RCE1

Summary

RCE1 (Ras converting CAAX endopeptidase 1, HGNC:13721) is a protein-coding gene on chromosome 11q13.2, encoding CAAX prenyl protease 2 (Q9Y256). Protease involved in the processing of a variety of prenylated proteins containing the C-terminal CAAX motif, where C is a cysteine modified with an isoprenoid lipid, A is an aliphatic amino acid and X is any C-terminal amino acid.

This gene encodes an integral membrane protein which is classified as a member of the metalloproteinase family. This enzyme is thought to function in the maintenance and processing of CAAX-type prenylated proteins.

Source: NCBI Gene 9986 — RefSeq curated summary.

At a glance

• GWAS associations: 2
• Clinical variants (ClinVar): 60 total
• Druggable target: yes — 1 molecules with ChEMBL bioactivity
• MANE Select transcript: NM_005133

Identifiers

Gene identifiers

Field	Value
HGNC ID	HGNC:13721
Approved symbol	RCE1
Name	Ras converting CAAX endopeptidase 1
Location	11q13.2
Locus type	gene with protein product
Status	Approved
Aliases	hRCE1, FACE-2, FACE2
Ensembl gene	ENSG00000173653
Ensembl biotype	protein_coding
OMIM	605385
Entrez	9986

Gene structure

Transcript identifiers

Ensembl transcripts: 9 — 4 retained_intron, 3 protein_coding, 1 nonsense_mediated_decay, 1 protein_coding_CDS_not_defined

ENST00000309657, ENST00000524506, ENST00000524849, ENST00000525356, ENST00000530610, ENST00000532775, ENST00000533277, ENST00000534645, ENST00000534822

RefSeq mRNA: 2 — MANE Select: NM_005133 NM_001032279, NM_005133

CCDS: CCDS8151

Canonical transcript exons

ENST00000309657 — 8 exons

Exon	Start	End
ENSE00001187750	66843441	66843640
ENSE00002180457	66845860	66846552
ENSE00003471289	66845166	66845237
ENSE00003535687	66844869	66845036
ENSE00003550198	66844286	66844364
ENSE00003600282	66843956	66844039
ENSE00003611465	66843759	66843861
ENSE00003672396	66845500	66845562

Expression profiles

Bgee: expression breadth ubiquitous, 228 present calls, max score 94.62.

FANTOM5 (CAGE): breadth ubiquitous, TPM avg 16.4296 / max 132.6821, expressed in 1797 samples.

FANTOM5 promoters (1 alternative TSS)

Promoter ID	TPM avg	Samples expressed
115374	16.4296	1797

Top tissues by expression

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

Tissue	Anatomy ID	Expression score	Quality
lower esophagus mucosa	UBERON:0035834	94.62	gold quality
mucosa of transverse colon	UBERON:0004991	92.93	gold quality
right hemisphere of cerebellum	UBERON:0014890	92.03	gold quality
cerebellar hemisphere	UBERON:0002245	91.96	gold quality
cerebellar cortex	UBERON:0002129	91.78	gold quality
granulocyte	CL:0000094	90.18	gold quality
right testis	UBERON:0004534	90.13	gold quality
left testis	UBERON:0004533	89.95	gold quality
cerebellum	UBERON:0002037	89.91	gold quality
skin of abdomen	UBERON:0001416	89.90	gold quality
parotid gland	UBERON:0001831	89.77	silver quality
primordial germ cell in gonad	CL:0000670 ∩ UBERON:0000991	89.10	gold quality
esophagus mucosa	UBERON:0002469	89.10	gold quality
metanephros cortex	UBERON:0010533	88.62	gold quality
adenohypophysis	UBERON:0002196	88.58	gold quality
transverse colon	UBERON:0001157	88.57	gold quality
pituitary gland	UBERON:0000007	88.38	gold quality
skin of leg	UBERON:0001511	88.35	gold quality
right lobe of liver	UBERON:0001114	88.18	gold quality
omental fat pad	UBERON:0010414	88.14	gold quality
body of stomach	UBERON:0001161	88.12	gold quality
peritoneum	UBERON:0002358	88.12	gold quality
testis	UBERON:0000473	87.85	gold quality
minor salivary gland	UBERON:0001830	87.81	gold quality
left ovary	UBERON:0002119	87.81	gold quality
saliva-secreting gland	UBERON:0001044	87.75	gold quality
small intestine Peyer’s patch	UBERON:0003454	87.68	gold quality
body of pancreas	UBERON:0001150	87.53	gold quality
adipose tissue of abdominal region	UBERON:0007808	87.02	gold quality
left uterine tube	UBERON:0001303	86.72	gold quality

Single-cell (SCXA)

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

Experiment	Marker?	Max mean expression
E-ANND-3	yes	4.64

Regulation

Is transcription factor: no

miRNA regulators (miRDB)

45 targeting RCE1, 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-548AW	99.99	72.57	3559
HSA-MIR-520D-5P	99.98	73.34	4883
HSA-MIR-524-5P	99.98	73.43	4882
HSA-MIR-6825-5P	99.96	69.81	3431
HSA-MIR-1468-3P	99.96	72.74	3797
HSA-MIR-4753-3P	99.90	71.03	3786
HSA-MIR-130B-5P	99.83	68.50	1888
HSA-MIR-7110-5P	99.80	67.84	1712
HSA-MIR-548AJ-5P	99.78	71.12	3085
HSA-MIR-548F-5P	99.78	71.02	3093
HSA-MIR-548G-5P	99.78	71.12	3085
HSA-MIR-548X-5P	99.78	71.12	3085
HSA-MIR-6763-5P	99.76	64.68	1767
HSA-MIR-3150A-3P	99.76	64.44	1640
HSA-MIR-92A-2-5P	99.75	67.01	2164
HSA-MIR-1200	99.71	70.42	1838
HSA-MIR-1283	99.69	72.42	3009
HSA-MIR-646	99.68	67.84	1645
HSA-MIR-3202	99.66	67.70	2737
HSA-MIR-378A-5P	99.65	66.33	1311
HSA-MIR-3175	99.65	66.30	2031
HSA-MIR-889-3P	99.40	69.76	2103
HSA-MIR-130A-5P	99.33	70.26	2623
HSA-MIR-329-5P	99.27	68.11	1597
HSA-MIR-7109-5P	99.18	66.13	1057
HSA-MIR-4292	99.16	65.57	1767
HSA-MIR-6791-5P	99.16	65.92	1844
HSA-MIR-491-5P	99.13	65.98	1468
HSA-MIR-548AS-3P	99.12	69.12	2294
HSA-MIR-4324	99.04	70.14	1569

Literature-anchored findings (GeneRIF, showing 8)

• We found that an 8-aa K-Ras-derived “CAA” peptide, KSKTKC(farnesyl)VI, was a better substrate for hRCE1 than a KSKTKC(f)VIM “CAAX” peptide, hRCE1 has important interaction with the P2’ and P3’ substrate positions in addition to the farnesylated cysteine (PMID:12818187)
• CAAX endoprotease Rce1 is required for lamin B1 endoproteolysis (PMID:14504265)
• the ras converting enzyme requires its glutamate and histidine residues (PMID:16361710)
• A novel RCE1 isoform is required for H-Ras plasma membrane localization regulated by ubiquitin specific peptidase (USP)17. (PMID:24134311)
• Suggests that expression of Rce1 can serve as an independent biomarker for the prognosis of prostate carcinoma patients. (PMID:26546252)
• High expression of Rce1 is associated with renal cell carcinoma. (PMID:28159979)
• RCE1 acts as a tumor suppressor in CRC, as its reduced expression may increase CRC cell invasion and independently predict an unsatisfactory prognosis in CRC patients. (PMID:28615075)
• Rce1 suppresses invasion and metastasis of hepatocellular carcinoma via epithelial-mesenchymal transition induced by the TGF-beta1/H-Ras signaling pathway. (PMID:31506952)

Cross-species orthologs

5 orthologs

Organism	Symbol	Gene ID
danio_rerio	rce1a	ENSDARG00000077909
mus_musculus	Rce1	ENSMUSG00000024889
rattus_norvegicus	Rce1	ENSRNOG00000019468
drosophila_melanogaster	Sras	FBGN0029121
caenorhabditis_elegans		WBGENE00001406

Protein

Protein identifiers

CAAX prenyl protease 2 — Q9Y256 (reviewed: Q9Y256)

Alternative names: Farnesylated proteins-converting enzyme 2, Prenyl protein-specific endoprotease 2, RCE1 homolog

All UniProt accessions (4): Q9Y256, E9PI08, E9PKA7, E9PPV9

UniProt curated annotations — full annotation on UniProt →

Function. Protease involved in the processing of a variety of prenylated proteins containing the C-terminal CAAX motif, where C is a cysteine modified with an isoprenoid lipid, A is an aliphatic amino acid and X is any C-terminal amino acid. Proteolytically removes the C-terminal three residues of farnesylated and geranylated proteins, leaving the prenylated cysteine as the new C-terminus. Is able to process K-Ras, N-Ras, H-Ras, RAP1B and G-gamma-1.

Subcellular location. Endoplasmic reticulum membrane.

Tissue specificity. Ubiquitous.

Post-translational modifications. Ubiquitinated. Undergoes ‘Lys-48’- and ‘Lys-63’-linked ubiquitination. ‘Lys-48’ ubiquitination induces its degradation. Deubiquitinated by USP17L2/USP17 that cleaves ‘Lys-63’-linked ubiquitin chains.

Activity regulation. Deubiquitination by USP17L2/USP17 negatively regulates the proteolytic activity toward Ras GTPases.

Similarity. Belongs to the peptidase U48 family.

RefSeq proteins (2): NP_001027450, NP_005124* (*=MANE)

Domains & families (InterPro)

ID	Name	Type
IPR003675	Rce1/LyrA-like_dom	Domain
IPR039731	Rce1	Family

Pfam: PF02517

Enzyme classification (BRENDA):

• EC 3.4.99.B1 — (BRENDA: organisms, substrates, inhibitors, Km, kcat entries)

UniProt features (15 total): transmembrane region 7, active site 2, site 2, initiator methionine 1, chain 1, modified residue 1, sequence variant 1

Structure

Experimental structures (PDB)

0 structures.

Predicted structure (AlphaFold)

Model	pLDDT	Fraction very-high
AF-Q9Y256-F1	85.61	0.59

Functional residue map

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

Catalytic / active sites (4): 208 (proton donor/acceptor); 261 (transition state stabilizer); 265 (transition state stabilizer); 175 (proton donor/acceptor)

Post-translational modifications (1): 2

Function

Pathways and Gene Ontology

Reactome pathways

2 pathways

ID	Pathway
R-HSA-5689880	Ub-specific processing proteases
R-HSA-9648002	RAS processing

MSigDB gene sets: 125 (showing top): ATF_B, GGGACCA_MIR133A_MIR133B, GOMF_METALLOPEPTIDASE_ACTIVITY, TTTGTAG_MIR520D, GRAESSMANN_APOPTOSIS_BY_DOXORUBICIN_DN, GRAESSMANN_RESPONSE_TO_MC_AND_DOXORUBICIN_DN, CREBP1_Q2, chr11q13, GOBP_PROTEIN_MATURATION, GOMF_CYSTEINE_TYPE_PEPTIDASE_ACTIVITY, PPAR_DR1_Q2, ATF3_Q6, NIKOLSKY_BREAST_CANCER_11Q12_Q14_AMPLICON, CTTTGTA_MIR524, P53_DECAMER_Q2

GO Biological Process (5): MAPK cascade (GO:0000165), protein prenylation (GO:0018342), CAAX-box protein processing (GO:0071586), proteolysis (GO:0006508), CAAX-box protein maturation (GO:0080120)

GO Molecular Function (6): endopeptidase activity (GO:0004175), cysteine-type endopeptidase activity (GO:0004197), metalloendopeptidase activity (GO:0004222), exopeptidase activity (GO:0008238), peptidase activity (GO:0008233), hydrolase activity (GO:0016787)

GO Cellular Component (5): endoplasmic reticulum membrane (GO:0005789), cytosol (GO:0005829), plasma membrane (GO:0005886), membrane (GO:0016020), endoplasmic reticulum (GO:0005783)

Reactome top-level categories

Rollup of top-2 pathways:

Category	Pathways
Deubiquitination	1
RAF/MAP kinase cascade	1

GO top-level categories

Rollup of top GO terms by namespace:

Category	Terms
protein processing	2
peptidase activity	2
endopeptidase activity	2
cytoplasm	2
cellular anatomical structure	2
intracellular signaling cassette	1
protein modification process	1
prenylation	1
CAAX-box protein maturation	1
protein metabolic process	1
protein prenylation	1
protein maturation	1
cysteine-type peptidase activity	1
metallopeptidase activity	1
hydrolase activity	1
catalytic activity, acting on a protein	1
catalytic activity	1
organelle membrane	1
nuclear outer membrane-endoplasmic reticulum membrane network	1
endoplasmic reticulum subcompartment	1
membrane	1
cell periphery	1
endomembrane system	1
intracellular membrane-bounded organelle	1

Protein interactions and networks

STRING

752 interactions, top by confidence (×1000):

Protein A	Protein B	Partner UniProt	Score
RCE1	ICMT	O60725	986
RCE1	ZMPSTE24	O75844	986
RCE1	SUN1	O94901	688
RCE1	FNTB	P49356	659
RCE1	SUN2	Q9UH99	659
RCE1	B4DL54	B4DL54	645
RCE1	DNAJA1	P31689	642
RCE1	USP17L25	Q0WX57	603
RCE1	LMNA	P02545	596
RCE1	LMNB1	P20700	593
RCE1	SYNE1	Q8NF91	585
RCE1	FNTA	P49354	573
RCE1	USP17L2	Q6R6M4	560
RCE1	NRAS	P01111	543
RCE1	KRAS	P01116	513

IntAct

8 interactions, top by confidence:

A	B	Type	Score
BBS4	TRAFD1	psi-mi:“MI:0914”(association)	0.510
HSCB	RBP5	psi-mi:“MI:0914”(association)	0.350
ESR1	ESYT2	psi-mi:“MI:0914”(association)	0.350
SPPL2B	HAS3	psi-mi:“MI:0914”(association)	0.350
AFG2A	ESYT2	psi-mi:“MI:0914”(association)	0.350
FHIP1A	ILVBL	psi-mi:“MI:2364”(proximity)	0.270
RCE1	BBS4	psi-mi:“MI:0915”(physical association)	0.000

BioGRID (13): RCE1 (Synthetic Lethality), RCE1 (Synthetic Lethality), BBS4 (Affinity Capture-MS), RCE1 (Affinity Capture-MS), RCE1 (Affinity Capture-MS), RCE1 (Affinity Capture-MS), RCE1 (Proximity Label-MS), RCE1 (Affinity Capture-MS), RCE1 (Affinity Capture-MS), RCE1 (Affinity Capture-MS), RCE1 (Proximity Label-MS), RCE1 (Affinity Capture-MS), RCE1 (Affinity Capture-RNA)

ESM2 similar proteins: A1A5C7, A6H7A0, B0BMW8, B0CM95, B0KWE9, B1MTH4, B2KI79, O43688, O62772, O75147, P0CK96, P35438, P35439, P52875, P57791, Q05586, Q28D01, Q2KJ29, Q3KNV8, Q3SZQ2, Q3UHH2, Q4L208, Q4V899, Q5R1P0, Q5R890, Q5SP67, Q5ZJ75, Q7TPB4, Q86YN1, Q8BTQ0, Q8C6G8, Q8C811, Q8R4D1, Q8VDI9, Q8VE98, Q90812, Q9BWV1, Q9D9E0, Q9H6U8, Q9H7D7

Diamond homologs: A6H7A0, B0BMW8, O94448, P57791, Q03530, Q9U1H8, Q9Y256, G5EEP3, Q8GW19

SIGNOR signaling

0 interactions.

Disease & clinical

Clinical variants and AI predictions

ClinVar

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

Classification	Count (floor)
Pathogenic	0
Likely pathogenic	0
Uncertain significance	44
Likely benign	0
Benign	0

Top pathogenic / likely-pathogenic (0)

SpliceAI

1085 predictions. Top by Δscore:

Variant	Effect	Δscore
11:66843623:G:GT	donor_gain	1.0000
11:66843804:G:GA	donor_gain	1.0000
11:66843858:CCAGG:C	donor_loss	1.0000
11:66843859:CAGGT:C	donor_loss	1.0000
11:66843860:AG:A	donor_loss	1.0000
11:66843861:GG:G	donor_loss	1.0000
11:66843948:T:TA	acceptor_gain	1.0000
11:66844864:T:TA	acceptor_gain	1.0000
11:66844867:A:AC	acceptor_loss	1.0000
11:66844867:A:AG	acceptor_gain	1.0000
11:66844868:G:GT	acceptor_gain	1.0000
11:66844868:GC:G	acceptor_gain	1.0000
11:66844868:GCC:G	acceptor_gain	1.0000
11:66844868:GCCC:G	acceptor_gain	1.0000
11:66844868:GCCCC:G	acceptor_gain	1.0000
11:66845032:AGTTG:A	donor_loss	1.0000
11:66845033:GTTG:G	donor_gain	1.0000
11:66845037:G:GC	donor_loss	1.0000
11:66845037:G:GG	donor_gain	1.0000
11:66845038:TGAG:T	donor_loss	1.0000
11:66845039:G:GT	donor_loss	1.0000
11:66845164:A:AG	acceptor_gain	1.0000
11:66845165:G:GA	acceptor_gain	1.0000
11:66845165:GC:G	acceptor_gain	1.0000
11:66845165:GCC:G	acceptor_gain	1.0000
11:66845165:GCCC:G	acceptor_gain	1.0000
11:66845165:GCCCA:G	acceptor_gain	1.0000
11:66845235:CTGGT:C	donor_loss	1.0000
11:66845239:T:G	donor_loss	1.0000
11:66845499:GC:G	acceptor_gain	1.0000

AlphaMissense

2086 scored. Top likely-pathogenic:

Variant	Protein change	am_pathogenicity
11:66843640:G:T	R62M	1.000
11:66844932:C:A	P172Q	1.000
11:66844941:A:T	E175V	1.000
11:66844942:G:C	E175D	1.000
11:66844942:G:T	E175D	1.000
11:66844944:A:T	E176V	1.000
11:66844952:T:A	F179I	1.000
11:66844952:T:C	F179L	1.000
11:66844952:T:G	F179V	1.000
11:66844953:T:C	F179S	1.000
11:66844953:T:G	F179C	1.000
11:66844954:C:A	F179L	1.000
11:66844954:C:G	F179L	1.000
11:66845027:T:C	F204L	1.000
11:66845029:T:A	F204L	1.000
11:66845029:T:G	F204L	1.000
11:66845526:T:C	F240L	1.000
11:66845528:C:A	F240L	1.000
11:66845528:C:G	F240L	1.000
11:66845530:G:A	G241D	1.000
11:66845886:C:G	H261D	1.000
11:66845900:T:A	N265K	1.000
11:66845900:T:G	N265K	1.000
11:66843607:G:A	G51D	0.999
11:66843609:A:C	S52R	0.999
11:66843611:C:A	S52R	0.999
11:66843611:C:G	S52R	0.999
11:66843784:C:A	R71S	0.999
11:66844292:T:A	F127I	0.999
11:66844292:T:C	F127L	0.999

dbSNP variants (sampled 300 via entrez): RS1000261368 (11:66844152 G>A), RS1001333350 (11:66842428 C>G), RS1001361831 (11:66842951 C>G,T), RS1001406266 (11:66844793 A>G), RS1001537769 (11:66846521 G>A), RS1001774141 (11:66844569 C>A,G,T), RS1002099928 (11:66842762 G>A), RS1002366887 (11:66843380 G>A,C,T), RS1002806523 (11:66843473 G>A,T), RS1003481119 (11:66846121 C>A,T), RS1003774491 (11:66843617 C>T), RS1004823184 (11:66844155 C>G,T), RS1005273662 (11:66845144 G>A,C), RS1006049383 (11:66845058 C>G,T), RS1006554557 (11:66844808 C>G,T)

Disease associations

OMIM: gene MIM:605385 | disease phenotypes:

GenCC curated gene-disease

Mondo (0):

Orphanet (0):

HPO phenotypes

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

GWAS associations

2 associations (top):

Study	Trait	p-value
GCST001241_12	Bipolar disorder	2.000000e-07
GCST008103_30	Bipolar disorder	4.000000e-08

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (1): CHEMBL3411 (SINGLE PROTEIN)

Molecules with ChEMBL bioactivity

1 molecules (phase ≥1), by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 189 (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
CHEMBL5315124	LEVOFLOXACIN	4	189

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

GtoPdb / IUPHAR curated pharmacology

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

Target class: enzyme — M79: Prenyl protease 2

Most potent curated ligand interactions (2 total), top 2:

Ligand	Action	Affinity	Parameter
CID16197121	Inhibition	6.73	pIC50
compound 3 [PMID: 17942791]	Inhibition	5.05	pIC50

ChEMBL bioactivities

107 potent at pChembl≥5 of 230 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).

pChembl	Type	Value	Unit	Molecule
6.74	AC50	183	nM	CHEMBL1302410
6.71	AC50	197	nM	CHEMBL1489919
6.46	AC50	345	nM	CHEMBL1502833
6.12	AC50	759	nM	CHEMBL1480899
6.11	AC50	769	nM	CHEMBL1556020
6.04	AC50	914	nM	CHEMBL1438058
5.99	AC50	1020	nM	CHEMBL1483593
5.94	AC50	1150	nM	CHEMBL1607592
5.89	AC50	1280	nM	CHEMBL1447981
5.87	AC50	1350	nM	CHEMBL1868919
5.87	AC50	1350	nM	CHEMBL1439591
5.77	AC50	1710	nM	CHEMBL1518304
5.74	AC50	1840	nM	CHEMBL1437349
5.68	AC50	2080	nM	CHEMBL1351626
5.67	AC50	2120	nM	CHEMBL1330989
5.66	AC50	2170	nM	CHEMBL3208660
5.65	AC50	2250	nM	CHEMBL1370674
5.64	AC50	2300	nM	CHEMBL1457908
5.62	AC50	2380	nM	CHEMBL1530208
5.61	AC50	2480	nM	CHEMBL1523930
5.60	AC50	2490	nM	CHEMBL1729477
5.59	AC50	2570	nM	CHEMBL1494764
5.58	AC50	2650	nM	CHEMBL1419182
5.58	AC50	2640	nM	CHEMBL3210528
5.56	AC50	2750	nM	CHEMBL1561078
5.55	AC50	2800	nM	CHEMBL1402907
5.50	AC50	3140	nM	CHEMBL1978082
5.50	AC50	3190	nM	CHEMBL1312600
5.48	AC50	3330	nM	CHEMBL1364803
5.43	AC50	3720	nM	CHEMBL1437987
5.42	IC50	3800	nM	CHEMBL3741765
5.42	AC50	3800	nM	CHEMBL1400666
5.41	IC50	3900	nM	CHEMBL3741937
5.41	AC50	3880	nM	CHEMBL1381508
5.41	AC50	3860	nM	CHEMBL1441135
5.38	IC50	4200	nM	CHEMBL3740962
5.37	AC50	4310	nM	CHEMBL1509494
5.37	AC50	4230	nM	CHEMBL1407834
5.37	AC50	4270	nM	CHEMBL1329111
5.36	AC50	4330	nM	CHEMBL1530823
5.35	AC50	4460	nM	CHEMBL3189821
5.32	AC50	4820	nM	CHEMBL1425691
5.32	AC50	4740	nM	CHEMBL1508764
5.31	IC50	4900	nM	CHEMBL3740249
5.30	IC50	5000	nM	CHEMBL3742211
5.29	AC50	5070	nM	CHEMBL146525
5.29	AC50	5180	nM	CHEMBL3197063
5.29	AC50	5170	nM	CHEMBL3190972
5.29	AC50	5170	nM	CHEMBL1453099
5.28	IC50	5300	nM	CHEMBL3741101

PubChem BioAssay actives

17 with measured affinity, of 144 total; 17 most potent distinct compounds. Largely complementary to BindingDB; screening values are coarse (µM, 4 dp), so sub-nM hits tie at the floor.

Compound	Assay	Type	Value	Unit
4-[[(4-bromo-2,6-difluorophenyl)-(1-hydroxynaphthalen-2-yl)methyl]amino]benzoic acid	1266273: Inhibition of human Rce1-mediated CaaX protease activity using ABZ-KSKTKC(farnesyl)QIIM and ABZ-KSKTKC(farnesyl)VIQI as substrate assessed as residual activity measured every 30 to 60 seconds for 60 mins	ic50	3.8000	uM
4-[[(4-bromophenyl)-(1-hydroxynaphthalen-2-yl)methyl]amino]benzoic acid	1266273: Inhibition of human Rce1-mediated CaaX protease activity using ABZ-KSKTKC(farnesyl)QIIM and ABZ-KSKTKC(farnesyl)VIQI as substrate assessed as residual activity measured every 30 to 60 seconds for 60 mins	ic50	3.9000	uM
4-[[(1-hydroxynaphthalen-2-yl)-phenylmethyl]amino]benzoic acid	1266273: Inhibition of human Rce1-mediated CaaX protease activity using ABZ-KSKTKC(farnesyl)QIIM and ABZ-KSKTKC(farnesyl)VIQI as substrate assessed as residual activity measured every 30 to 60 seconds for 60 mins	ic50	4.2000	uM
2-[anilino(phenyl)methyl]naphthalen-1-ol	1266273: Inhibition of human Rce1-mediated CaaX protease activity using ABZ-KSKTKC(farnesyl)QIIM and ABZ-KSKTKC(farnesyl)VIQI as substrate assessed as residual activity measured every 30 to 60 seconds for 60 mins	ic50	4.9000	uM
2-[(4-tert-butylanilino)-phenylmethyl]naphthalen-1-ol	1266273: Inhibition of human Rce1-mediated CaaX protease activity using ABZ-KSKTKC(farnesyl)QIIM and ABZ-KSKTKC(farnesyl)VIQI as substrate assessed as residual activity measured every 30 to 60 seconds for 60 mins	ic50	5.0000	uM
3-[[(1-hydroxynaphthalen-2-yl)-phenylmethyl]amino]benzoic acid	1266273: Inhibition of human Rce1-mediated CaaX protease activity using ABZ-KSKTKC(farnesyl)QIIM and ABZ-KSKTKC(farnesyl)VIQI as substrate assessed as residual activity measured every 30 to 60 seconds for 60 mins	ic50	5.3000	uM
2-[anilino(phenyl)methyl]-4-bromonaphthalen-1-ol	1266273: Inhibition of human Rce1-mediated CaaX protease activity using ABZ-KSKTKC(farnesyl)QIIM and ABZ-KSKTKC(farnesyl)VIQI as substrate assessed as residual activity measured every 30 to 60 seconds for 60 mins	ic50	5.4000	uM
4-[[(4-bromophenyl)-(8-hydroxyquinolin-7-yl)methyl]amino]benzoic acid	1266273: Inhibition of human Rce1-mediated CaaX protease activity using ABZ-KSKTKC(farnesyl)QIIM and ABZ-KSKTKC(farnesyl)VIQI as substrate assessed as residual activity measured every 30 to 60 seconds for 60 mins	ic50	6.7000	uM
4-[[(8-hydroxyquinolin-7-yl)-phenylmethyl]amino]benzoic acid	1266273: Inhibition of human Rce1-mediated CaaX protease activity using ABZ-KSKTKC(farnesyl)QIIM and ABZ-KSKTKC(farnesyl)VIQI as substrate assessed as residual activity measured every 30 to 60 seconds for 60 mins	ic50	6.9000	uM
N-[3-[(2,3-dimethylphenyl)sulfamoyl]phenyl]-3-[[(E)-3-(4-phenylphenyl)prop-2-enoyl]amino]propanamide	197660: Inhibition of recombinant prenyl protein-specific protease Rce1 expressed in Sf9 cells at 10 uM	ic50	7.0000	uM
N-[2-[3-[(2,3-dimethylphenyl)sulfamoyl]anilino]-2-oxoethyl]heptadecanamide	197660: Inhibition of recombinant prenyl protein-specific protease Rce1 expressed in Sf9 cells at 10 uM	ic50	7.0000	uM
4-[[(8-hydroxyquinolin-7-yl)-(4-methylphenyl)methyl]amino]benzoic acid	1266273: Inhibition of human Rce1-mediated CaaX protease activity using ABZ-KSKTKC(farnesyl)QIIM and ABZ-KSKTKC(farnesyl)VIQI as substrate assessed as residual activity measured every 30 to 60 seconds for 60 mins	ic50	7.1000	uM
4-[[(4-fluorophenyl)-(8-hydroxyquinolin-7-yl)methyl]amino]benzoic acid	1266273: Inhibition of human Rce1-mediated CaaX protease activity using ABZ-KSKTKC(farnesyl)QIIM and ABZ-KSKTKC(farnesyl)VIQI as substrate assessed as residual activity measured every 30 to 60 seconds for 60 mins	ic50	8.2000	uM
7-[(4-methylanilino)-phenylmethyl]quinolin-8-ol	1266273: Inhibition of human Rce1-mediated CaaX protease activity using ABZ-KSKTKC(farnesyl)QIIM and ABZ-KSKTKC(farnesyl)VIQI as substrate assessed as residual activity measured every 30 to 60 seconds for 60 mins	ic50	8.8000	uM
7-[anilino(phenyl)methyl]quinolin-8-ol	1266273: Inhibition of human Rce1-mediated CaaX protease activity using ABZ-KSKTKC(farnesyl)QIIM and ABZ-KSKTKC(farnesyl)VIQI as substrate assessed as residual activity measured every 30 to 60 seconds for 60 mins	ic50	8.9000	uM
2-[anilino-(4-bromo-2,6-difluorophenyl)methyl]naphthalen-1-ol	1266273: Inhibition of human Rce1-mediated CaaX protease activity using ABZ-KSKTKC(farnesyl)QIIM and ABZ-KSKTKC(farnesyl)VIQI as substrate assessed as residual activity measured every 30 to 60 seconds for 60 mins	ic50	9.4000	uM
4-[[cyclohexyl-(8-hydroxyquinolin-7-yl)methyl]amino]benzoic acid	1266273: Inhibition of human Rce1-mediated CaaX protease activity using ABZ-KSKTKC(farnesyl)QIIM and ABZ-KSKTKC(farnesyl)VIQI as substrate assessed as residual activity measured every 30 to 60 seconds for 60 mins	ic50	9.8000	uM

CTD chemical–gene interactions

15 total (human), top 15 by PubMed support.

Chemical	Actions (top 5)	PubMed papers
aristolochic acid I	increases expression	1
triphenyl phosphate	affects expression	1
vanadyl sulfate	increases expression	1
CGP 52608	affects binding, increases reaction	1
abrine	increases expression	1
MT19c compound	decreases expression	1
Temozolomide	decreases expression	1
Acetaminophen	decreases expression	1
Cadmium	increases abundance, increases expression	1
Phthalic Acids	increases methylation	1
Smoke	decreases expression	1
Dronabinol	decreases expression	1
Tobacco Smoke Pollution	increases expression	1
Cadmium Chloride	increases abundance, increases expression	1
Copper Sulfate	decreases expression	1

ChEMBL screening assays

12 unique, capped per target: 11 binding, 1 admet

Representative assays (with source publication via chembl_document):

Assay ID	Type	Description	Source paper
CHEMBL1055573	Binding	Inhibition of human RCE1	Scalarane-based sesterterpenoid RCE-protease inhibitors isolated from the Indonesian marine sponge Carteriospongia foliascens. — J Nat Prod
CHEMBL4360191	ADMET	Inhibition of Rce1 in human PC3 cells at 10 uM using KSKTKC(f)VI as substrate measured after 24 hrs by LC-MS/MS analysis	A Potent Isoprenylcysteine Carboxylmethyltransferase (ICMT) Inhibitor Improves Survival in Ras-Driven Acute Myeloid Leukemia. — J Med Chem

Clinical trials (associated diseases)

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