using histone H1 as substrate preincubated for 30 mins before substrate addition measured after 15 mins by autoradiography | ic50 | 0.0014 | uM |
| 3-[[4-[2-(methylamino)-4-(trifluoromethyl)-1,3-thiazol-5-yl]pyrimidin-2-yl]amino]benzenesulfonamide | 741494: Inhibition of human recombinant His6 tagged CDK1/Cyclin B expressed in Sf21 insect cells after 40 mins by scintillation counting analysis | ki | 0.0015 | uM |
| N-[2-methyl-4-(2-morpholin-4-ylethyl)phenyl]-4-(1H-pyrrolo[2,3-b]pyridin-3-yl)pyrimidin-2-amine | 270821: Inhibition of CDK1/cyclinB by Flashplate assay | ic50 | 0.0019 | 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 | 1317305: Inhibition of CDK1/cyclin B (unknown origin) | ic50 | 0.0020 | uM |
| (2R,3R)-3-[5-bromo-2-[4-(ethylsulfonimidoyl)anilino]pyrimidin-4-yl]oxybutan-2-ol | 1704619: Inhibition of GST-tagged recombinant human CDK1/GST-tagged human cyclin B expressed in Sf-9 cells incubated for 10 mins by scintillation counting method | ic50 | 0.0020 | uM |
| 4-N-[4-(1H-pyrrolo[2,3-b]pyridin-3-yl)pyrimidin-2-yl]cyclohexane-1,4-diamine | 270821: Inhibition of CDK1/cyclinB by Flashplate assay | ic50 | 0.0020 | uM |
| 4-[[4-[4-cyclopropyl-2-(methylamino)-1,3-thiazol-5-yl]pyrimidin-2-yl]amino]benzenesulfonamide | 741494: Inhibition of human recombinant His6 tagged CDK1/Cyclin B expressed in Sf21 insect cells after 40 mins by scintillation counting analysis | ki | 0.0020 | uM |
| 4-[[5-amino-1-(3-fluorothiophene-2-carbonyl)-1,2,4-triazol-3-yl]amino]benzenesulfonamide | 1795974: Kinase Inhibition Assay from Article 10.1021/jm050267e: “1-Acyl-1H-[1,2,4]triazole-3,5-diamine analogues as novel and potent anticancer cyclin-dependent kinase inhibitors: synthesis and evaluation of biological activities.” | ic50 | 0.0021 | uM |
| N-[[5-[3-(4,6-difluoro-1H-benzimidazol-2-yl)-1H-indazol-5-yl]-4-methyl-3-pyridinyl]methyl]ethanamine | 1549287: Inhibition of CDK1/Cyclin B (unknown origin) using histone H1 as substrate in presence of gamma[32P] ATP by phosphorimaging analysis | ic50 | 0.0023 | uM |
| 2-hydroxy-3-[(4-sulfamoylphenyl)diazenyl]-1H-indole-5-carboxamide | 1796078: Kinase Inhibition SPA Assay from Article 10.1021/jm010117d: “Oxindole-based inhibitors of cyclin-dependent kinase 2 (CDK2): design, synthesis, enzymatic activities, and X-ray crystallographic analysis.” | ic50 | 0.0028 | uM |
| 4-[[1-(2,6-difluoro-3-methylbenzoyl)-5-methyl-1,2,4-triazol-3-yl]amino]benzenesulfonamide | 241014: Inhibition of Cyclin B-cyclin-dependent kinase 1 | ic50 | 0.0030 | uM |
| N-(2-methylphenyl)-4-(1H-pyrrolo[2,3-b]pyridin-3-yl)pyrimidin-2-amine | 270821: Inhibition of CDK1/cyclinB by Flashplate assay | ic50 | 0.0030 | uM |
| 2-[(2S)-1-[3-ethyl-7-[(1-oxidopyridin-1-ium-3-yl)methylamino]pyrazolo[1,5-a]pyrimidin-5-yl]piperidin-2-yl]ethanol | 1317325: Inhibition of recombinant CDK1/cyclin B (unknown origin) expressed in baculovirus infected Sf9 insect cells using biotinylated histone H1 as substrate after 1 hr by gamma32P-ATP based liquid scintillation counting analysis | ic50 | 0.0030 | uM |
| N-(2-aminoethyl)-N-[5-[(1-cycloheptylpyrazolo[3,4-d]pyrimidin-6-yl)amino]-2-pyridinyl]methanesulfonamide | 617336: Inhibition of CDK1/Cyclin B assessed as phosphorylation of Z-lyte Peptide at 0.017 to 30 nM by FRET assay | ic50 | 0.0030 | uM |
| (2R,3R)-3-[[5-bromo-2-[4-(ethylsulfonimidoyl)anilino]pyrimidin-4-yl]amino]butan-2-ol | 1239767: Inhibition of recombinant CDK1/GST-fused cyclin B (unknown origin) expressed in baculovirus infected insect Sf9 cells by substrate phosphorylation assay in presence of [33P]-gamma adenosine triphosphate | ic50 | 0.0030 | uM |
| 4-[[5-methyl-1-(2,3,6-trifluorobenzoyl)-1,2,4-triazol-3-yl]amino]benzenesulfonamide | 241014: Inhibition of Cyclin B-cyclin-dependent kinase 1 | ic50 | 0.0032 | uM |
| 4-[[5-amino-2-(2,6-difluorobenzenecarbothioyl)-1,2,4-triazol-3-yl]amino]benzenesulfonamide | 241014: Inhibition of Cyclin B-cyclin-dependent kinase 1 | ic50 | 0.0032 | uM |
| N-[5-amino-1-[(4-methoxyphenyl)methyl]pyrazol-4-yl]-5-[[4-chloro-3-(trifluoromethyl)phenyl]carbamoylamino]-2-methylbenzamide | 578724: Inhibition of CDK1/cyclin B | ic50 | 0.0032 | uM |
| 4-[[5-amino-1-(2,3,6-trifluorobenzoyl)-1,2,4-triazol-3-yl]amino]benzenesulfonamide | 1795974: Kinase Inhibition Assay from Article 10.1021/jm050267e: “1-Acyl-1H-[1,2,4]triazole-3,5-diamine analogues as novel and potent anticancer cyclin-dependent kinase inhibitors: synthesis and evaluation of biological activities.” | ic50 | 0.0032 | uM |
| 4-[[5-amino-1-(3,5-dimethylthiophene-2-carbonyl)-1,2,4-triazol-3-yl]amino]benzenesulfonamide | 1795974: Kinase Inhibition Assay from Article 10.1021/jm050267e: “1-Acyl-1H-[1,2,4]triazole-3,5-diamine analogues as novel and potent anticancer cyclin-dependent kinase inhibitors: synthesis and evaluation of biological activities.” | ic50 | 0.0032 | uM |
| 3-amino-N-(2,6-difluorophenyl)-5-(4-sulfamoylanilino)-1,2,4-triazole-1-carbothioamide | 1795974: Kinase Inhibition Assay from Article 10.1021/jm050267e: “1-Acyl-1H-[1,2,4]triazole-3,5-diamine analogues as novel and potent anticancer cyclin-dependent kinase inhibitors: synthesis and evaluation of biological activities.” | ic50 | 0.0032 | uM |
| 5-amino-N-(2,6-difluorophenyl)-3-(4-sulfamoylanilino)-1,2,4-triazole-1-carboxamide | 1795974: Kinase Inhibition Assay from Article 10.1021/jm050267e: “1-Acyl-1H-[1,2,4]triazole-3,5-diamine analogues as novel and potent anticancer cyclin-dependent kinase inhibitors: synthesis and evaluation of biological activities.” | ic50 | 0.0037 | uM |
| N-(4-methoxyphenyl)-4-(2-methyl-3-propan-2-ylbenzimidazol-5-yl)pyrimidin-2-amine | 1239760: Inhibition of human CDK1/cyclin B1 (unknown origin) | ic50 | 0.0040 | uM |
| 4-[[5-bromo-4-[(2R,3R)-3-hydroxybutan-2-yl]oxypyrimidin-2-yl]amino]benzenesulfinamide | 1239767: Inhibition of recombinant CDK1/GST-fused cyclin B (unknown origin) expressed in baculovirus infected insect Sf9 cells by substrate phosphorylation assay in presence of [33P]-gamma adenosine triphosphate | ic50 | 0.0040 | uM |
| (2R)-2-[[6-(3-chloroanilino)-9-propan-2-ylpurin-2-yl]amino]-3-methylbutan-1-ol | 1798788: CDK Inhibition Assay from Article 10.1021/jm801340z: “Pyrazolo[1,5-a]-1,3,5-triazine as a purine bioisostere: access to potent cyclin-dependent kinase inhibitor (R)-roscovitine analogue.” | ic50 | 0.0040 | uM |
| 5-[(5-tert-butyl-1,3-oxazol-2-yl)methylsulfanyl]-N-pyridin-2-yl-1,3-thiazol-2-amine | 1795808: Kinase Inhibition assay from Article 10.1016/j.bmcl.2004.02.105: “Synthesis and biological activity of N-aryl-2-aminothiazoles: potent pan inhibitors of cyclin-dependent kinases.” | ic50 | 0.0040 | uM |
| N-[5-[(1-cycloheptylpyrazolo[3,4-d]pyrimidin-6-yl)amino]-2-pyridinyl]-N-(2-hydroxyethyl)methanesulfonamide | 617336: Inhibition of CDK1/Cyclin B assessed as phosphorylation of Z-lyte Peptide at 0.017 to 30 nM by FRET assay | ic50 | 0.0040 | uM |
| 3-[[5-fluoro-4-[4-methyl-2-(methylamino)-1,3-thiazol-5-yl]pyrimidin-2-yl]amino]benzenesulfonamide | 1940563: Inhibition of CDK1/Cyclin B (unknown origin) assessed as inhibition constant | ki | 0.0040 | uM |
| 3-[[4-[2-(methylamino)-1,3-thiazol-5-yl]pyrimidin-2-yl]amino]benzenesulfonamide | 741494: Inhibition of human recombinant His6 tagged CDK1/Cyclin B expressed in Sf21 insect cells after 40 mins by scintillation counting analysis | ki | 0.0040 | uM |
| 4-[[5-amino-1-(thiophene-2-carbonyl)-1,2,4-triazol-3-yl]amino]benzenesulfonamide | 1795974: Kinase Inhibition Assay from Article 10.1021/jm050267e: “1-Acyl-1H-[1,2,4]triazole-3,5-diamine analogues as novel and potent anticancer cyclin-dependent kinase inhibitors: synthesis and evaluation of biological activities.” | ic50 | 0.0045 | uM |
| 4-[[5-amino-1-(3-methylthiophene-2-carbonyl)-1,2,4-triazol-3-yl]amino]benzenesulfonamide | 1795974: Kinase Inhibition Assay from Article 10.1021/jm050267e: “1-Acyl-1H-[1,2,4]triazole-3,5-diamine analogues as novel and potent anticancer cyclin-dependent kinase inhibitors: synthesis and evaluation of biological activities.” | ic50 | 0.0048 | uM |
| 4-(4-methylpiperazin-1-yl)-N-[4-(2-methyl-3-propan-2-ylindazol-5-yl)pyrimidin-2-yl]quinolin-7-amine | 1771101: Inhibition of human CDK1/cyclinB using Histone H1 as substrate incubated for 2 hrs by [gamma-33P]-ATP assay | ic50 | 0.0049 | uM |
| [4-amino-2-[(1-methylsulfonylpiperidin-4-yl)amino]pyrimidin-5-yl]-(2,3,4-trifluoro-6-methoxyphenyl)methanone | 1796919: Homogeneous Time-resolved Fluorescence (HTRF) Assay from Article 10.1021/jm0606138: “Discovery of 4-Amino-2-(1-methanesulfonylpiperidin-4-ylamino)pyrimidin-5-ylmethanone (R547), a potent and selective cyclin-dependent kinase inhibitor with significant in vivo antitumor activity.” | ki | 0.0050 | uM |
| 4-[[5-chloro-4-(1-methylpyrazol-4-yl)pyrimidin-2-yl]amino]benzenesulfonamide | 1940568: Inhibition of CDK1/Cyclin B (unknown origin) assessed as inhibition constant incubated for 30 to 60 mins presence of dithiothreitol by Cheng-Prusoff equation analysis | ki | 0.0050 | uM |
| 3-[[5-fluoro-4-(1-methylpyrazol-4-yl)pyrimidin-2-yl]amino]benzenesulfonamide | 1940568: Inhibition of CDK1/Cyclin B (unknown origin) assessed as inhibition constant incubated for 30 to 60 mins presence of dithiothreitol by Cheng-Prusoff equation analysis | ki | 0.0050 | uM |
| 3-[[5-chloro-4-(1-methylpyrazol-4-yl)pyrimidin-2-yl]amino]benzenesulfonamide | 1940568: Inhibition of CDK1/Cyclin B (unknown origin) assessed as inhibition constant incubated for 30 to 60 mins presence of dithiothreitol by Cheng-Prusoff equation analysis | ki | 0.0050 | uM |
CTD chemical–gene interactions
422 total (human), top 30 by PubMed support.
| Chemical | Actions (top 5) | PubMed papers |
|---|---|---|
| Resveratrol | affects expression, affects binding, decreases activity, decreases expression, affects cotreatment (+2 more) | 12 |
| sodium arsenite | decreases degradation, increases stability, affects reaction, decreases reaction, decreases expression (+2 more) | 11 |
| Doxorubicin | affects response to substance, affects expression, increases reaction, decreases reaction, affects cotreatment (+3 more) | 11 |
| Paclitaxel | increases reaction, decreases reaction, increases response to substance, affects reaction, increases activity (+5 more) | 11 |
| bisphenol A | decreases expression, affects cotreatment, decreases reaction, increases expression, affects expression | 10 |
| Quercetin | affects cotreatment, increases expression, affects binding, decreases reaction, decreases expression | 10 |
| Arsenic Trioxide | decreases reaction, affects cotreatment, increases expression, decreases expression | 9 |
| Cisplatin | affects binding, decreases reaction, increases expression, affects cotreatment, decreases expression (+1 more) | 7 |
| Estradiol | affects expression, affects cotreatment, increases expression, decreases expression, decreases reaction | 6 |
| ochratoxin A | affects reaction, affects binding, decreases reaction, decreases expression, affects cotreatment (+1 more) | 5 |
| diallyl trisulfide | decreases activity, decreases expression, increases expression, affects localization, affects binding (+1 more) | 5 |
| alvocidib | affects cotreatment, decreases expression, decreases reaction, increases expression, decreases activity | 5 |
| Benzo(a)pyrene | decreases expression, increases degradation, increases expression | 5 |
| Cadmium | increases abundance, increases expression, decreases expression, affects reaction | 5 |
| Camptothecin | affects cotreatment, decreases expression, increases expression, affects reaction | 5 |
| Fluorouracil | decreases expression, increases reaction, affects reaction, decreases reaction | 5 |
| Troglitazone | decreases expression, decreases reaction, affects response to substance, decreases activity, increases response to substance | 4 |
| trichostatin A | decreases expression | 3 |
| perfluorooctanoic acid | affects expression, decreases expression, increases expression | 3 |
| ON 01910 | decreases expression, increases expression | 3 |
| 2,2’,4,4’-tetrabromodiphenyl ether | affects expression, affects cotreatment, increases expression | 3 |
| (+)-JQ1 compound | affects cotreatment, decreases expression | 3 |
| Bortezomib | increases expression, increases ubiquitination, increases response to substance | 3 |
| Acrolein | increases oxidation, decreases expression, increases abundance, affects localization, affects response to substance (+1 more) | 3 |
| Air Pollutants | increases abundance, increases oxidation, decreases expression, affects cotreatment | 3 |
| Curcumin | decreases expression | 3 |
| Oxygen | affects cotreatment, decreases expression, increases reaction, affects expression, affects reaction (+1 more) | 3 |
| 7,8-Dihydro-7,8-dihydroxybenzo(a)pyrene 9,10-oxide | decreases expression | 3 |
| Cyclosporine | decreases expression | 3 |
| Cadmium Chloride | affects cotreatment, decreases reaction, increases expression, decreases expression, increases abundance (+1 more) | 3 |
ChEMBL screening assays
631 unique, capped per target: 620 binding, 8 admet, 2 functional, 1 unclassified
Representative assays (with source publication via chembl_document):
| Assay ID | Type | Description | Source paper |
|---|---|---|---|
| CHEMBL1000364 | Binding | Inhibition of Cdc2/cyclin B assessed as inhibition of histone H1 phosphorylation in human HT29 cells | Synthesis and structure-activity relationships of N-6 substituted analogues of 9-hydroxy-4-phenylpyrrolo[3,4-c]carbazole-1,3(2H,6H)-diones as inhibitors of Wee1 and Chk1 checkpoint kinases. — Eur J Med Chem |
| CHEMBL4004950 | ADMET | Inhibition of recombinant human CDK1/Cyclin B expressed in baculovirus infected Sf9 cells at using PKTPKKAKKL-NH2 as substrate relative to untreated control | Cyclin-Dependent Kinase (CDK) Inhibitors: Structure-Activity Relationships and Insights into the CDK-2 Selectivity of 6-Substituted 2-Arylaminopurines. — J Med Chem |
| CHEMBL700201 | Functional | In vitro antiproliferative activity against myeloid leukemia K562 cell line | Pyrazolo[4,3-d]pyrimidines as new generation of cyclin-dependent kinase inhibitors. — Bioorg Med Chem Lett |
Cellosaurus cell lines
3 cell lines: 3 cancer cell line
First 10 cell lines (id-ordered, not curated):
| Cellosaurus | Name | Category | Sex |
|---|---|---|---|
| CVCL_B9ER | Abcam A-549 CCNB1 KO | Cancer cell line | Male |
| CVCL_SH30 | HAP1 CCNB1 (-) 1 | Cancer cell line | Male |
| CVCL_SH31 | HAP1 CCNB1 (-) 2 | Cancer cell line | Male |
Clinical trials (associated diseases)
0 trials via MONDO — disease-level, not drug-specific.
Related Atlas pages
No linked Atlas pages yet — the cross-entity mesh grows as the corpus expands.