ARL1

Summary

ARL1 (ARF like GTPase 1, HGNC:692) is a protein-coding gene on chromosome 12q23.2, encoding ADP-ribosylation factor-like protein 1 (P40616). GTP-binding protein that recruits several effectors, such as golgins, arfaptins and Arf-GEFs to the trans-Golgi network, and modulates their functions at the Golgi complex.

The protein encoded by this gene belongs to the ARL (ADP-ribosylation factor-like) family of proteins, which are structurally related to ADP-ribosylation factors (ARFs). ARFs, described as activators of cholera toxin (CT) ADP-ribosyltransferase activity, regulate intracellular vesicular membrane trafficking, and stimulate a phospholipase D (PLD) isoform. Although, ARL proteins were initially thought not to activate CT or PLD, later work showed that they are weak stimulators of PLD and CT in a phospholipid dependent manner. Alternative splicing results in multiple transcript variants encoding different isoforms.

Source: NCBI Gene 400 — RefSeq curated summary.

At a glance

• Clinical variants (ClinVar): 17 total
• Druggable target: yes
• MANE Select transcript: NM_001177

Identifiers

Gene identifiers

Field	Value
HGNC ID	HGNC:692
Approved symbol	ARL1
Name	ARF like GTPase 1
Location	12q23.2
Locus type	gene with protein product
Status	Approved
Aliases	ARFL1
Ensembl gene	ENSG00000120805
Ensembl biotype	protein_coding
OMIM	603425
Entrez	400

Gene structure

Transcript identifiers

Ensembl transcripts: 12 — 8 protein_coding, 2 protein_coding_CDS_not_defined, 1 retained_intron, 1 nonsense_mediated_decay

ENST00000261636, ENST00000536227, ENST00000539055, ENST00000548070, ENST00000549283, ENST00000549302, ENST00000550597, ENST00000551092, ENST00000551671, ENST00000551688, ENST00000551828, ENST00000872694

RefSeq mRNA: 2 — MANE Select: NM_001177 NM_001177, NM_001301068

CCDS: CCDS44958, CCDS73510

Canonical transcript exons

ENST00000261636 — 6 exons

Exon	Start	End
ENSE00001391106	101407642	101407772
ENSE00001476583	101393116	101395670
ENSE00003459325	101396399	101396577
ENSE00003518889	101405844	101405981
ENSE00003647679	101401062	101401173
ENSE00003650307	101402865	101402946

Expression profiles

Bgee: expression breadth ubiquitous, 297 present calls, max score 98.00.

FANTOM5 (CAGE): breadth ubiquitous, TPM avg 59.7448 / max 819.9124, expressed in 1822 samples.

FANTOM5 promoters (2 alternative TSS)

Promoter ID	TPM avg	Samples expressed
132900	59.7231	1822
132901	0.0217	6

Top tissues by expression

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

Tissue	Anatomy ID	Expression score	Quality
islet of Langerhans	UBERON:0000006	98.00	gold quality
stromal cell of endometrium	CL:0002255	97.98	gold quality
endothelial cell	CL:0000115	97.84	gold quality
calcaneal tendon	UBERON:0003701	97.22	gold quality
adrenal tissue	UBERON:0018303	97.19	gold quality
Brodmann (1909) area 23	UBERON:0013554	96.96	gold quality
pons	UBERON:0000988	96.92	gold quality
saphenous vein	UBERON:0007318	96.55	gold quality
rectum	UBERON:0001052	96.48	gold quality
colonic epithelium	UBERON:0000397	96.29	gold quality
superior surface of tongue	UBERON:0007371	96.15	gold quality
middle temporal gyrus	UBERON:0002771	96.09	gold quality
pancreatic ductal cell	CL:0002079	95.90	gold quality
vena cava	UBERON:0004087	95.74	gold quality
olfactory segment of nasal mucosa	UBERON:0005386	95.69	gold quality
pericardium	UBERON:0002407	95.51	gold quality
gall bladder	UBERON:0002110	95.49	gold quality
tendon	UBERON:0000043	95.46	gold quality
pituitary gland	UBERON:0000007	95.44	gold quality
superior vestibular nucleus	UBERON:0007227	95.44	gold quality
pancreas	UBERON:0001264	95.41	gold quality
oocyte	CL:0000023	95.37	gold quality
renal medulla	UBERON:0000362	95.32	gold quality
adenohypophysis	UBERON:0002196	95.32	gold quality
tibia	UBERON:0000979	95.28	gold quality
caput epididymis	UBERON:0004358	95.26	gold quality
smooth muscle tissue	UBERON:0001135	95.18	gold quality
adrenal gland	UBERON:0002369	95.11	gold quality
left adrenal gland	UBERON:0001234	95.10	gold quality
endometrium	UBERON:0001295	95.07	gold quality

Single-cell (SCXA)

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

Experiment	Marker?	Max mean expression
E-HCAD-5	yes	34.91
E-MTAB-6142	no	211.50
E-ANND-3	no	0.00

Regulation

Is transcription factor: no

miRNA regulators (miRDB)

106 targeting ARL1, top 30 by miRDB confidence (max_score; target_count = how many genes the miRNA targets in total — lower means more specific):

miRNA	Max score	Avg score	miRNA target_count
HSA-MIR-3163	100.00	77.23	8605
HSA-MIR-1277-5P	100.00	73.95	5056
HSA-MIR-5011-5P	100.00	83.46	5820
HSA-LET-7A-3P	100.00	74.03	3932
HSA-LET-7B-3P	100.00	74.08	3913
HSA-LET-7F-1-3P	100.00	74.02	3928
HSA-MIR-98-3P	100.00	74.08	3907
HSA-MIR-450A-1-3P	100.00	69.33	1837
HSA-MIR-4776-3P	100.00	68.73	1340
HSA-MIR-9-5P	100.00	72.28	2361
HSA-MIR-186-5P	99.99	70.83	3707
HSA-MIR-4775	99.98	75.00	6394
HSA-MIR-302C-5P	99.97	72.56	3642
HSA-MIR-590-3P	99.96	74.34	6478
HSA-MIR-9983-3P	99.94	71.48	3631
HSA-MIR-4760-3P	99.93	70.50	2385
HSA-MIR-205-3P	99.92	69.92	3165
HSA-MIR-10527-5P	99.91	72.28	3754
HSA-MIR-1305	99.91	71.43	3443
HSA-MIR-6809-3P	99.91	71.45	3814
HSA-MIR-1297	99.91	73.41	3162
HSA-MIR-4753-3P	99.90	71.03	3786
HSA-MIR-106A-5P	99.90	73.94	2683
HSA-MIR-17-5P	99.89	73.83	2665
HSA-MIR-4697-3P	99.89	67.09	1123
HSA-MIR-106B-5P	99.88	74.72	2795
HSA-MIR-20A-5P	99.88	74.76	2769
HSA-MIR-129-5P	99.88	70.26	3273
HSA-MIR-20B-5P	99.88	74.01	2621
HSA-MIR-519D-3P	99.88	73.97	2607

Literature-anchored findings (GeneRIF, showing 11)

• Data show that Arl1 regulates the membrane recruitment of Golgin-97, which plays a role in transport from the endosome to the trans-Golgi network. (PMID:15269279)
• These data suggest that lethality of Arfrp1 knockout embryos is due to a specific disruption of protein targeting, e.g., of ARL1 and Golgin-245, to the Golgi. (PMID:17127620)
• Results show that ARL1 and ARFRP1 regulate retrograde transport of Shiga toxin to the TGN and anterograde transport of VSVG from the TGN, respectively. (PMID:19224922)
• Study demonstrates that Golgi recruitment of endogenous GCC185 does not involve Rab6A/A’ and Arl1. (PMID:19703403)
• arfaptins are recruited onto trans-Golgi membranes by interacting with Arl1, and capable of inducing membrane deformation via their BAR domains. (PMID:21239483)
• The Arl1.Arfaptin-2 BAR structure suggests that one of the two Arl1 molecules competes with Rac1, which binds to the concave face of the Arfaptin-2 BAR homodimer and may hinder its membrane association. (PMID:22679020)
• results demonstrate that activated Arl1p can promote the spatial modulation of membrane organization at the trans-Golgi network through interacting with the effectors Gea2p and Drs2p (PMID:23345439)
• Together the findings indicate that Arl1 links Rab4-dependent formation of endosomal sorting domains with downstream assembly of adaptor protein complexes that constitute the endosomal sorting machinery. (PMID:24835460)
• Plasticity allows Arl1 to interact with different effectors of unrelated structure. (PMID:27373159)
• The ARFRP1 functions upstream of two other ARL GTPases, ARL1 and ARL5, which in turn recruit golgins and GARP, respectively, to the trans-Golgi network (TGN). (PMID:31575603)
• ArfGAP1 acts as a GTPase-activating protein for human ADP-ribosylation factor-like 1 protein. (PMID:33715220)

Cross-species orthologs

5 orthologs

Organism	Symbol	Gene ID
danio_rerio	arl1	ENSDARG00000101680
mus_musculus	Arl1	ENSMUSG00000060904
rattus_norvegicus	Arl1	ENSRNOG00000005763
drosophila_melanogaster	Arl1	FBGN0000115
caenorhabditis_elegans		WBGENE00000187

Paralogs (30): ARF5 (ENSG00000004059), SAR1A (ENSG00000079332), ARFRP1 (ENSG00000101246), TRIM23 (ENSG00000113595), ARL6 (ENSG00000113966), ARL4A (ENSG00000122644), ARL8B (ENSG00000134108), ARF3 (ENSG00000134287), ARL3 (ENSG00000138175), ARL5C (ENSG00000141748), ARF1 (ENSG00000143761), ARL8A (ENSG00000143862), ARL11 (ENSG00000152213), SAR1B (ENSG00000152700), ARL5A (ENSG00000162980), ARF6 (ENSG00000165527), ARL5B (ENSG00000165997), ARF4 (ENSG00000168374), ARL13B (ENSG00000169379), ARL13A (ENSG00000174225), ARL10 (ENSG00000175414), ARL4D (ENSG00000175906), ARL14 (ENSG00000179674), ARL15 (ENSG00000185305), ARL17A (ENSG00000185829), ARL4C (ENSG00000188042), ARL9 (ENSG00000196503), ARL2 (ENSG00000213465), ARL16 (ENSG00000214087), ARL17B (ENSG00000228696)

Protein

Protein identifiers

ADP-ribosylation factor-like protein 1 — P40616 (reviewed: P40616)

All UniProt accessions (6): B4DZG7, P40616, F8VP63, F8VP99, F8VYN9, F8W1Z8

UniProt curated annotations — full annotation on UniProt →

Function. GTP-binding protein that recruits several effectors, such as golgins, arfaptins and Arf-GEFs to the trans-Golgi network, and modulates their functions at the Golgi complex. Plays thereby a role in a wide range of fundamental cellular processes, including cell polarity, innate immunity, or protein secretion mediated by arfaptins, which were shown to play a role in maintaining insulin secretion from pancreatic beta cells.

Subunit / interactions. The GTP-bound form interacts with GOLGA1. The GTP-bound form interacts with GOLGA4 and RGPD8. The GTP-bound form directly interacts with ARFIP2. Binds to SCOC, preferentially in its GTP-bound form. May interact with UNC119. Interacts with ARFIP1; this interaction directs ARFIP1 to the trans-Golgi membranes. Interacts with ARFGEF1 (via N-terminus).

Subcellular location. Golgi apparatus membrane. Golgi apparatus. trans-Golgi network membrane. Membrane.

Tissue specificity. Detected in heart, liver, lung and liver (at protein level). Detected in fetal heart, lung, liver and kidney. Detected in adult heart, placenta, lung, liver, skeletal muscle, kidney and pancreas.

Similarity. Belongs to the small GTPase superfamily. Arf family.

Isoforms (2)

UniProt ID	Names	Canonical?
P40616-1	1	yes
P40616-2	2

RefSeq proteins (2): NP_001168, NP_001287997 (=MANE)

Domains & families (InterPro)

ID	Name	Type
IPR005225	Small_GTP-bd	Domain
IPR006689	Small_GTPase_ARF/SAR	Family
IPR024156	Small_GTPase_ARF	Family
IPR027417	P-loop_NTPase	Homologous_superfamily

Pfam: PF00025

UniProt features (28 total): helix 7, binding site 7, strand 6, mutagenesis site 2, turn 2, initiator methionine 1, chain 1, splice variant 1, lipid moiety-binding region 1

Structure

Experimental structures (PDB)

4 structures.

PDB	Method	Resolution (Å)
1UPT	X-RAY DIFFRACTION	1.7
5EE5	X-RAY DIFFRACTION	2.28
4DCN	X-RAY DIFFRACTION	3.01
5J5C	X-RAY DIFFRACTION	3.4

Predicted structure (AlphaFold)

Model	pLDDT	Fraction very-high
AF-P40616-F1	92.32	0.84

Functional residue map

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

Ligand- & substrate-binding residues (7): 24–31; 31; 45–48; 48; 70; 126–129; 160–161

Post-translational modifications (1): 2

Mutagenesis-validated functional residues (2):

Position	Phenotype
31	loss of interaction with arfip1 and arfip2.
71	altered golgi structure with an engorged lumen. interacts with arfip2, golga4, rgpd8, scoc and unc119.

Function

Pathways and Gene Ontology

Reactome pathways

4 pathways

ID	Pathway
R-HSA-6811440	Retrograde transport at the Trans-Golgi-Network
R-HSA-199991	Membrane Trafficking
R-HSA-5653656	Vesicle-mediated transport
R-HSA-6811442	Intra-Golgi and retrograde Golgi-to-ER traffic

MSigDB gene sets: 180 (showing top): BORCZUK_MALIGNANT_MESOTHELIOMA_UP, GOBP_INTRACELLULAR_PROTEIN_TRANSPORT, CMYB_01, GOBP_VESICLE_MEDIATED_TRANSPORT, REACTOME_MEMBRANE_TRAFFICKING, GOCC_TRANS_GOLGI_NETWORK, GAZDA_DIAMOND_BLACKFAN_ANEMIA_PROGENITOR_DN, OCT1_03, GOBP_TOXIN_METABOLIC_PROCESS, GOBP_ENDOMEMBRANE_SYSTEM_ORGANIZATION, MODULE_86, DOUGLAS_BMI1_TARGETS_DN, MODULE_226, GOBP_PROTEIN_LOCALIZATION_TO_GOLGI_APPARATUS, GOBP_PROTEIN_LOCALIZATION_TO_ORGANELLE

GO Biological Process (6): intracellular protein transport (GO:0006886), Golgi organization (GO:0007030), toxin metabolic process (GO:0009404), vesicle-mediated transport (GO:0016192), protein localization to Golgi apparatus (GO:0034067), retrograde transport, endosome to Golgi (GO:0042147)

GO Molecular Function (8): GTPase activity (GO:0003924), GTP binding (GO:0005525), enzyme activator activity (GO:0008047), protein domain specific binding (GO:0019904), metal ion binding (GO:0046872), phospholipase D activator activity (GO:1990583), nucleotide binding (GO:0000166), protein binding (GO:0005515)

GO Cellular Component (7): Golgi membrane (GO:0000139), cytoplasm (GO:0005737), Golgi apparatus (GO:0005794), trans-Golgi network (GO:0005802), cytosol (GO:0005829), trans-Golgi network membrane (GO:0032588), membrane (GO:0016020)

Reactome top-level categories

Rollup of top-3 pathways:

Category	Pathways
Intra-Golgi and retrograde Golgi-to-ER traffic	1
Vesicle-mediated transport	1
Membrane Trafficking	1

GO top-level categories

Rollup of top GO terms by namespace:

Category	Terms
cellular anatomical structure	3
cytoplasm	2
intracellular protein localization	1
protein transport	1
intracellular transport	1
organelle organization	1
endomembrane system organization	1
secondary metabolic process	1
transport	1
cellular process	1
protein localization to organelle	1
intercellular transport	1
endosomal transport	1
cytosolic transport	1
ribonucleoside triphosphate phosphatase activity	1
guanyl ribonucleotide binding	1
purine ribonucleoside triphosphate binding	1
catalytic activity	1
enzyme regulator activity	1
molecular function activator activity	1
protein binding	1
cation binding	1
D-type glycerophospholipase activity	1
phospholipase activator activity	1
nucleoside phosphate binding	1
heterocyclic compound binding	1
binding	1
Golgi apparatus	1
bounding membrane of organelle	1
intracellular anatomical structure	1
endomembrane system	1
intracellular membrane-bounded organelle	1
Golgi apparatus subcompartment	1
trans-Golgi network	1
organelle membrane	1

Protein interactions and networks

STRING

2717 interactions, top by confidence (×1000):

Protein A	Protein B	Partner UniProt	Score
ARL1	ARFGAP2	Q8N6H7	624
ARL1	CCDC185	Q8N715	606
ARL1	MRFAP1	Q9Y605	597
ARL1	E9PSI1	E9PSI1	590
ARL1	ARFGAP1	Q8N6T3	534
ARL1	CDKN2A	P42771	483
ARL1	GBF1	Q92538	481
ARL1	ARFGAP3	Q9NP61	473
ARL1	TSEN54	Q7Z6J9	469
ARL1	CIAO1	O76071	461
ARL1	SCOC	Q9UIL1	448
ARL1	AP5S1	Q9NUS5	412
ARL1	TSEN15	Q8WW01	398
ARL1	GOLGA1	Q92805	393
ARL1	HMBS	P08396	390

IntAct

94 interactions, top by confidence:

A	B	Type	Score
CFTR	ESYT2	psi-mi:“MI:0914”(association)	0.710
CFTR	ESYT2	psi-mi:“MI:2364”(proximity)	0.710
RAF1	CALU	psi-mi:“MI:0914”(association)	0.640
ARFIP1	ARL1	psi-mi:“MI:0915”(physical association)	0.640
ARFIP1	ARL1	psi-mi:“MI:0914”(association)	0.640
RAB8A	WDR91	psi-mi:“MI:0914”(association)	0.600
DDX21	MED19	psi-mi:“MI:2364”(proximity)	0.480
GCC2	ARL1	psi-mi:“MI:0407”(direct interaction)	0.440
TGOLN2	PGRMC1	psi-mi:“MI:0914”(association)	0.420
ARL1	DRD2	psi-mi:“MI:0915”(physical association)	0.370
NEDD1	ATP5MF-PTCD1	psi-mi:“MI:0914”(association)	0.350
JUN	TPM3	psi-mi:“MI:0914”(association)	0.350
		psi-mi:“MI:0914”(association)	0.350
	VWA8	psi-mi:“MI:0914”(association)	0.350
	ESYT2	psi-mi:“MI:0914”(association)	0.350
	PGRMC1	psi-mi:“MI:0914”(association)	0.350
MYC	ILVBL	psi-mi:“MI:0914”(association)	0.350

BioGRID (249): ARL1 (Affinity Capture-MS), ARL1 (Affinity Capture-MS), ARL1 (Two-hybrid), ARL1 (Two-hybrid), ARL1 (Affinity Capture-MS), ARL1 (Affinity Capture-MS), ARL1 (Affinity Capture-MS), ARL1 (Affinity Capture-MS), ARL1 (Affinity Capture-MS), ARL1 (Affinity Capture-MS), ARL1 (Affinity Capture-MS), ARL1 (Affinity Capture-MS), ARL1 (Affinity Capture-MS), ARL1 (Affinity Capture-MS), ARL1 (Affinity Capture-MS)

ESM2 similar proteins: A8ISN6, B5FYQ0, O00909, O45379, O48649, O48920, P0CM16, P0CM17, P0DH91, P18085, P25160, P36397, P36405, P37996, P38116, P40616, P40940, P49076, P49702, P51644, P51821, P56559, P61208, P61211, P61212, P61750, P61751, P84081, P84082, P84083, P84084, P84085, Q06396, Q19705, Q1MTE5, Q20758, Q2TBW6, Q2YDM1, Q3SZF2, Q52NJ4

Diamond homologs: A1CRG9, A1D4D1, A3LTA2, A5DR82, A5E5G3, O04266, O04267, O04834, O48649, O48920, P0C583, P0C950, P0C951, P0CM16, P0CM17, P0CR30, P0CR31, P0CT16, P0CT17, P0DH91, P11076, P18085, P20606, P22274, P25160, P34727, P36397, P36536, P36579, P40616, P40940, P49702, P51643, P51821, P51822, P51823, P52884, P52885, P61204, P61205

SIGNOR signaling

0 interactions.

Enriched among interaction partners

Reactome pathways and GO biological processes over-represented among this gene’s 93 IntAct physical interaction partners (hypergeometric vs the genome-wide background, BH-FDR, gene-set size 15–500, ranked by fold). A functional readout of the neighbourhood — distinct from this gene’s own memberships above, and biased toward well-studied / hub proteins, so read it as themes rather than proof.

Reactome pathways:

Pathway	Partners	Fold	FDR
Regulation of actin dynamics for phagocytic cup formation	5	13.8×	6e-03
Leishmania infection	5	12.2×	6e-03
Parasitic Infection Pathways	5	12.2×	6e-03
Translocation of SLC2A4 (GLUT4) to the plasma membrane	5	11.5×	6e-03

Disease & clinical

Clinical variants and AI predictions

ClinVar

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

Classification	Count (floor)
Pathogenic	0
Likely pathogenic	0
Uncertain significance	6
Likely benign	0
Benign	1

Top pathogenic / likely-pathogenic (0)

SpliceAI

0 predictions. Top by Δscore:

AlphaMissense

1164 scored. Top likely-pathogenic:

Variant	Protein change	am_pathogenicity
12:101396533:T:A	K127N	1.000
12:101396533:T:G	K127N	1.000
12:101396534:T:A	K127I	1.000
12:101401102:C:G	R99P	1.000
12:101401164:C:A	W78C	1.000
12:101401164:C:G	W78C	1.000
12:101402889:T:G	D67A	1.000
12:101402893:A:G	W66R	1.000
12:101402893:A:T	W66R	1.000
12:101402936:A:C	F51L	1.000
12:101402936:A:T	F51L	1.000
12:101402938:A:G	F51L	1.000
12:101402940:C:T	G50E	1.000
12:101405894:G:A	T31I	1.000
12:101405896:T:A	K30N	1.000
12:101405896:T:G	K30N	1.000
12:101405897:T:A	K30I	1.000
12:101405898:T:G	K30Q	1.000
12:101405900:C:T	G29E	1.000
12:101405916:C:G	G24R	1.000
12:101405916:C:T	G24R	1.000
12:101396534:T:G	K127T	0.999
12:101396535:T:C	K127E	0.999
12:101396536:A:C	N126K	0.999
12:101396536:A:T	N126K	0.999
12:101401116:A:C	S94R	0.999
12:101401116:A:T	S94R	0.999
12:101401118:T:G	S94R	0.999
12:101401120:T:A	D93V	0.999
12:101401121:C:G	D93H	0.999

dbSNP variants (sampled 300 via entrez): RS1000068405 (12:101405119 C>A,T), RS1000367497 (12:101406309 C>T), RS1000496402 (12:101399894 G>A), RS1000545183 (12:101400184 C>T), RS1000603693 (12:101392870 C>A,T), RS1000674053 (12:101406792 C>G), RS1000684662 (12:101400438 G>A), RS1000758650 (12:101407294 G>A), RS1001056146 (12:101393267 T>C), RS1001496082 (12:101401522 G>A), RS1001548479 (12:101401737 T>C,G), RS1001658759 (12:101394835 T>C), RS1001733956 (12:101408134 C>T), RS1001926878 (12:101406910 G>C,T), RS1002464427 (12:101406765 A>C)

Disease associations

OMIM: gene MIM:603425 | disease phenotypes:

GenCC curated gene-disease

Mondo (0):

Orphanet (0):

HPO phenotypes

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

GWAS associations

0 associations (top):

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (1): CHEMBL5725022 (SINGLE PROTEIN)

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

ChEMBL bioactivities

4 potent at pChembl≥5 of 4 total, top 4 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).

pChembl	Type	Value	Unit	Molecule
9.14	Kd	0.716	nM	CHEMBL3752910
9.14	ED50	0.716	nM	CHEMBL3752910
5.54	Kd	2849	nM	CHEMBL5653589
5.54	ED50	2849	nM	CHEMBL5653589

PubChem BioAssay actives

2 with measured affinity, of 10 total; 2 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-methyl-3-[(1-methyl-6-pyridin-3-ylpyrazolo[3,4-d]pyrimidin-4-yl)amino]-N-[3-(trifluoromethyl)phenyl]benzamide	2147888: Binding affinity to human ARL1 incubated for 45 mins by Kinobead based pull down assay	kd	0.0007	uM
4-methyl-3-[(2-methyl-6-pyridin-3-ylpyrazolo[3,4-d]pyrimidin-4-yl)amino]-N-[3-(trifluoromethyl)phenyl]benzamide	2147888: Binding affinity to human ARL1 incubated for 45 mins by Kinobead based pull down assay	kd	2.8494	uM

CTD chemical–gene interactions

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

Chemical	Actions (top 5)	PubMed papers
Cyclosporine	increases expression	3
Particulate Matter	decreases expression, increases abundance	2
aristolochic acid I	decreases expression	1
bisphenol F	increases expression	1
TAK-243	decreases sumoylation	1
dicrotophos	decreases expression	1
chloroacetaldehyde	increases expression	1
triphenyl phosphate	affects expression	1
bisphenol A	increases expression	1
sodium arsenite	increases expression	1
tetrabromobisphenol A	decreases expression	1
ochratoxin A	affects binding	1
di-n-butylphosphoric acid	affects expression	1
perfluorooctane sulfonic acid	increases expression	1
deguelin	increases expression	1
K 7174	increases expression	1
nutlin 3	increases secretion, affects cotreatment	1
bisphenol B	increases expression	1
2,2’,4,4’-tetrabromodiphenyl ether	decreases expression	1
pentabrominated diphenyl ether 100	decreases expression	1
bisphenol S	increases expression	1
bisphenol AF	increases expression	1
Vorinostat	increases expression	1
Air Pollutants	decreases expression, increases abundance	1
Cannabidiol	increases expression	1
Cisplatin	decreases expression	1
Dactinomycin	affects cotreatment, increases secretion	1
Clodronic Acid	increases expression	1
Diethylhexyl Phthalate	decreases expression	1
Dimethyl Sulfoxide	increases expression	1

ChEMBL screening assays

7 unique, capped per target: 7 binding

Representative assays (with source publication via chembl_document):

Assay ID	Type	Description	Source paper
CHEMBL5650930	Binding	Binding affinity to human ARL1 incubated for 45 mins by Kinobead based pull down assay	NVP-BHG712: Effects of Regioisomers on the Affinity and Selectivity toward the EPHrin Family. — ChemMedChem

Cellosaurus cell lines

1 cell lines: 1 cancer cell line

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

Cellosaurus	Name	Category	Sex
CVCL_E1QY	HAP1 ARL1 (-)	Cancer cell line	Male

Clinical trials (associated diseases)

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