ROR1

Summary

ROR1 (ROR family WNT receptor 1, HGNC:10256) is a protein-coding gene on chromosome 1p31.3, encoding Inactive tyrosine-protein kinase transmembrane receptor ROR1 (Q01973). Has very low kinase activity in vitro and is unlikely to function as a tyrosine kinase in vivo.

This gene encodes a receptor tyrosine kinase-like orphan receptor that modulates neurite growth in the central nervous system. The encoded protein is a glycosylated type I membrane protein that belongs to the ROR subfamily of cell surface receptors. It is a pseudokinase that lacks catalytic activity and may interact with the non-canonical Wnt signalling pathway. This gene is highly expressed during early embryonic development but expressed at very low levels in adult tissues. Increased expression of this gene is associated with B-cell chronic lymphocytic leukaemia. Alternative splicing results in multiple transcript variants encoding different isoforms.

Source: NCBI Gene 4919 — RefSeq curated summary.

At a glance

• Gene–disease (curated): hearing loss, autosomal recessive 108 (Moderate, GenCC) — +2 more curated relationships
• GWAS associations: 14
• Clinical variants (ClinVar): 296 total — 1 pathogenic
• GTEx eGene: eQTL in 19 tissues, sQTL in 3 (q < 0.05)
• Phenotypes (HPO): 5
• Drug target: yes — 1 curated mechanism-of-action drug
• Constraint (gnomAD): pLI 1.00 (loss-of-function intolerant), LOEUF 0.33 (highly constrained)
• MANE Select transcript: NM_005012
• Notable: 296 clinical variants but no curated precision-oncology (CIViC) evidence yet

Identifiers

Gene identifiers

Field	Value
HGNC ID	HGNC:10256
Approved symbol	ROR1
Name	ROR family WNT receptor 1
Location	1p31.3
Locus type	gene with protein product
Status	Approved
Ensembl gene	ENSG00000185483
Ensembl biotype	protein_coding
OMIM	602336
Entrez	4919

Gene structure

Transcript identifiers

Ensembl transcripts: 4 — 3 protein_coding, 1 protein_coding_CDS_not_defined

MANE Select: ENST00000371079

Transcript support level (Ensembl TSL; 1 = fully mRNA-supported): TSL 1: 2, TSL 5: 1

ENST00000371079, ENST00000371080, ENST00000482426, ENST00001140647

RefSeq mRNA: 2 — MANE Select: NM_005012 NM_001083592, NM_005012

CCDS: CCDS41344, CCDS626

Canonical transcript exons

ENST00000371079 — 9 exons

Exon	Start	End
ENSE00001454303	64177428	64181498
ENSE00001454305	63774017	63774508
ENSE00003516915	64050686	64050716
ENSE00003538526	64137369	64137496
ENSE00003553651	64049691	64049978
ENSE00003559494	64009305	64009376
ENSE00003719568	64158981	64159192
ENSE00003735973	64142405	64142650
ENSE00003746077	64140109	64140426

Expression profiles

Bgee: expression breadth ubiquitous, 213 present calls, max score 83.40.

FANTOM5 (CAGE): breadth ubiquitous, TPM avg 6.4138 / max 130.4036, expressed in 1109 samples.

Highest expression (Bgee): germinal epithelium of ovary, popliteal artery, tibial artery, islet of Langerhans, coronary artery.

Genetic regulation across tissues (GTEx eQTL / sQTL)

ROR1 is an eGene in GTEx v10 — its expression is genetically regulated (eQTL) in 19 tissues and its splicing (sQTL) in 3 (q < 0.05). Strongest associations first; slope = normalized effect of the lead variant’s alternative allele.

showing 20 of 22 significant tissue × QTL associations:

Tissue	QTL	q-value	Slope	Lead variant
Brain Cerebellum	eqtl	2.2e-54	-0.98	1:63917718:C:A
Brain Cerebellar Hemisphere	eqtl	8.7e-53	-0.86	1:63917718:C:A
Brain Putamen basal ganglia	eqtl	1.1e-16	-0.55	1:64090992:TG:T
Cells EBV-transformed lymphocytes	eqtl	6.7e-11	+0.57	1:63834416:G:GT
Esophagus Muscularis	eqtl	2.8e-06	+0.32	1:63704096:G:A
Artery Aorta	eqtl	4.2e-06	-0.18	1:63911914:A:C
Cells Cultured fibroblasts	eqtl	5.4e-06	-0.45	1:64042782:T:TA
Heart Atrial Appendage	sqtl	3.2e-05	-0.57	1:64124614:T:C
Testis	eqtl	6.5e-05	+0.30	1:64036374:T:A
Brain Caudate basal ganglia	eqtl	7.0e-05	-0.30	1:64096329:G:A
Esophagus Mucosa	eqtl	8.2e-05	+0.15	1:63661333:C:T
Artery Coronary	eqtl	1.6e-03	-0.23	1:63917077:G:T
Brain Hippocampus	eqtl	1.8e-03	-0.36	1:64095594:T:A
Heart Left Ventricle	sqtl	5.9e-03	-0.55	1:64112531:G:T
Testis	sqtl	1.0e-02	+1.28	1:63741663:T:C
Artery Tibial	eqtl	1.1e-02	-0.33	1:63800828:C:T
Brain Nucleus accumbens basal ganglia	eqtl	1.2e-02	-0.22	1:64096329:G:A
Brain Hypothalamus	eqtl	1.5e-02	-0.63	1:63707813:A:C
Skin Not Sun Exposed Suprapubic	eqtl	2.2e-02	+0.30	1:63834798:G:A
Nerve Tibial	eqtl	2.2e-02	+0.09	1:64339226:G:A

FANTOM5 promoters

3 alternative TSS:

Promoter ID	TPM avg	Samples expressed
3196	6.0786	1102
3197	0.1737	84
3198	0.1615	73

Top tissues by expression

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

Tissue	Anatomy ID	Expression score	Quality
germinal epithelium of ovary	UBERON:0001304	83.40	gold quality
popliteal artery	UBERON:0002250	82.98	gold quality
tibial artery	UBERON:0007610	82.97	gold quality
islet of Langerhans	UBERON:0000006	81.96	gold quality
right coronary artery	UBERON:0001625	81.81	gold quality
lower lobe of lung	UBERON:0008949	81.16	gold quality
aorta	UBERON:0000947	81.00	gold quality
saphenous vein	UBERON:0007318	81.00	gold quality
blood vessel layer	UBERON:0004797	79.90	gold quality
descending thoracic aorta	UBERON:0002345	79.58	gold quality
sural nerve	UBERON:0015488	79.29	gold quality
buccal mucosa cell	CL:0002336	78.80	gold quality
thoracic aorta	UBERON:0001515	78.41	gold quality
ascending aorta	UBERON:0001496	78.11	gold quality
left coronary artery	UBERON:0001626	77.24	gold quality
smooth muscle tissue	UBERON:0001135	77.05	gold quality
coronary artery	UBERON:0001621	76.92	gold quality
parietal pleura	UBERON:0002400	76.82	gold quality
male germ line stem cell (sensu Vertebrata) in testis	CL:0000089 ∩ UBERON:0000473	76.79	gold quality
colonic epithelium	UBERON:0000397	76.21	gold quality
stomach	UBERON:0000945	76.07	gold quality
lung	UBERON:0002048	75.87	gold quality
pancreas	UBERON:0001264	75.56	gold quality
skin of hip	UBERON:0001554	75.25	gold quality
gall bladder	UBERON:0002110	75.09	gold quality
body of stomach	UBERON:0001161	74.90	gold quality
ventricular zone	UBERON:0003053	74.79	gold quality
endocervix	UBERON:0000458	74.74	gold quality
heart	UBERON:0000948	74.19	gold quality
pleura	UBERON:0000977	73.99	gold quality
seminal vesicle	UBERON:0000998	73.97	gold quality
heart left ventricle	UBERON:0002084	73.92	gold quality
cardiac ventricle	UBERON:0002082	73.81	gold quality
heart right ventricle	UBERON:0002080	73.80	gold quality
mucosa of stomach	UBERON:0001199	73.63	gold quality
muscle layer of sigmoid colon	UBERON:0035805	73.43	gold quality
embryo	UBERON:0000922	73.37	gold quality
rectum	UBERON:0001052	73.24	gold quality
right lung	UBERON:0002167	73.01	gold quality
myocardium	UBERON:0002349	72.94	silver quality
hair follicle	UBERON:0002073	72.93	gold quality
upper lobe of lung	UBERON:0008948	72.90	gold quality
fundus of stomach	UBERON:0001160	72.77	gold quality
body of pancreas	UBERON:0001150	72.65	gold quality
endothelial cell	CL:0000115	72.60	gold quality
cauda epididymis	UBERON:0004360	72.60	gold quality
upper lobe of left lung	UBERON:0008952	72.11	gold quality
left uterine tube	UBERON:0001303	72.05	gold quality
myometrium	UBERON:0001296	71.88	gold quality
ectocervix	UBERON:0012249	71.70	gold quality
right ovary	UBERON:0002118	71.60	gold quality
ovary	UBERON:0000992	71.52	gold quality
right atrium auricular region	UBERON:0006631	71.42	gold quality
cardiac atrium	UBERON:0002081	71.27	gold quality
sigmoid colon	UBERON:0001159	71.12	gold quality
calcaneal tendon	UBERON:0003701	70.68	gold quality
body of uterus	UBERON:0009853	70.59	gold quality
left ovary	UBERON:0002119	70.57	gold quality
uterus	UBERON:0000995	70.40	gold quality
ganglionic eminence	UBERON:0004023	70.12	gold quality
uterine cervix	UBERON:0000002	69.79	gold quality
urinary bladder	UBERON:0001255	69.78	gold quality
visceral pleura	UBERON:0002401	69.76	gold quality
mucosa of paranasal sinus	UBERON:0005030	69.75	gold quality
omental fat pad	UBERON:0010414	69.71	gold quality
peritoneum	UBERON:0002358	69.69	gold quality
endometrium	UBERON:0001295	69.68	gold quality
tibial nerve	UBERON:0001323	69.67	gold quality
adipose tissue of abdominal region	UBERON:0007808	69.22	gold quality
apex of heart	UBERON:0002098	68.78	gold quality
primordial germ cell in gonad	CL:0000670 ∩ UBERON:0000991	68.77	gold quality
adrenal tissue	UBERON:0018303	68.75	gold quality
female reproductive system	UBERON:0000474	68.60	gold quality
cardiac muscle of right atrium	UBERON:0003379	68.52	silver quality
mammary duct	UBERON:0001765	68.43	gold quality
superficial temporal artery	UBERON:0001614	68.05	gold quality
cardia of stomach	UBERON:0001162	67.92	gold quality
vermiform appendix	UBERON:0001154	67.72	gold quality
adipose tissue	UBERON:0001013	67.61	gold quality
epithelium of mammary gland	UBERON:0003244	67.51	gold quality
esophagogastric junction muscularis propria	UBERON:0035841	67.39	gold quality
gingiva	UBERON:0001828	67.29	gold quality
subcutaneous adipose tissue	UBERON:0002190	67.17	gold quality
connective tissue	UBERON:0002384	67.14	gold quality
caecum	UBERON:0001153	66.98	gold quality
large intestine	UBERON:0000059	66.95	gold quality
esophagus mucosa	UBERON:0002469	66.94	gold quality
colon	UBERON:0001155	66.90	gold quality
zone of skin	UBERON:0000014	66.85	gold quality
left ventricle myocardium	UBERON:0006566	66.82	gold quality
skin of leg	UBERON:0001511	66.72	gold quality
nipple	UBERON:0002030	66.61	gold quality
synovial joint	UBERON:0002217	66.58	gold quality
skin of abdomen	UBERON:0001416	66.44	gold quality
cerebellar vermis	UBERON:0004720	66.12	gold quality
hindlimb stylopod muscle	UBERON:0004252	65.93	gold quality
layer of synovial tissue	UBERON:0007616	65.72	silver quality
pylorus	UBERON:0001166	65.70	gold quality
thoracic mammary gland	UBERON:0005200	65.70	gold quality
epithelial cell of pancreas	CL:0000083	65.68	silver quality

Single-cell (SCXA)

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

Experiment	Marker?	Max mean expression
E-CURD-119	yes	14.63
E-ANND-3	yes	5.40

HPA expression

RNA tissue specificity: Tissue enhanced

showing 60 of 76 HPA tissues / cells by nTPM:

Tissue / cell	Axis	nTPM
Parathyroid gland	tissue	23.1
Choroid plexus	tissue	12.5
Smooth muscle	tissue	6.5
Cervix	tissue	6.4
Heart muscle	tissue	6.4
Endometrium 1	tissue	6.1
Lung	tissue	6.0
Stomach 1	tissue	5.6
Seminal vesicle	tissue	5.5
Ovary	tissue	4.9
Pancreas	tissue	4.7
Prostate	tissue	4.7
Esophagus	tissue	4.4
Gallbladder	tissue	4.4
Adipose tissue	tissue	3.8
Rectum	tissue	3.5
Urinary bladder	tissue	3.5
Nucleus accumbens	tissue	3.4
Spinal cord	tissue	3.4
Hippocampus	tissue	3.4
Breast	tissue	3.2
Superior colliculi	tissue	3.1
Postcentral gyrus	tissue	3.1
Spleen	tissue	2.8
Colon	tissue	2.7
Placenta	tissue	2.7
Substantia nigra	tissue	2.7
Locus coeruleus	tissue	2.5
Caudate putamen	tissue	2.3
Thymus	tissue	2.1
Skeletal muscle	tissue	2.0
Kidney	tissue	2.0
Vagina	tissue	1.9
Duodenum	tissue	1.9
Appendix	tissue	1.9
Thalamus	tissue	1.7
Fallopian tube	tissue	1.7
Olfactory bulb	tissue	1.6
Midbrain	tissue	1.5
Small intestine	tissue	1.5
Tongue	tissue	1.4
Medulla oblongata	tissue	1.4
Hippocampal formation	tissue	1.4
Periaqueductal gray	tissue	1.4
Testis	tissue	1.3
Retina	tissue	1.3
Corpus callosum	tissue	1.3
Skin 1	tissue	1.2
Cerebral cortex	tissue	1.2
Pons	tissue	1.2
Epididymis	tissue	1.2
Hypothalamus	tissue	1.2
Cerebellum	tissue	1.2
Thyroid gland	tissue	1.2
Somatosensory cortex	tissue	1.2
Lymph node	tissue	1.1
Occipital cortex	tissue	1.1
Prefrontal cortex	tissue	1.0
Salivary gland	tissue	1.0
Motor cortex	tissue	1.0

Brain sub-regions (HPA Brain Atlas): detected in 289; highest nTPM — Cerebellar cortex (152.8), Flocculonodular lobe (148.5), Habenula (136.6), Lateral geniculate body (135.2), Medial dorsal thalamic nucleus (121.7).

Regulation

Is transcription factor: no

Upstream regulators (CollecTRI, top): FOXC1, RORA, STAT3

miRNA regulators (miRDB)

Targeting ROR1 by miRDB confidence (max_score; target_count = how many genes the miRNA targets in total — lower means more specific).

showing 30 of 208 miRNAs:

miRNA	Max score	Avg score	miRNA target_count
HSA-MIR-3163	100.00	77.23	8605
HSA-MIR-30A-5P	100.00	76.31	3233
HSA-MIR-30B-5P	100.00	76.29	3248
HSA-MIR-30C-5P	100.00	76.29	3248
HSA-MIR-30D-5P	100.00	76.32	3233
HSA-MIR-30E-5P	100.00	76.32	3242
HSA-MIR-5692A	100.00	74.40	6850
HSA-MIR-450A-1-3P	100.00	69.33	1837
HSA-MIR-513A-5P	100.00	69.77	2465
HSA-MIR-190A-3P	100.00	80.35	5520
HSA-MIR-188-3P	100.00	68.76	1240
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-3064-3P	100.00	70.09	1254
HSA-MIR-548AW	99.99	72.57	3559
HSA-MIR-548C-3P	99.99	74.01	7587
HSA-MIR-3662	99.99	73.82	5684
HSA-MIR-4534	99.99	66.58	1907
HSA-MIR-27A-3P	99.98	72.13	2955
HSA-MIR-27B-3P	99.98	72.13	2955
HSA-MIR-19A-3P	99.98	75.33	2762
HSA-MIR-19B-3P	99.98	75.44	2754
HSA-MIR-9985	99.98	72.11	2939
HSA-MIR-103A-3P	99.98	69.14	1595
HSA-MIR-107	99.98	69.14	1595
HSA-MIR-520D-5P	99.98	73.34	4883
HSA-MIR-524-5P	99.98	73.43	4882
HSA-MIR-8068	99.98	73.85	2376

Functional genomics

gnomAD constraint: pLI 1, LOEUF 0.326, missense Z 3.15 — population loss-of-function intolerance (pLI ≥ 0.9 = LoF-intolerant; lower LOEUF = more constrained). gnomAD

Regional missense constraint (gnomAD)

ENST00000371079 splits into 3 regions with different missense tolerance; 0 are missense-constrained. Missense variants in a constrained region (low observed/expected) are more likely to be pathogenic. gnomAD

Region (GRCh38)	Missense obs / exp	o/e	Constrained
1:63,774,418–64,009,349	63 / 57.0	1.10	no
1:64,009,350–64,049,792	19 / 50.9	0.37	no
1:64,049,793–64,178,852	835 / 1069.8	0.78	no

Literature-anchored findings (GeneRIF, showing 40)

• investigation of mutations in GCL modifier subunit and the GCL catalytic subunit that modify catalytic activity and lower glutathione levels (PMID:12954617)
• overexpression of GCLm extended the mean life span only up to 24% (PMID:16148000)
• The ROR1 protein modulates the growth of neurites as well as their branching pattern in hippocampal neurons. (PMID:15654020)
• finsings show ROR1 protein is selectively expressed on the surface of B-cell chronic lymphocytic leukemia (B-CLL) cells, whereas normal B cells, other normal blood cells, and normal adult tissues do not express cell surface ROR1 (PMID:18223214)
• ROR1 is an oncofetal surface antigen and survival-signaling receptor in chronic lymphocytic leukemia. (PMID:18287027)
• Overexpression of orphan receptor tyrosine kinase Ror1 is associated with acute lymphoblastic leukemia (PMID:18354269)
• The majority of CLL cells exhibited Ror1 surface expression (71% mean; range 36-92%). Two different variants of the Ror1 protein, 105 and 130 kDa, were identified. (PMID:18546292)
• expression of ROR1 and WT1 in B-ALL is associated with the differentiation stage of the leukemic cells (PMID:18604725)
• results indicate that ROR1 expression is not limited to chronic lymphoid leukaemia cases, but it is more prevalent in non-Hodgkin lymphomas (PMID:20597086)
• Data suggest that constitutively activated Stat3 binds to the ROR1 promoter and activates ROR1 in CLL cells. (PMID:20686606)
• ROR1 has characteristics of an oncofetal gene and is expressed in undifferentiated embryonic stem cells, B-cell chronic lymphocytic leukemia and mantle cell lymphoma, but not in major adult tissues. (PMID:20702778)
• Detection of a high level of ROR1 expression in blood cells might assist in early detection of renal malignancies. (PMID:21079657)
• Ror1 undergoes complex post-translational modifications by glycosylation and mono-ubiquitination. These modifications regulate Ror1 localization and signalling, and are highly variable among individual chronic lymphocytic leukemia patients. (PMID:21481194)
• Findings suggest a critical role for Ror1 in malignant phenotypes sustained by the Met oncogene. (PMID:21487037)
• ROR1 is uniformly and highly expressed in all in chronic lymphocytic leukemia (CLL) cases at initial diagnosis and can serve as a diagnostic tool. (PMID:21531460)
• A panel of mAbs demonstrated high affinity and specificity for a diverse set of epitopes that involve all three extracellular domains of ROR1, are accessible on the cell surface, and mediate internalization (PMID:21698301)
• ROR1 is expressed on hematogones (non-neoplastic human B-lymphocyte precursors) and a minority of precursor-B acute lymphoblastic leukemia. (PMID:21813176)
• nuclear-localized ROR1 may play an important role in cell migration and cytoskeleton remodeling (PMID:22199287)
• ROR1 was overexpressed in acute lymphoblastic leukemia (PMID:22369092)
• ROR1 is expressed in human breast cancers and has biological and clinical significance (PMID:22403610)
• that the receptor tyrosine kinase ROR1 was overexpressed in most patients with various hematological malignancies of both lymphoid and myeloid origins. (PMID:22988987)
• Many different human cancers express ROR1 and ROR1 may play a functional role in promoting tumor cell growth. (PMID:23041612)
• t(1;19) Acute Lymphoblastic Leukemia cells universally exhibit expression of and dependence on the cell surface receptor ROR1. (PMID:23153538)
• cell surface expression in pediatric B-ALL along with its virtual absence from normal tissues and circulating cells makes ROR1 a promising target for mAb-based therapies. (PMID:23285131)
• Our results show that customizing spacer design and increasing affinity of ROR1-CARs enhances T-cell effector function and recognition of ROR1(+) tumors. (PMID:23620405)
• Data indicate that type I receptor tyrosine kinase-like orphan receptor ROR1 may regulate EMT and metastasis and that antibodies targeting ROR1 can inhibit cancer progression and metastasis. (PMID:23771907)
• Data shows that ROR1 and ROR2 are inversely expressed in melanomas and negatively regulate each other. Also, hypoxia initiates a shift of ROR1-positive melanomas to a more invasive, ROR2-positive phenotype. (PMID:24104062)
• CLL cells expressed different isoforms of ROR1. (PMID:24205204)
• ROR1 can interact with TCL1 and enhance leukemogenesis in Emu-TCL1 transgenic mice. (PMID:24379361)
• ROR1 is only detectable in embryonic tissue and generally absent in adult tissue, making the protein an ideal drug target for cancer therapy. [Review] (PMID:24752542)
• Human ROR1 and ROR2 are receptor tyrosine kinase-like pseudokinases. (PMID:25029443)
• ROR1 expression is correlated with malignant attributes of ovarian cancer and it may serve as a novel prognostic marker in ovarian cancer. (PMID:25056203)
• Data indicate that shRNA silencing of type I receptor tyrosine kinase-like orphan receptor (ROR1) cells, or treatment with anti-ROR1 mAb UC-961 impaired the capacity of ovarian cancer cells to form spheroids or tumor xenografts. (PMID:25411317)
• The newly developed OSU-2S delivery using ROR1-directed immunonanoparticles provide selective targeting of OSU-2S to MCL and other ROR1(+) malignancies, sparing normal B cells. (PMID:25937048)
• Significantly down-regulates the activity of the PI3K/AKT/mTOR signaling pathway. (PMID:25978653)
• Both IGF1R and ROR1 can be effectively targeted by SB modified CAR T cells. (PMID:26173023)
• High expression of ROR1 (63%), pAkt (36%), and pCREB (20%) was observed in gastric adenocarcinomas, and expression of these proteins was well intercorrelated. (PMID:26245996)
• Data show that ROR1 contributes to melanoma progression by promoting cell growth and migration. (PMID:26509654)
• Data show that silencing receptor tyrosine kinases (RTKs) ROR2 and ROR1 has a strong inhibitory effect on the ability of ovarian cancer cells to proliferate, migrate and invade. (PMID:26515598)
• Data show that the majority of chronic lymphocytic leukemia (CLL) patients had antibodies against receptor tyrosine kinase ROR1. (PMID:26562161)

Cross-species orthologs

3 orthologs

Organism	Symbol	Gene ID
danio_rerio	ror1	ENSDARG00000015176
mus_musculus	Ror1	ENSMUSG00000035305
rattus_norvegicus	Ror1	ENSRNOG00000029449

Paralogs (53): INSRR (ENSG00000027644), MUSK (ENSG00000030304), FLT4 (ENSG00000037280), EPHA3 (ENSG00000044524), ROS1 (ENSG00000047936), LTK (ENSG00000062524), ERBB3 (ENSG00000065361), TIE1 (ENSG00000066056), FGFR2 (ENSG00000066468), FGFR3 (ENSG00000068078), EPHA8 (ENSG00000070886), FGFR1 (ENSG00000077782), EPHA6 (ENSG00000080224), TYRO3 (ENSG00000092445), FLT1 (ENSG00000102755), MET (ENSG00000105976), EPHB6 (ENSG00000106123), PDGFRB (ENSG00000113721), EPHA4 (ENSG00000116106), TEK (ENSG00000120156), FLT3 (ENSG00000122025), KDR (ENSG00000128052), EPHB2 (ENSG00000133216), PDGFRA (ENSG00000134853), EPHA7 (ENSG00000135333), IGF1R (ENSG00000140443), NTRK3 (ENSG00000140538), ERBB2 (ENSG00000141736), EPHA2 (ENSG00000142627), EPHA5 (ENSG00000145242), EGFR (ENSG00000146648), EPHA1 (ENSG00000146904), NTRK2 (ENSG00000148053), MERTK (ENSG00000153208), EPHB1 (ENSG00000154928), KIT (ENSG00000157404), FGFR4 (ENSG00000160867), DDR2 (ENSG00000162733), RYK (ENSG00000163785), MST1R (ENSG00000164078), LMTK2 (ENSG00000164715), RET (ENSG00000165731), AXL (ENSG00000167601), ROR2 (ENSG00000169071), ALK (ENSG00000171094), INSR (ENSG00000171105), ERBB4 (ENSG00000178568), CSF1R (ENSG00000182578), EPHB3 (ENSG00000182580), EPHA10 (ENSG00000183317), EPHB4 (ENSG00000196411), NTRK1 (ENSG00000198400), DDR1 (ENSG00000204580)

Mouse-model phenotypes

Observed phenotypes of the mouse ortholog (MGI:1347520) from MGI (Alliance of Genome Resources) — knockout/mutant phenotypes, ranked by annotation count. 26 distinct phenotype terms.

Mouse phenotype (MP)	Records
abnormal cochlea morphology	1
abnormal spleen morphology	1
enlarged spleen	1
abnormal thymus morphology	1
enlarged thymus	1
exencephaly	1
abnormal sensory neuron innervation pattern	1
abnormal uterus morphology	1
cyanosis	1
respiratory distress	1
deafness	1
abnormal respiratory system physiology	1
abnormal pulmonary alveolus morphology	1
abnormal cochlear hair cell morphology	1
small kidney	1
decreased cochlea coiling	1
increased prepulse inhibition	1
abnormal axon fasciculation	1
abnormal synapse morphology	1
abnormal blood homeostasis	1
hydrometra	1
neonatal lethality, complete penetrance	1
preweaning lethality, complete penetrance	1
increased or absent threshold for auditory brainstem response	1
decreased distortion product otoacoustic emission amplitude	1

+1 more (showing top 25).

Additional cross-species homologs

Sequence homologs in species beyond Ensembl Compara’s model organisms, by Diamond local protein alignment (% sequence identity; best hit per species). Lower-identity rows are more distant homologs. The matched accessions’ gene symbols aren’t in biobtree yet, so each row shows the UniProt accession.

Organism	UniProt	Identity	Method
Pan troglodytes	Q7YR43	99.6%	Diamond
Macaca fascicularis	Q5IFJ9	99.4%	Diamond
Drosophila sechellia	B4HNW4	99.0%	Diamond
Drosophila simulans	B4QC63	99.0%	Diamond
Saimiri boliviensis boliviensis	Q5IS82	99.0%	Diamond
Drosophila melanogaster	Q6AWJ9	98.5%	Diamond
Drosophila erecta	B3NS99	97.4%	Diamond
Drosophila yakuba	B4P5Q9	97.4%	Diamond
Sus scrofa	P24786	95.8%	Diamond
Gallus gallus	F1NY98	94.4%	Diamond
Capra hircus	Q7M323	92.9%	Diamond
Cavia porcellus	P14617	89.8%	Diamond
Canis lupus familiaris	P0DV84	89.1%	Diamond
Drosophila ananassae	B3MH43	88.7%	Diamond
Caenorhabditis elegans	Q8I7I5	84.2%	Diamond
Drosophila mojavensis	B4KPU0	79.8%	Diamond
Drosophila willistoni	B4MR28	79.4%	Diamond
Petromyzon marinus	P33574	55.6%	Diamond
Lymnaea stagnalis	O76997	54.2%	Diamond
Hydra vulgaris	Q25197	50.8%	Diamond
Toxoplasma gondii	A0A7J6K144	49.3%	Diamond
Geodia cydonium	P42159	48.4%	Diamond
Acanthamoeba polyphaga mimivirus	Q5UQC1	37.3%	Diamond

Genomic neighbors (locus context)

Genes flanking this one on the chromosome (NCBI/Entrez gene neighborhood). Positional context only — some neighbors share regulatory elements (bidirectional promoters, antisense/overlapping transcripts), but chromosomal adjacency is not itself a functional relationship (see Interactions for that).

Symbol	Type	Entrez
PGM1	protein-coding	5236
UBE2U	protein-coding	148581
DLEU2L	ncRNA	79469
EFCAB7	protein-coding	84455
ROR1-AS1	ncRNA	101927034

Protein

Protein identifiers

Inactive tyrosine-protein kinase transmembrane receptor ROR1 — Q01973 (reviewed: Q01973)

Alternative names: Neurotrophic tyrosine kinase, receptor-related 1

All UniProt accessions (1): Q01973

UniProt curated annotations — full annotation on UniProt →

Function. Has very low kinase activity in vitro and is unlikely to function as a tyrosine kinase in vivo. Receptor for ligand WNT5A which activates downstream NFkB signaling pathway and may result in the inhibition of WNT3A-mediated signaling. In the inner ear, crucial for spiral ganglion neurons to innervate auditory hair cells. Via IGFBP5 ligand, forms a complex with ERBB2 to enhance CREB oncogenic signaling.

Subunit / interactions. Interacts with ERBB2 and IGFBP5.

Subcellular location. Cell membrane. Cell projection. Axon.

Tissue specificity. Expressed strongly in human heart, lung and kidney, but weakly in the CNS. Isoform Short is strongly expressed in fetal and adult CNS and in a variety of human cancers, including those originating from CNS or PNS neuroectoderm.

Disease relevance. Deafness, autosomal recessive, 108 (DFNB108) [MIM:617654] A form of non-syndromic sensorineural hearing loss. Sensorineural deafness results from damage to the neural receptors of the inner ear, the nerve pathways to the brain, or the area of the brain that receives sound information. The disease is caused by variants affecting the gene represented in this entry.

Domain organisation. The activation loop of the kinase domain adopts an inactive conformation and the ATP-binding pocket is occluded and inaccessible. Despite lacking kinase activity, the kinase domain is required for signaling.

Similarity. Belongs to the protein kinase superfamily. Tyr protein kinase family. ROR subfamily.

Isoforms (3)

UniProt ID	Names	Canonical?
Q01973-1	Long	yes
Q01973-2	Short, T-ROR1
Q01973-3	3

RefSeq proteins (2): NP_001077061, NP_005003* (*=MANE)

Domains & families (InterPro)

ID	Name	Type
IPR000001	Kringle	Domain
IPR000719	Prot_kinase_dom	Domain
IPR001245	Ser-Thr/Tyr_kinase_cat_dom	Domain
IPR003598	Ig_sub2	Domain
IPR003599	Ig_sub	Domain
IPR007110	Ig-like_dom	Domain
IPR008266	Tyr_kinase_AS	Active_site
IPR011009	Kinase-like_dom_sf	Homologous_superfamily
IPR013098	Ig_I-set	Domain
IPR013783	Ig-like_fold	Homologous_superfamily
IPR013806	Kringle-like	Homologous_superfamily
IPR016247	Tyr_kinase_rcpt_ROR	Family
IPR018056	Kringle_CS	Conserved_site
IPR020067	Frizzled_dom	Domain
IPR036179	Ig-like_dom_sf	Homologous_superfamily
IPR036790	Frizzled_dom_sf	Homologous_superfamily
IPR038178	Kringle_sf	Homologous_superfamily
IPR050122	RTK	Family

Pfam: PF00051, PF01392, PF07679, PF07714

Enzyme classification (BRENDA)

• EC 2.7.10.1 — receptor protein-tyrosine kinase (BRENDA: 44 organisms, 214 substrates, 574 inhibitors, 11 Km, 0 kcat entries)

Substrate kinetics (BRENDA)

4 substrates with measured Km, best-characterized 4. Km ranges are aggregated across organisms/conditions.

Substrate	Km (mM)	Measurements
ATP	0.0011–0.129	4
AC-DYFE-6-CHLORO-W-NHME	0.0051	1
AC-DYFGW-NHME	0.07	1
YFEW	0.232	1

UniProt features (76 total): helix 19, strand 13, sequence variant 10, disulfide bond 9, compositionally biased region 4, glycosylation site 4, domain 4, splice variant 3, region of interest 2, topological domain 2, turn 2, signal peptide 1, chain 1, transmembrane region 1, mutagenesis site 1

Structure

Experimental structures (PDB)

5 structures by resolution:

PDB	Title	Method	Resolution (Å)
7TNG	Kringle domain of human Receptor Tyrosine Kinase-Like Orphan Receptor 1 (ROR1)	X-RAY DIFFRACTION	1.4
6BA5	Potent and Selective Antitumor Activity of a T-Cell Engaging Bispecific Antibody …	X-RAY DIFFRACTION	1.62
6TU9	The ROR1 Pseudokinase Domain Bound To Ponatinib	X-RAY DIFFRACTION	1.94
6BAN	Potent and Selective Antitumor Activity of a T-Cell Engaging Bispecific Antibody …	X-RAY DIFFRACTION	1.95
5Z55	NMR Solution Structure of the Kringle domain of human receptor tyrosine kinase-like …	SOLUTION NMR

Predicted structure (AlphaFold)

Model	pLDDT	Fraction very-high
AF-Q01973-F1	69.17	0.26

Antibody-complex structures (SAbDab)

2 antibodies co-crystallized with this protein: 6BA5, 6BAN

Human Protein Atlas

Protein class: Enzymes, Kinases, Tyr protein kinases, Predicted membrane proteins, Predicted intracellular proteins, Disease related genes, Potential drug targets, Human disease related genes, Ear disease

Protein evidence: Evidence at protein level

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 (9)

Type	Positions
Disulfide bond	79–131, 170–235, 178–228, 219–260, 248–296, 252–282, 313–391, 334–374, 362–386

Glycosylation sites (4)

Type	Positions
N-linked (glcnac…) asparagine	47, 66, 184, 315

Mutagenesis-validated functional residues (1)

Position	Phenotype
482	no effect on kinase activity.

Function

Pathways and Gene Ontology

Reactome pathways

1 curated (TAS) of 5; 0 disease pathways. Curated-first; evidence = TAS (manually curated) vs IEA (electronic inference).

5 pathways:

ID	Pathway	Evidence
R-HSA-5140745	WNT5A-dependent internalization of FZD2, FZD5 and ROR2	curated
R-HSA-3858494	Beta-catenin independent WNT signaling	—
R-HSA-4086400	PCP/CE pathway	—
R-HSA-162582	Signal Transduction	—
R-HSA-195721	Signaling by WNT	—

MSigDB gene sets: 251 (showing top): GSE45365_NK_CELL_VS_CD8A_DC_MCMV_INFECTION_UP, RODRIGUES_THYROID_CARCINOMA_ANAPLASTIC_UP, FREAC2_01, BUYTAERT_PHOTODYNAMIC_THERAPY_STRESS_DN, RODRIGUES_THYROID_CARCINOMA_POORLY_DIFFERENTIATED_UP, XU_GH1_AUTOCRINE_TARGETS_UP, GOBP_SENSORY_PERCEPTION_OF_MECHANICAL_STIMULUS, MODULE_64, GOBP_CANONICAL_NF_KAPPAB_SIGNAL_TRANSDUCTION, MAZ_Q6, GRAESSMANN_APOPTOSIS_BY_DOXORUBICIN_DN, GRAESSMANN_RESPONSE_TO_MC_AND_DOXORUBICIN_DN, AAAYRNCTG_UNKNOWN, MODULE_66, GOBP_EAR_DEVELOPMENT

GO Biological Process (7): cell surface receptor protein tyrosine kinase signaling pathway (GO:0007169), sensory perception of sound (GO:0007605), cell population proliferation (GO:0008283), positive regulation of canonical NF-kappaB signal transduction (GO:0043123), inner ear development (GO:0048839), protein phosphorylation (GO:0006468), Wnt signaling pathway (GO:0016055)

GO Molecular Function (11): transmembrane receptor protein tyrosine kinase activity (GO:0004714), ATP binding (GO:0005524), coreceptor activity (GO:0015026), Wnt-protein binding (GO:0017147), signaling receptor activity (GO:0038023), Wnt receptor activity (GO:0042813), nucleotide binding (GO:0000166), protein kinase activity (GO:0004672), protein binding (GO:0005515), kinase activity (GO:0016301), transferase activity (GO:0016740)

GO Cellular Component (6): cytoplasm (GO:0005737), plasma membrane (GO:0005886), axon (GO:0030424), signaling receptor complex (GO:0043235), axon terminus (GO:0043679), membrane (GO:0016020)

Reactome top-level categories

4 top-level categories:

Category	Pathways
PCP/CE pathway	1
Signal Transduction	1
Signaling by WNT	1
Beta-catenin independent WNT signaling	1

GO top-level categories

39 GO namespaces:

Category	Terms
cellular anatomical structure	2
enzyme-linked receptor protein signaling pathway	1
sensory perception of mechanical stimulus	1
cellular process	1
canonical NF-kappaB signal transduction	1
regulation of canonical NF-kappaB signal transduction	1
positive regulation of intracellular signal transduction	1
ear development	1
animal gross anatomical part developmental process	1
phosphorylation	1
protein modification process	1
cell surface receptor signaling pathway	1
protein tyrosine kinase activity	1
transmembrane receptor protein kinase activity	1
adenyl ribonucleotide binding	1
purine ribonucleoside triphosphate binding	1
anion binding	1
signaling receptor activity	1
protein binding	1
molecular transducer activity	1
transmembrane signaling receptor activity	1
Wnt signaling pathway	1
Wnt-protein binding	1
nucleoside phosphate binding	1
heterocyclic compound binding	1
kinase activity	1
phosphotransferase activity, alcohol group as acceptor	1
catalytic activity, acting on a protein	1
binding	1
transferase activity, transferring phosphorus-containing groups	1
catalytic activity	1
intracellular anatomical structure	1
membrane	1
cell periphery	1
neuron projection	1
protein-containing complex	1
neuron projection terminus	1
presynapse	1
distal axon	1

Experimentally-supported GO annotations

GO terms backed by direct experimental evidence (ECO experimental codes) — 8 of 24 annotations. The rest are phylogenetic / computational / electronic (IEA).

8 experimentally-supported GO terms:

GO term	NS	Evidence
cell population proliferation	BP	direct assay
positive regulation of canonical NF-kappaB signal transduction	BP	mutant phenotype
sensory perception of sound	BP	mutant phenotype
plasma membrane	CC	direct assay
signaling receptor complex	CC	direct assay
Wnt receptor activity	MF	mutant phenotype
Wnt-protein binding	MF	physical interaction
signaling receptor activity	MF	direct assay

Protein interactions and networks

STRING

showing 15 of 626 interactions by confidence (×1000):

Protein A	Protein B	Partner UniProt	Score
ROR1	CAP1	Q01518	548
ROR1	WNT5A	P41221	521
ROR1	DCN	P07585	501
ROR1	RETN	Q9HD89	469
ROR1	CAVIN1	Q6NZI2	459
ROR1	DVL1	O14640	450
ROR1	MSLN	Q13421	441
ROR1	RETNLB	Q9BQ08	432
ROR1	PACSIN2	Q9UNF0	410
ROR1	FZD4	Q9ULV1	386
ROR1	EHD2	Q9NZN4	380
ROR1	CD19	P15391	376
ROR1	RYK	P34925	369
ROR1	FANK1	Q8TC84	361
ROR1	CTNNB1	P35222	358

IntAct

Human interaction partners of ROR1 in IntAct, one row per partner (best MIscore; records = supporting IntAct interaction records).

19 partners by confidence:

Partner	Interaction type	MIscore	Records
SRC	physical association	0.680	8
EGFR	association	0.580	5
MFHAS1	direct interaction	0.440	1
PLEC	physical association	0.400	1
DUSP14	physical association	0.370	1
DUSP18	physical association	0.370	1
DUSP19	physical association	0.370	1
DUSP21	physical association	0.370	1
DUSP29	physical association	0.370	1
ILKAP	physical association	0.370	1
PPM1B	physical association	0.370	1
PPM1F	physical association	0.370	1
PTPN6	physical association	0.370	1
PTPRR	physical association	0.370	1
STYX	physical association	0.370	1
TBC1D4	association	0.350	3
CLGN	association	0.350	1
TRIM21	association	0.350	1
ARHGAP32	proximity	0.270	1

BioGRID (154 interactions; top human partners by supporting records): ROR2 (Affinity Capture-MS; 5 records), DOCK2 (Affinity Capture-Western; 3 records), YWHAZ (Affinity Capture-MS; 3 records), CDC37 (Proximity Label-MS; 2 records), CTTN (Affinity Capture-Western; 2 records), HSPA1B (Proximity Label-MS; 2 records), KRAS (Proximity Label-MS; 2 records), RNF43 (Affinity Capture-Western; 2 records), SERPINB13 (Affinity Capture-MS; 2 records), SRSF9 (Proximity Label-MS; 2 records), XPNPEP3 (Proximity Label-MS; 2 records), ACBD3 (Proximity Label-MS), AHNAK2 (Proximity Label-MS), ALK (Proximity Label-MS), APP (Reconstituted Complex)

SIGNOR signaling

showing 4 of 6 signaling interactions:

A	Effect	B	Mechanism
WNT5A	up-regulates	ROR1	binding
ROR1	up-regulates	SRC	phosphorylation
hsa-miR-382-5p	“down-regulates quantity by repression”	ROR1	“post transcriptional regulation”
ROR1	“up-regulates activity”	ERBB3	phosphorylation

Ligand–receptor pairs (CellPhoneDB) (1)

Curated ligand–receptor partners (cell-cell communication), distinct from the protein–protein interactions above.

1 ligand–receptor pairs:

Partner	This gene’s role	Signaling class
WNT5A	receptor	Signaling by WNT

Disease & clinical

Genetic variants

Variant evidence for ROR1: 296 ClinVar records (1 pathogenic / likely pathogenic); 14 GWAS associations. Per-variant detail is on Sugi Variant.

ClinVar

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

Classification	Count (floor)
Pathogenic	1
Likely pathogenic	0
Uncertain significance	182
Likely benign	57
Benign	21

Top pathogenic / likely-pathogenic (1)

Showing all 1 pathogenic / likely-pathogenic ClinVar records, ranked by ClinVar review status (expert panel → multiple submitters → single submitter), then by number of submitting labs.

Variant ID	HGVS	Classification	Review	Submitters
59971	GRCh38/hg38 1p32.1-31.1(chr1:59632500-76730877)x1	Pathogenic	criteria provided, single submitter	1

Per-variant reference — Sugi Variant

Explore ROR1’s pathogenic and likely-pathogenic variants individually — each with its ClinVar classification and conditions, applied ACMG criteria (ClinGen expert panel, where curated), the calibrated in-silico predictors (AlphaMissense, REVEL, SaProt, conservation), gnomAD frequency, and the predictor-disagreement QC signal — on Sugi Variant.

SpliceAI

Top 10 splice-impact sites by Δscore (adjacent positions with the same effect merged into one range; 27 predictions of 2,306):

Position(s)	Effect	Δscore	Sites
1:64049935	donor_gain	1.0000
1:64049975	donor_gain	1.0000
1:64049979–64049980	donor_loss	1.0000	5
1:64050677	acceptor_gain	1.0000
1:64137367–64137368	acceptor_loss	1.0000	6
1:64158968	acceptor_gain	1.0000
1:64158972	acceptor_gain	1.0000
1:64158976	acceptor_gain	1.0000
1:64158979–64158980	acceptor_loss	1.0000	6
1:63774509–63774510	donor_loss	0.9900	4

AlphaMissense

2,676 missense substitutions predicted likely pathogenic (of 6,167 scored), across 640 residues. Top 20 hotspot residues, ranked by the number of likely-pathogenic substitutions (of those reachable by a single-nucleotide change), then by mean score:

Residue	Likely-pathogenic substitutions	Mean am_pathogenicity	Max am_pathogenicity
M725	9	0.911	0.992
D125	8	0.997	0.999
H359	8	0.996	0.998
F232	8	0.990	1.000
N364	8	0.990	0.999
N94	8	0.985	0.999
D615	8	0.977	0.994
D122	8	0.965	0.990
D674	8	0.965	0.993
H345	8	0.964	0.989
H613	8	0.963	0.990
N66	8	0.960	0.998
F206	8	0.951	0.999
N620	8	0.946	0.991
F475	8	0.942	0.998
F739	8	0.933	0.995
D250	8	0.932	0.990
D572	8	0.932	0.981
S860	8	0.925	0.999
D644	8	0.922	0.981

HPA cancer prognostics

RNA cancer specificity: Low cancer specificity

Human Protein Atlas survival analysis — favorable = higher expression predicts better survival.

4 prognostic cancer types:

Cancer	Prognostic	p-value
Kidney Renal Clear Cell Carcinoma (TCGA)	favorable	2.45e-09
Kidney Renal Clear Cell Carcinoma (TCGA)	favorable	8.09e-07
Kidney Renal Clear Cell Carcinoma (validation)	favorable	1.69e-05
Liver Hepatocellular Carcinoma (validation)	favorable	0.00076

Disease associations

OMIM: gene MIM:602336 | disease phenotypes:

GenCC curated gene-disease

3 curated gene-disease records:

Disease	Classification	Inheritance	Records
hearing loss, autosomal recessive 108	Moderate	Autosomal recessive	3
hearing loss, autosomal recessive	Supportive	Autosomal recessive
nonsyndromic genetic hearing loss	Limited	Autosomal recessive

ClinGen Gene-Disease Validity

Expert-panel classifications — Definitive > Strong > Moderate > Limited > Disputed > Refuted.

1 validity classifications:

Disease	Classification	Inheritance
nonsyndromic genetic hearing loss	Limited	AR

Genomics England panels (PanelApp)

Clinical diagnostic gene panels including this gene (2 panels, 0 green/diagnostic-grade). Confidence: green = diagnostic, amber = moderate.

2 panels:

Panel	Rating
Monogenic hearing loss	amber
Paediatric disorders	amber

Mondo (3): hearing loss, autosomal recessive 108 (MONDO:0033200), nonsyndromic genetic hearing loss (MONDO:0019497), hearing loss, autosomal recessive (MONDO:0019588)

HPO phenotypes

5 phenotypes (HPO-id order):

HPO	Term
HP:0000007	Autosomal recessive inheritance
HP:0000612	Iris coloboma
HP:0001270	Motor delay
HP:0003593	Infantile onset
HP:0008527	Congenital sensorineural hearing impairment

GWAS associations

14 associations:

Study	Trait	p-value
GCST010697_39	Cortical surface area (min-P)	2e-27
GCST006585_2493	Blood protein levels	3e-15
GCST006585_1970	Blood protein levels	3e-14
GCST007448_19	Normal facial asymmetry (angle of surface orientation score)	2e-10
GCST010701_78	Cortical surface area (MOSTest)	5e-10
GCST010696_14	Cortical thickness (min-P)	2e-9
GCST010700_64	Cortical thickness (MOSTest)	2e-9
GCST010703_175	Brain morphology (MOSTest)	1e-8
GCST009088_2	Severe bacterial meningitis	2e-8
GCST010699_20	Brain morphology (min-P)	2e-8
GCST010698_34	Subcortical volume (min-P)	4e-8
GCST010702_49	Subcortical volume (MOSTest)	5e-8
GCST006585_156	Blood protein levels	2e-7
GCST002991_6	Pancreatic cancer	7e-6

EFO canonical traits (from GWAS)

3 canonical traits:

EFO ID	Trait name
EFO:0009751	facial asymmetry measurement
EFO:0004346	neuroimaging measurement
EFO:0004840	cortical thickness

MeSH disease descriptors

2 disease descriptors:

Descriptor	Name	Tree numbers
C564609	Deafness, Autosomal Recessive *(supp.)*
C580334	Nonsyndromic Deafness *(supp.)*

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (3): CHEMBL4665585 (SINGLE PROTEIN), CHEMBL6195509 (PROTEIN-PROTEIN INTERACTION), CHEMBL6195558 (PROTEIN-PROTEIN INTERACTION)

Drugs by curated mechanism of action (ChEMBL)

Drugs whose curated ChEMBL mechanism of action targets the ROR1 protein itself — single-protein targets only (drugs acting on a protein family or complex that merely includes it are excluded). Includes antibodies and oligonucleotides that bioactivity screening does not capture.

1 curated-mechanism drugs:

Drug	Modality	Max phase
CIRMTUZUMAB	Antibody	3

PharmGKB: 1 entry (CPIC guideline: no)

GtoPdb / IUPHAR curated pharmacology

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

Target class: catalytic receptor — Type VIII RTKs: ROR family

Binding affinities (BindingDB)

18 measured of 37 human assays (121 total across all organisms); most potent 18 below. Values come from heterogeneous assays and are not directly comparable.

Ligand	Measure	Value
CHEMBL5397768	KD	3 nM
CHEMBL5557876	KD	110 nM
CHEMBL5505848	KD	140 nM
CHEMBL5512504	KD	180 nM
CHEMBL5542135	KD	260 nM
CHEMBL5523378	KD	330 nM
CHEMBL5558585	KD	470 nM
CHEMBL5559233	KD	570 nM
CHEMBL5557671	KD	580 nM
CHEMBL5527914	KD	620 nM
CHEMBL5559545	KD	700 nM
CHEMBL5532423	KD	780 nM
CHEMBL5523614	KD	850 nM
CHEMBL5555958	KD	880 nM
CHEMBL5559095	KD	950 nM
CHEMBL5518147	KD	1810 nM
CHEMBL5523654	KD	2480 nM
CHEMBL5517821	KD	8250 nM

ChEMBL bioactivities

77 potent at pChembl≥5 of 78 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).

pChembl	Type	Value	Unit	Molecule
8.92	Kd	1.21	nM	CHEMBL6145153
8.80	Kd	1.57	nM	CHEMBL6150322
8.76	Kd	1.72	nM	CHEMBL6152828
8.66	IC50	2.2	nM	CHEMBL5428267
8.53	Kd	2.98	nM	CHEMBL6167251
8.52	Kd	3	nM	CHEMBL5397768
8.28	IC50	5.3	nM	CHEMBL5397895
8.28	IC50	5.2	nM	CHEMBL5399065
8.20	IC50	6.3	nM	CHEMBL5427174
8.14	IC50	7.2	nM	CHEMBL5437151
8.14	IC50	7.2	nM	CHEMBL5408107
8.07	IC50	8.6	nM	CHEMBL5410563
8.00	IC50	10	nM	CHEMBL5396415
8.00	IC50	9.9	nM	CHEMBL5424562
7.96	Kd	11	nM	CHEMBL5416192
7.91	IC50	12.3	nM	CHEMBL5422581
7.89	IC50	13	nM	CHEMBL5416192
7.84	IC50	14.4	nM	CHEMBL5427967
7.75	IC50	17.6	nM	CHEMBL6192385
7.66	Kd	22	nM	CHEMBL5411958
7.58	Kd	26.5	nM	CHEMBL6164860
7.54	Kd	28.5	nM	CHEMBL6103061
7.54	Kd	29	nM	CHEMBL6192385
7.52	Kd	30.4	nM	CHEMBL6192248
7.47	Kd	34	nM	CHEMBL5415252
7.40	Kd	39.8	nM	CHEMBL6142760
7.39	Kd	40.5	nM	CHEMBL6148650
7.18	IC50	66	nM	CHEMBL5411958
7.18	Kd	66.5	nM	CHEMBL6171958
7.10	Kd	80	nM	CHEMBL6190382
7.00	Kd	100	nM	CHEMBL5559059
6.96	Kd	110	nM	CHEMBL5557876
6.92	Kd	119	nM	CHEMBL6191357
6.91	Kd	124	nM	CHEMBL6134237
6.85	Kd	140	nM	CHEMBL5505848
6.83	Kd	147	nM	CHEMBL6134395
6.83	Kd	148	nM	CHEMBL6188793
6.82	Kd	152	nM	CHEMBL6147692
6.80	Kd	160	nM	CHEMBL5559363
6.75	Kd	180	nM	CHEMBL5512504
6.73	Kd	188	nM	CHEMBL6192589
6.70	Kd	200	nM	CHEMBL6191663
6.58	Kd	260	nM	CHEMBL5542135
6.58	Kd	261	nM	CHEMBL6146330
6.55	Kd	284	nM	CHEMBL6192897
6.50	Kd	313	nM	CHEMBL6193424
6.49	IC50	324.6	nM	CHEMBL5559059
6.48	Kd	330	nM	CHEMBL5523378
6.47	Kd	335	nM	CHEMBL6192640
6.46	Kd	348	nM	CHEMBL6193066

PubChem BioAssay actives

77 with measured affinity, of 250 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
(3S)-3-[[2-[[(2S)-2-[[(2S)-2-[[(2S,3R)-2-[[(2S)-2-[[(2S)-2-[[2-[[(2S)-1-[2-[[(2S)-2-[[(2S)-4-amino-2-[[(2S,3S)-2-amino-3-methylpentanoyl]amino]-4-oxobutanoyl]amino]-3-hydroxypropanoyl]amino]acetyl]pyrrolidine-2-carbonyl]amino]acetyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-3-hydroxypropanoyl]amino]-3-hydroxybutanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]acetyl]amino]-4-[[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]amino]-4-oxobutanoic acid	2213442: Binding affinity to N-terminal His/GST-tagged recombinant human ROR1 (453 to 783 residues) extracted from baculovirus infected insect cells assessed as dissociation constant by SPR analysis	kd	0.0012	uM
(3S)-3-[[2-[[(2S)-2-[[(2S)-2-[[(2S,3R)-2-[[(2S)-2-[[(2S)-2-[[2-[[(2S)-1-[(2S,3S)-2-[[(2S)-5-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-4-amino-2-[[(2S,3S)-2-[[(2S)-2-[[(2S)-2-amino-3-hydroxypropanoyl]amino]-3-carboxypropanoyl]amino]-3-methylpentanoyl]amino]-4-oxobutanoyl]amino]-3-carboxypropanoyl]amino]-5-carbamimidamidopentanoyl]amino]-5-oxopentanoyl]amino]-3-methylpentanoyl]pyrrolidine-2-carbonyl]amino]acetyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-3-hydroxypropanoyl]amino]-3-hydroxybutanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-3-(1H-indol-3-yl)propanoyl]amino]acetyl]amino]-4-[[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]amino]-4-oxobutanoic acid	2213442: Binding affinity to N-terminal His/GST-tagged recombinant human ROR1 (453 to 783 residues) extracted from baculovirus infected insect cells assessed as dissociation constant by SPR analysis	kd	0.0016	uM
18-[[(2S)-1-[2-[2-[2-[2-[2-[2-[[(2S)-6-amino-1-[[2-[[(2R)-1-[[2-[[(2S)-1-[[(2S)-1-[[(2S,3S)-1-[[(2S)-4-amino-1-[[(2S)-1-[[(2S)-1-[[(2S)-5-amino-1-[[(2S,3S)-1-[(2S)-2-[[2-[[(2S)-1-[[(2S)-1-[[(2S,3R)-1-[[(2S)-1-[[(2S)-1-[[2-[[(2S)-1-[[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]amino]-3-carboxy-1-oxopropan-2-yl]amino]-2-oxoethyl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxobutan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-2-oxoethyl]carbamoyl]pyrrolidin-1-yl]-3-methyl-1-oxopentan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-3-carboxy-1-oxopropan-2-yl]amino]-1,4-dioxobutan-2-yl]amino]-3-methyl-1-oxopentan-2-yl]amino]-3-carboxy-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-2-oxoethyl]amino]-3-[1-[6-[[1-[[5-(carbamoylamino)-1-[4-[[(2S,3S,4S,6R)-3-hydroxy-2-methyl-6-[[(1S,3S)-3,5,12-trihydroxy-3-(2-hydroxyacetyl)-10-methoxy-6,11-dioxo-2,4-dihydro-1H-tetracen-1-yl]oxy]oxan-4-yl]carbamoyloxymethyl]anilino]-1-oxopentan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-6-oxohexyl]-2,5-dioxopyrrolidin-3-yl]sulfanyl-1-oxopropan-2-yl]amino]-2-oxoethyl]amino]-1-oxohexan-2-yl]amino]-2-oxoethoxy]ethoxy]ethylamino]-2-oxoethoxy]ethoxy]ethylamino]-4-carboxy-1-oxobutan-2-yl]amino]-18-oxooctadecanoic acid	2213442: Binding affinity to N-terminal His/GST-tagged recombinant human ROR1 (453 to 783 residues) extracted from baculovirus infected insect cells assessed as dissociation constant by SPR analysis	kd	0.0017	uM
(3R,6S,9S,12S,15S,21S,24S,27S,30S,33S,36S)-N-(2-amino-2-oxoethyl)-9-benzyl-21-(hydroxymethyl)-12,24,33-tris[(4-hydroxyphenyl)methyl]-15,36-bis(1H-indol-3-ylmethyl)-10-methyl-6,30-bis(2-methylpropyl)-5,8,11,14,17,20,23,26,29,32,35,38-dodecaoxo-27-propan-2-yl-1-thia-4,7,10,13,16,19,22,25,28,31,34,37-dodecazacyclononatriacontane-3-carboxamide	2005027: Binding affinity to human ROR1 expressed in HEK293 cells by cell based assay	ic50	0.0022	uM
(3R,9S,12S,15S,21S,24S,30S,33S)-N-(2-amino-2-oxoethyl)-33-benzyl-9,12,15-tris(3-carbamimidamidopropyl)-24-(hydroxymethyl)-30-[(4-hydroxyphenyl)methyl]-28-methyl-5,8,11,14,17,20,23,26,29,32,35-undecaoxo-21-[(4-phenylphenyl)methyl]-1-thia-4,7,10,13,16,19,22,25,28,31,34-undecazacyclohexatriacontane-3-carboxamide	2005019: Binding affinity to full length human His-tagged ROR1 (937 residues ) assessed as dissociation constant by SPR analysis	kd	0.0030	uM
(3S)-3-[[2-[[(2S)-2-[[(2S)-2-[[(2S,3R)-2-[[(2S)-2-[[(2S)-2-[[2-[[(2S)-1-[(2S,3S)-2-[[(2S)-1-[(2S)-2-[[(2S)-2-[[(2S)-4-amino-2-[[(2S,3S)-2-[[(2S)-2-[[(2S)-2-amino-3-hydroxypropanoyl]amino]-3-carboxypropanoyl]amino]-3-methylpentanoyl]amino]-4-oxobutanoyl]amino]-3-carboxypropanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]pyrrolidine-2-carbonyl]amino]-3-methylpentanoyl]pyrrolidine-2-carbonyl]amino]acetyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-3-hydroxypropanoyl]amino]-3-hydroxybutanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]acetyl]amino]-4-[[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]amino]-4-oxobutanoic acid	2213442: Binding affinity to N-terminal His/GST-tagged recombinant human ROR1 (453 to 783 residues) extracted from baculovirus infected insect cells assessed as dissociation constant by SPR analysis	kd	0.0030	uM
(3S,6S,12R,15S,18S,21S,24S,30S,33S,36S,39S)-N-(2-amino-2-oxoethyl)-6,18-dibenzyl-30-(hydroxymethyl)-3,21,33-tris[(4-hydroxyphenyl)methyl]-24-(1H-indol-3-ylmethyl)-19-methyl-15-(2-methylpropyl)-2,5,8,14,17,20,23,26,29,32,35,38-dodecaoxo-36-propan-2-yl-10-thia-1,4,7,13,16,19,22,25,28,31,34,37-dodecazabicyclo[37.3.0]dotetracontane-12-carboxamide	2005027: Binding affinity to human ROR1 expressed in HEK293 cells by cell based assay	ic50	0.0052	uM
(3R,6S,9S,12S,15S,21S,24S,27S,30S,33S,36S)-N,21-bis(2-amino-2-oxoethyl)-9,36-dibenzyl-12-(4-hydroxyphenyl)-24,33-bis[(4-hydroxyphenyl)methyl]-15-(1H-indol-3-ylmethyl)-10-methyl-30-(2-methylpropyl)-5,8,11,14,17,20,23,26,29,32,35,38-dodecaoxo-6,27-di(propan-2-yl)-1-thia-4,7,10,13,16,19,22,25,28,31,34,37-dodecazacyclononatriacontane-3-carboxamide	2005027: Binding affinity to human ROR1 expressed in HEK293 cells by cell based assay	ic50	0.0053	uM
(3R,6S,9S,12S,15S,21S,24S,27S,30S,33S,36S)-N-(2-amino-2-oxoethyl)-9,36-dibenzyl-30-(3-carbamimidamidopropyl)-21-(hydroxymethyl)-12,24,33-tris[(4-hydroxyphenyl)methyl]-15-(1H-indol-3-ylmethyl)-10-methyl-6-(2-methylpropyl)-5,8,11,14,17,20,23,26,29,32,35,38-dodecaoxo-27-propan-2-yl-1-thia-4,7,10,13,16,19,22,25,28,31,34,37-dodecazacyclononatriacontane-3-carboxamide	2005027: Binding affinity to human ROR1 expressed in HEK293 cells by cell based assay	ic50	0.0063	uM
(3R,6S,9S,12S,15S,21S,24S,27S,30S,33S,36S)-9,36-dibenzyl-21-(hydroxymethyl)-12,24,33-tris[(4-hydroxyphenyl)methyl]-15-(1H-indol-3-ylmethyl)-10-methyl-6,30-bis(2-methylpropyl)-5,8,11,14,17,20,23,26,29,32,35,38-dodecaoxo-27-propan-2-yl-1-thia-4,7,10,13,16,19,22,25,28,31,34,37-dodecazacyclononatriacontane-3-carboxamide	2005027: Binding affinity to human ROR1 expressed in HEK293 cells by cell based assay	ic50	0.0072	uM
(3R,6S,9S,12S,15S,21S,24S,27S,30S,33S,36S)-N-(2-amino-2-oxoethyl)-21-(3-amino-3-oxopropyl)-9,36-dibenzyl-12,24,33-tris[(4-hydroxyphenyl)methyl]-15-(1H-indol-3-ylmethyl)-10-methyl-6,30-bis(2-methylpropyl)-5,8,11,14,17,20,23,26,29,32,35,38-dodecaoxo-27-propan-2-yl-1-thia-4,7,10,13,16,19,22,25,28,31,34,37-dodecazacyclononatriacontane-3-carboxamide	2005027: Binding affinity to human ROR1 expressed in HEK293 cells by cell based assay	ic50	0.0072	uM
(3R,6S,9S,12S,15S,21S,24S,27S,30S,33S,36S)-N-(2-amino-2-oxoethyl)-9,36-dibenzyl-12,21,24,33-tetrakis[(4-hydroxyphenyl)methyl]-15-(1H-indol-3-ylmethyl)-10-methyl-6,30-bis(2-methylpropyl)-5,8,11,14,17,20,23,26,29,32,35,38-dodecaoxo-27-propan-2-yl-1-thia-4,7,10,13,16,19,22,25,28,31,34,37-dodecazacyclononatriacontane-3-carboxamide	2005027: Binding affinity to human ROR1 expressed in HEK293 cells by cell based assay	ic50	0.0086	uM
3-[(5S,8S,11S,14S,17S,20S,26S,29S,32S,35S,38R)-38-[(2-amino-2-oxoethyl)carbamoyl]-5,32-dibenzyl-8,17,29-tris[(4-hydroxyphenyl)methyl]-26-(1H-indol-3-ylmethyl)-31-methyl-11,35-bis(2-methylpropyl)-3,6,9,12,15,18,21,24,27,30,33,36-dodecaoxo-14-propan-2-yl-1-thia-4,7,10,13,16,19,22,25,28,31,34,37-dodecazacyclononatriacont-20-yl]propanoic acid	2005027: Binding affinity to human ROR1 expressed in HEK293 cells by cell based assay	ic50	0.0099	uM
(3R,6S,9S,12S,15S,21S,24S,27S,30S,33S,36S)-30-(4-aminobutyl)-N-(2-amino-2-oxoethyl)-9,36-dibenzyl-21-(hydroxymethyl)-12,24,33-tris[(4-hydroxyphenyl)methyl]-15-(1H-indol-3-ylmethyl)-10-methyl-6-(2-methylpropyl)-5,8,11,14,17,20,23,26,29,32,35,38-dodecaoxo-27-propan-2-yl-1-thia-4,7,10,13,16,19,22,25,28,31,34,37-dodecazacyclononatriacontane-3-carboxamide	2005027: Binding affinity to human ROR1 expressed in HEK293 cells by cell based assay	ic50	0.0100	uM
(3R,6S,9S,12S,15S,21S,24S,27S,30S,33S,36S)-N-(2-amino-2-oxoethyl)-9,36-dibenzyl-21-(hydroxymethyl)-12,24,33-tris[(4-hydroxyphenyl)methyl]-15-(1H-indol-3-ylmethyl)-10-methyl-6,30-bis(2-methylpropyl)-5,8,11,14,17,20,23,26,29,32,35,38-dodecaoxo-27-propan-2-yl-1-thia-4,7,10,13,16,19,22,25,28,31,34,37-dodecazacyclononatriacontane-3-carboxamide	2005019: Binding affinity to full length human His-tagged ROR1 (937 residues ) assessed as dissociation constant by SPR analysis	kd	0.0110	uM
(3R,6S,9S,12S,15S,21S,24S,27S,30S,33S,36S)-N-(2-amino-2-oxoethyl)-9,36-dibenzyl-21-(hydroxymethyl)-12,24,33-tris[(4-hydroxyphenyl)methyl]-15-(1H-indol-3-ylmethyl)-10,27-dimethyl-6,30-bis(2-methylpropyl)-5,8,11,14,17,20,23,26,29,32,35,38-dodecaoxo-1-thia-4,7,10,13,16,19,22,25,28,31,34,37-dodecazacyclononatriacontane-3-carboxamide	2005027: Binding affinity to human ROR1 expressed in HEK293 cells by cell based assay	ic50	0.0123	uM
2-[(5S,8S,11S,14S,17S,20S,26S,29S,32S,35S,38R)-38-[(2-amino-2-oxoethyl)carbamoyl]-5,32-dibenzyl-8,17,29-tris[(4-hydroxyphenyl)methyl]-26-(1H-indol-3-ylmethyl)-31-methyl-11,35-bis(2-methylpropyl)-3,6,9,12,15,18,21,24,27,30,33,36-dodecaoxo-14-propan-2-yl-1-thia-4,7,10,13,16,19,22,25,28,31,34,37-dodecazacyclononatriacont-20-yl]acetic acid	2005027: Binding affinity to human ROR1 expressed in HEK293 cells by cell based assay	ic50	0.0144	uM
3-[[4-(4-cyclopropyloxyphenyl)pyrimidin-2-yl]amino]-N-[3-(6-methoxy-3-pyridinyl)-1-methylindol-6-yl]-4-methylbenzamide	2279841: Inhibition of N-terminal GST tagged human wild type ROR1 (452 to 753 residues) extracted from Escherichia coli using biotinylated TK-peptide as substrate incubated for 12 hrs by HTRF kinase assay	ic50	0.0176	uM
(3R,6S,9S,12S,15S,18S,24S,27S)-15-(2-amino-2-hydroxyethyl)-18,27-dibenzyl-9,24-bis[(4-hydroxyphenyl)methyl]-6-(1H-indol-3-ylmethyl)-16-methyl-12-(2-methylpropyl)-5,8,11,14,17,20,23,26,29-nonaoxo-1-thia-4,7,10,13,16,19,22,25,28-nonazacyclotriacontane-3-carboxamide	2005019: Binding affinity to full length human His-tagged ROR1 (937 residues ) assessed as dissociation constant by SPR analysis	kd	0.0220	uM
(3S)-3-[[(2S)-4-amino-2-[[(2S,3S)-2-[[(2S)-2-[[(2S)-2-amino-3-hydroxypropanoyl]amino]-3-carboxypropanoyl]amino]-3-methylpentanoyl]amino]-4-oxobutanoyl]amino]-4-[[(2S)-1-[[(2S)-5-amino-1-[[(2S,3S)-1-amino-3-methyl-1-oxopentan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-4-oxobutanoic acid	2213442: Binding affinity to N-terminal His/GST-tagged recombinant human ROR1 (453 to 783 residues) extracted from baculovirus infected insect cells assessed as dissociation constant by SPR analysis	kd	0.0265	uM
18-[[4-[2-[2-[2-[2-[2-[2-[[(2S)-6-amino-1-[[2-[[(2R)-1-[[2-[[(2S)-1-[[(2S)-1-[[(2S,3S)-1-[[(3S,6S)-1-amino-7-[[(2S)-1-[[(2S)-5-amino-1-[[(2S,3S)-1-[(2S)-2-[[2-[[(2S)-1-[[(2S)-1-[[(2S,3R)-1-[[(2S)-1-[[(2S)-1-[[2-[[(2S)-1-[[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]amino]-3-carboxy-1-oxopropan-2-yl]amino]-2-oxoethyl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxobutan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-2-oxoethyl]carbamoyl]pyrrolidin-1-yl]-3-methyl-1-oxopentan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-6-(carboxymethyl)-1,4,7-trioxoheptan-3-yl]amino]-3-methyl-1-oxopentan-2-yl]amino]-3-carboxy-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-2-oxoethyl]amino]-3-[1-[6-[[1-[[1-[4-[[5-(4-amino-2-oxopyrimidin-1-yl)-4,4-difluoro-3-hydroxyoxolan-2-yl]methoxy]anilino]-5-(carbamoylamino)-1-oxopentan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-6-oxohexyl]-2,5-dioxopyrrolidin-3-yl]sulfanyl-1-oxopropan-2-yl]amino]-2-oxoethyl]amino]-1-oxohexan-2-yl]amino]-2-oxoethoxy]ethoxy]ethylamino]-2-oxoethoxy]ethoxy]ethylamino]-1-carboxy-4-oxobutyl]amino]-18-oxooctadecanoic acid	2213442: Binding affinity to N-terminal His/GST-tagged recombinant human ROR1 (453 to 783 residues) extracted from baculovirus infected insect cells assessed as dissociation constant by SPR analysis	kd	0.0285	uM
N-[3-(6-ethoxy-3-pyridinyl)-1-methylindol-6-yl]-3-(2-imidazo[1,2-b]pyridazin-3-ylethynyl)-4-methylbenzamide	2279840: Binding affinity to N-terminal poly his tagged recombinant human ROR1 (Met453 to Asn783 residues) extracted from Baculovirus infected in Insect cell immobilized in CM5 sensor chip assessed as dissociation constant measured up to 120 secs by surface plasmon resonance assay	kd	0.0304	uM
(3R,6S,9S,12S,15S,21S,24S,27S,30S,33S,36S)-N-[2-[[2-[[2-[[(2R)-1-amino-6-[(3’,6’-dihydroxy-3-oxospiro[2-benzofuran-1,9’-xanthene]-5-carbonyl)amino]-1-oxohexan-2-yl]amino]-2-oxoethyl]amino]-2-oxoethyl]amino]-2-oxoethyl]-9,36-dibenzyl-21-(hydroxymethyl)-12,24,33-tris[(4-hydroxyphenyl)methyl]-15-(1H-indol-3-ylmethyl)-10-methyl-6,30-bis(2-methylpropyl)-5,8,11,14,17,20,23,26,29,32,35,38-dodecaoxo-27-propan-2-yl-1-thia-4,7,10,13,16,19,22,25,28,31,34,37-dodecazacyclononatriacontane-3-carboxamide	2005019: Binding affinity to full length human His-tagged ROR1 (937 residues ) assessed as dissociation constant by SPR analysis	kd	0.0340	uM
18-[[4-[2-[2-[2-[2-[2-[2-[[5-[3-[3-[(2R)-3-[[2-[[(2S)-1-[[(2S)-1-[[(2S,3S)-1-[[(2S)-4-amino-1-[[(2S)-1-[[(2S)-1-[[(2S)-5-amino-1-[[(2S,3S)-1-[(2S)-2-[[2-[[(2S)-1-[[(2S)-1-[[(2S,3R)-1-[[(2S)-1-[[(2S)-1-[[2-[[(2S)-1-[[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]amino]-3-carboxy-1-oxopropan-2-yl]amino]-2-oxoethyl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxobutan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-2-oxoethyl]carbamoyl]pyrrolidin-1-yl]-3-methyl-1-oxopentan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-3-carboxy-1-oxopropan-2-yl]amino]-1,4-dioxobutan-2-yl]amino]-3-methyl-1-oxopentan-2-yl]amino]-3-carboxy-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-2-oxoethyl]amino]-2-[[2-[[(2S)-6-amino-2-[[5-[[5-(4-amino-2-oxopyrimidin-1-yl)-4,4-difluoro-3-hydroxyoxolan-2-yl]methoxy]-5-oxopentanoyl]amino]hexanoyl]amino]acetyl]amino]-3-oxopropyl]sulfanyl-2,5-dioxopyrrolidin-1-yl]propanoylamino]-1-carboxypentyl]amino]-2-oxoethoxy]ethoxy]ethylamino]-2-oxoethoxy]ethoxy]ethylamino]-1-carboxy-4-oxobutyl]amino]-18-oxooctadecanoic acid	2213442: Binding affinity to N-terminal His/GST-tagged recombinant human ROR1 (453 to 783 residues) extracted from baculovirus infected insect cells assessed as dissociation constant by SPR analysis	kd	0.0398	uM
(3S)-3-[[(2S)-4-amino-2-[[(2S,3S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-1-[2-[[(2S)-2-[[(2S)-4-amino-2-[[(2S,3S)-2-amino-3-methylpentanoyl]amino]-4-oxobutanoyl]amino]-3-hydroxypropanoyl]amino]acetyl]pyrrolidine-2-carbonyl]amino]-3-hydroxypropanoyl]amino]-3-carboxypropanoyl]amino]-3-methylpentanoyl]amino]-4-oxobutanoyl]amino]-4-[[(2S)-1-[(2S)-2-[[(2S,3S)-1-amino-3-methyl-1-oxopentan-2-yl]carbamoyl]pyrrolidin-1-yl]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-4-oxobutanoic acid	2213442: Binding affinity to N-terminal His/GST-tagged recombinant human ROR1 (453 to 783 residues) extracted from baculovirus infected insect cells assessed as dissociation constant by SPR analysis	kd	0.0405	uM
18-[[4-[2-[2-[2-[2-[2-[2-[[5-[3-[3-[(2R)-3-[[2-[[(2S)-1-[[(2S)-1-[[(2S,3S)-1-[[(2S)-4-amino-1-[[(2S)-1-[[(2S)-1-[[(2S)-5-amino-1-[[(2S,3S)-1-[(2S)-2-[[2-[[(2S)-1-[[(2S)-1-[[(2S,3R)-1-[[(2S)-1-[[(2S)-1-[[2-[[(2S)-1-[[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]amino]-3-carboxy-1-oxopropan-2-yl]amino]-2-oxoethyl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxobutan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-2-oxoethyl]carbamoyl]pyrrolidin-1-yl]-3-methyl-1-oxopentan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-3-carboxy-1-oxopropan-2-yl]amino]-1,4-dioxobutan-2-yl]amino]-3-methyl-1-oxopentan-2-yl]amino]-3-carboxy-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-2-oxoethyl]amino]-2-[[2-[[(2S)-6-amino-2-[[5-[2-[(2S,4S)-4-[(2R,4S,5S,6S)-4-amino-5-hydroxy-6-methyloxan-2-yl]oxy-2,5,12-trihydroxy-7-methoxy-6,11-dioxo-3,4-dihydro-1H-tetracen-2-yl]-2-oxoethoxy]-5-oxopentanoyl]amino]hexanoyl]amino]acetyl]amino]-3-oxopropyl]sulfanyl-2,5-dioxopyrrolidin-1-yl]propanoylamino]-1-carboxypentyl]amino]-2-oxoethoxy]ethoxy]ethylamino]-2-oxoethoxy]ethoxy]ethylamino]-1-carboxy-4-oxobutyl]amino]-18-oxooctadecanoic acid	2213442: Binding affinity to N-terminal His/GST-tagged recombinant human ROR1 (453 to 783 residues) extracted from baculovirus infected insect cells assessed as dissociation constant by SPR analysis	kd	0.0665	uM
N-[3-(6-ethoxy-3-pyridinyl)-1-methylindol-6-yl]-4-methyl-3-[[4-[4-(trifluoromethyl)phenyl]pyrimidin-2-yl]amino]benzamide	2279840: Binding affinity to N-terminal poly his tagged recombinant human ROR1 (Met453 to Asn783 residues) extracted from Baculovirus infected in Insect cell immobilized in CM5 sensor chip assessed as dissociation constant measured up to 120 secs by surface plasmon resonance assay	kd	0.0800	uM
N-[3-[4-(methoxymethoxy)phenyl]-1-methylindol-6-yl]-4-methyl-3-[2-(1H-pyrazolo[3,4-b]pyridin-4-yl)ethynyl]benzamide	2066076: Binding affinity to ROR1 kinase domain (453 to 783 residues) (unknown origin) assessed as dissociation constant by SPR analysis	kd	0.1000	uM
3-[2-(6-acetamido-3-pyridinyl)ethynyl]-N-[3-[4-(methoxymethoxy)phenyl]-1-methylindol-6-yl]-4-methylbenzamide	2066076: Binding affinity to ROR1 kinase domain (453 to 783 residues) (unknown origin) assessed as dissociation constant by SPR analysis	kd	0.1100	uM
N-[3-(6-ethoxy-3-pyridinyl)-1-methylindol-6-yl]-4-methyl-3-[[4-(4-methylphenyl)pyrimidin-2-yl]amino]benzamide	2279840: Binding affinity to N-terminal poly his tagged recombinant human ROR1 (Met453 to Asn783 residues) extracted from Baculovirus infected in Insect cell immobilized in CM5 sensor chip assessed as dissociation constant measured up to 120 secs by surface plasmon resonance assay	kd	0.1190	uM
18-[[4-[2-[2-[2-[2-[2-[2-[[(2S)-6-amino-1-[[2-[[(2R)-1-[[2-[[(2S)-1-[[(2S)-1-[[(2S,3S)-1-[[(2S)-4-amino-1-[[(2S)-1-[[(2S)-1-[[(2S)-5-amino-1-[[(2S,3S)-1-[(2S)-2-[[2-[[(2S)-1-[[(2S)-1-[[(2S,3R)-1-[[(2S)-1-[[(2S)-1-[[2-[[(2S)-1-[[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]amino]-3-carboxy-1-oxopropan-2-yl]amino]-2-oxoethyl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxobutan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-2-oxoethyl]carbamoyl]pyrrolidin-1-yl]-3-methyl-1-oxopentan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-3-carboxy-1-oxopropan-2-yl]amino]-1,4-dioxobutan-2-yl]amino]-3-methyl-1-oxopentan-2-yl]amino]-3-carboxy-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-2-oxoethyl]amino]-3-[1-[6-[[5-(4-amino-2-oxopyrimidin-1-yl)-4,4-difluoro-3-hydroxyoxolan-2-yl]methoxy]-6-oxohexyl]-2,5-dioxopyrrolidin-3-yl]sulfanyl-1-oxopropan-2-yl]amino]-2-oxoethyl]amino]-1-oxohexan-2-yl]amino]-2-oxoethoxy]ethoxy]ethylamino]-2-oxoethoxy]ethoxy]ethylamino]-1-carboxy-4-oxobutyl]amino]-18-oxooctadecanoic acid	2213442: Binding affinity to N-terminal His/GST-tagged recombinant human ROR1 (453 to 783 residues) extracted from baculovirus infected insect cells assessed as dissociation constant by SPR analysis	kd	0.1240	uM
3-(2-imidazo[1,2-b]pyridazin-3-ylethynyl)-4-methyl-N-[1-methyl-3-[4-[(2-methylpropan-2-yl)oxy]phenyl]indol-6-yl]benzamide	2066076: Binding affinity to ROR1 kinase domain (453 to 783 residues) (unknown origin) assessed as dissociation constant by SPR analysis	kd	0.1400	uM
(3S)-3-[[2-[[(2S)-2-[[(2S)-2-[[(2S,3R)-2-[[(2S)-2-[[(2S)-2-[(2-aminoacetyl)amino]-3-(4-hydroxyphenyl)propanoyl]amino]-3-hydroxypropanoyl]amino]-3-hydroxybutanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-3-(1H-indol-3-yl)propanoyl]amino]acetyl]amino]-4-[[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]amino]-4-oxobutanoic acid	2213442: Binding affinity to N-terminal His/GST-tagged recombinant human ROR1 (453 to 783 residues) extracted from baculovirus infected insect cells assessed as dissociation constant by SPR analysis	kd	0.1470	uM
N-[3-(6-chloro-3-pyridinyl)-1-methylindol-6-yl]-3-[[4-(4-cyclopropyloxyphenyl)pyrimidin-2-yl]amino]-4-methylbenzamide	2279840: Binding affinity to N-terminal poly his tagged recombinant human ROR1 (Met453 to Asn783 residues) extracted from Baculovirus infected in Insect cell immobilized in CM5 sensor chip assessed as dissociation constant measured up to 120 secs by surface plasmon resonance assay	kd	0.1480	uM
18-[[(2S)-1-[2-[2-[2-[2-[2-[2-[[(2S)-6-amino-1-[[2-[[(2R)-1-[[2-[[(2S)-1-[[(2S)-1-[[(2S,3S)-1-[[(2S)-4-amino-1-[[(2S)-1-[[(2S)-1-[[(2S)-5-amino-1-[[(2S,3S)-1-[(2S)-2-[[2-[[(2S)-1-[[(2S)-1-[[(2S,3R)-1-[[(2S)-1-[[(2S)-1-[[2-[[(2S)-1-[[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]amino]-3-carboxy-1-oxopropan-2-yl]amino]-2-oxoethyl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxobutan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-2-oxoethyl]carbamoyl]pyrrolidin-1-yl]-3-methyl-1-oxopentan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-3-carboxy-1-oxopropan-2-yl]amino]-1,4-dioxobutan-2-yl]amino]-3-methyl-1-oxopentan-2-yl]amino]-3-carboxy-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-2-oxoethyl]amino]-3-[1-[6-[[(2S,3S,4S,6R)-3-hydroxy-2-methyl-6-[[(1S,3S)-3,5,12-trihydroxy-3-(2-hydroxyacetyl)-10-methoxy-6,11-dioxo-2,4-dihydro-1H-tetracen-1-yl]oxy]oxan-4-yl]amino]-6-oxohexyl]-2,5-dioxopyrrolidin-3-yl]sulfanyl-1-oxopropan-2-yl]amino]-2-oxoethyl]amino]-1-oxohexan-2-yl]amino]-2-oxoethoxy]ethoxy]ethylamino]-2-oxoethoxy]ethoxy]ethylamino]-4-carboxy-1-oxobutan-2-yl]amino]-18-oxooctadecanoic acid	2213442: Binding affinity to N-terminal His/GST-tagged recombinant human ROR1 (453 to 783 residues) extracted from baculovirus infected insect cells assessed as dissociation constant by SPR analysis	kd	0.1520	uM
N-[3-[4-(methoxymethoxy)phenyl]-1-methylindol-6-yl]-4-methyl-3-[2-(1H-pyrazolo[5,4-b]pyridin-5-yl)ethynyl]benzamide	2066076: Binding affinity to ROR1 kinase domain (453 to 783 residues) (unknown origin) assessed as dissociation constant by SPR analysis	kd	0.1600	uM
N-[3-(6-fluoro-3-pyridinyl)-1-methylindol-6-yl]-3-(2-imidazo[1,2-b]pyridazin-3-ylethynyl)-4-methylbenzamide	2066076: Binding affinity to ROR1 kinase domain (453 to 783 residues) (unknown origin) assessed as dissociation constant by SPR analysis	kd	0.1800	uM
3-[[4-(4-chlorophenyl)pyrimidin-2-yl]amino]-N-[3-(6-ethoxy-3-pyridinyl)-1-methylindol-6-yl]-4-methylbenzamide	2279840: Binding affinity to N-terminal poly his tagged recombinant human ROR1 (Met453 to Asn783 residues) extracted from Baculovirus infected in Insect cell immobilized in CM5 sensor chip assessed as dissociation constant measured up to 120 secs by surface plasmon resonance assay	kd	0.1880	uM
N-[3-(6-ethoxy-3-pyridinyl)-1-methylindol-6-yl]-3-[[4-(4-ethylphenyl)pyrimidin-2-yl]amino]-4-methylbenzamide	2279840: Binding affinity to N-terminal poly his tagged recombinant human ROR1 (Met453 to Asn783 residues) extracted from Baculovirus infected in Insect cell immobilized in CM5 sensor chip assessed as dissociation constant measured up to 120 secs by surface plasmon resonance assay	kd	0.2000	uM
3-(2-imidazo[1,2-b]pyridazin-3-ylethynyl)-N-[3-[4-(methoxymethoxy)phenyl]-1-methylindol-6-yl]-4-methylbenzamide	2066076: Binding affinity to ROR1 kinase domain (453 to 783 residues) (unknown origin) assessed as dissociation constant by SPR analysis	kd	0.2600	uM
(3S)-3-[[2-[[(2S)-2-[[(2S)-2-[[(2S,3R)-2-[[(2S)-2-[[(2S)-2-[[2-[[(2S)-1-[(2S,3S)-2-[[(2S)-5-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-4-amino-2-[[(2S,3S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-1-[2-[[(2S)-2-[[(2S)-4-amino-2-[[(2S,3S)-2-amino-3-methylpentanoyl]amino]-4-oxobutanoyl]amino]-3-hydroxypropanoyl]amino]acetyl]pyrrolidine-2-carbonyl]amino]-3-hydroxypropanoyl]amino]-3-carboxypropanoyl]amino]-3-methylpentanoyl]amino]-4-oxobutanoyl]amino]-3-carboxypropanoyl]amino]-5-carbamimidamidopentanoyl]amino]-5-oxopentanoyl]amino]-3-methylpentanoyl]pyrrolidine-2-carbonyl]amino]acetyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-3-hydroxypropanoyl]amino]-3-hydroxybutanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-3-(1H-indol-3-yl)propanoyl]amino]acetyl]amino]-4-[[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]amino]-4-oxobutanoic acid	2213442: Binding affinity to N-terminal His/GST-tagged recombinant human ROR1 (453 to 783 residues) extracted from baculovirus infected insect cells assessed as dissociation constant by SPR analysis	kd	0.2610	uM
3-[[4-(3,4-difluorophenyl)pyrimidin-2-yl]amino]-N-[3-(6-ethoxy-3-pyridinyl)-1-methylindol-6-yl]-4-methylbenzamide	2279840: Binding affinity to N-terminal poly his tagged recombinant human ROR1 (Met453 to Asn783 residues) extracted from Baculovirus infected in Insect cell immobilized in CM5 sensor chip assessed as dissociation constant measured up to 120 secs by surface plasmon resonance assay	kd	0.2840	uM
3-[[4-(4-cyclopropyloxyphenyl)pyrimidin-2-yl]amino]-N-[3-(6-fluoro-3-pyridinyl)-1-methylindol-6-yl]-4-methylbenzamide	2279840: Binding affinity to N-terminal poly his tagged recombinant human ROR1 (Met453 to Asn783 residues) extracted from Baculovirus infected in Insect cell immobilized in CM5 sensor chip assessed as dissociation constant measured up to 120 secs by surface plasmon resonance assay	kd	0.3130	uM
3-(2-imidazo[1,2-b]pyridazin-3-ylethynyl)-4-methyl-N-[1-methyl-3-[4-(4-methylpiperazin-1-yl)phenyl]indol-6-yl]benzamide	2066076: Binding affinity to ROR1 kinase domain (453 to 783 residues) (unknown origin) assessed as dissociation constant by SPR analysis	kd	0.3300	uM
N-[3-(6-ethoxy-3-pyridinyl)-1-methylindol-6-yl]-3-[[4-(3-fluorophenyl)pyrimidin-2-yl]amino]-4-methylbenzamide	2279840: Binding affinity to N-terminal poly his tagged recombinant human ROR1 (Met453 to Asn783 residues) extracted from Baculovirus infected in Insect cell immobilized in CM5 sensor chip assessed as dissociation constant measured up to 120 secs by surface plasmon resonance assay	kd	0.3350	uM
N-[3-(6-ethoxy-3-pyridinyl)-1-methylindol-6-yl]-4-methyl-3-[[4-(3-methylphenyl)pyrimidin-2-yl]amino]benzamide	2279840: Binding affinity to N-terminal poly his tagged recombinant human ROR1 (Met453 to Asn783 residues) extracted from Baculovirus infected in Insect cell immobilized in CM5 sensor chip assessed as dissociation constant measured up to 120 secs by surface plasmon resonance assay	kd	0.3480	uM
3-[[4-(4-cyclopropyloxyphenyl)pyrimidin-2-yl]amino]-N-[3-(6-ethoxy-3-pyridinyl)-1-methylindol-6-yl]-4-methylbenzamide	2279840: Binding affinity to N-terminal poly his tagged recombinant human ROR1 (Met453 to Asn783 residues) extracted from Baculovirus infected in Insect cell immobilized in CM5 sensor chip assessed as dissociation constant measured up to 120 secs by surface plasmon resonance assay	kd	0.3790	uM
N-[3-(6-ethoxy-3-pyridinyl)-1-methylindol-6-yl]-4-methyl-3-[(4-phenyl-1,3,5-triazin-2-yl)amino]benzamide	2279840: Binding affinity to N-terminal poly his tagged recombinant human ROR1 (Met453 to Asn783 residues) extracted from Baculovirus infected in Insect cell immobilized in CM5 sensor chip assessed as dissociation constant measured up to 120 secs by surface plasmon resonance assay	kd	0.4610	uM
N-[3-(6-ethoxy-3-pyridinyl)-1-methylindol-6-yl]-4-methyl-3-[(4-phenylpyrimidin-2-yl)amino]benzamide	2279840: Binding affinity to N-terminal poly his tagged recombinant human ROR1 (Met453 to Asn783 residues) extracted from Baculovirus infected in Insect cell immobilized in CM5 sensor chip assessed as dissociation constant measured up to 120 secs by surface plasmon resonance assay	kd	0.4690	uM
(2R)-5,7-bis(methoxymethoxy)-2-(4-methoxyphenyl)-2,3-dihydrochromen-4-one	2066205: Binding affinity to N-terminal His-tagged ROR1 frizzled domain (61 to 393 residues) (unknown origin) transfected in baculovirus infected High Five cells assessed as dissociation constant by SPR analysis	kd	0.4700	uM

CTD chemical–gene interactions

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

Chemical	Actions (top 5)	PubMed papers
Valproic Acid	affects cotreatment, increases expression, decreases expression, decreases methylation	6
Benzo(a)pyrene	decreases expression, increases methylation	4
trichostatin A	affects cotreatment, increases expression	3
Air Pollutants	increases abundance, increases expression, decreases expression	3
Dexamethasone	affects cotreatment, increases expression	3
Formaldehyde	decreases expression	3
Particulate Matter	increases abundance, increases expression, decreases expression	3
sodium arsenite	decreases expression, increases abundance, increases expression	2
entinostat	affects cotreatment, increases expression	2
Panobinostat	affects cotreatment, increases expression	2
Arsenic	affects methylation, increases abundance, increases expression	2
Estradiol	affects expression, affects cotreatment, increases expression	2
Phenylmercuric Acetate	affects cotreatment, decreases expression	2
Tetrachlorodibenzodioxin	increases expression	2
1-Methyl-3-isobutylxanthine	affects cotreatment, increases expression	2
8-Bromo Cyclic Adenosine Monophosphate	affects cotreatment, increases expression, decreases expression	2
aristolochic acid I	decreases expression	1
bisphenol F	affects cotreatment, increases expression	1
methylmercuric chloride	decreases expression	1
bisphenol A	affects cotreatment, increases expression	1
terbufos	increases methylation	1
tris(1,3-dichloro-2-propyl)phosphate	decreases expression, affects expression	1
butyraldehyde	decreases expression	1
versicolorin A	decreases expression	1
nickel sulfate	decreases expression	1
cupric oxide	decreases expression	1
hydroquinone	decreases expression	1
N,N,N’,N’-tetrakis(2-pyridylmethyl)ethylenediamine	increases expression	1
cylindrospermopsin	decreases expression	1
CGP 52608	affects binding, increases reaction	1

ChEMBL screening assays

40 unique, capped per target: 40 binding

Representative assays (with source publication via chembl_document):

Assay ID	Type	Description	Source paper
CHEMBL5358430	Binding	Binding affinity to full length human His-tagged ROR1 (937 residues ) assessed as dissociation constant by SPR analysis	Exploration of macrocyclic peptide binders to the extracellular CRD domain of human receptor tyrosine kinase-like orphan receptor 1 (ROR1). — *Bioorg Med Chem Lett*

Cellosaurus cell lines

11 cell lines: 8 cancer cell line, 2 transformed cell line, 1 spontaneously immortalized cell line

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

Cellosaurus	Name	Category	Sex
CVCL_B9R7	Abcam A-549 ROR1 KO	Cancer cell line	Male
CVCL_D7ZL	Ubigene A-549 ROR1 KO	Cancer cell line	Male
CVCL_E0MX	Ubigene HeLa ROR1 KO	Cancer cell line	Female
CVCL_E6RL	Genomeditech CHO-K1 H_ROR1	Spontaneously immortalized cell line	Female
CVCL_E6UT	Genomeditech HEK-293 H_ROR1	Transformed cell line	Female
CVCL_E8II	Jurkat-NFAT-Luc2-ROR1-KO-CD16-V158 clone 2A6	Cancer cell line	Male
CVCL_F4QI	HyCyte Caov-3 stable cell line for hROR1 overexpression	Cancer cell line	Female
CVCL_TJ53	HAP1 ROR1 (-) 1	Cancer cell line	Male
CVCL_TJ54	HAP1 ROR1 (-) 2	Cancer cell line	Male
CVCL_TJ55	HAP1 ROR1 (-) 3	Cancer cell line	Male

Clinical trials (associated diseases)

Via MONDO — disease-level, not drug-specific.

1 trials:

NCT	Phase	Status	Title
NCT01802190	Not specified	TERMINATED	Prevalence of POU4F3 and SLC17A8 Mutations

Predicted chemistry — Sugi Predict

The predicted patent-compound landscape for ROR1 across ~30M SureChEMBL compounds — explore on Sugi Predict.