MNAT1

Summary

MNAT1 (MNAT1 component of CDK activating kinase, HGNC:7181) is a protein-coding gene on chromosome 14q23.1, encoding CDK-activating kinase assembly factor MAT1 (P51948). Stabilizes the cyclin H-CDK7 complex to form a functional CDK-activating kinase (CAK) enzymatic complex. It is a selective cancer dependency (DepMap: 86.9% of cell lines).

The protein encoded by this gene, along with cyclin H and CDK7, forms the CDK-activating kinase (CAK) enzymatic complex. This complex activates several cyclin-associated kinases and can also associate with TFIIH to activate transcription by RNA polymerase II. Two transcript variants encoding different isoforms have been found for this gene.

Source: NCBI Gene 4331 — RefSeq curated summary.

At a glance

• GWAS associations: 4
• Clinical variants (ClinVar): 45 total
• Druggable target: yes — 17 molecules with ChEMBL bioactivity
• Cancer dependency (DepMap): dependent in 86.9% of screened cell lines
• MANE Select transcript: NM_002431

Identifiers

Gene identifiers

Field	Value
HGNC ID	HGNC:7181
Approved symbol	MNAT1
Name	MNAT1 component of CDK activating kinase
Location	14q23.1
Locus type	gene with protein product
Status	Approved
Aliases	MAT1, RNF66
Ensembl gene	ENSG00000020426
Ensembl biotype	protein_coding
OMIM	602659
Entrez	4331

Gene structure

Transcript identifiers

Ensembl transcripts: 15 — 10 protein_coding, 3 protein_coding_CDS_not_defined, 2 retained_intron

ENST00000261245, ENST00000539616, ENST00000553354, ENST00000554002, ENST00000554641, ENST00000555545, ENST00000556525, ENST00000556764, ENST00000557134, ENST00000931365, ENST00000931366, ENST00000931367, ENST00000959999, ENST00000960000, ENST00000960001

RefSeq mRNA: 2 — MANE Select: NM_002431 NM_001177963, NM_002431

CCDS: CCDS53899, CCDS9750

Canonical transcript exons

ENST00000261245 — 8 exons

Exon	Start	End
ENSE00001137574	60968229	60969965
ENSE00001207312	60734761	60734951
ENSE00003506378	60879714	60879835
ENSE00003533987	60808325	60808428
ENSE00003535073	60796217	60796369
ENSE00003538471	60818722	60818847
ENSE00003554119	60811987	60812127
ENSE00003641506	60798087	60798160

Expression profiles

Bgee: expression breadth ubiquitous, 224 present calls, max score 97.24.

FANTOM5 (CAGE): breadth ubiquitous, TPM avg 33.7869 / max 819.9124, expressed in 1812 samples.

FANTOM5 promoters (1 alternative TSS)

Promoter ID	TPM avg	Samples expressed
139890	33.7869	1812

Top tissues by expression

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

Tissue	Anatomy ID	Expression score	Quality
calcaneal tendon	UBERON:0003701	97.24	gold quality
hindlimb stylopod muscle	UBERON:0004252	95.42	gold quality
gastrocnemius	UBERON:0001388	95.21	gold quality
muscle of leg	UBERON:0001383	95.10	gold quality
olfactory segment of nasal mucosa	UBERON:0005386	94.26	gold quality
ventricular zone	UBERON:0003053	93.87	gold quality
muscle organ	UBERON:0001630	93.05	gold quality
adrenal tissue	UBERON:0018303	92.43	gold quality
ganglionic eminence	UBERON:0004023	92.28	gold quality
popliteal artery	UBERON:0002250	91.79	gold quality
tibial artery	UBERON:0007610	91.79	gold quality
right uterine tube	UBERON:0001302	91.37	gold quality
artery	UBERON:0001637	91.21	gold quality
male germ line stem cell (sensu Vertebrata) in testis	CL:0000089 ∩ UBERON:0000473	91.17	gold quality
aorta	UBERON:0000947	91.12	gold quality
skeletal muscle tissue of rectus abdominis	UBERON:0004511	90.99	gold quality
sural nerve	UBERON:0015488	90.67	gold quality
ascending aorta	UBERON:0001496	90.55	gold quality
colonic epithelium	UBERON:0000397	90.52	gold quality
thoracic aorta	UBERON:0001515	90.49	gold quality
descending thoracic aorta	UBERON:0002345	90.27	gold quality
right frontal lobe	UBERON:0002810	89.95	gold quality
stromal cell of endometrium	CL:0002255	89.88	gold quality
left coronary artery	UBERON:0001626	89.82	gold quality
adenohypophysis	UBERON:0002196	89.76	gold quality
primordial germ cell in gonad	CL:0000670 ∩ UBERON:0000991	89.71	gold quality
tendon	UBERON:0000043	89.39	gold quality
biceps brachii	UBERON:0001507	89.33	gold quality
islet of Langerhans	UBERON:0000006	89.27	gold quality
mucosa of stomach	UBERON:0001199	89.20	gold quality

Single-cell (SCXA)

Detected in 1 experiment(s), a significant marker in 1.

Experiment	Marker?	Max mean expression
E-ANND-3	yes	8.96

Regulation

Is transcription factor: no

Upstream regulators (CollecTRI, top): MTA1, YBX1

miRNA regulators (miRDB)

22 targeting MNAT1, 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-4533	100.00	69.48	2758
HSA-MIR-5011-5P	100.00	83.46	5820
HSA-MIR-340-5P	100.00	72.50	4437
HSA-MIR-4789-3P	99.99	70.75	2484
HSA-MIR-4775	99.98	75.00	6394
HSA-MIR-590-3P	99.96	74.34	6478
HSA-MIR-1236-3P	99.94	68.04	1695
HSA-MIR-335-3P	99.93	73.36	4958
HSA-MIR-944	99.82	70.85	3042
HSA-MIR-4766-5P	99.75	69.23	2662
HSA-MIR-4719	99.73	72.10	3329
HSA-MIR-3188	98.58	65.60	878
HSA-MIR-3944-5P	98.50	67.55	997
HSA-MIR-6780A-3P	98.42	67.49	1518
HSA-MIR-6773-3P	98.17	65.51	1213
HSA-MIR-1245B-3P	98.01	68.91	1387
HSA-MIR-7111-3P	97.80	66.75	1467
HSA-MIR-3190-3P	97.61	66.95	1406
HSA-MIR-148B-5P	97.29	66.30	992
HSA-MIR-6874-3P	97.29	66.34	975
HSA-MIR-6736-3P	96.98	65.22	1342
HSA-MIR-6800-5P	94.59	64.80	525

Functional genomics

DepMap (CRISPR cell-line fitness): dependent in 86.9% of screened cell lines.

Literature-anchored findings (GeneRIF, showing 12)

• The cyclin H/cdk7/Mat1 kinase activity is regulated by CK2 phosphorylation of cyclin H. (PMID:12140753)
• Retinoid-induced G1 arrest and differentiation activation are associated with a switch to enzyme hypophosphorylation of retinoic acid receptor alpha. (PMID:12213824)
• interaction with MTA1 and role in regulating estrogen receptor transactivation functions (PMID:12527756)
• In response to ATRA, PML/RARalpha is dissociated from CAK, leading to MAT1 degradation, G1 arrest, and decreased CAK phosphorylation of PML/RARalpha (PMID:16935935)
• Retinoic-acid-induced RAR-CAK signaling events appear to proceed intrinsically during granulocytic development of normal primitive hematopoietic cells. ALDH-governed RA availability may mediate this process by initiating RAR-CAK signaling. (PMID:17628022)
• These results suggested that genetic variants in CAK genes, Cdk7, cyclin H, MAT1, might modulate the risk of lung cancer in a gene-gene interaction mode, which consist to the biochemical interaction of corresponding proteins. (PMID:17707548)
• The intrinsically programmed MAT1 expression and fragmentation regulate granulopoiesis. (PMID:23765726)
• Expressions of components of the CAK complex, CDK7, MAT1, and Cyclin H are elevated in breast cancer. (PMID:27301701)
• MAT1 serves as a promoter in the lung metastasis of osteosarcoma through increasing AKT1 expression. (PMID:31421084)
• Study presents the high-resolution crystal structure of the Arch domain of XPD with its interaction partner MAT1, a central component of the CDK activating kinase complex. The analysis of the interface led to the identification of amino acid residues that are crucial for the MAT1-XPD interaction. (PMID:32245994)
• The regulatory effect of has-circ-0001146/miR-26a-5p/MNAT1 network on the proliferation and invasion of osteosarcoma. (PMID:32453410)
• Potentially functional variants in nucleotide excision repair pathway genes predict platinum treatment response of Chinese ovarian cancer patients. (PMID:32663249)

Cross-species orthologs

5 orthologs

Organism	Symbol	Gene ID
danio_rerio	mnat1	ENSDARG00000002077
mus_musculus	Mnat1	ENSMUSG00000021103
rattus_norvegicus	Mnat1	ENSRNOG00000007267
drosophila_melanogaster	Mat1	FBGN0024956
caenorhabditis_elegans		WBGENE00018769

Protein

Protein identifiers

CDK-activating kinase assembly factor MAT1 — P51948 (reviewed: P51948)

Alternative names: CDK7/cyclin-H assembly factor, Cyclin-G1-interacting protein, Menage a trois, RING finger protein 66, RING finger protein MAT1, p35, p36

All UniProt accessions (4): A0A024R688, P51948, H0YJ92, H0YJF2

UniProt curated annotations — full annotation on UniProt →

Function. Stabilizes the cyclin H-CDK7 complex to form a functional CDK-activating kinase (CAK) enzymatic complex. CAK activates the cyclin-associated kinases CDK1, CDK2, CDK4 and CDK6 by threonine phosphorylation. CAK complexed to the core-TFIIH basal transcription factor activates RNA polymerase II by serine phosphorylation of the repetitive C-terminal domain (CTD) of its large subunit (POLR2A), allowing its escape from the promoter and elongation of the transcripts. Involved in cell cycle control and in RNA transcription by RNA polymerase II.

Subunit / interactions. Associates primarily with CDK7 and cyclin H to form the CAK complex. CAK can further associate with the core-TFIIH to form the TFIIH basal transcription factor.

Subcellular location. Nucleus.

Tissue specificity. Highest levels in colon and testis. Moderate levels are present thymus, prostate, ovary, and small intestine. The lowest levels are found in spleen and leukocytes.

Isoforms (2)

UniProt ID	Names	Canonical?
P51948-1	1	yes
P51948-2	2

RefSeq proteins (2): NP_001171434, NP_002422* (*=MANE)

Domains & families (InterPro)

ID	Name	Type
IPR001841	Znf_RING	Domain
IPR003903	UIM_dom	Conserved_site
IPR004575	MAT1/Tfb3	Family
IPR013083	Znf_RING/FYVE/PHD	Homologous_superfamily
IPR015877	MAT1_centre	Domain
IPR017907	Znf_RING_CS	Conserved_site
IPR057657	MAT1_CAK-anch	Domain

Pfam: PF06391, PF17121, PF25811

UniProt features (28 total): helix 10, strand 5, turn 4, modified residue 3, chain 1, domain 1, zinc finger region 1, splice variant 1, sequence variant 1, sequence conflict 1

Structure

Experimental structures (PDB)

67 structures, top 30 by resolution.

PDB	Method	Resolution (Å)
8P79	ELECTRON MICROSCOPY	1.7
8P77	ELECTRON MICROSCOPY	1.8
8ORM	ELECTRON MICROSCOPY	1.9
8P6V	ELECTRON MICROSCOPY	1.9
8P6W	ELECTRON MICROSCOPY	1.9
8P6X	ELECTRON MICROSCOPY	1.9
8P6Y	ELECTRON MICROSCOPY	1.9
8P72	ELECTRON MICROSCOPY	1.9
8P78	ELECTRON MICROSCOPY	1.9
8PLZ	ELECTRON MICROSCOPY	1.9
8P70	ELECTRON MICROSCOPY	2
8P71	ELECTRON MICROSCOPY	2
8P73	ELECTRON MICROSCOPY	2
8P75	ELECTRON MICROSCOPY	2
8P76	ELECTRON MICROSCOPY	2
6TUN	X-RAY DIFFRACTION	2.07
8P6Z	ELECTRON MICROSCOPY	2.1
8P7L	ELECTRON MICROSCOPY	2.1
8PYR	X-RAY DIFFRACTION	2.15
8P74	ELECTRON MICROSCOPY	2.2
8S0T	ELECTRON MICROSCOPY	2.3
9HIY	ELECTRON MICROSCOPY	2.3
8S0R	ELECTRON MICROSCOPY	2.4
9I9K	ELECTRON MICROSCOPY	2.4
9QJN	ELECTRON MICROSCOPY	2.4
7B5O	ELECTRON MICROSCOPY	2.5
7B5Q	ELECTRON MICROSCOPY	2.5
9QCV	ELECTRON MICROSCOPY	2.5
9HIX	ELECTRON MICROSCOPY	2.6
9HJ0	ELECTRON MICROSCOPY	2.6

Predicted structure (AlphaFold)

Model	pLDDT	Fraction very-high
AF-P51948-F1	85.57	0.42

Antibody-complex structures (SAbDab): 1 — 8PYR

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 (3): 1, 51, 279

Function

Pathways and Gene Ontology

Reactome pathways

61 pathways

ID	Pathway
R-HSA-112382	Formation of RNA Pol II elongation complex
R-HSA-113418	Formation of the Early Elongation Complex
R-HSA-167152	Formation of HIV elongation complex in the absence of HIV Tat
R-HSA-167158	Formation of the HIV-1 Early Elongation Complex
R-HSA-167160	RNA Pol II CTD phosphorylation and interaction with CE during HIV infection
R-HSA-167161	HIV Transcription Initiation
R-HSA-167162	RNA Polymerase II HIV Promoter Escape
R-HSA-167172	Transcription of the HIV genome
R-HSA-167200	Formation of HIV-1 elongation complex containing HIV-1 Tat
R-HSA-167246	Tat-mediated elongation of the HIV-1 transcript
R-HSA-427413	NoRC negatively regulates rRNA expression
R-HSA-5696395	Formation of Incision Complex in GG-NER
R-HSA-674695	RNA Polymerase II Pre-transcription Events
R-HSA-6781823	Formation of TC-NER Pre-Incision Complex
R-HSA-6781827	Transcription-Coupled Nucleotide Excision Repair (TC-NER)
R-HSA-6782135	Dual incision in TC-NER
R-HSA-6782210	Gap-filling DNA repair synthesis and ligation in TC-NER
R-HSA-6796648	TP53 Regulates Transcription of DNA Repair Genes
R-HSA-69202	Cyclin E associated events during G1/S transition
R-HSA-69231	Cyclin D associated events in G1
R-HSA-69273	Cyclin A/B1/B2 associated events during G2/M transition
R-HSA-69656	Cyclin A:Cdk2-associated events at S phase entry
R-HSA-72086	mRNA Capping
R-HSA-73762	RNA Polymerase I Transcription Initiation
R-HSA-73772	RNA Polymerase I Promoter Escape
R-HSA-73776	RNA Polymerase II Promoter Escape
R-HSA-73779	RNA Polymerase II Transcription Pre-Initiation And Promoter Opening
R-HSA-73863	RNA Polymerase I Transcription Termination
R-HSA-75953	RNA Polymerase II Transcription Initiation
R-HSA-75955	RNA Polymerase II Transcription Elongation

MSigDB gene sets: 263 (showing top): REACTOME_FORMATION_OF_INCISION_COMPLEX_IN_GG_NER, YAGI_AML_WITH_INV_16_TRANSLOCATION, ENK_UV_RESPONSE_KERATINOCYTE_UP, CMYB_01, REACTOME_RNA_POLYMERASE_I_TRANSCRIPTION_INITIATION, GOBP_CELL_CYCLE_PHASE_TRANSITION, HOEGERKORP_CD44_TARGETS_TEMPORAL_DN, GRAESSMANN_APOPTOSIS_BY_DOXORUBICIN_DN, GOBP_MUSCLE_CELL_PROLIFERATION, KAUFFMANN_DNA_REPAIR_GENES, GOBP_VENTRICULAR_SYSTEM_DEVELOPMENT, GGGTGGRR_PAX4_03, GOBP_RESPONSE_TO_METAL_ION, PUJANA_CHEK2_PCC_NETWORK, GOMF_KINASE_ACTIVATOR_ACTIVITY

GO Biological Process (13): G1/S transition of mitotic cell cycle (GO:0000082), DNA repair (GO:0006281), nucleotide-excision repair (GO:0006289), regulation of transcription by RNA polymerase II (GO:0006357), transcription initiation at RNA polymerase II promoter (GO:0006367), adult heart development (GO:0007512), ventricular system development (GO:0021591), negative regulation of apoptotic process (GO:0043066), positive regulation of smooth muscle cell proliferation (GO:0048661), response to calcium ion (GO:0051592), regulation of G1/S transition of mitotic cell cycle (GO:2000045), regulation of DNA-templated transcription (GO:0006355), positive regulation of cyclin-dependent protein serine/threonine kinase activity (GO:0045737)

GO Molecular Function (4): zinc ion binding (GO:0008270), cyclin-dependent protein serine/threonine kinase activator activity (GO:0061575), protein binding (GO:0005515), metal ion binding (GO:0046872)

GO Cellular Component (7): cyclin-dependent protein kinase holoenzyme complex (GO:0000307), transcription factor TFIIH core complex (GO:0000439), nucleoplasm (GO:0005654), transcription factor TFIIH holo complex (GO:0005675), CAK-ERCC2 complex (GO:0070516), transcription factor TFIIK complex (GO:0070985), nucleus (GO:0005634)

Reactome top-level categories

Rollup of top-13 pathways:

Category	Pathways
Transcription of the HIV genome	4
Transcription-Coupled Nucleotide Excision Repair (TC-NER)	3
RNA Polymerase II Transcription Elongation	2
HIV Transcription Elongation	2
Late Phase of HIV Life Cycle	1
Tat-mediated elongation of the HIV-1 transcript	1
Negative epigenetic regulation of rRNA expression	1
Global Genome Nucleotide Excision Repair (GG-NER)	1
RNA Polymerase II Transcription	1
Nucleotide Excision Repair	1
Transcriptional Regulation by TP53	1
G1/S Transition	1
G1 Phase	1

GO top-level categories

Rollup of top GO terms by namespace:

Category	Terms
RNA polymerase II transcription regulator complex	3
transcription by RNA polymerase II	2
cyclin-dependent protein serine/threonine kinase activity	2
mitotic cell cycle	1
mitotic cell cycle phase transition	1
cell cycle G1/S phase transition	1
DNA metabolic process	1
DNA damage response	1
DNA repair	1
regulation of DNA-templated transcription	1
DNA-templated transcription initiation	1
heart development	1
brain development	1
system development	1
apoptotic process	1
regulation of apoptotic process	1
negative regulation of programmed cell death	1
positive regulation of cell population proliferation	1
smooth muscle cell proliferation	1
regulation of smooth muscle cell proliferation	1
response to metal ion	1
G1/S transition of mitotic cell cycle	1
regulation of mitotic cell cycle phase transition	1
regulation of cell cycle G1/S phase transition	1
DNA-templated transcription	1
regulation of gene expression	1
regulation of RNA biosynthetic process	1
regulation of cyclin-dependent protein serine/threonine kinase activity	1
positive regulation of cell cycle	1
positive regulation of protein serine/threonine kinase activity	1
positive regulation of cyclin-dependent protein kinase activity	1
transition metal ion binding	1
cyclin-dependent protein serine/threonine kinase regulator activity	1
protein serine/threonine kinase activator activity	1
binding	1
cation binding	1
serine/threonine protein kinase complex	1
nuclear lumen	1
cellular anatomical structure	1
transcription factor TFIIH core complex	1

Protein interactions and networks

STRING

1710 interactions, top by confidence (×1000):

Protein A	Protein B	Partner UniProt	Score
MNAT1	CDK7	P50613	998
MNAT1	CCNH	P51946	998
MNAT1	CCL1	P22362	953
MNAT1	GTF2H4	Q92759	931
MNAT1	ERCC3	P19447	899
MNAT1	GTF2H1	P32780	881
MNAT1	GTF2H3	Q13889	866
MNAT1	ERCC2	P18074	811
MNAT1	GTF2H2	Q13888	808
MNAT1	NAT1	P18440	776
MNAT1	GTF2H5	Q6ZYL4	769
MNAT1	NAA15	Q9BXJ9	762
MNAT1	MTA1	Q13330	686
MNAT1	ESR1	P03372	634
MNAT1	MED6	O75586	629

IntAct

135 interactions, top by confidence:

A	B	Type	Score
CDK7	CCNH	psi-mi:“MI:0914”(association)	0.950
CCNH	CDK7	psi-mi:“MI:0915”(physical association)	0.950
CDK7	ERCC2	psi-mi:“MI:0914”(association)	0.890
CCNH	CDK2	psi-mi:“MI:0217”(phosphorylation reaction)	0.860
CDK2	CCNB2	psi-mi:“MI:0914”(association)	0.860
CDK8	MED19	psi-mi:“MI:2364”(proximity)	0.850
GTF2H1	CDK7	psi-mi:“MI:0915”(physical association)	0.820
CCNH	ERCC2	psi-mi:“MI:0915”(physical association)	0.750
CETN2	SFI1	psi-mi:“MI:0914”(association)	0.740
CNOT3	CNOT1	psi-mi:“MI:0914”(association)	0.740
GTF2H1	MNAT1	psi-mi:“MI:0914”(association)	0.670
MNAT1	ERCC2	psi-mi:“MI:0914”(association)	0.640
GNG8	GNB5	psi-mi:“MI:0914”(association)	0.640
CDK2	GMNN	psi-mi:“MI:0914”(association)	0.640
MNAT1	GOLGA2	psi-mi:“MI:0915”(physical association)	0.560
MNAT1		psi-mi:“MI:0915”(physical association)	0.560
PRKN	MNAT1	psi-mi:“MI:0915”(physical association)	0.560
MNAT1	RNF11	psi-mi:“MI:0915”(physical association)	0.560
HTT	MNAT1	psi-mi:“MI:0915”(physical association)	0.560
MNAT1	TARDBP	psi-mi:“MI:0915”(physical association)	0.560

BioGRID (204): CDK7 (Affinity Capture-MS), ERCC2 (Affinity Capture-MS), CCNH (Affinity Capture-MS), CDK7 (Co-fractionation), MNAT1 (Co-fractionation), SFR1 (Co-fractionation), MNAT1 (Proximity Label-MS), MNAT1 (Affinity Capture-MS), MNAT1 (Affinity Capture-MS), MNAT1 (Affinity Capture-MS), POLR2A (Biochemical Activity), MNAT1 (Two-hybrid), MNAT1 (Two-hybrid), CCNH (Affinity Capture-MS), CDK7 (Affinity Capture-MS)

ESM2 similar proteins: A0PJP4, A2AHJ4, A4IIZ9, D3YZP9, F4HRI2, F4HRV8, I6PL68, O09000, O75665, O94967, P49140, P51948, P70365, Q0IHE5, Q15788, Q16204, Q17QG3, Q2QLI6, Q3LGD4, Q3SYW5, Q4PJW2, Q4R3X1, Q4R8G4, Q4V891, Q5R8Q4, Q5RD40, Q5RKN3, Q5ZKF4, Q5ZLY0, Q62739, Q653N3, Q66IJ0, Q68FY1, Q86Z20, Q8CFE5, Q8CGF6, Q8L7S4, Q8NA72, Q8NFH5, Q8R4R6

Diamond homologs: O94684, P51948, P51949, P51950, P51951, Q03290, Q6BP96, Q6C7D0, Q6CT73, Q6FMP4, Q75D20

SIGNOR signaling

4 interactions.

A	Effect	B	Mechanism
MNAT1	“up-regulates activity”	ESR1	phosphorylation
MNAT1	“form complex”	“CAK complex”	binding
Ub:E2	“up-regulates activity”	MNAT1	ubiquitination
MNAT1	“down-regulates quantity by destabilization”	TP53	ubiquitination

Enriched among interaction partners

Reactome pathways and GO biological processes over-represented among this gene’s 131 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
RNA Pol II CTD phosphorylation and interaction with CE during HIV infection	10	43.9×	7e-13
RNA Pol II CTD phosphorylation and interaction with CE	10	43.9×	7e-13
mRNA Capping	10	40.9×	1e-12
Formation of the Early Elongation Complex	10	36.1×	3e-12
Formation of the HIV-1 Early Elongation Complex	10	36.1×	3e-12
RNA Polymerase I Transcription Termination	10	35.1×	4e-12
Formation of HIV-1 elongation complex containing HIV-1 Tat	11	30.7×	2e-12
Tat-mediated elongation of the HIV-1 transcript	11	30.7×	2e-12

GO biological processes:

GO term	Partners	Fold	FDR
nucleotide-excision repair	9	29.5×	1e-08
transcription initiation at RNA polymerase II promoter	8	25.6×	3e-07
protein destabilization	5	12.4×	7e-03
protein autoubiquitination	6	12.0×	2e-03
transcription by RNA polymerase II	13	7.8×	3e-06
regulation of gene expression	8	5.7×	9e-03
DNA repair	10	5.5×	3e-03

Disease & clinical

Clinical variants and AI predictions

ClinVar

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

Classification	Count (floor)
Pathogenic	0
Likely pathogenic	0
Uncertain significance	38
Likely benign	1
Benign	1

Top pathogenic / likely-pathogenic (0)

SpliceAI

3080 predictions. Top by Δscore:

Variant	Effect	Δscore
14:60734952:G:GG	donor_gain	1.0000
14:60752307:T:G	donor_gain	1.0000
14:60796214:C:G	acceptor_gain	1.0000
14:60796214:CA:C	acceptor_loss	1.0000
14:60796215:A:AG	acceptor_gain	1.0000
14:60796215:A:AT	acceptor_loss	1.0000
14:60796215:AGCT:A	acceptor_gain	1.0000
14:60796216:G:GA	acceptor_gain	1.0000
14:60796216:GC:G	acceptor_gain	1.0000
14:60796216:GCT:G	acceptor_gain	1.0000
14:60796216:GCTG:G	acceptor_gain	1.0000
14:60796216:GCTGT:G	acceptor_gain	1.0000
14:60796338:G:GT	donor_gain	1.0000
14:60796365:AAGAT:A	donor_gain	1.0000
14:60796366:AGAT:A	donor_gain	1.0000
14:60796367:GAT:G	donor_gain	1.0000
14:60796367:GATG:G	donor_gain	1.0000
14:60796367:GATGT:G	donor_loss	1.0000
14:60796368:AT:A	donor_gain	1.0000
14:60796368:ATGTA:A	donor_loss	1.0000
14:60796369:TG:T	donor_loss	1.0000
14:60796370:G:GG	donor_gain	1.0000
14:60796371:T:A	donor_loss	1.0000
14:60798083:A:AG	acceptor_gain	1.0000
14:60798083:AAAG:A	acceptor_loss	1.0000
14:60798084:A:G	acceptor_gain	1.0000
14:60798085:A:AG	acceptor_gain	1.0000
14:60798086:G:GG	acceptor_gain	1.0000
14:60798086:G:GT	acceptor_loss	1.0000
14:60798086:GAT:G	acceptor_gain	1.0000

AlphaMissense

2040 scored. Top likely-pathogenic:

Variant	Protein change	am_pathogenicity
14:60734878:T:C	C6R	1.000
14:60734887:T:A	C9S	1.000
14:60734887:T:C	C9R	1.000
14:60734888:G:C	C9S	1.000
14:60734938:T:C	C26R	1.000
14:60734939:G:A	C26Y	1.000
14:60734942:G:A	G27E	1.000
14:60796218:T:A	C31S	1.000
14:60796218:T:C	C31R	1.000
14:60796219:G:A	C31Y	1.000
14:60796219:G:C	C31S	1.000
14:60796219:G:T	C31F	1.000
14:60796220:T:G	C31W	1.000
14:60796227:T:A	C34S	1.000
14:60796227:T:C	C34R	1.000
14:60796228:G:A	C34Y	1.000
14:60796228:G:C	C34S	1.000
14:60796228:G:T	C34F	1.000
14:60796229:T:G	C34W	1.000
14:60796263:T:C	C46R	1.000
14:60796351:G:T	R75M	1.000
14:60734878:T:A	C6S	0.999
14:60734879:G:A	C6Y	0.999
14:60734879:G:C	C6S	0.999
14:60734880:C:G	C6W	0.999
14:60734888:G:A	C9Y	0.999
14:60734888:G:T	C9F	0.999
14:60734889:T:G	C9W	0.999
14:60734906:G:C	R15P	0.999
14:60734934:T:A	N24K	0.999

dbSNP variants (sampled 300 via entrez): RS1000028630 (14:60905557 A>C,T), RS1000045006 (14:60853816 G>T), RS1000053753 (14:60823324 T>C), RS1000056995 (14:60919320 C>A), RS1000102149 (14:60763771 T>A), RS1000109371 (14:60842467 A>G), RS1000131172 (14:60942246 A>C,G), RS1000153223 (14:60881589 GAT>G), RS1000153252 (14:60859837 G>A), RS1000156071 (14:60839581 G>A,C), RS1000170627 (14:60915546 G>A), RS1000197112 (14:60759332 A>G), RS1000202332 (14:60848062 T>C,G), RS1000209582 (14:60839336 A>G), RS1000218935 (14:60889628 T>G)

Disease associations

OMIM: gene MIM:602659 | disease phenotypes:

GenCC curated gene-disease

Mondo (0):

Orphanet (0):

HPO phenotypes

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

GWAS associations

4 associations (top):

Study	Trait	p-value
GCST001538_17	Immune reponse to smallpox (secreted IFN-alpha)	3.000000e-10
GCST005919_2	Exhaled carbon monoxide levels in smokers with chronic obstructive pulmonary disease	6.000000e-08
GCST010002_153	Refractive error	2.000000e-40
GCST010397_107	Gut microbiota (bacterial taxa, rank normal transformation method)	2.000000e-07

EFO canonical traits (4, from GWAS)

EFO ID	Trait name
EFO:0004645	response to vaccine
EFO:0004873	cytokine measurement
EFO:0006520	carbon monoxide exhalation measurement
EFO:0007874	gut microbiome measurement

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (2): CHEMBL3038473 (PROTEIN COMPLEX), CHEMBL5053 (SINGLE PROTEIN)

Molecules with ChEMBL bioactivity

17 molecules (phase ≥1), by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 54,025 (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
CHEMBL3301610	ABEMACICLIB	4	7,045
CHEMBL4594350	ADAGRASIB	4	2,814
CHEMBL2103840	DINACICLIB	3	2,257
CHEMBL428690	ALVOCIDIB	3	27,781
CHEMBL14762	SELICICLIB	2	3,787
CHEMBL1944698	ZOTIRACICLIB	2	2,915
CHEMBL3115681	NARAZACICLIB	2	287
CHEMBL4297488	CT-7001	2	379
CHEMBL4442620	RONICICLIB	2	367
CHEMBL445813	AT-7519	2	2,614
CHEMBL4462530	ZEMIRCICLIB	2	429
CHEMBL564829	MILCICLIB	2	821
CHEMBL258805	SU-9516	1	76
CHEMBL296468	BMS-387032	1	2,075
CHEMBL3128043	PF-03758309	1	233
CHEMBL4225966	SEL-120 FREE BASE	1	91
CHEMBL5090754	SY-5609	1	54

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

Binding affinities (BindingDB)

32 measured of 120 human assays (121 total across all organisms); most potent 32 below. Values come from heterogeneous assays and are not directly comparable.

Ligand	Measure	Value	Patent
28-dimethylphosphoryl-11-methyl-25-(trifluoromethyl)-4,11,16,21,23,26-hexazapentacyclo[20.3.1.15,9.116,20.02,6]octacosa-1(26),2,5,7,9(28),22,24-heptaen-10-one	IC50	1 nM	US-20250109156: INDOLE-CONTAINING MACROCYCLIC COMPOUNDS AND USES THEREOF
(20S)-28-dimethylphosphoryl-25-(trifluoromethyl)-4,11,16,21,23,26-hexazapentacyclo[20.3.1.15,9.116,20.02,6]octacosa-1(26),2,5,7,9(28),22,24-heptaen-10-one	IC50	1.2 nM	US-20250109156: INDOLE-CONTAINING MACROCYCLIC COMPOUNDS AND USES THEREOF
(1S)-28-dimethylphosphoryl-6-(trifluoromethyl)-2,4,10,17,22,29-hexazapentacyclo[20.4.1.13,7.111,15.08,12]nonacosa-3,5,7(29),8,11,13,15(28)-heptaen-16-one	IC50	1.4 nM	US-20250109156: INDOLE-CONTAINING MACROCYCLIC COMPOUNDS AND USES THEREOF
(21S)-29-dimethylphosphoryl-26-(trifluoromethyl)-10-oxa-4,17,22,24,27-pentazapentacyclo[21.3.1.15,9.117,21.02,6]nonacosa-1(27),2,5,7,9(29),23,25-heptaene	IC50	1.6 nM	US-20250109156: INDOLE-CONTAINING MACROCYCLIC COMPOUNDS AND USES THEREOF
(19R)-24-(trifluoromethyl)-4,11,16,20,22,25-hexazapentacyclo[19.3.1.15,9.116,19.02,6]heptacosa-1(25),2,5,7,9(27),21,23-heptaen-10-one	IC50	4.58 nM	US-20250145632: Pyrimidine Heterocyclic Compound, Preparation Method Thereof and use Thereof in Medicine
[(6R)-6-methyl-2-[(2-methyl-1H-imidazol-5-yl)methylamino]-6,8-dihydro-5H-pyrido[3,4-d]pyrimidin-7-yl]-[(3S,4S)-1-methyl-3-phenylpiperidin-4-yl]methanone	IC50	11 nM	WO-2022064009: CYCLIN-DEPENDENT KINASE 7 (CDK7) NON-COVALENT INHIBITORS
(20R)-25-(trifluoromethyl)-14-oxa-4,11,17,21,23,26-hexazapentacyclo[20.3.1.15,9.117,20.02,6]octacosa-1(26),2,5,7,9(28),22,24-heptaen-10-one	IC50	11 nM	US-20250145632: Pyrimidine Heterocyclic Compound, Preparation Method Thereof and use Thereof in Medicine
(E)-N-[4-[3-[1-[(5-cyclopropyl-1H-pyrazol-3-yl)amino]-1-oxopropan-2-yl]phenyl]phenyl]-4-(dimethylamino)but-2-enamide	IC50	62.5 nM	US-11174232: Substituted heterocyclyl derivatives as CDK inhibitors
(E)-N-[4-[3-[(2S)-1-[(5-cyclopropyl-1H-pyrazol-3-yl)amino]-1-oxopropan-2-yl]phenyl]phenyl]-4-(dimethylamino)but-2-enamide	IC50	62.5 nM	US-11174232: Substituted heterocyclyl derivatives as CDK inhibitors
N-(5-cyclopropyl-1H-pyrazol-3-yl)-2-[3-[4-[[(E)-4-(dimethylamino)but-2-enoyl]amino]phenyl]phenyl]butanamide	IC50	62.5 nM	US-11174232: Substituted heterocyclyl derivatives as CDK inhibitors
(E)-N-[6-[3-[1-[(5-cyclopropyl-1H-pyrazol-3-yl)amino]-1-oxopropan-2-yl]phenyl]-3-pyridinyl]-4-(dimethylamino)but-2-enamide	IC50	62.5 nM	US-11174232: Substituted heterocyclyl derivatives as CDK inhibitors
N-(5-cyclopropyl-1H-pyrazol-3-yl)-2-[3-[3-fluoro-4-(prop-2-enoylamino)phenyl]phenyl]propanamide	IC50	62.5 nM	US-11174232: Substituted heterocyclyl derivatives as CDK inhibitors
N-(5-cyclopropyl-1H-pyrazol-3-yl)-2-[4-fluoro-3-[3-fluoro-4-(prop-2-enoylamino)phenyl]phenyl]propanamide	IC50	62.5 nM	US-11174232: Substituted heterocyclyl derivatives as CDK inhibitors
N-(5-cyclopropyl-1H-pyrazol-3-yl)-2-[3-[5-(prop-2-enoylamino)-2-pyridinyl]phenyl]propanamide	IC50	62.5 nM	US-11174232: Substituted heterocyclyl derivatives as CDK inhibitors
N-(5-cyclopropyl-1H-pyrazol-3-yl)-2-[3-[3-fluoro-4-(prop-2-enoylamino)phenyl]phenyl]-3-methylbutanamide	IC50	62.5 nM	US-11174232: Substituted heterocyclyl derivatives as CDK inhibitors
(E)-N-[4-[3-[1-[(5-cyclopentyl-1H-pyrazol-3-yl)amino]-1-oxopropan-2-yl]phenyl]-2-fluorophenyl]-4-(dimethylamino)but-2-enamide	IC50	62.5 nM	US-11174232: Substituted heterocyclyl derivatives as CDK inhibitors
(E)-N-[4-[3-[1-[(5-cyclopropyl-1H-pyrazol-3-yl)amino]-1-oxopropan-2-yl]phenyl]-2-fluorophenyl]-4-pyrrolidin-1-ylbut-2-enamide	IC50	62.5 nM	US-11174232: Substituted heterocyclyl derivatives as CDK inhibitors
(E)-N-[5-[3-[1-[(5-cyclopropyl-1H-pyrazol-3-yl)amino]-1-oxopropan-2-yl]phenyl]-6-fluoro-2-pyridinyl]-4-morpholin-4-ylbut-2-enamide	IC50	62.5 nM	US-11174232: Substituted heterocyclyl derivatives as CDK inhibitors
(E)-N-[5-[3-[1-[(5-cyclopropyl-1H-pyrazol-3-yl)amino]-1-oxopropan-2-yl]phenyl]-3-pyridinyl]-4-morpholin-4-ylbut-2-enamide	IC50	62.5 nM	US-11174232: Substituted heterocyclyl derivatives as CDK inhibitors
(E)-N-[5-[3-[1-[(5-cyclopropyl-1H-pyrazol-3-yl)amino]-1-oxopropan-2-yl]phenyl]-3-fluoro-2-pyridinyl]-4-morpholin-4-ylbut-2-enamide	IC50	62.5 nM	US-11174232: Substituted heterocyclyl derivatives as CDK inhibitors
(E)-N-[6-[3-[1-[(5-cyclopropyl-1H-pyrazol-3-yl)amino]-1-oxopropan-2-yl]phenyl]-2-fluoro-3-pyridinyl]-4-(3-fluoropyrrolidin-1-yl)but-2-enamide	IC50	62.5 nM	US-11174232: Substituted heterocyclyl derivatives as CDK inhibitors
(E)-N-[5-[3-[1-[(5-cyclopropyl-1H-pyrazol-3-yl)amino]-1-oxopropan-2-yl]phenyl]-2-pyridinyl]-4-imidazol-1-ylbut-2-enamide	IC50	62.5 nM	US-11174232: Substituted heterocyclyl derivatives as CDK inhibitors
(E)-N-[5-[3-[1-[(5-cyclopropyl-1H-pyrazol-3-yl)amino]-1-oxopropan-2-yl]phenyl]-2-pyridinyl]-4-[(2S)-2-(methoxymethyl)pyrrolidin-1-yl]but-2-enamide	IC50	62.5 nM	US-11174232: Substituted heterocyclyl derivatives as CDK inhibitors
(E)-N-[5-[3-[1-[(5-cyclopropyl-1H-pyrazol-3-yl)amino]-1-oxopropan-2-yl]phenyl]-2-pyridinyl]-4-[(2S,4S)-4-fluoro-2-(methoxymethyl)pyrrolidin-1-yl]but-2-enamide	IC50	62.5 nM	US-11174232: Substituted heterocyclyl derivatives as CDK inhibitors
(E)-4-(3-cyanopyrrolidin-1-yl)-N-[5-[3-[1-[(5-cyclopropyl-1H-pyrazol-3-yl)amino]-1-oxopropan-2-yl]phenyl]-2-pyridinyl]but-2-enamide	IC50	62.5 nM	US-11174232: Substituted heterocyclyl derivatives as CDK inhibitors
(E)-N-[4-[3-[1-[(5-cyclopropyl-1H-pyrazol-3-yl)amino]-1-oxopropan-2-yl]phenyl]-2-fluorophenyl]-4-[(3S)-3-fluoropyrrolidin-1-yl]but-2-enamide	IC50	62.5 nM	US-11174232: Substituted heterocyclyl derivatives as CDK inhibitors
methyl (2S)-1-[(E)-4-[[5-[3-[1-[(5-cyclopropyl-1H-pyrazol-3-yl)amino]-1-oxopropan-2-yl]phenyl]-2-pyridinyl]amino]-4-oxobut-2-enyl]pyrrolidine-2-carboxylate	IC50	62.5 nM	US-11174232: Substituted heterocyclyl derivatives as CDK inhibitors
(E)-4-[(2S)-2-(cyanomethyl)pyrrolidin-1-yl]-N-[5-[3-[1-[(5-cyclopropyl-1H-pyrazol-3-yl)amino]-1-oxopropan-2-yl]phenyl]-2-pyridinyl]but-2-enamide	IC50	62.5 nM	US-11174232: Substituted heterocyclyl derivatives as CDK inhibitors
(E)-N-[6-[3-[1-[(5-cyclopropyl-1H-pyrazol-3-yl)amino]-1-oxopropan-2-yl]phenyl]pyrazin-2-yl]-4-pyrrolidin-1-ylbut-2-enamide	IC50	62.5 nM	US-11174232: Substituted heterocyclyl derivatives as CDK inhibitors
Pyrazolopyrimidone analog, RGB-286147	IC50	71 nM
N-[(1S)-2-(dimethylamino)-1-phenylethyl]-6,6-dimethyl-3-[4-(prop-2-enoylamino)anilino]-1,2,3,3a,4,6a-hexahydropyrrolo[3,4-c]pyrazole-5-carboxamide	IC50	300 nM	US-10870651: Inhibitors of cyclin-dependent kinase 7 (CDK7)
N-[(1S)-2-(dimethylamino)-1-phenylethyl]-3-[[4-(prop-2-enoylamino)benzoyl]amino]spiro[1,2,3,3a,4,6a-hexahydropyrrolo[3,4-c]pyrazole-6,1’-cyclohexane]-5-carboxamide	IC50	300 nM	US-10870651: Inhibitors of cyclin-dependent kinase 7 (CDK7)

ChEMBL bioactivities

653 potent at pChembl≥5 of 724 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).

pChembl	Type	Value	Unit	Molecule
8.89	IC50	1.3	nM	ADAGRASIB
8.77	Ki	1.7	nM	CHEMBL5573062
8.68	Ki	2.1	nM	CHEMBL5571052
8.66	Ki	2.2	nM	CHEMBL5571158
8.66	Ki	2.2	nM	CHEMBL5612622
8.64	IC50	2.3	nM	SY-5609
8.60	IC50	2.5	nM	SY-5609
8.55	Ki	2.8	nM	CHEMBL5570901
8.54	Ki	2.9	nM	CHEMBL5573958
8.52	IC50	3	nM	ZOTIRACICLIB
8.52	IC50	3	nM	CHEMBL5573062
8.52	Ki	3	nM	CHEMBL5569632
8.49	Ki	3.2	nM	CT-7001
8.47	Ki	3.4	nM	CHEMBL5573301
8.43	IC50	3.7	nM	CHEMBL5589668
8.42	Ki	3.8	nM	CHEMBL5594541
8.40	EC50	4	nM	CHEMBL4436535
8.34	IC50	4.6	nM	CHEMBL6152747
8.25	IC50	5.6	nM	CHEMBL5612636
8.21	IC50	6.1	nM	CHEMBL5574236
8.21	IC50	6.1	nM	CHEMBL5573301
8.19	IC50	6.5	nM	CHEMBL5574001
8.19	IC50	6.4	nM	CHEMBL5613276
8.17	IC50	6.8	nM	CHEMBL5594541
8.17	IC50	6.8	nM	CHEMBL5613531
8.17	IC50	6.7	nM	CHEMBL5613200
8.16	IC50	6.9	nM	CHEMBL5613393
8.15	IC50	7	nM	PF-03758309
8.14	IC50	7.3	nM	CHEMBL5573695
8.14	IC50	7.2	nM	CHEMBL5569504
8.12	IC50	7.6	nM	CHEMBL4434871
8.12	IC50	7.6	nM	CHEMBL5574336
8.12	IC50	7.6	nM	CHEMBL5612049
8.11	IC50	7.8	nM	CHEMBL5612354
8.09	IC50	8.1	nM	CHEMBL5613342
8.07	IC50	8.6	nM	CHEMBL5611964
8.07	Kd	8.533	nM	CHEMBL3752910
8.06	IC50	8.8	nM	CHEMBL5573538
8.06	IC50	8.7	nM	CHEMBL5594350
8.06	IC50	8.7	nM	CHEMBL5613703
8.05	IC50	8.9	nM	CHEMBL5570731
8.04	IC50	9.2	nM	CHEMBL5613991
8.03	IC50	9.4	nM	CHEMBL5612986
8.02	Ki	9.5	nM	CHEMBL5592213
8.01	IC50	9.7	nM	CHEMBL4450322
8.01	ED50	9.716	nM	CHEMBL3752910
8.00	EC50	10	nM	CHEMBL3603847
8.00	IC50	10.1	nM	CHEMBL5542311
7.99	IC50	10.2	nM	CHEMBL5572618
7.96	IC50	11	nM	CHEMBL5594861

PubChem BioAssay actives

280 with measured affinity, of 537 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
Adagrasib	1853202: Inhibition of CDK7/Cyclin H/MAT1 (unknown origin) in leukemia cells	ic50	0.0013	uM
22-propan-2-ylspiro[10-oxa-2,18,20,24,25,26-hexazatetracyclo[17.6.1.04,9.021,25]hexacosa-1(26),4,6,8,19,21,23-heptaene-16,3’-azetidine]	2104174: Inhibition of CDK7/cyclin H/MNAT1 (unknown origin) preincubated for 10 mins followed by substrate addition and measured after 60 mins in presence of ATP by ADP-Glo reagent based luminescence microtiter plate reader analysis	ki	0.0017	uM
23-propan-2-ylspiro[10-oxa-2,19,21,25,26,27-hexazatetracyclo[18.6.1.04,9.022,26]heptacosa-1(27),4,6,8,20,22,24-heptaene-17,4’-piperidine]	2104174: Inhibition of CDK7/cyclin H/MNAT1 (unknown origin) preincubated for 10 mins followed by substrate addition and measured after 60 mins in presence of ATP by ADP-Glo reagent based luminescence microtiter plate reader analysis	ki	0.0021	uM
N-[(1R)-2-(dimethylamino)-1-phenylethyl]-6,6-dimethyl-3-[[4-(prop-2-enoylamino)benzoyl]amino]-1,4-dihydropyrrolo[3,4-d]pyrazole-5-carboxamide	2125276: Inhibition of recombinant GST-tagged CDK7/CycH/MAT1 (unknown origin) extracted from baculo-virus infected Sf9 insect cells assessed as inhibition constant using ATP containing 32P measured after 15 mins by Beckman liquid scintillation counter analysis	ki	0.0022	uM
(12R)-22-propan-2-ylspiro[10-oxa-2,18,20,24,25,26-hexazatetracyclo[17.6.1.04,9.021,25]hexacosa-1(26),4,6,8,19,21,23-heptaene-16,4’-piperidine]-12-ol	2104174: Inhibition of CDK7/cyclin H/MNAT1 (unknown origin) preincubated for 10 mins followed by substrate addition and measured after 60 mins in presence of ATP by ADP-Glo reagent based luminescence microtiter plate reader analysis	ki	0.0022	uM
7-dimethylphosphoryl-3-[2-[[(3S)-6,6-dimethylpiperidin-3-yl]amino]-5-(trifluoromethyl)pyrimidin-4-yl]-1H-indole-6-carbonitrile	2092594: Inhibition of human His-tagged CDK7/cyclin H/MNAT1 expressed in baculovirus infected insect cells preincubated for 10 mins followed by substrate and ATP addition and measured after 60 mins by ADP-Glo kinase assay	ic50	0.0025	uM
(3S,4S)-4-[(20-propan-2-yl-10-oxa-2,16,18,22,23,24-hexazatetracyclo[15.6.1.04,9.019,23]tetracosa-1(24),4,6,8,17,19,21-heptaen-16-yl)methyl]pyrrolidin-3-ol	2107679: Inhibition of recombinant human His-tagged CDK7/cyclin H/MNAT1 expressed in baculovirus expression system using histone H1 as substrate preincubated for 10 mins followed by substrate and ATP addition and measured after 60 mins by ADP-Glo reagent based microplate reader assay	ki	0.0028	uM
12-methoxy-22-propan-2-ylspiro[10-oxa-2,18,20,24,25,26-hexazatetracyclo[17.6.1.04,9.021,25]hexacosa-1(26),4,6,8,19,21,23-heptaene-16,4’-piperidine]	2104174: Inhibition of CDK7/cyclin H/MNAT1 (unknown origin) preincubated for 10 mins followed by substrate addition and measured after 60 mins in presence of ATP by ADP-Glo reagent based luminescence microtiter plate reader analysis	ki	0.0029	uM
(16E)-14-methyl-20-oxa-5,7,14,27-tetrazatetracyclo[19.3.1.12,6.18,12]heptacosa-1(25),2(27),3,5,8,10,12(26),16,21,23-decaene	1317353: Inhibition of recombinant human full length C-terminal His6-tagged CDK7/cyclin H/N-terminal GST-tagged MAT1 expressed in baculovirus infected Sf21 insect cells using cdk7 substrate peptide	ic50	0.0030	uM
(12S)-22-propan-2-ylspiro[10-oxa-2,18,20,24,25,26-hexazatetracyclo[17.6.1.04,9.021,25]hexacosa-1(26),4,6,8,19,21,23-heptaene-16,4’-piperidine]-12-ol	2104174: Inhibition of CDK7/cyclin H/MNAT1 (unknown origin) preincubated for 10 mins followed by substrate addition and measured after 60 mins in presence of ATP by ADP-Glo reagent based luminescence microtiter plate reader analysis	ki	0.0030	uM
(3R,4R)-4-[[[7-(benzylamino)-3-propan-2-ylpyrazolo[1,5-a]pyrimidin-5-yl]amino]methyl]piperidin-3-ol	2104174: Inhibition of CDK7/cyclin H/MNAT1 (unknown origin) preincubated for 10 mins followed by substrate addition and measured after 60 mins in presence of ATP by ADP-Glo reagent based luminescence microtiter plate reader analysis	ki	0.0032	uM
22-propan-2-ylspiro[10-oxa-2,18,20,24,25,26-hexazatetracyclo[17.6.1.04,9.021,25]hexacosa-1(26),4,6,8,19,21,23-heptaene-16,4’-piperidine]	2104174: Inhibition of CDK7/cyclin H/MNAT1 (unknown origin) preincubated for 10 mins followed by substrate addition and measured after 60 mins in presence of ATP by ADP-Glo reagent based luminescence microtiter plate reader analysis	ki	0.0034	uM
7-methyl-22-propan-2-ylspiro[10-oxa-2,8,18,20,24,25,26-heptazatetracyclo[17.6.1.04,9.021,25]hexacosa-1(26),4(9),5,7,19,21,23-heptaene-16,4’-piperidine]	2104174: Inhibition of CDK7/cyclin H/MNAT1 (unknown origin) preincubated for 10 mins followed by substrate addition and measured after 60 mins in presence of ATP by ADP-Glo reagent based luminescence microtiter plate reader analysis	ic50	0.0037	uM
20-propan-2-ylspiro[2,16,18,22,23,24-hexazatetracyclo[15.6.1.04,9.019,23]tetracosa-1(24),4,6,8,17,19,21-heptaene-14,4’-piperidine]	2104174: Inhibition of CDK7/cyclin H/MNAT1 (unknown origin) preincubated for 10 mins followed by substrate addition and measured after 60 mins in presence of ATP by ADP-Glo reagent based luminescence microtiter plate reader analysis	ki	0.0038	uM
N-[(1S,3R)-3-[[5-chloro-4-(1H-indol-3-yl)pyrimidin-2-yl]amino]cyclohexyl]-5-[[(E)-4-(dimethylamino)but-2-enoyl]amino]pyridine-2-carboxamide	1609458: Competitive irreversible inhibition of CDK7/cyclinH/MAT1 (unknown origin)	ec50	0.0040	uM
4-N-[5-[[(1S)-2-(dimethylamino)-1-phenylethyl]carbamoyl]-6,6-dimethyl-1,4-dihydropyrrolo[3,4-d]pyrazol-3-yl]-1-N-[4-[[(2S)-1-[(2S,4R)-4-hydroxy-2-[[(1S)-1-[4-(4-methyl-1,3-thiazol-5-yl)phenyl]ethyl]carbamoyl]pyrrolidin-1-yl]-3,3-dimethyl-1-oxobutan-2-yl]amino]-4-oxobutyl]benzene-1,4-dicarboxamide	2125279: Inhibition of CDK7/CycH/MNAT1 (unknown origin) assessed as change in TR-FRET ratio using Cdk7/9tide as substrate and ATP by in vitro Adapta Eu kinase assay	ic50	0.0056	uM
4-(7-dimethylphosphoryl-1H-indol-3-yl)-N-[(3S)-piperidin-3-yl]thieno[3,2-d]pyrimidin-2-amine	2092594: Inhibition of human His-tagged CDK7/cyclin H/MNAT1 expressed in baculovirus infected insect cells preincubated for 10 mins followed by substrate and ATP addition and measured after 60 mins by ADP-Glo kinase assay	ic50	0.0061	uM
4-N-[5-[[(1S)-2-(dimethylamino)-1-phenylethyl]carbamoyl]-6,6-dimethyl-1,4-dihydropyrrolo[3,4-d]pyrazol-3-yl]-1-N-[2-[2-[2-[[2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindol-4-yl]amino]ethoxy]ethoxy]ethyl]benzene-1,4-dicarboxamide	2125279: Inhibition of CDK7/CycH/MNAT1 (unknown origin) assessed as change in TR-FRET ratio using Cdk7/9tide as substrate and ATP by in vitro Adapta Eu kinase assay	ic50	0.0064	uM
7-dimethylphosphoryl-3-[2-[[(3S,5S)-5-fluoropiperidin-3-yl]amino]thieno[3,2-d]pyrimidin-4-yl]-1H-indole-6-carbonitrile	2092594: Inhibition of human His-tagged CDK7/cyclin H/MNAT1 expressed in baculovirus infected insect cells preincubated for 10 mins followed by substrate and ATP addition and measured after 60 mins by ADP-Glo kinase assay	ic50	0.0065	uM
4-N-[5-[[(1S)-2-(dimethylamino)-1-phenylethyl]carbamoyl]-6,6-dimethyl-1,4-dihydropyrrolo[3,4-d]pyrazol-3-yl]-1-N-[2-[[2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindol-4-yl]amino]ethyl]benzene-1,4-dicarboxamide	2125279: Inhibition of CDK7/CycH/MNAT1 (unknown origin) assessed as change in TR-FRET ratio using Cdk7/9tide as substrate and ATP by in vitro Adapta Eu kinase assay	ic50	0.0067	uM
N-[(1R)-2-(dimethylamino)-1-phenylethyl]-6,6-dimethyl-3-[[4-(propanoylamino)benzoyl]amino]-1,4-dihydropyrrolo[3,4-d]pyrazole-5-carboxamide	2125278: Inhibition of CDK7/CycH/MAT1 (unknown origin)	ic50	0.0068	uM
4-N-[5-[[(1S)-2-(dimethylamino)-1-phenylethyl]carbamoyl]-6,6-dimethyl-1,4-dihydropyrrolo[3,4-d]pyrazol-3-yl]-1-N-[5-[2-(2,4-dioxocyclohexyl)-1,3-dioxoisoindol-4-yl]pent-4-ynyl]benzene-1,4-dicarboxamide	2125279: Inhibition of CDK7/CycH/MNAT1 (unknown origin) assessed as change in TR-FRET ratio using Cdk7/9tide as substrate and ATP by in vitro Adapta Eu kinase assay	ic50	0.0069	uM
N-[(1S)-2-(dimethylamino)-1-phenylethyl]-6,6-dimethyl-3-[(2-methylthieno[3,2-d]pyrimidin-4-yl)amino]-1,4-dihydropyrrolo[3,4-d]pyrazole-5-carboxamide	1651611: Inhibition of CDK7/cyclin H/MNAT1 (unknown origin) pre incubated up to 60 mins followed by substrate and ATP addition	ic50	0.0070	uM
7-dimethylphosphoryl-3-[2-[[(3S,5S)-5-methylpiperidin-3-yl]amino]thieno[3,2-d]pyrimidin-4-yl]-1H-indole-6-carbonitrile	2092594: Inhibition of human His-tagged CDK7/cyclin H/MNAT1 expressed in baculovirus infected insect cells preincubated for 10 mins followed by substrate and ATP addition and measured after 60 mins by ADP-Glo kinase assay	ic50	0.0072	uM
4-(7-dimethylphosphoryl-4-fluoro-1H-indol-3-yl)-N-[(3S)-piperidin-3-yl]thieno[3,2-d]pyrimidin-2-amine	2092594: Inhibition of human His-tagged CDK7/cyclin H/MNAT1 expressed in baculovirus infected insect cells preincubated for 10 mins followed by substrate and ATP addition and measured after 60 mins by ADP-Glo kinase assay	ic50	0.0073	uM
N-[(1S)-2-(dimethylamino)-1-phenylethyl]-6,6-dimethyl-3-[3-[[4-(prop-2-enoylamino)benzoyl]amino]anilino]-1,4-dihydropyrrolo[3,4-d]pyrazole-5-carboxamide	1651611: Inhibition of CDK7/cyclin H/MNAT1 (unknown origin) pre incubated up to 60 mins followed by substrate and ATP addition	ic50	0.0076	uM
4-N-[5-[[(1S)-2-(dimethylamino)-1-phenylethyl]carbamoyl]-4,6-dihydro-1H-pyrrolo[3,4-d]pyrazol-3-yl]-1-N-[2-[2-[3-[[(2S)-1-[(2S,4R)-4-hydroxy-2-[[(1S)-1-[4-(4-methyl-1,3-thiazol-5-yl)phenyl]ethyl]carbamoyl]pyrrolidin-1-yl]-3,3-dimethyl-1-oxobutan-2-yl]amino]-3-oxopropoxy]ethoxy]ethyl]benzene-1,4-dicarboxamide	2125279: Inhibition of CDK7/CycH/MNAT1 (unknown origin) assessed as change in TR-FRET ratio using Cdk7/9tide as substrate and ATP by in vitro Adapta Eu kinase assay	ic50	0.0076	uM
8-fluoro-20-propan-2-ylspiro[2,16,18,22,23,24-hexazatetracyclo[15.6.1.04,9.019,23]tetracosa-1(24),4(9),5,7,17,19,21-heptaene-14,4’-piperidine]	2104174: Inhibition of CDK7/cyclin H/MNAT1 (unknown origin) preincubated for 10 mins followed by substrate addition and measured after 60 mins in presence of ATP by ADP-Glo reagent based luminescence microtiter plate reader analysis	ic50	0.0076	uM
4-N-[5-[[(1S)-2-(dimethylamino)-1-phenylethyl]carbamoyl]-6,6-dimethyl-1,4-dihydropyrrolo[3,4-d]pyrazol-3-yl]-1-N-[8-[[(2S)-1-[(2S,4R)-4-hydroxy-2-[2-[[(1S)-1-[4-(4-methyl-1,3-thiazol-5-yl)phenyl]ethyl]amino]-2-oxoethyl]pyrrolidin-1-yl]-3,3-dimethyl-1-oxobutan-2-yl]amino]-8-oxooctyl]benzene-1,4-dicarboxamide	2125279: Inhibition of CDK7/CycH/MNAT1 (unknown origin) assessed as change in TR-FRET ratio using Cdk7/9tide as substrate and ATP by in vitro Adapta Eu kinase assay	ic50	0.0078	uM
4-N-[5-[[(1S)-2-(dimethylamino)-1-phenylethyl]carbamoyl]-6,6-dimethyl-1,4-dihydropyrrolo[3,4-d]pyrazol-3-yl]-1-N-[6-[[(2S)-1-[(2S,4R)-4-hydroxy-2-[[(1S)-1-[4-(4-methyl-1,3-thiazol-5-yl)phenyl]ethyl]carbamoyl]pyrrolidin-1-yl]-3,3-dimethyl-1-oxobutan-2-yl]amino]-6-oxohexyl]benzene-1,4-dicarboxamide	2125279: Inhibition of CDK7/CycH/MNAT1 (unknown origin) assessed as change in TR-FRET ratio using Cdk7/9tide as substrate and ATP by in vitro Adapta Eu kinase assay	ic50	0.0081	uM
4-methyl-3-[(1-methyl-6-pyridin-3-ylpyrazolo[3,4-d]pyrimidin-4-yl)amino]-N-[3-(trifluoromethyl)phenyl]benzamide	2148760: Binding affinity to human MNAT1 incubated for 45 mins by Kinobead based pull down assay	kd	0.0085	uM
1-N-[5-[[5-[4-[(1S)-1-[[(2S,4R)-1-[(2S)-2-acetamido-3,3-dimethylbutanoyl]-4-hydroxypyrrolidine-2-carbonyl]amino]ethyl]phenyl]-1,3-thiazole-4-carbonyl]amino]pentyl]-4-N-[5-[[(1S)-2-(dimethylamino)-1-phenylethyl]carbamoyl]-6,6-dimethyl-1,4-dihydropyrrolo[3,4-d]pyrazol-3-yl]benzene-1,4-dicarboxamide	2125279: Inhibition of CDK7/CycH/MNAT1 (unknown origin) assessed as change in TR-FRET ratio using Cdk7/9tide as substrate and ATP by in vitro Adapta Eu kinase assay	ic50	0.0086	uM
4-N-[5-[[(1S)-2-(dimethylamino)-1-phenylethyl]carbamoyl]-6,6-dimethyl-1,4-dihydropyrrolo[3,4-d]pyrazol-3-yl]-1-N-[3-[[(2S)-1-[(2S,4R)-4-hydroxy-2-[[(1S)-1-[4-(4-methyl-1,3-thiazol-5-yl)phenyl]ethyl]carbamoyl]pyrrolidin-1-yl]-3,3-dimethyl-1-oxobutan-2-yl]amino]-3-oxopropyl]benzene-1,4-dicarboxamide	2125279: Inhibition of CDK7/CycH/MNAT1 (unknown origin) assessed as change in TR-FRET ratio using Cdk7/9tide as substrate and ATP by in vitro Adapta Eu kinase assay	ic50	0.0087	uM
4-(7-dimethylphosphoryl-5-fluoro-1H-indol-3-yl)-N-[(3S)-piperidin-3-yl]thieno[3,2-d]pyrimidin-2-amine	2092594: Inhibition of human His-tagged CDK7/cyclin H/MNAT1 expressed in baculovirus infected insect cells preincubated for 10 mins followed by substrate and ATP addition and measured after 60 mins by ADP-Glo kinase assay	ic50	0.0087	uM
7-dimethylphosphoryl-3-[2-[[(3S)-piperidin-3-yl]amino]thieno[3,2-d]pyrimidin-4-yl]-1H-indole-6-carbonitrile	2092594: Inhibition of human His-tagged CDK7/cyclin H/MNAT1 expressed in baculovirus infected insect cells preincubated for 10 mins followed by substrate and ATP addition and measured after 60 mins by ADP-Glo kinase assay	ic50	0.0088	uM
4-(7-diethylphosphoryl-1H-indol-3-yl)-N-[(3S)-piperidin-3-yl]thieno[3,2-d]pyrimidin-2-amine	2092594: Inhibition of human His-tagged CDK7/cyclin H/MNAT1 expressed in baculovirus infected insect cells preincubated for 10 mins followed by substrate and ATP addition and measured after 60 mins by ADP-Glo kinase assay	ic50	0.0089	uM
4-N-[5-[[(1S)-2-(dimethylamino)-1-phenylethyl]carbamoyl]-6,6-dimethyl-1,4-dihydropyrrolo[3,4-d]pyrazol-3-yl]-1-N-[5-[2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindol-4-yl]oxypentyl]benzene-1,4-dicarboxamide	2125279: Inhibition of CDK7/CycH/MNAT1 (unknown origin) assessed as change in TR-FRET ratio using Cdk7/9tide as substrate and ATP by in vitro Adapta Eu kinase assay	ic50	0.0092	uM
4-N-[5-[[(1S)-2-(dimethylamino)-1-phenylethyl]carbamoyl]-6,6-dimethyl-1,4-dihydropyrrolo[3,4-d]pyrazol-3-yl]-1-N-[6-[[2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindol-4-yl]amino]hexyl]benzene-1,4-dicarboxamide	2125279: Inhibition of CDK7/CycH/MNAT1 (unknown origin) assessed as change in TR-FRET ratio using Cdk7/9tide as substrate and ATP by in vitro Adapta Eu kinase assay	ic50	0.0094	uM
20-propan-2-yl-16-(pyrrolidin-3-ylmethyl)-10-oxa-2,16,18,22,23,24-hexazatetracyclo[15.6.1.04,9.019,23]tetracosa-1(24),4,6,8,17,19,21-heptaene	2107679: Inhibition of recombinant human His-tagged CDK7/cyclin H/MNAT1 expressed in baculovirus expression system using histone H1 as substrate preincubated for 10 mins followed by substrate and ATP addition and measured after 60 mins by ADP-Glo reagent based microplate reader assay	ki	0.0095	uM
N-[(1S)-2-(dimethylamino)-1-phenylethyl]-6,6-dimethyl-3-[[4-(prop-2-enoylamino)benzoyl]amino]-1,4-dihydropyrrolo[3,4-d]pyrazole-5-carboxamide	1651611: Inhibition of CDK7/cyclin H/MNAT1 (unknown origin) pre incubated up to 60 mins followed by substrate and ATP addition	ic50	0.0097	uM
N-[3-[[5-chloro-4-(1H-indol-3-yl)pyrimidin-2-yl]amino]phenyl]-4-[[(E)-4-(dimethylamino)but-2-enoyl]amino]benzamide	1609458: Competitive irreversible inhibition of CDK7/cyclinH/MAT1 (unknown origin)	ec50	0.0100	uM
4-(7-bromo-1H-indol-3-yl)-N-[(3S)-piperidin-3-yl]thieno[3,2-d]pyrimidin-2-amine	2092594: Inhibition of human His-tagged CDK7/cyclin H/MNAT1 expressed in baculovirus infected insect cells preincubated for 10 mins followed by substrate and ATP addition and measured after 60 mins by ADP-Glo kinase assay	ic50	0.0101	uM
4-(7-methylsulfonyl-1H-indol-3-yl)-N-[(3S)-piperidin-3-yl]thieno[3,2-d]pyrimidin-2-amine	2092594: Inhibition of human His-tagged CDK7/cyclin H/MNAT1 expressed in baculovirus infected insect cells preincubated for 10 mins followed by substrate and ATP addition and measured after 60 mins by ADP-Glo kinase assay	ic50	0.0102	uM
4-(7-dimethylphosphoryl-1H-pyrrolo[2,3-c]pyridin-3-yl)-N-[(3S)-piperidin-3-yl]thieno[3,2-d]pyrimidin-2-amine	2092594: Inhibition of human His-tagged CDK7/cyclin H/MNAT1 expressed in baculovirus infected insect cells preincubated for 10 mins followed by substrate and ATP addition and measured after 60 mins by ADP-Glo kinase assay	ic50	0.0110	uM
4-N-[5-[[(1S)-2-(dimethylamino)-1-phenylethyl]carbamoyl]-6,6-dimethyl-1,4-dihydropyrrolo[3,4-d]pyrazol-3-yl]-1-N-[2-[3-[[(2S)-1-[(2S,4R)-4-hydroxy-2-[[(1S)-1-[4-(4-methyl-1,3-thiazol-5-yl)phenyl]ethyl]carbamoyl]pyrrolidin-1-yl]-3,3-dimethyl-1-oxobutan-2-yl]amino]-3-oxopropoxy]ethyl]benzene-1,4-dicarboxamide	2125279: Inhibition of CDK7/CycH/MNAT1 (unknown origin) assessed as change in TR-FRET ratio using Cdk7/9tide as substrate and ATP by in vitro Adapta Eu kinase assay	ic50	0.0111	uM
4-N-[5-[[(1S)-2-(dimethylamino)-1-phenylethyl]carbamoyl]-6,6-dimethyl-1,4-dihydropyrrolo[3,4-d]pyrazol-3-yl]-1-N-[2-[2-[[2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindol-4-yl]amino]ethoxy]ethyl]benzene-1,4-dicarboxamide	2125279: Inhibition of CDK7/CycH/MNAT1 (unknown origin) assessed as change in TR-FRET ratio using Cdk7/9tide as substrate and ATP by in vitro Adapta Eu kinase assay	ic50	0.0113	uM
4-N-[5-[[(1S)-2-(dimethylamino)-1-phenylethyl]carbamoyl]-6,6-dimethyl-1,4-dihydropyrrolo[3,4-d]pyrazol-3-yl]-1-N-[8-[2-[[[1-[2-[(1-fluorocyclopropanecarbonyl)amino]-3,3-dimethylbutanoyl]-3-hydroxypyrrolidine-2-carbonyl]amino]methyl]-5-(4-methyl-1,3-thiazol-5-yl)phenoxy]octyl]benzene-1,4-dicarboxamide	2125279: Inhibition of CDK7/CycH/MNAT1 (unknown origin) assessed as change in TR-FRET ratio using Cdk7/9tide as substrate and ATP by in vitro Adapta Eu kinase assay	ic50	0.0121	uM
N-[(1S)-2-(dimethylamino)-1-phenylethyl]-3-[[4-[5-[[(2S)-1-[(2S,4R)-4-hydroxy-2-[[(1S)-1-[4-(4-methyl-1,3-thiazol-5-yl)phenyl]ethyl]carbamoyl]pyrrolidin-1-yl]-3,3-dimethyl-1-oxobutan-2-yl]amino]-5-oxopentoxy]benzoyl]amino]-6,6-dimethyl-1,4-dihydropyrrolo[3,4-d]pyrazole-5-carboxamide	2125279: Inhibition of CDK7/CycH/MNAT1 (unknown origin) assessed as change in TR-FRET ratio using Cdk7/9tide as substrate and ATP by in vitro Adapta Eu kinase assay	ic50	0.0126	uM
N-[(1S,3R)-3-[[5-chloro-4-(1H-indol-3-yl)pyrimidin-2-yl]amino]-1-methylcyclohexyl]-5-[[(E)-4-(dimethylamino)but-2-enoyl]amino]pyridine-2-carboxamide	1609458: Competitive irreversible inhibition of CDK7/cyclinH/MAT1 (unknown origin)	ec50	0.0130	uM
4-N-[5-[[(1S)-2-(dimethylamino)-1-phenylethyl]carbamoyl]-6,6-dimethyl-1,4-dihydropyrrolo[3,4-d]pyrazol-3-yl]-1-N-[6-[2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindol-4-yl]hex-5-ynyl]benzene-1,4-dicarboxamide	2125279: Inhibition of CDK7/CycH/MNAT1 (unknown origin) assessed as change in TR-FRET ratio using Cdk7/9tide as substrate and ATP by in vitro Adapta Eu kinase assay	ic50	0.0133	uM

CTD chemical–gene interactions

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

Chemical	Actions (top 5)	PubMed papers
Benzo(a)pyrene	increases expression, affects methylation, decreases expression	3
bisphenol A	decreases expression, decreases methylation	2
sodium arsenite	increases expression	2
Cisplatin	decreases expression	2
Valproic Acid	increases expression	2
Cadmium Chloride	decreases expression, increases expression	2
FR900359	affects phosphorylation	1
dicrotophos	decreases expression	1
trichostatin A	affects expression	1
beta-lapachone	increases expression	1
mono-(2-ethylhexyl)phthalate	increases expression	1
aflatoxin B2	decreases methylation	1
coumarin	increases phosphorylation	1
CGP 52608	affects binding, increases reaction	1
U 0126	affects expression, affects reaction	1
fenpyroximate	decreases expression	1
4-chloro-N-((4-(1,1-dimethylethyl)phenyl)methyl)-3-ethyl-1-methyl-1H-pyrazole-5-carboxamide	decreases expression	1
ICG 001	decreases expression	1
abrine	increases expression	1
picoxystrobin	decreases expression	1
Vorinostat	increases expression	1
Air Pollutants	decreases expression, increases abundance	1
Antimycin A	decreases expression	1
Gold	decreases expression	1
Ivermectin	decreases expression	1
Parabens	affects cotreatment, decreases expression	1
Phthalic Acids	affects cotreatment, decreases expression	1
Smoke	decreases expression, increases abundance	1
Tretinoin	increases degradation, increases ubiquitination	1
7,8-Dihydro-7,8-dihydroxybenzo(a)pyrene 9,10-oxide	decreases expression	1

ChEMBL screening assays

206 unique, capped per target: 204 binding, 2 functional

Representative assays (with source publication via chembl_document):

Assay ID	Type	Description	Source paper
CHEMBL2405930	Binding	Inhibition of CDK7/cyclinH/MNAT1 (unknown origin) at 10 uM relative to control	Design and synthesis of highly selective, orally active Polo-like kinase-2 (Plk-2) inhibitors. — Bioorg Med Chem Lett
CHEMBL5724508	Functional	Biochemical CDK7 assay (KIapp) ( CDK7 catalyzed, ATP-dependent, phosphorylation of a peptide substrate derived from RNA Pol II (CDK7/9-tide). Coupled via lactate dehydrogenase (LDH) and pyruvate kinase (PK) to lactate and NAD+ production, w	Data for DCP probe JNJ-3738

Clinical trials (associated diseases)

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