CETP

Summary

CETP (cholesteryl ester transfer protein, HGNC:1869) is a protein-coding gene on chromosome 16q13, encoding Cholesteryl ester transfer protein (P11597). Involved in the transfer of neutral lipids, including cholesteryl ester and triglyceride, among lipoprotein particles.

The protein encoded by this gene is found in plasma, where it is involved in the transfer of cholesteryl ester from high density lipoprotein (HDL) to other lipoproteins. Defects in this gene are a cause of hyperalphalipoproteinemia 1 (HALP1). Two transcript variants encoding different isoforms have been found for this gene.

Source: NCBI Gene 1071 — RefSeq curated summary.

At a glance

• Gene–disease (curated): cholesterol-ester transfer protein deficiency (Strong, GenCC)
• GWAS associations: 308
• Clinical variants (ClinVar): 384 total — 4 pathogenic, 5 likely-pathogenic
• Phenotypes (HPO): 2
• Druggable target: yes — 5 molecules with ChEMBL bioactivity
• MANE Select transcript: NM_000078

Identifiers

Gene identifiers

Field	Value
HGNC ID	HGNC:1869
Approved symbol	CETP
Name	cholesteryl ester transfer protein
Location	16q13
Locus type	gene with protein product
Status	Approved
Aliases	BPIFF
Ensembl gene	ENSG00000087237
Ensembl biotype	protein_coding
OMIM	118470
Entrez	1071

Gene structure

Transcript identifiers

Ensembl transcripts: 16 — 14 protein_coding, 1 protein_coding_CDS_not_defined, 1 retained_intron

ENST00000200676, ENST00000379780, ENST00000566128, ENST00000569082, ENST00000650358, ENST00000858282, ENST00000858283, ENST00000858284, ENST00000858285, ENST00000858286, ENST00000858287, ENST00000858288, ENST00000858289, ENST00000858290, ENST00000858291, ENST00000954203

RefSeq mRNA: 2 — MANE Select: NM_000078 NM_000078, NM_001286085

CCDS: CCDS10772, CCDS67032

Canonical transcript exons

ENST00000200676 — 16 exons

Exon	Start	End
ENSE00000685092	56983326	56983411
ENSE00000685093	56982165	56982237
ENSE00000685094	56981647	56981680
ENSE00000685095	56981158	56981225
ENSE00000685096	56978091	56978255
ENSE00000685099	56975101	56975151
ENSE00000685100	56973331	56973510
ENSE00000685102	56971321	56971381
ENSE00001820497	56961950	56962097
ENSE00001925693	56983592	56983845
ENSE00003509141	56971033	56971102
ENSE00003581433	56969386	56969520
ENSE00003585849	56963010	56963124
ENSE00003597005	56969914	56970001
ENSE00003634915	56971992	56972083
ENSE00003666311	56969611	56969681

Expression profiles

Bgee: expression breadth ubiquitous, 165 present calls, max score 89.43.

FANTOM5 (CAGE): breadth broad, TPM avg 1.5097 / max 150.8059, expressed in 214 samples.

FANTOM5 promoters (2 alternative TSS)

Promoter ID	TPM avg	Samples expressed
154297	1.4627	213
154296	0.0470	25

Top tissues by expression

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

Tissue	Anatomy ID	Expression score	Quality
lymph node	UBERON:0000029	89.43	gold quality
spleen	UBERON:0002106	87.79	gold quality
liver	UBERON:0002107	78.68	gold quality
male germ line stem cell (sensu Vertebrata) in testis	CL:0000089 ∩ UBERON:0000473	77.65	gold quality
right lobe of liver	UBERON:0001114	75.76	gold quality
monocyte	CL:0000576	74.15	gold quality
mononuclear cell	CL:0000842	73.93	gold quality
omental fat pad	UBERON:0010414	73.89	gold quality
peritoneum	UBERON:0002358	73.80	gold quality
adipose tissue of abdominal region	UBERON:0007808	73.51	gold quality
leukocyte	CL:0000738	73.34	gold quality
gall bladder	UBERON:0002110	72.76	gold quality
left lobe of thyroid gland	UBERON:0001120	71.99	gold quality
vermiform appendix	UBERON:0001154	70.85	gold quality
thyroid gland	UBERON:0002046	70.42	gold quality
right lobe of thyroid gland	UBERON:0001119	69.11	gold quality
adipose tissue	UBERON:0001013	68.49	gold quality
placenta	UBERON:0001987	68.00	gold quality
left adrenal gland cortex	UBERON:0035825	67.79	gold quality
left adrenal gland	UBERON:0001234	67.74	gold quality
connective tissue	UBERON:0002384	67.68	gold quality
granulocyte	CL:0000094	67.58	gold quality
adenohypophysis	UBERON:0002196	67.30	gold quality
upper lobe of left lung	UBERON:0008952	66.79	gold quality
pituitary gland	UBERON:0000007	66.50	gold quality
subcutaneous adipose tissue	UBERON:0002190	66.50	gold quality
adrenal gland	UBERON:0002369	66.01	gold quality
caecum	UBERON:0001153	65.74	gold quality
adrenal tissue	UBERON:0018303	65.70	gold quality
adrenal cortex	UBERON:0001235	65.48	gold quality

Single-cell (SCXA)

Detected in 3 experiment(s), a significant marker in 2.

Experiment	Marker?	Max mean expression
E-HCAD-10	yes	34.04
E-MTAB-10553	yes	25.09
E-ANND-3	no	3.13

Regulation

Is transcription factor: no

Upstream regulators (CollecTRI, top): CEBPA, CEBPB, CEBPG, NR0B2, NR1H2, NR1H3, NR1H4, NR2F2, NR5A2, PITX2, PPARA, SP1, SP3, SREBF1, SREBF2, YY1

miRNA regulators (miRDB)

8 targeting CETP, 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-4267	99.96	66.53	2368
HSA-MIR-4739	99.84	65.25	1832
HSA-MIR-1321	99.84	65.30	1811
HSA-MIR-4756-5P	99.84	64.98	1809
HSA-MIR-765	99.84	68.24	2442
HSA-MIR-11181-3P	99.75	66.38	2205
HSA-MIR-651-5P	99.64	68.49	1104
HSA-MIR-6827-5P	98.46	64.88	1256

Literature-anchored findings (GeneRIF, showing 40)

• genetic variation at the CETP gene locus may account for a significant proportion of the difference in HDL-C levels (PMID:11810297)
• The activity and mass of cholesteryl ester transfer protein (CETP) in cord blood were higher than those in adult blood. (PMID:11882335)
• A novel mutation in the intron 1 splice donor site of the cholesterol ester transfer protein (CETP) gene as a cause of hyperalphalipoproteinemia. (PMID:11887180)
• TaqIB2 allele was found not to be associated with significant changes in coronary artery disease risk (PMID:11903340)
• role in the regulation of the vascular cell functions (PMID:11915346)
• Association between HDL-cholesterol and the Taq1B polymorphism in the cholesterol ester transfer protein gene in obese women. (PMID:11996962)
• CETP genotype may contribute to the interindividual differences in plasma HDL-C subfraction changes occurring with endurance exercise training in sedentary middle- to older-aged men and women (PMID:12037734)
• B2 allele of the TaqIB polymorphism is less frequent in African Americans compared with Caucasians;this polymorphism is unlikely to contribute to higher levels of HDL-C reported in African Americans. (PMID:12048136)
• CETP is increased and associated with the atherogenic lipoprotein profile in obese children (PMID:12055319)
• present observations provide direct support for a potent specific inhibition of CETP by plasma apoCI in vivo (PMID:12070157)
• Two novel missense mutations in the CETP gene in Japanese hyperalphalipoproteinemic subjects: high-throughput assay by Invader assay. (PMID:12091484)
• CETP gene mutation (D442G) increases low-density lipoprotein particle size in patients with coronary heart disease. (PMID:12104085)
• In men with coronary heart disease (CHD) and high density lipoprotein cholesterol (HDL-C)deficiency, the CETP TaqI B2B2 genotype is significantly reduced and is associated with higher levels of plasma HDL-C and lower CHD risk. (PMID:12117730)
• D442G mutation is common in Korean postmenopausal women and it is associated with increased plasma HDL cholesterol level. (PMID:12164095)
• elevated PLTP activity in human cholesteryl ester transfer protein (huCEPT) transgenic mice results in an increase in VLDL secretion (PMID:12401886)
• attenuates atherosclerosis in ovariectomized mice [Cholesteryl ester transfer protein ] (PMID:12518020)
• IVS14A and 451Q mutants of cholesteryl ester transfer protein (CETP) gene were rare in Chinese population and 442G mutant gene was possibly one of the susceptibility factors to Coronary Arteriosclerosis in Chinese. (PMID:12579494)
• Reviewed studies reveal that human subjects with heterozygous CETP deficiency and an HDL cholesterol level >60 mg/dL have a reduced risk of coronary heart disease. (PMID:12588754)
• CEPT gene locus have an additional and interactive influence on plasma lipid and lipoprotein levels in children. (PMID:12669678)
• Sp1 and Sp3 regulate human CETP promoter activity through three Sp1/Sp3 binding sites in a distinct manner (PMID:12730302)
• In I405V CETP polymorphism, percentage reductions in plasma total cholesterol with consumption of plant sterol ester were not significant. CETP concentration diminished only in the II phenotype. (PMID:12771320)
• the association between high (HDL) and low-density (LDL) cholesterol concentrations and family-derived haplotypes based on six common SNPs in the cholesteryl-ester transfer protein (CETP) gene (PMID:12771549)
• The expression of human CETP in db/db mice prevented the formation of diet-induced lesions, suggesting an antiatherogenic effect of CETP in the context of diabetic obesity. (PMID:12791674)
• In patients with CAD, the CETP/-629A allele had a strong protective effect on future mortality from cardiovascular causes, independent of its role on HDL cholesterol and CETP activity levels. (PMID:12798569)
• Genetic variation in the CETP gene is associated with protective HDL-cholestrol levels. (PMID:12818401)
• CETP polymorphism were associated with moderately increased LDL peak aprticle size. (PMID:12818414)
• data collected in a cohort of 779 patients of whom 342 had developed restenosis indicate that the common variants for CETP and PON are not associated with incidence of restenosis after PTCA (PMID:12871320)
• CETP is modified by LTIP and has a role in remodeling of HDL3 and HDL2 particles in subclass-specific ways, strongly implicating it as a regulator of HDL metabolism (PMID:12907677)
• negative charge of LDL surface lipids, but not protein, is an important regulator of CETP and LTIP activity (PMID:12951364)
• The TT genotype of HL mutation may serve as a protective factor against vascular disease by increasing HDL cholesterol levels in hemodialysis patients with higher CETP levels. (PMID:14531818)
• Association of exceptional longevity with homozygosity for the valine 405 allele of CETP may explain in part the link between lipoprotein particle size and exceptional longevity (PMID:14559957)
• induction of CETP constitutes a major determinant of the effect of LXR agonists on cholesterol transport and excretion (PMID:14679166)
• CETP genotype did not influence lipid and lipoprotein levels in pregnant women. (PMID:14687732)
• Men with a CETP mutation had the lowest rates of coronary heart disease; whether a CETP mutation offers additional protection against CHD warrants further investigation. (PMID:14967821)
• No statistically significant differences have emerged with respect to either genotype or allele frequencies between late onset Alzheimer’s disease and control populations when examining CETP TaqI B polymorphism. (PMID:15036597)
• Postprandial chylomicrons may play an important role in promoting reverse cholesterol transport in vivo by serving as the preferred ultimate vehicle for transporting cholesterol released from cell membranes to the liver via LCAT and CETP. (PMID:15102891)
• Cholesteryl ester transfer protein, plasma (CETP) Taq1B gene polymorphism is an association with low HDL cholesterol levels in patients with type II diabetes mellitus and healthy controls. (PMID:15138631)
• CETP localizes B cells in germinal centres, a proportion of post-germinal centre B cells and their neoplastic counterparts. (PMID:15228446)
• overexpression of apoCI does not represent a suitable method for decreasing total CE transfer activity in CETPTg/apoCITg mice, owing to an hyperlipidaemia-mediated effect on CETP gene expression (PMID:15339254)
• Data describe a variable length tandem repeat in the cholesteryl ester transfer protein promoter that is highly polymorphic with respect to both length and sequence; the short allele of this repeat is associated with high HDL cholesterol levels in vivo. (PMID:15450208)

Cross-species orthologs

9 orthologs

Organism	Symbol	Gene ID
danio_rerio	cetp	ENSDARG00000030872
caenorhabditis_elegans		WBGENE00003812
caenorhabditis_elegans		WBGENE00007325
caenorhabditis_elegans		WBGENE00008512
caenorhabditis_elegans	F10D11.6	WBGENE00008652
caenorhabditis_elegans		WBGENE00015545
caenorhabditis_elegans		WBGENE00016951
caenorhabditis_elegans		WBGENE00020563
caenorhabditis_elegans		WBGENE00022627

Paralogs (12): BPIFB2 (ENSG00000078898), PLTP (ENSG00000100979), BPI (ENSG00000101425), BPIFB1 (ENSG00000125999), LBP (ENSG00000129988), BPIFA2 (ENSG00000131050), BPIFA3 (ENSG00000131059), BPIFB6 (ENSG00000167104), BPIFC (ENSG00000184459), BPIFB3 (ENSG00000186190), BPIFB4 (ENSG00000186191), BPIFA1 (ENSG00000198183)

Protein

Protein identifiers

Cholesteryl ester transfer protein — P11597 (reviewed: P11597)

Alternative names: Lipid transfer protein I

All UniProt accessions (4): P11597, A0A0S2Z3F6, A0A0S2Z3I8, H3BRJ9

UniProt curated annotations — full annotation on UniProt →

Function. Involved in the transfer of neutral lipids, including cholesteryl ester and triglyceride, among lipoprotein particles. Allows the net movement of cholesteryl ester from high density lipoproteins/HDL to triglyceride-rich very low density lipoproteins/VLDL, and the equimolar transport of triglyceride from VLDL to HDL. Regulates the reverse cholesterol transport, by which excess cholesterol is removed from peripheral tissues and returned to the liver for elimination.

Subcellular location. Secreted.

Tissue specificity. Expressed by the liver and secreted in plasma.

Disease relevance. Hyperalphalipoproteinemia 1 (HALP1) [MIM:143470] A condition characterized by high levels of high density lipoprotein (HDL) and increased HDL cholesterol levels. The disease is caused by variants affecting the gene represented in this entry.

Polymorphism. Genetic variations in CETP define the high density lipoprotein cholesterol level quantitative trait locus 10 (HDLCQ10) [MIM:143470].

Similarity. Belongs to the BPI/LBP/Plunc superfamily. BPI/LBP family.

Isoforms (2)

UniProt ID	Names	Canonical?
P11597-1	1	yes
P11597-2	2

RefSeq proteins (2): NP_000069, NP_001273014 (=MANE)

Domains & families (InterPro)

ID	Name	Type
IPR001124	Lipid-bd_serum_glycop_C	Domain
IPR017130	Cholesteryl_ester_transfer	Family
IPR017942	Lipid-bd_serum_glycop_N	Domain
IPR017943	Bactericidal_perm-incr_a/b_dom	Homologous_superfamily
IPR017954	Lipid-bd_serum_glycop_CS	Conserved_site

Pfam: PF01273, PF02886

Catalyzed reactions (Rhea), 3 shown:

• cholesteryl (9Z-octadecenoate)(in) = cholesteryl (9Z-octadecenoate)(out) (RHEA:43348)
• 1,2,3-tri-(9Z-octadecenoyl)-glycerol(in) = 1,2,3-tri-(9Z-octadecenoyl)-glycerol(out) (RHEA:43352)
• cholesteryl (9Z,12Z)-octadecadienoate(in) = cholesteryl (9Z,12Z)-octadecadienoate(out) (RHEA:43356)

UniProt features (71 total): strand 19, helix 18, sequence variant 12, mutagenesis site 11, glycosylation site 4, turn 3, signal peptide 1, chain 1, disulfide bond 1, splice variant 1

Structure

Experimental structures (PDB)

3 structures.

PDB	Method	Resolution (Å)
2OBD	X-RAY DIFFRACTION	2.1
4EWS	X-RAY DIFFRACTION	2.59
4F2A	X-RAY DIFFRACTION	3.11

Predicted structure (AlphaFold)

Model	pLDDT	Fraction very-high
AF-P11597-F1	91.45	0.77

Functional residue map

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

Disulfide bonds (1): 160–201

Glycosylation sites (4): 105, 257, 358, 413

Mutagenesis-validated functional residues (11):

Position	Phenotype
155	reduces triglyceride transfer and cholesteryl ester transfer 5-fold.
215	reduces triglyceride transfer 10-fold. no effect on cholesteryl ester transfer.
218	reduces triglyceride transfer 10-fold. slight reduction of cholesteryl ester transfer.
247	reduces triglyceride transfer 5-fold. slight reduction of cholesteryl ester transfer.
282	not secreted.
287	not secreted.
309	not secreted.
313	reduces cholesteryl ester transfer by 60%.
392	not secreted.
399	not secreted.
433	reduces activity by 60%.

Function

Pathways and Gene Ontology

Reactome pathways

3 pathways

ID	Pathway
R-HSA-8964041	LDL remodeling
R-HSA-8964058	HDL remodeling
R-HSA-9029569	NR1H3 & NR1H2 regulate gene expression linked to cholesterol transport and efflux

MSigDB gene sets: 149 (showing top): GOBP_ACYLGLYCEROL_HOMEOSTASIS, GOBP_PHOSPHOLIPID_METABOLIC_PROCESS, GOBP_PHOSPHATIDYLCHOLINE_METABOLIC_PROCESS, GOBP_STEROL_HOMEOSTASIS, GOBP_REGULATION_OF_CHOLESTEROL_EFFLUX, GOBP_POSITIVE_REGULATION_OF_STEROL_TRANSPORT, GOBP_ORGANOPHOSPHATE_METABOLIC_PROCESS, GOBP_POSITIVE_REGULATION_OF_LIPID_TRANSPORT, GOBP_ORGANIC_HYDROXY_COMPOUND_TRANSPORT, GOBP_ORGANOPHOSPHATE_ESTER_TRANSPORT, GOBP_LIPID_HOMEOSTASIS, GOBP_GLYCEROLIPID_METABOLIC_PROCESS, GOBP_CHOLESTEROL_EFFLUX, PICCALUGA_ANGIOIMMUNOBLASTIC_LYMPHOMA_UP, GOBP_PROTEIN_LIPID_COMPLEX_ORGANIZATION

GO Biological Process (21): triglyceride metabolic process (GO:0006641), lipid transport (GO:0006869), cholesterol metabolic process (GO:0008203), negative regulation of macrophage derived foam cell differentiation (GO:0010745), regulation of cholesterol efflux (GO:0010874), cholesterol transport (GO:0030301), positive regulation of cholesterol transport (GO:0032376), triglyceride transport (GO:0034197), very-low-density lipoprotein particle remodeling (GO:0034372), low-density lipoprotein particle remodeling (GO:0034374), high-density lipoprotein particle remodeling (GO:0034375), cholesterol homeostasis (GO:0042632), reverse cholesterol transport (GO:0043691), phosphatidylcholine metabolic process (GO:0046470), lipid homeostasis (GO:0055088), phospholipid homeostasis (GO:0055091), triglyceride homeostasis (GO:0070328), positive regulation of phospholipid transport (GO:2001140), lipid metabolic process (GO:0006629), steroid metabolic process (GO:0008202), phospholipid transport (GO:0015914)

GO Molecular Function (6): obsolete phospholipid transporter activity (GO:0005548), lipid binding (GO:0008289), cholesterol binding (GO:0015485), triglyceride binding (GO:0017129), phosphatidylcholine binding (GO:0031210), cholesterol transfer activity (GO:0120020)

GO Cellular Component (5): extracellular region (GO:0005576), obsolete extracellular space (GO:0005615), vesicle (GO:0031982), high-density lipoprotein particle (GO:0034364), extracellular exosome (GO:0070062)

Reactome top-level categories

Rollup of top-2 pathways:

Category	Pathways
Plasma lipoprotein remodeling	2
NR1H2 and NR1H3-mediated signaling	1

GO top-level categories

Rollup of top GO terms by namespace:

Category	Terms
regulation of cholesterol transport	2
cholesterol transport	2
plasma lipoprotein particle remodeling	2
acylglycerol metabolic process	1
transport	1
lipid localization	1
sterol metabolic process	1
secondary alcohol metabolic process	1
macrophage derived foam cell differentiation	1
regulation of macrophage derived foam cell differentiation	1
negative regulation of cell differentiation	1
cholesterol efflux	1
sterol transport	1
positive regulation of sterol transport	1
acylglycerol transport	1
triglyceride-rich lipoprotein particle remodeling	1
sterol homeostasis	1
glycerophospholipid metabolic process	1
chemical homeostasis	1
lipid homeostasis	1
acylglycerol homeostasis	1
phospholipid transport	1
positive regulation of lipid transport	1
regulation of phospholipid transport	1
primary metabolic process	1
lipid metabolic process	1
binding	1
sterol binding	1
alcohol binding	1
lipid binding	1
phospholipid binding	1
cation binding	1
quaternary ammonium group binding	1
cholesterol binding	1
sterol transfer activity	1
cellular anatomical structure	1
membrane-bounded organelle	1
plasma lipoprotein particle	1
extracellular vesicle	1

Protein interactions and networks

STRING

1382 interactions, top by confidence (×1000):

Protein A	Protein B	Partner UniProt	Score
CETP	APOA1	P02647	965
CETP	APOB	P04114	959
CETP	LCAT	P04180	955
CETP	APOF	Q13790	927
CETP	APOC3	P02656	921
CETP	APOE	P02649	904
CETP	APOA2	P02652	898
CETP	LIPC	P11150	891
CETP	PON1	P27169	890
CETP	LPL	P06858	874
CETP	APOC1	P02654	855
CETP	ABCA1	O95477	830
CETP	SCARB1	Q8WTV0	797
CETP	APOA4	P06727	787
CETP	NPC1L1	Q9UHC9	787

IntAct

6 interactions, top by confidence:

A	B	Type	Score
CETP	TP53	psi-mi:“MI:0915”(physical association)	0.370
CETP	PRKACG	psi-mi:“MI:0915”(physical association)	0.370
CETP	EWSR1	psi-mi:“MI:0915”(physical association)	0.370
CDH5	ESYT2	psi-mi:“MI:2364”(proximity)	0.270
ARPC3	CETP	psi-mi:“MI:0915”(physical association)	0.000

BioGRID (3): EWSR1 (Two-hybrid), CETP (Two-hybrid), PRKACG (Two-hybrid)

ESM2 similar proteins: A0A481NSZ4, A0JPN3, A2BGH0, A6QP57, D4A5U3, G3HIK4, O02668, O76879, P11597, P17213, P17453, P17454, P18428, P19823, P19827, P22687, P47896, P55058, P55065, P59826, P59827, P97278, Q05701, Q05704, Q08188, Q08189, Q0VCM5, Q10011, Q24764, Q28739, Q29052, Q2TBI0, Q61114, Q61702, Q61703, Q61805, Q63313, Q67E05, Q6AXU0, Q80ZU7

Diamond homologs: G3HIK4, P11597, P22687, P25914, P47896, Q3V6R6

SIGNOR signaling

2 interactions.

A	Effect	B	Mechanism
Anacetrapib	down-regulates	CETP	“chemical inhibition”
“2-methylpropanethioic acid S-[2-[[[1-(2-ethylbutyl)cyclohexyl]-oxomethyl]amino]phenyl] ester”	down-regulates	CETP	“chemical inhibition”

Disease & clinical

Clinical variants and AI predictions

ClinVar

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

Classification	Count (floor)
Pathogenic	4
Likely pathogenic	5
Uncertain significance	172
Likely benign	98
Benign	62

Top pathogenic / likely-pathogenic (9)

Variant ID	HGVS	Classification
1322066	NM_000078.3(CETP):c.268C>T (p.Gln90Ter)	Pathogenic
1324062	NM_000078.3(CETP):c.981+2T>C	Pathogenic
1675625	NM_000078.3(CETP):c.165del (p.Ser56fs)	Pathogenic
17528	NM_000078.3(CETP):c.1321+2dup	Pathogenic
1324061	NM_000078.3(CETP):c.160C>T (p.Arg54Ter)	Likely pathogenic
2690563	NM_000078.3(CETP):c.266del (p.Ser89fs)	Likely pathogenic
2690564	NM_000078.3(CETP):c.964C>T (p.Gln322Ter)	Likely pathogenic
3349566	NM_000078.3(CETP):c.598-1G>C	Likely pathogenic
3779056	NM_000078.3(CETP):c.976C>T (p.Gln326Ter)	Likely pathogenic

SpliceAI

2663 predictions. Top by Δscore:

Variant	Effect	Δscore
16:56962094:GTGT:G	donor_gain	1.0000
16:56962096:GT:G	donor_gain	1.0000
16:56962098:G:GG	donor_gain	1.0000
16:56963005:TCTA:T	acceptor_loss	1.0000
16:56963006:CTAGT:C	acceptor_loss	1.0000
16:56963007:TAGT:T	acceptor_loss	1.0000
16:56963008:A:AG	acceptor_gain	1.0000
16:56963008:AGT:A	acceptor_gain	1.0000
16:56963009:G:GA	acceptor_gain	1.0000
16:56963009:GT:G	acceptor_gain	1.0000
16:56963009:GTG:G	acceptor_gain	1.0000
16:56963009:GTGA:G	acceptor_gain	1.0000
16:56963105:GTCAA:G	donor_gain	1.0000
16:56963125:G:GG	donor_gain	1.0000
16:56969381:CCCA:C	acceptor_loss	1.0000
16:56969384:A:AC	acceptor_loss	1.0000
16:56969384:A:AG	acceptor_gain	1.0000
16:56969385:G:GG	acceptor_gain	1.0000
16:56969385:GC:G	acceptor_gain	1.0000
16:56969494:G:GT	donor_gain	1.0000
16:56969516:TGGTG:T	donor_gain	1.0000
16:56969517:GGTGG:G	donor_gain	1.0000
16:56969518:GTG:G	donor_gain	1.0000
16:56969519:TG:T	donor_gain	1.0000
16:56969520:GG:G	donor_gain	1.0000
16:56969521:G:C	donor_loss	1.0000
16:56969677:GCTGA:G	donor_gain	1.0000
16:56969678:C:G	donor_gain	1.0000
16:56969682:G:GG	donor_gain	1.0000
16:56969913:GCCT:G	acceptor_gain	1.0000

AlphaMissense

3256 scored. Top likely-pathogenic:

Variant	Protein change	am_pathogenicity
16:56962071:G:C	R31P	0.988
16:56969661:T:C	L140P	0.980
16:56969486:G:T	G112W	0.979
16:56969486:G:A	G112R	0.974
16:56969486:G:C	G112R	0.974
16:56962067:T:C	C30R	0.966
16:56972072:T:C	S247P	0.965
16:56973331:G:C	G251R	0.957
16:56983622:T:C	F480L	0.956
16:56983624:C:A	F480L	0.956
16:56983624:C:G	F480L	0.956
16:56969493:T:C	L114P	0.954
16:56969952:T:C	C160R	0.953
16:56969954:C:G	C160W	0.951
16:56969487:G:A	G112E	0.949
16:56973411:G:A	M277I	0.949
16:56973411:G:C	M277I	0.949
16:56973411:G:T	M277I	0.949
16:56983616:T:C	F478L	0.949
16:56983618:T:A	F478L	0.949
16:56983618:T:G	F478L	0.949
16:56963118:T:C	L76S	0.947
16:56983623:T:G	F480C	0.947
16:56972067:T:C	L245P	0.946
16:56969417:A:C	S89R	0.945
16:56969419:C:A	S89R	0.945
16:56969419:C:G	S89R	0.945
16:56971357:G:C	A212P	0.945
16:56971092:T:C	L196P	0.944
16:56963010:T:C	L40S	0.941

dbSNP variants (sampled 300 via entrez): RS1000004206 (16:56974916 T>A), RS1000243375 (16:56979811 T>A,G), RS1000371677 (16:56964118 C>T), RS1000755129 (16:56983465 C>A,T), RS1000835698 (16:56978836 A>T), RS1001623756 (16:56980837 G>A), RS1001815105 (16:56975918 C>T), RS1001842245 (16:56965157 C>T), RS1002599666 (16:56973293 G>A,T), RS1002673884 (16:56960002 A>C,G), RS1002690375 (16:56961960 C>T), RS1002828688 (16:56967834 G>A), RS1002957278 (16:56967603 C>A,G,T), RS1003296237 (16:56981929 C>A,T), RS1003492329 (16:56977095 G>A)

Disease associations

OMIM: gene MIM:118470 | disease phenotypes: MIM:614067, MIM:143470

GenCC curated gene-disease

Disease	Classification	Inheritance
cholesterol-ester transfer protein deficiency	Strong	Autosomal dominant

Mondo (3): coronary artery disorder (MONDO:0005010), hereditary spastic paraplegia 52 (MONDO:0013552), cholesterol-ester transfer protein deficiency (MONDO:0007744)

Orphanet (2): Severe intellectual disability and progressive spastic paraplegia (Orphanet:280763), OBSOLETE: Cholesterol-ester transfer protein deficiency (Orphanet:79506)

HPO phenotypes

2 total (2 of 2 shown, HPO-id order):

HPO	Term
HP:0000006	Autosomal dominant inheritance
HP:0012184	Increased HDL cholesterol concentration

GWAS associations

308 associations (top):

Study	Trait	p-value
GCST000133_3	HDL cholesterol	1.000000e-73
GCST000135_10	HDL cholesterol	7.000000e-39
GCST000135_2	HDL cholesterol	3.000000e-31
GCST000135_4	HDL cholesterol	2.000000e-57
GCST000184_2	Waist circumference and related phenotypes	1.000000e-27
GCST000240_3	HDL cholesterol	9.000000e-27
GCST000284_1	HDL cholesterol	7.000000e-29
GCST000288_5	HDL cholesterol	9.000000e-94
GCST000290_14	HDL cholesterol	4.000000e-75
GCST000328_2	Biochemical measures	9.000000e-06
GCST000331_1	HDL cholesterol	4.000000e-93
GCST000377_1	HDL cholesterol	3.000000e-12
GCST000533_10	Lipid metabolism phenotypes	1.000000e-39
GCST000533_11	Lipid metabolism phenotypes	3.000000e-93
GCST000533_12	Lipid metabolism phenotypes	1.000000e-81
GCST000533_13	Lipid metabolism phenotypes	2.000000e-59
GCST000533_14	Lipid metabolism phenotypes	5.000000e-87
GCST000533_15	Lipid metabolism phenotypes	1.000000e-53
GCST000533_17	Lipid metabolism phenotypes	2.000000e-14
GCST000533_24	Lipid metabolism phenotypes	1.000000e-66
GCST000533_25	Lipid metabolism phenotypes	3.000000e-55
GCST000533_43	Lipid metabolism phenotypes	8.000000e-78
GCST000533_45	Lipid metabolism phenotypes	1.000000e-20
GCST000533_46	Lipid metabolism phenotypes	7.000000e-22
GCST000533_47	Lipid metabolism phenotypes	3.000000e-25
GCST000559_1	Cholesterol	3.000000e-20
GCST000583_2	Hematological and biochemical traits	5.000000e-29
GCST000753_15	Metabolic syndrome	1.000000e-48
GCST000755_11	HDL cholesterol	0.000000e+00
GCST000758_26	Triglycerides	1.000000e-12

EFO canonical traits (21, from GWAS)

EFO ID	Trait name
EFO:0004612	high density lipoprotein cholesterol measurement
EFO:0004529	lipid measurement
EFO:0004574	total cholesterol measurement
EFO:0000195	metabolic syndrome
EFO:0004530	triglyceride measurement
EFO:0004611	low density lipoprotein cholesterol measurement
EFO:0004746	lipoprotein-associated phospholipase A(2) measurement
EFO:0004723	coronary artery calcification
EFO:0006995	response to diisocyanate
EFO:1001492	atrophic macular degeneration
EFO:0007805	HDL cholesterol change measurement
EFO:0004458	C-reactive protein measurement
EFO:0004614	apolipoprotein A 1 measurement
EFO:0009133	cholesteryl ester transfer protein measurement
EFO:0009132	cholesterol efflux capacity measurement
EFO:0004329	alcohol drinking
EFO:0005105	lipid or lipoprotein measurement
EFO:0004615	apolipoprotein B measurement
EFO:0006925	lipoprotein A measurement
EFO:0004980	appendicular lean mass
EFO:0004736	aspartate aminotransferase measurement

MeSH disease descriptors (1)

Descriptor	Name	Tree numbers
D003324	Coronary Artery Disease	C14.280.647.250.260; C14.907.137.126.339; C14.907.585.250.260

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (1): CHEMBL3572 (SINGLE PROTEIN)

Molecules with ChEMBL bioactivity

5 molecules (phase ≥1), by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 31,100 (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
CHEMBL1800807	ANACETRAPIB	3	854
CHEMBL2017179	EVACETRAPIB	3	302
CHEMBL313006	DALCETRAPIB	3	1,316
CHEMBL479527	TORCETRAPIB	3	7,803
CHEMBL169	URSOLIC ACID	2	20,825

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

PharmGKB clinical annotations

11 annotations.

Variant	Type	Level	Drugs	Phenotypes
rs1532624	Efficacy	3	HMG-CoA reductase inhibitors	Hyperlipidemias
rs4783961	Efficacy	3	fluvastatin	Hypercholesterolemia
rs5882	Efficacy	3	fluvastatin	Hypercholesterolemia
rs5882	Efficacy	3	simvastatin	Hypercholesterolemia
rs5882	Efficacy	3	rosuvastatin
rs708272	Efficacy	3	lovastatin
rs708272	Efficacy	3	pravastatin	Coronary Artery Disease
rs708272	Efficacy	3	rosuvastatin
rs708272	Efficacy	3	HMG-CoA reductase inhibitors	Coronary Artery Disease
rs708272	Efficacy,Toxicity	4	atorvastatin
rs708272	Efficacy	4	simvastatin	Hypercholesterolemia;Hyperlipoproteinemia Type II

PharmGKB variants

8 variants.

Variant	Genes	Level	Score	#Clin annots	Drugs
rs5882	CETP	3	3.25	3	fluvastatin;simvastatin;rosuvastatin
rs5883	CETP		0.00	0
rs708272	CETP	3	4.25	6	lovastatin;pravastatin;simvastatin;atorvastatin;rosuvastatin;HMG-CoA reductase inhibitors
rs1532624	CETP	3	3.50	1	HMG-CoA reductase inhibitors
rs1800775	CETP		0.00	0
rs3764261	CETP		0.00	0
rs4783961	CETP	3	1.75	1	fluvastatin
rs9930761	CETP		0.00	0

GtoPdb / IUPHAR curated pharmacology

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

Target class: other protein — Lipid transfer/lipopolysaccharide binding proteins

Most potent curated ligand interactions (5 total), top 5:

Ligand	Action	Affinity	Parameter
anacetrapib	Inhibition	7.76	pIC50
evacetrapib	Inhibition	7.59	pIC50
MK-8262	Inhibition	7.28	pIC50
DRL-17822	Inhibition	6.0	pIC50
dalcetrapib	Inhibition	5.39	pIC50

Binding affinities (BindingDB)

342 measured of 342 human assays (342 total across all organisms); most potent 50 below. Values come from heterogeneous assays and are not directly comparable.

Ligand	Measure	Value	Patent
4-[3-[2-[[(4S,5R)-5-[3,5-bis(trifluoromethyl)phenyl]-4-methyl-2-oxo-1,3-oxazolidin-3-yl]methyl]-4,4-dimethylcyclohexen-1-yl]-4-methoxyphenyl]-3,5-difluorobenzoic acid	IC50	1.5 nM	US-9493430: Biaryl- or heterocyclic biaryl-substituted cyclohexene derivative compounds as CETP inhibitors
4-[3-[2-[[(4S,5R)-5-[3,5-bis(trifluoromethyl)phenyl]-4-methyl-2-oxo-1,3-oxazolidin-3-yl]methyl]-4,4-dimethylcyclohexen-1-yl]-4-methoxyphenyl]-3-(trifluoromethyl)benzoic acid	IC50	1.6 nM	US-9493430: Biaryl- or heterocyclic biaryl-substituted cyclohexene derivative compounds as CETP inhibitors
4-[5-[2-[[(4S,5R)-5-[3,5-bis(trifluoromethyl)phenyl]-4-methyl-2-oxo-1,3-oxazolidin-3-yl]methyl]-4,4-dimethylcyclohexen-1-yl]-2-fluoro-4-methoxyphenyl]-3-chlorobenzoic acid	IC50	1.9 nM	US-9493430: Biaryl- or heterocyclic biaryl-substituted cyclohexene derivative compounds as CETP inhibitors
4-[5-[2-[[(4S,5R)-5-[3,5-bis(trifluoromethyl)phenyl]-4-methyl-2-oxo-1,3-oxazolidin-3-yl]methyl]-4,4-dimethylcyclohexen-1-yl]-4-methoxy-2-methylphenyl]-3-methylbenzoic acid	IC50	1.9 nM	US-9493430: Biaryl- or heterocyclic biaryl-substituted cyclohexene derivative compounds as CETP inhibitors
4-[5-[2-[[(4S,5R)-5-[3,5-bis(trifluoromethyl)phenyl]-4-methyl-2-oxo-1,3-oxazolidin-3-yl]methyl]-4,4-dimethylcyclohexen-1-yl]-2-fluoro-4-methoxyphenyl]-3-fluorobenzoic acid	IC50	2.5 nM	US-9493430: Biaryl- or heterocyclic biaryl-substituted cyclohexene derivative compounds as CETP inhibitors
(4S,5R)-5-[3,5-bis(trifluoromethyl)phenyl]-3-[[5-[5-(2,4-dimethyl-1,3-thiazol-5-yl)-2-methoxy-3-pyridinyl]-2-(3-fluoroazetidin-1-yl)pyrimidin-4-yl]methyl]-4-methyl-1,3-oxazolidin-2-one	IC50	3 nM	US-9353101: Cyclic amine substituted heterocyclic CETP inhibitors
(4S,5R)-5-[3,5-bis(trifluoromethyl)phenyl]-3-[[2-(3-fluoroazetidin-1-yl)-5-[2-methoxy-5-(1,3,5-trimethylpyrazol-4-yl)-3-pyridinyl]pyrimidin-4-yl]methyl]-4-methyl-1,3-oxazolidin-2-one	IC50	3 nM	US-9353101: Cyclic amine substituted heterocyclic CETP inhibitors
(4S,5R)-5-[3,5-bis(trifluoromethyl)phenyl]-3-[[5-[5-(3,5-dimethyl-1,2-oxazol-4-yl)-2-methoxy-3-pyridinyl]-2-(3-fluoroazetidin-1-yl)pyrimidin-4-yl]methyl]-4-methyl-1,3-oxazolidin-2-one	IC50	3 nM	US-9353101: Cyclic amine substituted heterocyclic CETP inhibitors
4-[5-[2-[[(4S,5R)-5-[3,5-bis(trifluoromethyl)phenyl]-4-methyl-2-oxo-1,3-oxazolidin-3-yl]methyl]-4,4-dimethylcyclohexen-1-yl]-2-fluoro-4-methoxyphenyl]-3-methylbenzoic acid	IC50	3.9 nM	US-9493430: Biaryl- or heterocyclic biaryl-substituted cyclohexene derivative compounds as CETP inhibitors
(4S,5R)-5-[3,5-bis(trifluoromethyl)phenyl]-3-[[5-[5-(3,5-dimethyl-1H-pyrazol-4-yl)-2-methoxy-3-pyridinyl]-2-(3-fluoroazetidin-1-yl)pyrimidin-4-yl]methyl]-4-methyl-1,3-oxazolidin-2-one	IC50	5 nM	US-9353101: Cyclic amine substituted heterocyclic CETP inhibitors
(4S,5R)-5-[3,5-bis(trifluoromethyl)phenyl]-3-[[2-(3,3-difluoroazetidin-1-yl)-5-(2-methoxy-5-propan-2-yl-3-pyridinyl)pyrimidin-4-yl]methyl]-4-methyl-1,3-oxazolidin-2-one	IC50	5 nM	US-9353101: Cyclic amine substituted heterocyclic CETP inhibitors
(4S,5R)-3-[[2-(azetidin-1-yl)-5-(2-methoxy-5-propan-2-yl-3-pyridinyl)pyrimidin-4-yl]methyl]-5-[3,5-bis(trifluoromethyl)phenyl]-4-methyl-1,3-oxazolidin-2-one	IC50	5 nM	US-9353101: Cyclic amine substituted heterocyclic CETP inhibitors
tert-butyl 4-[5-[2-[[(4S,5R)-5-[3,5-bis(trifluoromethyl)phenyl]-4-methyl-2-oxo-1,3-oxazolidin-3-yl]methyl]-6-(3,3-difluoroazetidin-1-yl)-3-pyridinyl]-6-methoxy-3-pyridinyl]-3,5-dimethylbenzoate	IC50	5 nM	US-9353101: Cyclic amine substituted heterocyclic CETP inhibitors
4-[5-[2-[[(4S,5R)-5-[3,5-bis(trifluoromethyl)phenyl]-4-methyl-2-oxo-1,3-oxazolidin-3-yl]methyl]-6-(3,3-difluoroazetidin-1-yl)-3-pyridinyl]-6-methoxy-3-pyridinyl]-3-methylbenzoic acid	IC50	5 nM	US-9353101: Cyclic amine substituted heterocyclic CETP inhibitors
4-[3-[2-[[(4S,5R)-5-[3,5-bis(trifluoromethyl)phenyl]-4-methyl-2-oxo-1,3-oxazolidin-3-yl]methyl]-4,4-dimethylcyclohexen-1-yl]-5-fluorophenyl]-3-(trifluoromethyl)benzoic acid	IC50	5 nM	US-9493430: Biaryl- or heterocyclic biaryl-substituted cyclohexene derivative compounds as CETP inhibitors
4-[5-[2-[[(4S,5R)-5-[3,5-bis(trifluoromethyl)phenyl]-4-methyl-2-oxo-1,3-oxazolidin-3-yl]methyl]-4,4-dimethylcyclohexen-1-yl]-6-methoxy-3-pyridinyl]-3-chlorobenzoic acid	IC50	5.3 nM	US-9493430: Biaryl- or heterocyclic biaryl-substituted cyclohexene derivative compounds as CETP inhibitors
4-[5-[2-[[(4S,5R)-5-[3,5-bis(trifluoromethyl)phenyl]-4-methyl-2-oxo-1,3-oxazolidin-3-yl]methyl]-4,4-dimethylcyclohexen-1-yl]-6-methoxy-3-pyridinyl]-3-methylbenzoic acid	IC50	5.4 nM	US-9493430: Biaryl- or heterocyclic biaryl-substituted cyclohexene derivative compounds as CETP inhibitors
4-[3-[2-[[(4S,5R)-5-[3,5-bis(trifluoromethyl)phenyl]-4-methyl-2-oxo-1,3-oxazolidin-3-yl]methyl]-4,4-dimethylcyclohexen-1-yl]-4-methoxyphenyl]-3-methylbenzoic acid	IC50	5.8 nM	US-9493430: Biaryl- or heterocyclic biaryl-substituted cyclohexene derivative compounds as CETP inhibitors
4-[3-[2-[[(4S,5R)-5-[3,5-bis(trifluoromethyl)phenyl]-4-methyl-2-oxo-1,3-oxazolidin-3-yl]methyl]-4,4-dimethylcyclohexen-1-yl]-4-fluorophenyl]-N-ethyl-3-(trifluoromethyl)benzamide	IC50	5.9 nM	US-9493430: Biaryl- or heterocyclic biaryl-substituted cyclohexene derivative compounds as CETP inhibitors
N-[[2-[4-[(5S)-4-(4,4-difluorocyclohexyl)-3-[(S)-fluoro-[4-(trifluoromethyl)phenyl]methyl]-5-hydroxy-7,7-dimethyl-6,8-dihydro-5H-quinolin-2-yl]piperidin-1-yl]pyrimidin-5-yl]methyl]-N-methylmethanesulfonamide	IC50	6 nM	US-9187450: Substituted pyridine compound
N-[[2-[4-[(5S)-4-(4,4-difluorocyclohexyl)-3-[(S)-fluoro-[4-(trifluoromethyl)phenyl]methyl]-5-hydroxy-7,7-dimethyl-6,8-dihydro-5H-quinolin-2-yl]piperidin-1-yl]pyrimidin-5-yl]methyl]-N-methylpropane-2-sulfonamide	IC50	6 nM	US-9187450: Substituted pyridine compound
4-[5-[2-[[(4S,5R)-5-[3,5-bis(trifluoromethyl)phenyl]-4-methyl-2-oxo-1,3-oxazolidin-3-yl]methyl]-6-(3-fluoroazetidin-1-yl)-3-pyridinyl]-6-methoxy-3-pyridinyl]-3-methylbenzoic acid	IC50	6 nM	US-9353101: Cyclic amine substituted heterocyclic CETP inhibitors
4-[3-[2-[[(4S,5R)-5-[3,5-bis(trifluoromethyl)phenyl]-4-methyl-2-oxo-1,3-oxazolidin-3-yl]methyl]-4,4-dimethylcyclohexen-1-yl]-4-fluorophenyl]-3-(trifluoromethyl)benzoic acid	IC50	6.4 nM	US-9493430: Biaryl- or heterocyclic biaryl-substituted cyclohexene derivative compounds as CETP inhibitors
4-[5-[2-[[(4S,5R)-5-[3,5-bis(trifluoromethyl)phenyl]-4-methyl-2-oxo-1,3-oxazolidin-3-yl]methyl]-4,4-dimethylcyclohexen-1-yl]-2-fluorophenyl]-3-methylbenzoic acid	IC50	6.6 nM	US-9493430: Biaryl- or heterocyclic biaryl-substituted cyclohexene derivative compounds as CETP inhibitors
4-[5-[2-[[(4S,5R)-5-[3,5-bis(trifluoromethyl)phenyl]-4-methyl-2-oxo-1,3-oxazolidin-3-yl]methyl]-4,4-dimethylcyclohexen-1-yl]-4-methoxy-2-(trifluoromethyl)phenyl]benzoic acid	IC50	6.9 nM	US-9493430: Biaryl- or heterocyclic biaryl-substituted cyclohexene derivative compounds as CETP inhibitors
4-[5-[4-[[(4S,5R)-5-[3,5-bis(trifluoromethyl)phenyl]-4-methyl-2-oxo-1,3-oxazolidin-3-yl]methyl]-2-(3-fluoroazetidin-1-yl)pyrimidin-5-yl]-6-methoxy-3-pyridinyl]-3,5-dimethylbenzoic acid	IC50	7 nM	US-9353101: Cyclic amine substituted heterocyclic CETP inhibitors
4-[5-[2-[[(4S,5R)-5-[3,5-bis(trifluoromethyl)phenyl]-4-methyl-2-oxo-1,3-oxazolidin-3-yl]methyl]-6-(3,3-difluoroazetidin-1-yl)-3-pyridinyl]-6-methoxy-3-pyridinyl]-3,5-dimethylbenzoic acid	IC50	7 nM	US-9353101: Cyclic amine substituted heterocyclic CETP inhibitors
(4S,5R)-5-[3,5-bis(trifluoromethyl)phenyl]-3-[[2-[2-fluoro-5-[4-(morpholine-4-carbonyl)-2-(trifluoromethyl)phenyl]phenyl]-5,5-dimethylcyclohexen-1-yl]methyl]-4-methyl-1,3-oxazolidin-2-one	IC50	7.1 nM	US-9493430: Biaryl- or heterocyclic biaryl-substituted cyclohexene derivative compounds as CETP inhibitors
4-[3-[2-[[(4S,5R)-5-[3,5-bis(trifluoromethyl)phenyl]-4-methyl-2-oxo-1,3-oxazolidin-3-yl]methyl]-4,4-dimethylcyclohexen-1-yl]-4-methoxyphenyl]-3-chlorobenzoic acid	IC50	7.3 nM	US-9493430: Biaryl- or heterocyclic biaryl-substituted cyclohexene derivative compounds as CETP inhibitors
(2R)-3-[2-[3-(difluoromethoxy)phenyl]-4-[[3-(trifluoromethoxy)phenyl]methyl]-2,3-dihydroquinoxalin-1-yl]-1,1,1-trifluoropropan-2-ol	IC50	7.5 nM	US-9126976: Substituted benzopiperazines as CETP inhibitors
4-[3-[2-[[(4S,5R)-5-[3,5-bis(trifluoromethyl)phenyl]-4-methyl-2-oxo-1,3-oxazolidin-3-yl]methyl]-4,4-dimethylcyclohexen-1-yl]-4-chlorophenyl]-3-(trifluoromethyl)benzoic acid	IC50	7.5 nM	US-9493430: Biaryl- or heterocyclic biaryl-substituted cyclohexene derivative compounds as CETP inhibitors
4-[5-[2-[[(4S,5R)-5-[3,5-bis(trifluoromethyl)phenyl]-4-methyl-2-oxo-1,3-oxazolidin-3-yl]methyl]-4,4-dimethylcyclohexen-1-yl]-4-methoxy-2-(trifluoromethyl)phenyl]-3-methylbenzoic acid	IC50	7.6 nM	US-9493430: Biaryl- or heterocyclic biaryl-substituted cyclohexene derivative compounds as CETP inhibitors
(2R)-3-[(2R)-4-(cyclohexen-1-ylmethyl)-2-[3-(trifluoromethoxy)phenyl]-2,3-dihydroquinoxalin-1-yl]-1,1,1-trifluoropropan-2-ol	IC50	8 nM	US-9126976: Substituted benzopiperazines as CETP inhibitors
2-[[2-[4-[(5S)-4-(4,4-difluorocyclohexyl)-3-[(S)-fluoro-[4-(trifluoromethyl)phenyl]methyl]-5-hydroxy-7,7-dimethyl-6,8-dihydro-5H-quinolin-2-yl]piperidin-1-yl]pyrimidin-5-yl]oxymethyl]propane-1,3-diol	IC50	8 nM	US-9187450: Substituted pyridine compound
5-[4-[5-[4-[[(4S,5R)-5-[3,5-bis(trifluoromethyl)phenyl]-4-methyl-2-oxo-1,3-oxazolidin-3-yl]methyl]-2-(3-fluoroazetidin-1-yl)pyrimidin-5-yl]-6-methoxy-3-pyridinyl]-3,5-dimethylphenyl]-3H-1,3,4-oxadiazol-2-one	IC50	8 nM	US-9353101: Cyclic amine substituted heterocyclic CETP inhibitors
4-[3-[2-[[(4S,5R)-5-[3,5-bis(trifluoromethyl)phenyl]-4-methyl-2-oxo-1,3-oxazolidin-3-yl]methyl]-4,4-dimethylcyclohexen-1-yl]-4-methoxyphenyl]-2,3-difluorobenzoic acid	IC50	8.4 nM	US-9493430: Biaryl- or heterocyclic biaryl-substituted cyclohexene derivative compounds as CETP inhibitors
4-[6-[2-[[(4S,5R)-5-[3,5-bis(trifluoromethyl)phenyl]-4-methyl-2-oxo-1,3-oxazolidin-3-yl]methyl]-4,4-dimethylcyclohexen-1-yl]-5-methoxy-2-pyridinyl]-3-(trifluoromethyl)benzoic acid	IC50	8.9 nM	US-9493430: Biaryl- or heterocyclic biaryl-substituted cyclohexene derivative compounds as CETP inhibitors
(2R)-3-[[2-(5-chloro-2-pyridinyl)-2-[3-fluoro-5-(1,1,2,2-tetrafluoroethoxy)phenyl]-3-phenylpropyl]amino]-1,1,1-trifluoropropan-2-ol	IC50	9 nM	US-9102599: N-((3-benzyl)-2,2-(bis-phenyl)-propan-1-amine derivatives as CETP inhibitors for the treatment of atherosclerosis and cardiovascular diseases
(2R)-1,1,1-trifluoro-3-[[3-(4-methylphenyl)-2,2-bis[3-(trifluoromethoxy)phenyl]propyl]amino]propan-2-ol	IC50	9 nM	US-9102599: N-((3-benzyl)-2,2-(bis-phenyl)-propan-1-amine derivatives as CETP inhibitors for the treatment of atherosclerosis and cardiovascular diseases
US9150583, 5	IC50	9 nM	US-9150583: Furo[3,4-c]quinoline derivatives, medicaments containing such compounds, their use and process for their preparation
(5S)-4-(4,4-difluorocyclohexyl)-3-[(S)-fluoro-[4-(trifluoromethyl)phenyl]methyl]-2-[1-[5-(3-hydroxy-3-methylbutoxy)pyrimidin-2-yl]piperidin-4-yl]-7,7-dimethyl-6,8-dihydro-5H-quinolin-5-ol	IC50	9 nM	US-9187450: Substituted pyridine compound
(4S,5R)-5-[3,5-bis(trifluoromethyl)phenyl]-3-[[5-[5-(1-ethyl-3,5-dimethylpyrazol-4-yl)-2-methoxy-3-pyridinyl]-2-(3-fluoroazetidin-1-yl)pyrimidin-4-yl]methyl]-4-methyl-1,3-oxazolidin-2-one	IC50	9 nM	US-9353101: Cyclic amine substituted heterocyclic CETP inhibitors
4-[5-[4-[[(4S,5R)-5-[3,5-bis(trifluoromethyl)phenyl]-4-methyl-2-oxo-1,3-oxazolidin-3-yl]methyl]-2-(3,3-difluoroazetidin-1-yl)pyrimidin-5-yl]-6-methoxy-3-pyridinyl]-3-methylbenzoic acid	IC50	9 nM	US-9353101: Cyclic amine substituted heterocyclic CETP inhibitors
4-[5-[2-(3,3-difluoroazetidin-1-yl)-4-[[(4S,5R)-5-[3-fluoro-5-(trifluoromethyl)phenyl]-4-methyl-2-oxo-1,3-oxazolidin-3-yl]methyl]pyrimidin-5-yl]-6-methoxy-3-pyridinyl]-3-methylbenzoic acid	IC50	9 nM	US-9353101: Cyclic amine substituted heterocyclic CETP inhibitors
4-[5-[2-[[(4S,5R)-5-[3,5-bis(trifluoromethyl)phenyl]-4-methyl-2-oxo-1,3-oxazolidin-3-yl]methyl]-6-morpholin-4-yl-3-pyridinyl]-6-methoxy-3-pyridinyl]-3-methylbenzoic acid	IC50	9 nM	US-9353101: Cyclic amine substituted heterocyclic CETP inhibitors
4-[5-[2-[[(4S,5R)-5-[3,5-bis(trifluoromethyl)phenyl]-4-methyl-2-oxo-1,3-oxazolidin-3-yl]methyl]-4,4-dimethylcyclohexen-1-yl]-4-methoxy-2-(trifluoromethyl)phenyl]-3-fluorobenzoic acid	IC50	9.1 nM	US-9493430: Biaryl- or heterocyclic biaryl-substituted cyclohexene derivative compounds as CETP inhibitors
4-[5-[2-[[(4S,5R)-5-[3,5-bis(trifluoromethyl)phenyl]-4-methyl-2-oxo-1,3-oxazolidin-3-yl]methyl]-4,4-dimethylcyclohexen-1-yl]-2-fluorophenyl]-3-(trifluoromethyl)benzoic acid	IC50	9.6 nM	US-9493430: Biaryl- or heterocyclic biaryl-substituted cyclohexene derivative compounds as CETP inhibitors
(5S)-4-(4,4-difluorocyclohexyl)-3-[(S)-fluoro-[4-(trifluoromethyl)phenyl]methyl]-7,7-dimethyl-2-[1-[5-(1-methylpiperidin-4-yl)oxypyrimidin-2-yl]piperidin-4-yl]-6,8-dihydro-5H-quinolin-5-ol	IC50	10 nM	US-9187450: Substituted pyridine compound
4-[5-[4-[[(4S,5R)-5-[3,5-bis(trifluoromethyl)phenyl]-4-methyl-2-oxo-1,3-oxazolidin-3-yl]methyl]-2-morpholin-4-ylpyrimidin-5-yl]-6-methoxy-3-pyridinyl]-3,5-dimethylbenzoic acid	IC50	10 nM	US-9353101: Cyclic amine substituted heterocyclic CETP inhibitors
5-[4-[5-[4-[[(4S,5R)-5-[3,5-bis(trifluoromethyl)phenyl]-4-methyl-2-oxo-1,3-oxazolidin-3-yl]methyl]-2-morpholin-4-ylpyrimidin-5-yl]-6-methoxy-3-pyridinyl]-3,5-dimethylphenyl]-3H-1,3,4-oxadiazol-2-one	IC50	10 nM	US-9353101: Cyclic amine substituted heterocyclic CETP inhibitors

ChEMBL bioactivities

1523 potent at pChembl≥5 of 1799 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).

pChembl	Type	Value	Unit	Molecule
9.11	IC50	0.77	nM	CHEMBL67129
9.00	IC50	1	nM	CHEMBL2152167
9.00	IC50	1	nM	CHEMBL4439823
8.89	IC50	1.3	nM	CHEMBL3814374
8.82	IC50	1.5	nM	CHEMBL3813720
8.82	IC50	1.5	nM	CHEMBL3906320
8.80	IC50	1.6	nM	CHEMBL3914103
8.74	IC50	1.8	nM	CHEMBL3813836
8.72	IC50	1.9	nM	CHEMBL3965631
8.72	IC50	1.9	nM	CHEMBL3955558
8.70	IC50	2	nM	CHEMBL2152180
8.70	IC50	2	nM	CHEMBL4574163
8.60	IC50	2.5	nM	CHEMBL3814963
8.60	IC50	2.5	nM	CHEMBL3982930
8.54	IC50	2.9	nM	CHEMBL3814418
8.52	IC50	3	nM	CHEMBL2152183
8.52	IC50	3	nM	CHEMBL3913846
8.52	IC50	3	nM	CHEMBL3932157
8.52	IC50	3	nM	CHEMBL3907705
8.52	IC50	3	nM	CHEMBL4457286
8.52	IC50	3	nM	CHEMBL303954
8.52	IC50	3	nM	CHEMBL69563
8.52	IC50	3	nM	TORCETRAPIB
8.41	IC50	3.9	nM	CHEMBL3972983
8.30	IC50	5	nM	CHEMBL2152166
8.30	IC50	5	nM	CHEMBL3971102
8.30	IC50	5	nM	CHEMBL3938675
8.30	IC50	5	nM	CHEMBL3927563
8.30	IC50	5	nM	CHEMBL3979835
8.30	IC50	5	nM	CHEMBL3970660
8.30	IC50	5	nM	CHEMBL3953367
8.30	IC50	5	nM	CHEMBL4552555
8.30	IC50	5	nM	CHEMBL4469874
8.28	IC50	5.3	nM	CHEMBL3948773
8.27	IC50	5.4	nM	CHEMBL3986115
8.24	IC50	5.8	nM	CHEMBL3927226
8.23	IC50	5.9	nM	CHEMBL3898351
8.22	IC50	6	nM	CHEMBL2152158
8.22	IC50	6	nM	CHEMBL2152165
8.22	IC50	6	nM	CHEMBL2152181
8.22	IC50	6	nM	CHEMBL3934696
8.22	IC50	6	nM	CHEMBL3912224
8.22	IC50	6	nM	CHEMBL3895147
8.22	IC50	6	nM	CHEMBL4439856
8.19	IC50	6.4	nM	CHEMBL3987174
8.18	IC50	6.6	nM	CHEMBL3941193
8.16	IC50	6.9	nM	CHEMBL2152165
8.16	IC50	6.9	nM	CHEMBL3915159
8.15	IC50	7	nM	CHEMBL2152168
8.15	IC50	7	nM	CHEMBL2152170

PubChem BioAssay actives

1140 with measured affinity, of 1917 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
(2R)-3-[3-(4-chloro-3-ethylphenoxy)-N-[[3-(1,1,2,2-tetrafluoroethoxy)phenyl]methyl]anilino]-1,1,1-trifluoropropan-2-ol	219561: Compound was tested in vitro for inhibitory activity against recombinant human cholesteryl ester transfer protein in buffer with <1 nM [CETP] for 18 hr assay time	ic50	0.0008	uM
1-[(1S)-1-(5-chloro-2-pyridinyl)-1-[3-fluoro-5-(1,1,2,2-tetrafluoroethoxy)phenyl]-2-phenylethyl]-3-[(1R)-3,3-difluorocyclopentyl]urea	691532: Inhibition of human recombinant CETP using [3H]cholesterol ester/HDL as substrate by scintillation proximity assay	ic50	0.0010	uM
4,4,4-trifluoro-N-[(1R)-1-(4-fluoro-3-propan-2-yloxyphenyl)-1-[3-fluoro-5-(1,1,2,2-tetrafluoroethoxy)phenyl]-2-phenylethyl]-2,3-dihydroxy-3-(trifluoromethyl)butanamide	1568147: Inhibition of human recombinant CETP assessed as reduction in [3H]CE/HDL transfer incubated for 4 hrs by scintillation proximity assay	ic50	0.0010	uM
(2R)-4,4,4-trifluoro-1-[[(1R)-1-(4-fluoro-3-propan-2-yloxyphenyl)-1-[3-fluoro-5-(1,1,2,2-tetrafluoroethoxy)phenyl]-2-phenylethyl]amino]butan-2-ol	1306114: Inhibition of human recombinant CETP assessed as reduction in [3H]cholesteryl ester transfer from [3H]CE-HDL to biotinylated LDL by scintillation proximity assay	ic50	0.0013	uM
1-[[(1S)-1-(5-chloro-2-pyridinyl)-1-[3-fluoro-5-(1,1,2,2-tetrafluoroethoxy)phenyl]-2-phenylethyl]amino]-4,4,4-trifluorobutan-2-ol	1306114: Inhibition of human recombinant CETP assessed as reduction in [3H]cholesteryl ester transfer from [3H]CE-HDL to biotinylated LDL by scintillation proximity assay	ic50	0.0015	uM
(2R)-1,1,1-trifluoro-3-[[(1R)-1-(4-fluoro-3-propan-2-yloxyphenyl)-1-[3-fluoro-5-(1,1,2,2-tetrafluoroethoxy)phenyl]-2-phenylethyl]amino]propan-2-ol	1306114: Inhibition of human recombinant CETP assessed as reduction in [3H]cholesteryl ester transfer from [3H]CE-HDL to biotinylated LDL by scintillation proximity assay	ic50	0.0018	uM
2-amino-N-[(1R)-1-(3-cyclopropyloxy-4-fluorophenyl)-1-[3-fluoro-5-(1,1,2,2-tetrafluoroethoxy)phenyl]-2-phenylethyl]-4,4,4-trifluoro-3-hydroxy-3-(trifluoromethyl)butanamide	1568147: Inhibition of human recombinant CETP assessed as reduction in [3H]CE/HDL transfer incubated for 4 hrs by scintillation proximity assay	ic50	0.0020	uM
1-[(1S)-1-(5-chloro-2-pyridinyl)-1-[3-fluoro-5-(1,1,2,2-tetrafluoroethoxy)phenyl]-2-phenylethyl]-3-(3,3,3-trifluoropropyl)urea	691532: Inhibition of human recombinant CETP using [3H]cholesterol ester/HDL as substrate by scintillation proximity assay	ic50	0.0020	uM
(2S)-4,4,4-trifluoro-1-[[(1R)-1-(4-fluoro-3-propan-2-yloxyphenyl)-1-[3-fluoro-5-(1,1,2,2-tetrafluoroethoxy)phenyl]-2-phenylethyl]amino]butan-2-ol	1306114: Inhibition of human recombinant CETP assessed as reduction in [3H]cholesteryl ester transfer from [3H]CE-HDL to biotinylated LDL by scintillation proximity assay	ic50	0.0025	uM
(2S)-1,1,1-trifluoro-3-[[(1R)-1-(4-fluoro-3-propan-2-yloxyphenyl)-1-[3-fluoro-5-(1,1,2,2-tetrafluoroethoxy)phenyl]-2-phenylethyl]amino]propan-2-ol	1306114: Inhibition of human recombinant CETP assessed as reduction in [3H]cholesteryl ester transfer from [3H]CE-HDL to biotinylated LDL by scintillation proximity assay	ic50	0.0029	uM
ethyl (2R,4S)-4-[[3,5-bis(trifluoromethyl)phenyl]methyl-methoxycarbonylamino]-2-ethyl-6-(trifluoromethyl)-3,4-dihydro-2H-quinoline-1-carboxylate	464756: Inhibition of human plasma CETP assessed as [3H]cholesterol ester transfer after 18 hrs by scintillation proximity assay	ic50	0.0030	uM
1-[(1S)-1-(5-chloro-2-pyridinyl)-1-[3-fluoro-5-(1,1,2,2-tetrafluoroethoxy)phenyl]-2-phenylethyl]-3-(2,2,2-trifluoroethyl)urea	691532: Inhibition of human recombinant CETP using [3H]cholesterol ester/HDL as substrate by scintillation proximity assay	ic50	0.0030	uM
2-amino-4,4,4-trifluoro-N-[(1R)-1-(4-fluoro-3-propan-2-yloxyphenyl)-1-[3-fluoro-5-(1,1,2,2-tetrafluoroethoxy)phenyl]-2-phenylethyl]-3-hydroxy-3-(trifluoromethyl)butanamide	1568147: Inhibition of human recombinant CETP assessed as reduction in [3H]CE/HDL transfer incubated for 4 hrs by scintillation proximity assay	ic50	0.0030	uM
(2R)-1,1,1-trifluoro-3-[3-phenoxy-N-[[3-(1,1,2,2-tetrafluoroethoxy)phenyl]methyl]anilino]propan-2-ol	329651: Inhibition of human CETP by scintillation proximity assay	ic50	0.0030	uM
3-[3-(4-chloro-3-ethylphenoxy)-N-[[3-(1,1,2,2-tetrafluoroethoxy)phenyl]methyl]anilino]-1,1,1-trifluoropropan-2-ol	394612: Inhibition of CETP-mediated transfer of [3H]cholesteryl ester from HDL donar particles to LDL acceptor particles in presence of buffer	ic50	0.0030	uM
2-amino-4,4,4-trifluoro-N-[(1R)-1-[4-fluoro-3-[(2-methylpropan-2-yl)oxy]phenyl]-1-[3-fluoro-5-(1,1,2,2-tetrafluoroethoxy)phenyl]-2-phenylethyl]-3-hydroxy-3-(trifluoromethyl)butanamide	1568147: Inhibition of human recombinant CETP assessed as reduction in [3H]CE/HDL transfer incubated for 4 hrs by scintillation proximity assay	ic50	0.0050	uM
1-[(1S)-1-(5-chloro-2-pyridinyl)-1-[3-fluoro-5-(1,1,2,2-tetrafluoroethoxy)phenyl]-2-phenylethyl]-3-(3,3-difluorocyclopentyl)urea	691532: Inhibition of human recombinant CETP using [3H]cholesterol ester/HDL as substrate by scintillation proximity assay	ic50	0.0050	uM
1,1,1-trifluoro-4-[[(1R)-1-(4-fluoro-3-propan-2-yloxyphenyl)-1-[3-fluoro-5-(1,1,2,2-tetrafluoroethoxy)phenyl]-2-phenylethyl]amino]-2-(trifluoromethyl)butane-2,3-diol	1568147: Inhibition of human recombinant CETP assessed as reduction in [3H]CE/HDL transfer incubated for 4 hrs by scintillation proximity assay	ic50	0.0050	uM
1-[(1S)-1-(5-chloro-2-pyridinyl)-1-[3-fluoro-5-(1,1,2,2-tetrafluoroethoxy)phenyl]-2-phenylethyl]-3-cyclopentylurea	691532: Inhibition of human recombinant CETP using [3H]cholesterol ester/HDL as substrate by scintillation proximity assay	ic50	0.0060	uM
1-[(1S)-1-(5-chloro-2-pyridinyl)-1-[3-fluoro-5-(trifluoromethyl)phenyl]-2-phenylethyl]-3-(3,3-difluorocyclopentyl)urea	691532: Inhibition of human recombinant CETP using [3H]cholesterol ester/HDL as substrate by scintillation proximity assay	ic50	0.0060	uM
1-[(1S)-1-(5-chloro-2-pyridinyl)-1-[3-fluoro-5-(1,1,2,2-tetrafluoroethoxy)phenyl]-2-phenylethyl]-3-(2,2,3,3,3-pentafluoropropyl)urea	691532: Inhibition of human recombinant CETP using [3H]cholesterol ester/HDL as substrate by scintillation proximity assay	ic50	0.0060	uM
2-amino-4,4,4-trifluoro-N-[(1R)-1-(4-fluoro-3-propan-2-yloxyphenyl)-1-[3-fluoro-5-(1,1,2,2-tetrafluoroethoxy)phenyl]-2-phenylethyl]-3-hydroxybutanamide	1568147: Inhibition of human recombinant CETP assessed as reduction in [3H]CE/HDL transfer incubated for 4 hrs by scintillation proximity assay	ic50	0.0060	uM
(4S,5R)-5-[3,5-bis(trifluoromethyl)phenyl]-3-[[2-(2-methoxy-5-propan-2-ylphenyl)-5-(trifluoromethyl)phenyl]methyl]-4-methyl-1,3-oxazolidin-2-one	1783852: Inhibition of recombinant CETP (unknown origin) assessed as inhibition of transfer of [3H]cholesteryl oleate or [3H]triolein using exogenous LDL and HDL in 2% human serum by liquid scintillation analysis	ic50	0.0070	uM
(5S)-4-cyclohexyl-2-cyclopentyl-3-[(S)-fluoro-[4-(trifluoromethyl)phenyl]methyl]-7,7-dimethyl-6,8-dihydro-5H-quinolin-5-ol	464756: Inhibition of human plasma CETP assessed as [3H]cholesterol ester transfer after 18 hrs by scintillation proximity assay	ic50	0.0070	uM
1-[(1S)-1-(5-chloro-2-pyridinyl)-1-[3-fluoro-5-(1,1,2,2-tetrafluoroethoxy)phenyl]-2-phenylethyl]-3-[(1S)-3,3-difluorocyclopentyl]urea	691532: Inhibition of human recombinant CETP using [3H]cholesterol ester/HDL as substrate by scintillation proximity assay	ic50	0.0070	uM
1-[(1S)-1-(5-chloro-2-pyridinyl)-1-[3-fluoro-5-(1,1,2,2-tetrafluoroethoxy)phenyl]-2-phenylethyl]-3-(3,3-difluorocyclobutyl)urea	691532: Inhibition of human recombinant CETP using [3H]cholesterol ester/HDL as substrate by scintillation proximity assay	ic50	0.0070	uM
1-[(1S)-1-(5-chloro-2-pyridinyl)-1-[3-fluoro-5-(1,1,2,2-tetrafluoroethoxy)phenyl]-2-phenylethyl]-3-propylurea	691532: Inhibition of human recombinant CETP using [3H]cholesterol ester/HDL as substrate by scintillation proximity assay	ic50	0.0080	uM
4-[3-[2-[[(4S,5R)-5-[3,5-bis(trifluoromethyl)phenyl]-4-methyl-2-oxo-1,3-oxazolidin-3-yl]methyl]-4-(trifluoromethyl)phenyl]-4-methoxyphenyl]-3-methylbenzoic acid	1783852: Inhibition of recombinant CETP (unknown origin) assessed as inhibition of transfer of [3H]cholesteryl oleate or [3H]triolein using exogenous LDL and HDL in 2% human serum by liquid scintillation analysis	ic50	0.0090	uM
1-[[(1S)-1-(5-chloro-2-pyridinyl)-1-[3-fluoro-5-(trifluoromethyl)phenyl]-2-phenylethyl]amino]-4,4,4-trifluorobutan-2-ol	1306114: Inhibition of human recombinant CETP assessed as reduction in [3H]cholesteryl ester transfer from [3H]CE-HDL to biotinylated LDL by scintillation proximity assay	ic50	0.0090	uM
N-[(1S)-1-(5-chloro-2-pyridinyl)-1-[3-fluoro-5-(1,1,2,2-tetrafluoroethoxy)phenyl]-2-phenylethyl]-3,3,4,4-tetrafluoropyrrolidine-1-carboxamide	691532: Inhibition of human recombinant CETP using [3H]cholesterol ester/HDL as substrate by scintillation proximity assay	ic50	0.0090	uM
2-(4-chloro-2,3-dimethylphenoxy)-N-[4-(5-cyano-1,3-benzoxazol-2-yl)phenyl]acetamide	329651: Inhibition of human CETP by scintillation proximity assay	ic50	0.0100	uM
1-[(1S)-1-(5-chloro-2-pyridinyl)-1-[3-fluoro-5-(1,1,2,2-tetrafluoroethoxy)phenyl]-2-phenylethyl]-3-(2,2-difluorocyclopropyl)urea	691532: Inhibition of human recombinant CETP using [3H]cholesterol ester/HDL as substrate by scintillation proximity assay	ic50	0.0100	uM
2-(4-bromo-2-methylphenoxy)-N-[4-(5-cyano-1,3-benzoxazol-2-yl)phenyl]acetamide	329651: Inhibition of human CETP by scintillation proximity assay	ic50	0.0110	uM
2-amino-4,4,4-trifluoro-N-[(1R)-1-(4-fluorophenyl)-1-[3-fluoro-5-(trifluoromethyl)phenyl]-2-phenylethyl]-3-hydroxy-3-(trifluoromethyl)butanamide	1568147: Inhibition of human recombinant CETP assessed as reduction in [3H]CE/HDL transfer incubated for 4 hrs by scintillation proximity assay	ic50	0.0110	uM
(2R)-1,1,1-trifluoro-3-[(2R)-2-[3-(1,1,2,2-tetrafluoroethoxy)phenyl]-4-[[3-(trifluoromethoxy)phenyl]methyl]-2,3-dihydroquinoxalin-1-yl]propan-2-ol	1299929: Inhibition of CETP in 95% human serum assessed as suppression of transfer of [3H]-cholesterol oleate/[3H]-triolein from LDL to HDL after 1 hr by liquid scintillation assay	ic50	0.0110	uM
propan-2-yl (2R,4S)-4-[[3-chloro-5-(trifluoromethyl)phenyl]methyl-(2-methyltetrazol-5-yl)amino]-2-ethyl-6-methyl-3,4-dihydro-2H-1,5-naphthyridine-1-carboxylate	657499: Inhibition of CETP in human plasma assessed as reduction in fluorescent intensity by fluorescence analysis	ic50	0.0120	uM
4-[3-[2-[[(4S,5R)-5-[3,5-bis(trifluoromethyl)phenyl]-4-methyl-2-oxo-1,3-oxazolidin-3-yl]methyl]-4-(trifluoromethyl)phenyl]-4-chlorophenyl]-3-methylbenzoic acid	1783824: Inhibition of recombinant CETP (unknown origin) assessed as inhibition of transfer of [3H]cholesteryl oleate or [3H]triolein between exogenous [3H]LDL in 95% human serum by liquid scintillation analysis	ic50	0.0127	uM
4-(5-cyano-7-propan-2-yl-1,3-benzoxazol-2-yl)-N-[[1-[5-(5-fluoro-2-propan-2-yloxyphenyl)-2-pyridinyl]piperidin-4-yl]methyl]benzamide	577779: Inhibition of CETP	ic50	0.0130	uM
N-[4-(5-cyano-7-methyl-1,3-benzoxazol-2-yl)phenyl]-2-[4-[3-(trifluoromethyl)phenyl]piperazin-1-yl]acetamide	550806: Inhibition of human recombinant CETP-mediated cholesteryl ester transfer by fluorescence-based assay	ic50	0.0130	uM
propan-2-yl (2R,4S)-4-[[3,5-bis(trifluoromethyl)phenyl]methyl-(2-methyltetrazol-5-yl)amino]-2-ethyl-6-(trifluoromethyl)-3,4-dihydro-2H-quinoline-1-carboxylate	661658: Inhibition of CETP in human plasma assessed as transfer of fluorescently labelled cholesteryl ester to VLDL by fluorimetry	ic50	0.0130	uM
(4S,5R)-5-[3,5-bis(trifluoromethyl)phenyl]-3-[[2-(4-fluoro-2-methoxy-5-propan-2-ylphenyl)-5-nitrophenyl]methyl]-4-methyl-1,3-oxazolidin-2-one	638019: Inhibition of CETP-mediated neutral lipid transfer by fluorometric analysis	ic50	0.0133	uM
(2S)-1-fluoro-3-[(3S)-3-[3-(1,1,2,2-tetrafluoroethoxy)phenyl]-8-[3-(trifluoromethoxy)phenyl]-2,3-dihydro-1,4-benzoxazin-4-yl]propan-2-ol	460160: Inhibition of human cholesteryl ester transfer protein by scintillation proximity assay	ic50	0.0140	uM
(2R)-3-[[(1S)-1-(5-chloro-2-pyridinyl)-1-[3-fluoro-5-(1,1,2,2-tetrafluoroethoxy)phenyl]-2-phenylethyl]amino]-1,1,1-trifluoropropan-2-ol	1306114: Inhibition of human recombinant CETP assessed as reduction in [3H]cholesteryl ester transfer from [3H]CE-HDL to biotinylated LDL by scintillation proximity assay	ic50	0.0140	uM
propan-2-yl (2R,4S)-4-[[3,5-bis(trifluoromethyl)phenyl]methyl-[2-(3-hydroxypropyl)tetrazol-5-yl]amino]-2-ethyl-6-(trifluoromethyl)-3,4-dihydro-2H-quinoline-1-carboxylate	661658: Inhibition of CETP in human plasma assessed as transfer of fluorescently labelled cholesteryl ester to VLDL by fluorimetry	ic50	0.0150	uM
propan-2-yl (2R,4S)-4-[[3,5-bis(trifluoromethyl)phenyl]methyl-[2-(2-cyanoethyl)tetrazol-5-yl]amino]-2-ethyl-6-(trifluoromethyl)-3,4-dihydro-2H-quinoline-1-carboxylate	661658: Inhibition of CETP in human plasma assessed as transfer of fluorescently labelled cholesteryl ester to VLDL by fluorimetry	ic50	0.0150	uM
[4-chloro-2-ethyl-8-[(1S)-1-hydroxy-3,3-dimethylbutyl]-7-methoxy-3-methyl-6-oxobenzo[b][1,4]benzodioxepin-1-yl] 7-methylbicyclo[2.2.1]heptane-7-carboxylate	242152: Inhibitory concentration against Cholesterol ester transfer protein (CETP) in CETP fluorescence assay	ic50	0.0150	uM
2-[(7-chloro-2,3-dihydro-1H-inden-4-yl)oxy]-N-[4-(5-cyano-1,3-benzoxazol-2-yl)phenyl]acetamide	329651: Inhibition of human CETP by scintillation proximity assay	ic50	0.0150	uM
N-[4-(5-cyano-7-methyl-1,3-benzoxazol-2-yl)phenyl]-2-[4-[5-(trifluoromethyl)-2-pyridinyl]piperazin-1-yl]acetamide	577779: Inhibition of CETP	ic50	0.0150	uM
1-cyclopentyl-3-[(1S)-1-[3-fluoro-5-(trifluoromethyl)phenyl]-1-(6-methoxy-3-pyridinyl)-2-phenylethyl]urea	699940: Inhibition of human recombinant CETP-mediated [3H]cholesteryl ester transfer from HDL to biotinylated LDL by scintillation proximity assay	ic50	0.0150	uM
propan-2-yl (2R,4S)-4-[[3,5-bis(trifluoromethyl)phenyl]methyl-[2-(2-hydroxyethyl)tetrazol-5-yl]amino]-2-ethyl-6-(trifluoromethyl)-3,4-dihydro-2H-quinoline-1-carboxylate	661658: Inhibition of CETP in human plasma assessed as transfer of fluorescently labelled cholesteryl ester to VLDL by fluorimetry	ic50	0.0160	uM

CTD chemical–gene interactions

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

Chemical	Actions (top 5)	PubMed papers
Cholesterol, HDL	affects reaction, decreases activity, increases abundance, affects abundance, affects response to substance (+2 more)	4
torcetrapib	decreases activity	3
Simvastatin	affects response to substance, affects abundance, decreases expression	3
T0901317	affects cotreatment, increases expression	2
Triglycerides	affects abundance, affects response to substance, decreases abundance, increases reaction	2
Valproic Acid	increases methylation	2
Aflatoxin B1	affects methylation, increases methylation	2
aristolochic acid I	increases expression	1
22-hydroxycholesterol	increases expression, affects cotreatment	1
triphenyl phosphate	affects expression	1
sodium arsenite	increases expression	1
N-(2-(4-bromocinnamylamino)ethyl)-5-isoquinolinesulfonamide	decreases reaction, increases expression, increases secretion	1
GW 3965	increases expression	1
anacetrapib	decreases activity	1
theaflavin-3,3’-digallate	affects expression	1
Arsenic Trioxide	increases expression	1
Fluvastatin	affects response to substance, affects cotreatment	1
Alitretinoin	affects cotreatment, increases expression	1
Benzo(a)pyrene	decreases methylation, increases methylation	1
Bezafibrate	decreases activity, affects reaction, increases abundance	1
Biological Factors	increases expression	1
Cholesterol	decreases abundance, increases reaction	1
Cholesterol, Dietary	increases expression	1
Etoposide	increases expression, increases reaction, decreases reaction, affects cotreatment	1
Formaldehyde	increases expression	1
Methyl Methanesulfonate	increases expression	1
Teniposide	increases secretion, affects cotreatment, decreases abundance, increases reaction, decreases reaction (+1 more)	1
Thiram	increases expression	1
Tosylphenylalanyl Chloromethyl Ketone	increases expression, increases reaction, increases secretion	1
Tretinoin	affects cotreatment, increases expression, increases reaction	1

ChEMBL screening assays

132 unique, capped per target: 127 binding, 5 functional

Representative assays (with source publication via chembl_document):

Assay ID	Type	Description	Source paper
CHEMBL1010540	Binding	Inhibition of human plasma derived CETP relative to control	Design and synthesis of potent inhibitors of cholesteryl ester transfer protein (CETP) exploiting a 1,2,3,4-tetrahydroquinoline platform. — Bioorg Med Chem Lett
CHEMBL4687983	Functional	In vivo inhibition of CETP in human assessed as increase in HDL-C level	Cholesteryl ester transfer protein (CETP) inhibitors based on cyclic urea, bicyclic urea and bicyclic sulfamide cores. — Bioorg Med Chem Lett

Clinical trials (associated diseases)

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

Trial	Phase	Status	Title
NCT00025766	PHASE4	COMPLETED	Angioplasty and Heart Stents to Treat Individuals With an Occluded Artery Following a Heart Attack
NCT00079638	PHASE4	COMPLETED	Comparative Efficacy Evaluation of Lipids When Treated With Niaspan & Statin or Other Lipid-Modifying Therapies-COMPELL
NCT00110448	PHASE4	COMPLETED	Japanese Primary Prevention of Atherosclerosis With Aspirin for Diabetes (JPAD) Trial
NCT00111566	PHASE4	COMPLETED	BRIEF-PCI: Brief Infusion of Eptifibatide Following Percutaneous Coronary Intervention
NCT00129038	PHASE4	COMPLETED	Modified-release Dipyridamole/Aspirin (200mg/25mg bd) Versus Aspirin (75mg) in Aspirin-resistant Patients
NCT00133003	PHASE4	COMPLETED	Abciximab, Clopidogrel and Percutaneous Coronary Intervention in Acute Coronary Syndrome (ISAR-REACT-2)
NCT00133237	PHASE4	COMPLETED	Drug-eluting-stents for Unprotected Left Main Stem Disease (ISAR-LEFT-MAIN)
NCT00133692	PHASE4	COMPLETED	INVEST: INternational VErapamil SR Trandolapril STudy
NCT00139386	PHASE4	COMPLETED	Candesartan for Prevention of Cardiovascular Events After Cypher or Taxus Coronary Stenting (4C) Trial
NCT00140465	PHASE4	COMPLETED	75 or 150 mg Clopidogrel Maintenance Doses Following PCI (ISAR-CHOICE-2)
NCT00140530	PHASE4	COMPLETED	Nonpolymer- and Polymer-Based Drug-Eluting Stents for Restenosis (ISAR-TEST-1)
NCT00146575	PHASE4	COMPLETED	Sirolimus- and Paclitaxel-Eluting Stents for Small Vessels (ISAR-SMART-3)
NCT00152308	PHASE4	TERMINATED	Non-Polymer-Based, Rapamycin-Eluting Stents to Prevent Restenosis
NCT00155350	PHASE4	UNKNOWN	Treatment of Coronary Atherosclerosis by Insulin Sensitizers in Insulin-Resistant Patients
NCT00162370	PHASE4	COMPLETED	A Study of Stress Echocardiography in Post-Menopausal Women at Risk for Coronary Disease
NCT00163202	PHASE4	COMPLETED	Comparative Atorvastatin Pleiotropic Effects
NCT00169819	PHASE4	COMPLETED	EArly Discharge After Transradial Stenting of CoronarY Arteries: The EASY Study
NCT00171275	PHASE4	COMPLETED	Fluvastatin in the Therapy of Acute Coronary Syndrome
NCT00175240	PHASE4	COMPLETED	Enhancing the Secondary Prevention of Coronary Artery Disease
NCT00180388	PHASE4	TERMINATED	VENEK: Healing in Different Vein Harvesting Methods During Aortocoronary Coronary Artery Bypass Graft Surgery (CABG)
NCT00180583	PHASE4	COMPLETED	Vision II: Evaluation of GALILEO Intravascular Radiotherapy System
NCT00189215	PHASE4	COMPLETED	Long-Term Cognitive Decline After Coronary Artery Bypass Grafting: is Off-Pump Surgery Beneficial?
NCT00200629	PHASE4	TERMINATED	Both Exercise and Adenosine Stress Testing
NCT00202904	PHASE4	COMPLETED	Effectiveness and Safety of Ezetimibe Added to Atorvastatin in Patients With High Cholesterol and Coronary Heart Disease (Study P03740)
NCT00209404	PHASE4	COMPLETED	Iodixanol in Multidetector-Row Computed Tomography-Coronary Angiography (MDCT-CA)
NCT00209430	PHASE4	COMPLETED	Renal Effects of Two Iodinated Contrast Media in Patients at Risk Undergoing Coronary Angiography
NCT00220558	PHASE4	UNKNOWN	GISSOC II: Sirolimus Eluting Stent Versus Bare Metal Stent in Chronic Total Coronary Occlusions
NCT00222261	PHASE4	COMPLETED	Aspirin Non-responsiveness and Clopidogrel Endpoint Trial.
NCT00229528	PHASE4	COMPLETED	Effect of Paroxetine on COAT-Platelet Production in Normal Volunteers and Patients With Cardiovascular Disease
NCT00232804	PHASE4	COMPLETED	The BRIDGE Registry: Safety and Efficacy Registry of Bx Cypher Stent
NCT00232856	PHASE4	COMPLETED	A Study of the Cypher SES to Treat Restenotic Native Coronary Artery Lesions.
NCT00235066	PHASE4	COMPLETED	The CYPHER™ Stent Study in Patients With Small de Novo Coronary Artery Lesions.
NCT00235092	PHASE4	COMPLETED	The REALITY Study - Head-to-Head Comparison Between Cypher and Taxus
NCT00235950	PHASE4	COMPLETED	Assessment of the Lipid Lowering Effect of Rosuvastatin Compared to Atorvastatin in Subjects With Coronary Heart Disease
NCT00238004	PHASE4	UNKNOWN	The Low HDL On Six Weeks Statin Therapy (LOW) Study
NCT00241904	PHASE4	COMPLETED	Reducing Total Cardiovascular Risk in an Urban Community
NCT00242944	PHASE4	COMPLETED	Japan Assessment of Pitavastatin and Atorvastatin in Acute Coronary Syndrome (JAPAN-ACS)
NCT00243477	PHASE4	COMPLETED	MOTIV Study- Effect of Antidepressive Treatment by Escitalopram in Patients Undergoing Coronary Artery Bypass Grafting
NCT00244530	PHASE4	COMPLETED	Prophylactic Effect of Nifedipine on Further Decline in Renal Function in Patients Undergoing Open-Heart Surgery
NCT00245401	PHASE4	COMPLETED	CYPHERTM Stent Post-Marketing Surveillance Registry (US-PMS)