chlorambucil profile

Chlorambucil is an alkylating agent used in the treatment of chronic lymphocytic leukemia (CLL), non-Hodgkin's lymphoma, and multiple myeloma. It was first synthesized in the 1950s and has been used clinically for decades. The synthesis involves a multi-step process starting with phenylalanine. Chlorambucil exerts its effects by binding to DNA and preventing its replication, thereby inhibiting the growth of cancer cells. It has also been studied for its potential use in other conditions, including autoimmune diseases and organ transplantation. Its importance lies in its ability to effectively treat certain types of cancers while having a manageable toxicity profile. It is still studied today to optimize its use and explore new applications in cancer treatment.'

Chlorambucil: A nitrogen mustard alkylating agent used as antineoplastic for chronic lymphocytic leukemia, Hodgkin's disease, and others. Although it is less toxic than most other nitrogen mustards, it has been listed as a known carcinogen in the Fourth Annual Report on Carcinogens (NTP 85-002, 1985). (Merck Index, 11th ed) [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

chlorambucil : A monocarboxylic acid that is butanoic acid substituted at position 4 by a 4-[bis(2-chloroethyl)amino]phenyl group. A chemotherapy drug that can be used in combination with the antibody obinutuzumab for the treatment of chronic lymphocytic leukemia. [Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

ID Source	ID
PubMed CID	2708
CHEMBL ID	515
CHEBI ID	28830
SCHEMBL ID	4308
MeSH ID	M0004118

Synonym
MLS001076130
AB00051938-14
BRD-K29458283-001-05-9
chlorbutin
elcoril
4-[p-bis(.beta.-chloroethyl)aminophenyl]butyric acid
ambochlorin
.gamma.-[p-di(2-chloroethyl)aminophenyl]butyric acid
chlorobutine
linfolizin
4-[bis(2-chloroethyl)amino]phenylbutyric acid
linfolysin
cb 1348
nsc-3088
chlorbutine
phenylbutyric acid nitrogen mustard
amboclorin
.gamma.-[p-bis(2-chloroethyl)aminophenyl]butyric acid
p-(n,n-di-2-chloroethyl)aminophenyl butyric acid
n,n-di-2-chloroethyl-.gamma.-p-aminophenylbutyric acid
4[p-bis(.beta.-chloroethyl)aminophenyl]butyric acid
chloraminophene
chloroambucil
p-n,n-di-(.beta.-chloroethyl)aminophenyl butyric acid
4-[bis(2-chloroethyl)amino]benzenebutanoic acid
ecloril
benzenebutanoic acid, 4-[bis(2-chloroethyl)amino]-
nsc3088
leukoran
nci-c03485
wln: qv3r dn2g2g
butyric acid, 4-(p-bis(2-chloroethyl)aminophenyl)-
.gamma.-(p-bis(2-chloroethyl)aminophenyl)butyric acid
nsc 3088
chlorobutin
butyric acid, 4-[p-[bis(2-chloroethyl)amino]phenyl]-
4-[p-[bis(2-chloroethyl)amino]phenyl]butyric acid
leukeran
leukersan
chloraminophen
cb l348
butyric acid, 4-(p-[bis(2-chloroethyl)amino]phenyl)-
smr000058372
DIVK1C_000688
KBIO1_000688
NCI60_002639
n,n-di-2-chloroethyl-gamma-p-aminophenylbutyric acid
gamma-[p-di(2-chloroethyl)aminophenyl]butyric acid
CHEBI:28830 ,
4-(p-bis(beta-chloroethyl)aminophenyl)butyric acid
4-{4-[bis(2-chloroethyl)amino]phenyl}butanoic acid
EU-0100227
SPECTRUM_000118
NCGC00015199-02
cas-305-03-3
NCGC00015199-01
lopac-c-0253
SPECTRUM5_000677
BPBIO1_001208
NCGC00023250-10
4-[4-[bis(2-chloroethyl)amino]phenyl]butanoic acid
BSPBIO_001971
PRESTWICK2_001079
IDI1_000688
BSPBIO_001098
LOPAC0_000227
NCGC00023250-03
AB00051938
rcra waste no. u035
phenylbuttersaeure-lost [german]
para-(di(2-chloroethyl)aminophenyl)butyric acid
p-n,n-di-(beta-chloroethyl)aminophenyl butyric acid
kyselina 4-(n,n-bis-(2-chlorethyl)-p-aminofenyl)maselna [czech]
ccris 126
chlorambucilum [inn-latin]
butyric acid, 4-(p-(bis(2-chloroethyl)amino)phenyl)
benzenebutanoic acid, 4-(bis(2-chloroethyl)amino)-
4-(bis(2-chloroethyl)amino)benzenebutanoic acid
butanoic acid, 4-(bis(2-chloroethyl)amino) benzene
n,n-di-2-chloroethyl-gamma-para-aminophenyl butyric acid
gamma-(p-di(2-chloroethyl)aminophenyl)butyric acid
para-n,n-di(beta-chloroethyl)aminophenyl butyric acid
rcra waste number u035
gamma-(p-bis(2-chloroethyl)aminophenyl)butyricacid
p-(n,n-di-2-chlorethylaminophenyl)butyric acid
lympholysin
ai3-26083
clorambucile [dcit]
chlorbutinum
c14h19cl2no2
elcorin
einecs 206-162-0
chloorambucol
brn 0999011
4-(p-(bis(2-chloroethyl)amino)phenyl)butyric acid
cb-1348 ,
gamma-(p-bis(2-chloroethyl)aminophenyl)butyric acid
4-(bis(2-chloroethyl)amino)phenylbutyric acid
hsdb 3026
clorambucilo [inn-spanish]
chlorambucil
305-03-3
C06900
DB00291
NCGC00023250-08
D00266
chlorambucil (jan/usp/inn)
leukeran (tn)
NCGC00023250-05
NCGC00023250-06
NCGC00023250-00
NCGC00023250-07
MLS000028443 ,
KBIO3_001191
KBIO2_005694
KBIO2_000558
KBIOGR_000766
KBIO2_003126
KBIOSS_000558
PRESTWICK1_001079
NINDS_000688
SPECTRUM3_000336
SPBIO_000249
SPECTRUM2_000065
PRESTWICK0_001079
SPECTRUM4_000273
SPBIO_002999
SPECTRUM1500171
PRESTWICK3_001079
NCGC00015199-03
NCGC00023250-09
NCGC00023250-04
NCGC00015199-07
HMS2090M19
4-[bis(2-chloroethyl)amino]benzenebutyric acid
C 0253
HMS2091A22
NCGC00015199-14
CHEMBL515 ,
chlorambucilum
nci-3088
HMS502C10
HMS1920M15
HMS1571G20
bdbm50003677
NCGC00015199-08
4-(4-(bis(2-chloroethyl)amino)phenyl)butanoic acid
A18607
HMS2098G20
HMS3259I10
clorambucile
phenylbuttersaeure-lost
18d0sl7309 ,
unii-18d0sl7309
clorambucilo
kyselina 4-(n,n-bis-(2-chlorethyl)-p-aminofenyl)maselna
chlorambucil [usp:inn:ban]
4-14-00-01715 (beilstein handbook reference)
dtxsid7020263 ,
NCGC00256464-01
tox21_302996
dtxcid30263
NCGC00258941-01
tox21_201390
AKOS024319346
pharmakon1600-01500171
nsc756674
nsc-756674
tox21_110096
chlocambucil
leukeran tablets
4-(4-[bis(2-chloroethyl)amino]phenyl)butyric acid
HMS2235A04
S4288
CCG-39872
NCGC00015199-09
NCGC00015199-12
NCGC00015199-17
NCGC00015199-05
NCGC00015199-11
NCGC00015199-06
NCGC00015199-16
NCGC00015199-10
NCGC00015199-15
NCGC00015199-13
NCGC00015199-04
FT-0617365
NCGC00015199-19
LP00227
chlorambucil [mi]
chlorambucil [mart.]
chlorambucil [inn]
chlorambucil [ep monograph]
chlorambucil [jan]
chlorambucil [iarc]
chlorambucil [hsdb]
chlorambucil [orange book]
chlorambucil [usp monograph]
chlorambucil [vandf]
chlorambucil [who-ip]
chlorambucil [who-dd]
chlorambucilum [who-ip latin]
chlorambucil [usp-rs]
EPITOPE ID:139977
HMS3372O04
gtpl7143
HY-13593
CS-3118
NC00555
SCHEMBL4308
NCGC00015199-20
tox21_110096_1
AB00051938-15
4-[4-(n,n-bis(2-chloroethyl)-amino]phenyl)butanoic acid
W-106940
.gamma.-(p-bis(2-chloroethyl)aminophenyl)butyricacid
4-(p-bis(.beta.-chloroethyl)aminophenyl)butyric acid
4-(4-[bis(2-chloroethyl)amino]phenyl)butanoic acid #
butanoic acid, 4-(bis(2-chloroethyl)amino)benzene-
C2939
4-[4-[bis(2-chloroethyl)amino]phenyl]butyric acid
OPERA_ID_51
AB00051938_16
mfcd00021783
chlorambucil, european pharmacopoeia (ep) reference standard
wr-139013
GS-6200
sr-01000000062
SR-01000000062-2
chlorambucil, united states pharmacopeia (usp) reference standard
chlorambucil, purum, >=98.0% (t)
HMS3652P08
EN300-123640
chlorambucil for system suitability, european pharmacopoeia (ep) reference standard
SR-01000000062-7
SR-01000000062-4
SBI-0050215.P004
SW197258-4
chlorambucilddv
Q415939
Z1552153009
BP-24028
4-(4-(bis(2-chloroethyl)amino)
phenyl)butanoic acid
chlorambucil,(s)
BCP28394
BRD-K29458283-001-17-4
BRD-K29458283-001-04-2
A14252
SDCCGSBI-0050215.P005
AMY33445
H10484
4-(4-(bis(2-chloroethyl)amino)phenyl)butanoicacid
chlorambucil for system suitability
chlorambucil with impurity g
SY031075

Excerpt	Reference	Relevance
"Chlorambucil is an exception."	( Structure-activity relationships in antitumor aniline mustards. Hansch, C; Leo, A; Panthananickal, A, 1978)	0.98
"Chlorambucil is a nitrogen mustard-based DNA alkylating drug, which is widely used as a front-line treatment of chronic lymphocytic leukaemia (CLL). "	( Hybrid inhibitors of DNA and HDACs remarkably enhance cytotoxicity in leukaemia cells. Liu, KH; Park, SY; Seo, YH; Song, Y; Wu, Z, 2020)	2
"Chlorambucil is an anticancer drug that is still commonly used as a primary treatment in treating some cancers, but it can cause side effects."	( Chlorambucil-Chitosan Nano-Conjugate: An Efficient Agent Against Breast Cancer Targeted Therapy. Ali, V; Ardestani, MS; Ebrahimi, SES; Farzaneh, J; Hadadian, S; Hamedani, MP; Hejazinia, H; Khalatbari, F; Monavvari, F; Seyedhamzeh, M; Shayegh, A; Zarazvand, F; Zonoubi, N, 2021)	2.79
"Chlorambucil is an anticancer drug with alkylating and immunosuppressive activities. "	( Chlorambucil and ascorbic acid-mediated anticancer activity and hematological toxicity in Dalton's ascites lymphoma-bearing mice. Kalita, S; Prasad, SB; Verma, AK, 2014)	3.29
"Chlorambucil is an alkylating agent used in combination with prednisolone for the treatment of idiopathic membranous nephropathy. "	( Chlorambucil-induced cytomegalovirus infection: a case report. Arambarri-Segura, M; de la Nieta-García, MD; López-Lluva, MT; Martínez-Calero, A; Piqueras-Flores, J; Rivera-Hernández, F, 2014)	3.29
"Chlorambucil (CHL) is a water-insoluble antineoplastic drug having a short elimination half-life. "	( Long-circulating lipoprotein-mimic nanoparticles for smart intravenous delivery of a practically-insoluble antineoplastic drug: Development, preliminary safety evaluations and preclinical pharmacokinetic studies. Al-Mahallawi, AM; Tadros, MI, 2015)	1.86
"Chlorambucil appears to be an effective and well tolerated prednisolone sparing agent for treatment of CEG."	( Canine eosinophilic granuloma of the digits treated with prednisolone and chlorambucil. Knight, EC; Shipstone, MA, 2016)	1.39
"Chlorambucil (CMB) is an anticancer drug used for the treatment of variety of cancers. "	( Spectroscopic and molecular docking studies on chlorambucil interaction with DNA. Charak, S; Mehrotra, R; Shandilya, M; Tyagi, G, 2012)	2.08
"Chlorambucil (CLB) is a bifunctional alkylating drug widely used as an anticancer agent and as an immunosuppressant. "	( Induction of SOS response, cellular efflux and oxidative stress response genes by chlorambucil in DNA repair-deficient Escherichia coli cells (ada, ogt and mutS). Salmelin, C; Vilpo, J, 2003)	1.99
"Chlorambucil is an alkylating agent commonly used in veterinary oncology for conditions including lymphoma. "	( Chlorambucil-induced myoclonus in a cat with lymphoma. Benitah, N; de Lorimier, LP; Gaspar, M; Kitchell, BE, )	3.02
"Chlorambucil is a nitrogen mustard alkylating agent that is used as an antineoplastic drug."	( Irreversible inhibition of bovine lung angiotensin I-converting enzyme with p-[N,N-bis(chloroethyl)amino]phenylbutyric acid (chlorambucil) and chlorambucyl L-proline and with evidence that an active site carboxyl group is labeled. Harris, RB; Wilson, IB, 1982)	1.19
"Chlorambucil is a bifunctional nitrogen mustard which alkylates the N-7 position of guanine in the major groove of double-stranded DNA (dsDNA)."	( Sequence-specific covalent modification of DNA by cross-linking oligonucleotides. Catalysis by RecA and implication for the mechanism of synaptic joint formation. Gamper, HB; Meyer, RB; Podyminogin, MA, 1995)	1.01
"Chlorambucil is a weak acid (pKa = 3.7) and is concentrated within cells exposed to culture media at low pH or to the acidic microenvironment in vivo."	( Enhancement of chlorambucil cytotoxicity by combination with flavone acetic acid in a murine tumour. Chadwick, JA; Chaplin, DJ; Parkins, CS, )	1.21
"Chlorambucil is a rare cause of pulmonary disease."	( Interstitial lung disease--an underdiagnosed side effect of chlorambucil? Huhn, D; Kingreen, D; Mohr, M; Rühl, H, 1993)	1.25
"Chlorambucil was found to be a very potent drug for JCA with acceptable short term, but serious longterm side effects. "	( Chlorambucil in severe juvenile chronic arthritis: longterm followup with special reference to amyloidosis. Savolainen, HA, 1999)	3.19
"Chlorambucil is an alkylating agent that preferentially affects B cells over T cells and has been shown to be effective in the treatment of bullous pemphigoid."	( The use of chlorambucil with prednisone in the treatment of pemphigus. Elgart, GW; Green, AR; Kerdel, F; Shah, N, 2000)	2.14
"Chlorambucil is an effective agent and should be compared with purine analogues or rituxan (Rituximab) in a prospective study."	( Waldenström's macroglobulinaemia: a prospective study comparing daily with intermittent oral chlorambucil. Gertz, MA; Greipp, PR; Kyle, RA; Lacy, MQ; Lust, JA; Therneau, TM; Witzig, TE, 2000)	1.25
"Chlorambucil (CLB) is a bifunctional nitrogen mustard whose therapeutic and major side-effects are thought to be caused by binding to DNA. "	( Studies of chlorambucil-DNA adducts. Bank, BB, 1992)	2.12
"Chlorambucil (CLB) is an alkylating agent commonly used in the treatment of several neoplastic disorders. "	( Lack of drug-induced DNA cross-links in chlorambucil-resistant Chinese hamster ovary cells. Bank, BB; Hsiang, YH; Jiang, BZ; Potmesil, M; Shen, T; Silber, R, 1989)	1.99

Excerpt	Reference	Relevance
"Chlorambucil has been shown to be detoxified by human glutathione transferase Pi (GST P1-1), an enzyme that is often found over-expressed in cancer tissues."	( The anti-cancer drug chlorambucil as a substrate for the human polymorphic enzyme glutathione transferase P1-1: kinetic properties and crystallographic characterisation of allelic variants. Bello, ML; Ciccone, S; Hancock, NC; Italiano, LC; Morton, CJ; Oakley, AJ; Parker, LJ; Parker, MW; Primavera, A, 2008)	1.39
"Chlorambucil has been used for treatment of B cell chronic lymphocytic leukemia, non-Hodgkin's and Hodgkin's disease."	( Growth arrest of BCR-ABL positive cells with a sequence-specific polyamide-chlorambucil conjugate. Alvarez, D; Chou, CJ; Druker, BJ; Eide, CA; Gottesfeld, JM; Lefebvre, S; O'Hare, T; Tyner, JW, 2008)	1.3
"Chlorambucil has been used for patients with primary biliary cirrhosis as it possesses immunosuppressive properties. "	( Chlorambucil for patients with primary biliary cirrhosis. Li, WX; Shi, CR; Yan, X; Zhang, AP, 2012)	3.26
"Chlorambucil neurotoxicity has been well recognized in human patients."	( Chlorambucil-induced myoclonus in a cat with lymphoma. Benitah, N; de Lorimier, LP; Gaspar, M; Kitchell, BE, )	2.3
"Chlorambucil has only rarely been implicated in this complication."	( Fatal interstitial pneumonitis following high-dose intermittent chlorambucil therapy for chronic lymphocyte leukemia. Besa, EC; Joseph, RR; Justh, G; Lane, SD, 1981)	1.22
"Chlorambucil has been used for many years for the treatment of low-grade B-cell lymphoproliferative disorders, including chronic lymphocytic leukaemia and low-grade non-Hodgkin's lymphoma. "	( High-dose chlorambucil for the treatment of chronic lymphocytic leukaemia and low-grade non-Hodgkin's lymphoma. Mounter, PJ; Proctor, SJ; Summerfield, GP; Taylor, PR, 2002)	2.16

Excerpt	Reference	Relevance
"Chlorambucil is a rare cause of pulmonary disease."	( Interstitial lung disease--an underdiagnosed side effect of chlorambucil? Huhn, D; Kingreen, D; Mohr, M; Rühl, H, 1993)	1.25
"Chlorambucil may cause pulmonary fibrosis similar to busulfan and cyclophosphamide and this may be a potential complication of all alkylating agents."	( Pulmonary disease with chlorambucil therapy. Cole, SR; Klatsky, AU; Myers, TJ, 1978)	1.29
"Chlorambucil did not increase global NK activity (21.7% +/- 7.1), whereas alpha 2b-IFN did so (44.3% +/- 19.1)."	( Recombinant alpha-2b-interferon may restore natural-killer activity in patients with B-chronic lymphocytic leukemia. Montserrat, E; Reverter, JC; Rozman, C; Urbano-Ispízua, A; Villamor, N; Vives-Corrons, JL, 1992)	1

Excerpt	Reference	Relevance
"Chlorambucil treatment was continued every other day and a single, variably timed sample collection was obtained on day 14."	( Population pharmacokinetics identifies rapid gastrointestinal absorption and plasma clearance of oral chlorambucil administered to cats with indolent lymphoproliferative malignancies. Al-Nadaf, S; Burton, JH; Skorupski, KA; Wittenburg, LA, 2022)	1.66
"Chlorambucil treatment also caused morphological abnormalities in red blood cells, majority of which include acanthocytes, burr and microcystis."	( Chlorambucil and ascorbic acid-mediated anticancer activity and hematological toxicity in Dalton's ascites lymphoma-bearing mice. Kalita, S; Prasad, SB; Verma, AK, 2014)	2.57
"Chlorambucil (CLB) treatment is used in chronic lymphocytic leukemia (CLL) but resistance to CLB develops in association with accelerated repair of CLB-induced DNA damage. "	( Chlorambucil cytotoxicity in malignant B lymphocytes is synergistically increased by 2-(morpholin-4-yl)-benzo[h]chomen-4-one (NU7026)-mediated inhibition of DNA double-strand break repair via inhibition of DNA-dependent protein kinase. Aloyz, R; Amrein, L; Dunn, M; Goulet, AC; Jean-Claude, B; Loignon, M; Panasci, L, 2007)	3.23
"For chlorambucil treatment, this increased MRPI-mRNA expression was accompanied by increased drug resistance while paclitaxel treatment had no effect on drug resistance in the H82 cells."	( Induction of broad drug resistance in small cell lung cancer cells and its reversal by paclitaxel. Davey, MW; Davey, RA; Su, GM, 1998)	0.78
"Four chlorambucil-treated patients developed ESRD, and five needed a second course of therapy, whereas only one cyclophosphamide-treated patient developed ESRD (p < 0.05)."	( Oral cyclophosphamide versus chlorambucil in the treatment of patients with membranous nephropathy and renal insufficiency. Branten, AJ; Koene, RA; Reichert, LJ; Wetzels, JF, 1998)	1.05
"Chlorambucil treatment was responsible for a decrease in circulating T4+ and T8+ cells; nevertheless, T lymphocyte function was slightly improved during relapses."	( Immunosuppressive effects of isoprinosine in man: a comparison to chlorambucil effects in multiple sclerosis. Buge, A; Cour, V; Delsaux, MC; Meunier, C; Pompidou, A; Rancurel, G; Telvi, L, 1987)	1.23
"Chlorambucil treatment was helpful in patients with amyloidosis and in those patients in whom all other drugs had failed."	( Slow-acting antirheumatic drug use in systemic onset juvenile chronic arthritis. Ansell, BM; Manners, PJ, 1986)	0.99
"The treatment with chlorambucil led to long-term management of the cat without any side effects."	( Long-term management of a cat with nasopharyngeal lymphoma by chlorambucil. Baba, T; Hirokawa, M; Kimura, J; Kishimoto, M; Kondo, H; Miyajima, M; Ohmori, K; Takahashi, K, )	0.69
"Treatment with chlorambucil and prednisone administered orally over a 1.8-year period decreased the leukocyte and lymphocyte counts to within reference intervals with no adverse effects. "	( Diagnosis and treatment of chronic lymphocytic leukemia in a bat-eared fox (Otocyon megalotis). Adkesson, MJ; Landolfi, JA; Langan, JN; Nevitt, BN; Wilson, R, 2014)	0.76
"Treatment with chlorambucil and corticosteroids was started at standard doses, based on published protocols."	( Acquired Fanconi syndrome in four cats treated with chlorambucil. Feldman, DG; Reinert, NC, 2016)	1.02
"Cats treated with chlorambucil should be monitored for the development of glucosuria, and discontinuation of chlorambucil should be considered if FS is identified."	( Acquired Fanconi syndrome in four cats treated with chlorambucil. Feldman, DG; Reinert, NC, 2016)	1.01
"Treatment with chlorambucil was started in the early 1990s and continued for a period of 9 1/2 and 3(3/4) years, respectively, with the symptoms remitting during and after this therapy."	( [Chlorambucil treatment of Behçet's syndrome. Retrospective evaluation of two cases]. Eichhorn, A; Kirch, W; Siepmann, M, 2010)	1.61
"Treatment with chlorambucil, 0.1 mg/kg daily, compared favorably with corticosteroids."	( Chlorambucil in the treatment of uveitis and meningoencephalitis of Behçet's disease. Goldstein, NP; O'Duffy, JD; Robertson, DM, 1984)	2.05
"Treatment with chlorambucil intra-articularly was clearly more effective than with methylprednisolone or 90Y at the doses employed and deserves further study as a potential treatment for chronic synovitis."	( Treatment of antigen-induced arthritis in rabbits by the intra-articular injection of methylprednisolone, 90Y or chlorambucil. Foong, WC; Green, KL, 1993)	0.84
"Treatment with chlorambucil, prednisolone, and renal bed irradiation resulted in a substantial improvement in renal function which persisted until the the patient's death from marrow failure some eight years later."	( Renal failure caused by leukaemic infiltration in chronic lymphocytic leukaemia. Bass, PS; Davies, DR; Jones, NF; Majumdar, G; Pearson, TC; Phillips, JK, 1993)	0.63
"Treatment with chlorambucil (10-20 mg/d) and prednisolone (25 mg/d), for 14 days every 4 weeks, and finally interferon alpha-2b (5 mill."	( [Pseudoleukocytosis in cryoglobulinemia type I]. Bremer, K; Hansmann, E; Wöltjen, HH, 1993)	0.63
"Treatment with chlorambucil induced a 10-fold sensitivity to steroids; cyclophosphamide induced greater resistance to anthracyclines than alkylating agents; anthracyclines induced greatest resistance to chlorambucil, cisplatin, carboplatin, and cladribine."	( Novel ex vivo analysis of nonclassical, pleiotropic drug resistance and collateral sensitivity induced by therapy provides a rationale for treatment strategies in chronic lymphocytic leukemia. Bell, PB; Bosanquet, AG, 1996)	0.63
"Treatment with chlorambucil, started in 59 patients, was in accordance with the guidelines of the national programme for 52 of them."	( [Chronic lymphatic leukemia. A population-based study of symptoms, findings, complications and choice of treatment]. Bergheim, J; Dahl, IM; Grøttum, KA; Hammerstrøm, J; Ly, B; Lødemel, B, 1998)	0.64
"Treatment with chlorambucil and prednisone improved the patient's function from being wheelchair bound to walking unaided."	( Improvement of myelopathy in Sjögren's syndrome with chlorambucil and prednisone therapy. O'Duffy, JD; Rodriguez, M; Wright, RA, 1999)	0.89
"Treatment with chlorambucil resulted in normalization of the peripheral blood smear, but the malignant infiltration of the bone marrow continued and manifested itself by appearance of new osteolytic lesions, though some of the old lesions underwent recalcification after treatment."	( Macroglobulinemia of Waldenström associated with severe osteolytic lesions. Krausz, Y; Zlotnick, A, 1977)	0.6
"Treatment with chlorambucil produced complete reversal of hepatosplenomegaly, anemia, neutropenia and lymphocytosis, and reduction of marrow infiltration."	( Lymphoproliferative disorder of large granular lymphocytes: reversal of lymphocyte proliferation, anemia and neutropenia with chlorambucil. Cazzola, M; Ippoliti, G; Meloni, F; Pedrazzoli, P; Stella, CC, 1987)	0.82

Excerpt	Reference	Relevance
" The cell toxicity observed with Chl-arachidonic acid and Chl-docosahexaenoic acid against lymphoma cells was, at any experimental condition used, equal or higher than the individual toxic potential of either chlorambucil or fatty acids."	( Cytotoxicity of chlorambucil and chlorambucil-fatty acid conjugates against human lymphomas and normal human peripheral blood lymphocytes. Anel, A; Antonakis, K; Halmos, T; Piñeiro, A; Torres, JM; Uriel, J, 1990)	0.81
" Apart from infections, there were more adverse effects reported in the immunosuppressive therapy group."	( Comparative toxicity of total lymphoid irradiation and immunosuppressive drug treated patients with intractable rheumatoid arthritis. Bloch, D; Fries, J; Sherrer, Y; Strober, S, 1987)	0.27
" In 59 patients with advanced disease who received no other treatment, a 5-year survival rate of 66% was comparable with that achieved by more toxic mustine-containing combinations."	( Five years' experience with ChlVPP: effective low-toxicity combination chemotherapy for Hodgkin's disease. Austin, DE; Barrett, A; Dady, PJ; McElwain, TJ; Peckham, MJ, 1982)	0.26
" In mol/kg, the chlorambucil-spermidine conjugate was 10-fold more toxic than chlorambucil, on the basis of their neurotoxicity, but only 2- to 3-fold more toxic on the basis of their effects on lymphocyte depression."	( The comparative toxicity of chlorambucil and chlorambucil-spermidine conjugate to BALB/c mice. Carthew, P; Cohen, GM; Cullis, P; Holley, JL; Verschoyle, RD, 1994)	0.93
"Chlorambucil can be a safe and effective alternative for preserving vision in patients with otherwise treatment resistant uveitis."	( Efficacy and safety of chlorambucil in intractable noninfectious uveitis: the Massachusetts Eye and Ear Infirmary experience. Baltatzis, S; Ekong, A; Foster, CS; Miserocchi, E; Roque, M, 2002)	2.07
"O6-Benzylguanine (BG) inactivates O6-alkylguanine-DNA alkyltransferase (AGT), resulting in an increase in the sensitivity of cells to the toxic effects of O6-alkylating agents."	( Effect of O6-benzylguanine on nitrogen mustard-induced toxicity, apoptosis, and mutagenicity in Chinese hamster ovary cells. Cai, Y; Chung, AB; Dolan, ME; Ludeman, SM; Wilson, LR, 2001)	0.31
" The toxicity of these compounds against hepatoma cells (MH3924A) and, to a lesser extent, against mouse fibroblast (NIH 3T3) and cervix carcinoma (HeLa) cells was also enhanced, but they were not as toxic as dacarbazine (HeLa)."	( Alkylating benzamides with melanoma cytotoxicity. Bauder-Wüst, U; Eisenhut, M; Haberkorn, U; Mier, W; Mohammed, A; Schönsiegel, F; Wolf, M, 2004)	0.32
" Similar side effect intensity of BZA2 and dacarbazine was observed, whereas BZA1 was more toxic."	( Alkylating benzamides with melanoma cytotoxicity: experimental chemotherapy in a mouse melanoma model. Bauder-Wüst, U; Eisenhut, M; Eskerski, H; Haberkorn, U; Wolf, M, 2006)	0.33
"Obinutuzumab, a third-generation anti-CD20 MoAb, is a safe and effective treatment for elderly patients who are un-fit for fludarabine-based regimen."	( Treating chronic lymphocytic leukemia with obinutuzumab: safety and efficacy considerations. Cassin, R; Cortelezzi, A; Fattizzo, B; Orofino, N; Reda, G; Sciumè, M, 2016)	0.43
" Grade ≥3 adverse events occurred in 80."	( Safety of obinutuzumab alone or combined with chemotherapy for previously untreated or relapsed/refractory chronic lymphocytic leukemia in the phase IIIb GREEN study. Aktan, M; Bosch, F; Dartigeas, C; Ferra Coll, CM; Foà, R; Gresko, E; Kisro, J; Leblond, V; Merot, JL; Montillo, M; Raposo, J; Robson, S; Stilgenbauer, S, 2018)	0.48
" The most frequent adverse events were neutropenia and infusion‑related reactions (IRRs)."	( Efficacy and safety of the obinutuzumab-chlorambucil combination in the frontline treatment of elderly CLL patients with comorbidities - Polish Adult Leukemia Group (PALG) real-life analysis. Chmielowska, E; Dudziński, M; Długosz-Danecka, M; Gawroński, K; Hus, I; Jurczak, W; Morawska, M; Wąsik-Szczepanek, E; Wdowiak, K; Wiśniewska, A; Łabędź, A; Łątka-Cabała, E, 2018)	0.75
"We conducted an integrated safety analysis to characterize the frequency, severity, natural history, and outcomes of adverse events (AEs) with ibrutinib versus comparators."	( Safety Analysis of Four Randomized Controlled Studies of Ibrutinib in Patients With Chronic Lymphocytic Leukemia/Small Lymphocytic Lymphoma or Mantle Cell Lymphoma. Barr, PM; Burger, JA; Chang, S; Coutre, S; Cramer, P; Dilhuydy, MS; Fraser, G; Graef, T; Hess, G; Hillmen, P; Howes, A; James, DF; Liu, E; Moreno, C; O'Brien, S; Patel, K; Styles, L; Tedeschi, A; Valentino, R; Vermeulen, J, 2018)	0.48
" Common grade ≥3 adverse events (AEs) included neutropenia (13%), pneumonia (12%), hypertension (8%), anemia (7%), and hyponatremia (6%); occurrence of most events as well as discontinuations due to AEs decreased over time."	( Long-term efficacy and safety of first-line ibrutinib treatment for patients with CLL/SLL: 5 years of follow-up from the phase 3 RESONATE-2 study. Bairey, O; Barr, PM; Burger, JA; Coutre, SE; Dai, S; Dean, JP; Devereux, S; Ghia, P; Grosicki, S; Hillmen, P; Kipps, TJ; Lal, I; McCarthy, H; Moreno, C; Offner, F; Owen, C; Robak, T; Simpson, D; Tedeschi, A, 2020)	0.56
" RTX-related adverse events were mostly mild (most infusion-related reactions) in nature and serious adverse events were rare."	( Efficacy and safety of rituximab in the treatment of membranous nephropathy: A systematic review and meta-analysis. Gong, S; Li, J; Lu, W; Luo, H; Wang, Y, 2020)	0.56
"RTX proved to be efficient, well-tolerated and a safe drug in the treatment of membranous nephropathy."	( Efficacy and safety of rituximab in the treatment of membranous nephropathy: A systematic review and meta-analysis. Gong, S; Li, J; Lu, W; Luo, H; Wang, Y, 2020)	0.56
" At the final analysis, no new safety signals were observed [Grade ≥ 3 adverse events (AEs): 1L 82·7%, R/R 84·5%; serious AEs: 1L 58·1%, R/R 62·5%]."	( Safety and efficacy of obinutuzumab alone or with chemotherapy in previously untreated or relapsed/refractory chronic lymphocytic leukaemia patients: Final analysis of the Phase IIIb GREEN study. Bosch, F; Böttcher, S; Foà, R; Ilhan, O; Kisro, J; Leblond, V; Mahé, B; Mikuskova, E; Osmanov, D; Perretti, T; Reda, G; Robinson, S; Stilgenbauer, S; Tausch, E; Trask, P; Turgut, M; Van Hoef, M; Wójtowicz, M, 2021)	0.62

Excerpt	Reference	Relevance
"The pharmacokinetic characteristics of prednisolone and of chlorambucil and its beta-oxidized metabolite, phenylacetic mustard (PAM) were studied in plasma after the oral administration of 200 mg prednimustine (Sterecyt) and a regimen consisting of 20 mg prednisolone plus 20 mg chlorambucil, respectively."	( A pharmacokinetic study of prednimustine as compared with prednisolone plus chlorambucil in cancer patients. Bastholt, L; Gunnarsson, PO; Johansson, CJ; Johansson, SA; Mouridsen, H; Pfeiffer, P; Svensson, L, 1991)	0.75
"This report describes the physicochemical and pharmacokinetic parameters of seven chlorambucil esters, which were compared with those of chlorambucil."	( Physicochemical and pharmacokinetic parameters of seven lipophilic chlorambucil esters designed for brain penetration. Daly, EM; Genka, S; Greig, NH; Rapoport, SI; Sweeney, DJ, 1990)	0.74
" Chlorambucil demonstrated a monophasic disappearance from plasma following its administration, with a half-life of 28 min."	( Pharmacokinetics of chlorambucil-tertiary butyl ester, a lipophilic chlorambucil derivative that achieves and maintains high concentrations in brain. Daly, EM; Greig, NH; Rapoport, SI; Sweeney, DJ, 1990)	1.51
" This different pharmacokinetic behavior might offer an explanation for the superior therapeutic effects of prednimustine demonstrated by clinical studies."	( Studies on the pharmacokinetics of chlorambucil and prednimustine in patients using a new high-performance liquid chromatographic assay. Loos, U; Malek, M; Mühlenbruch, B; Musch, E; Oppitz, MM; Rüb, HP; von Unruh, GE, 1989)	0.55
" On a pharmacokinetic basis, chlorambucil's greater in vitro stability, its more rapid and predictable systemic availability after oral dosing, and its extremely low urinary excretion make it a more predictable alkylating agent for clinical use than melphalan, especially for patients with reduced renal function."	( Comparative pharmacokinetics of chlorambucil and melphalan in man. Alberts, DS; Chang, SY; Chen, HS; Evans, TL; Larcom, BJ, 1980)	0.84
" The synthesis and the physicochemical and pharmacokinetic evaluation of a CDS modeling the lipoyl and other ester derivatives of chlorambucil (an antineoplastic agent) and cromolyn (a bischromone used in antiasthma prophylaxis) as compared with their respective parent drugs are described."	( Design, synthesis, and pharmacokinetic evaluation of a chemical delivery system for drug targeting to lung tissue. Bodor, N; Eberst, K; Marvanyos, E; Saah, M; Wu, WM, 1996)	0.5
" Biological studies performed in rats showed that [14C]-CQA and [14C]-chlorambucil exhibited different pharmacokinetic profiles."	( Synthesis and pharmacokinetic profile of a quaternary ammonium derivative of chlorambucil, a potential anticancer drug for the chemotherapy of chondrosarcoma. Giraud, I; Madelmont, JC; Maurizis, JC; Rapp, M, 2003)	0.78
" pharmacokinetic data on 670 drugs representing, to our knowledge, the largest publicly available set of human clinical pharmacokinetic data."	( Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds. Lombardo, F; Obach, RS; Waters, NJ, 2008)	0.35
" 180+/-7 ml/kg) and elimination half-life (1."	( Pharmacokinetics and pharmacodynamics of chlorambucil delivered in parenteral emulsion. Baguley, BC; Ganta, S; Garg, S; Paxton, JW, 2008)	0.61
" Pharmacokinetic studies of the intravenous LN formulation revealed plasma clearance kinetics were comparable to that of CLB solution (p>0."	( Formulation and pharmacokinetics of lipid nanoparticles of a chemically sensitive nitrogen mustard derivative: Chlorambucil. Denny, WA; Ganta, S; Garg, S; Sharma, P, 2009)	0.56
" The validated method was successfully applied to the pharmacokinetic study of CHLS and CHL in mice after intravenous administration."	( Validated LC-MS/MS method for the simultaneous determination of chlorambucil and its prodrug in mouse plasma and brain, and application to pharmacokinetics. Lin, Q; Wang, X; Zhang, Q; Zhang, Y; Zhang, ZR, 2014)	0.64

Excerpt	Reference	Relevance
" The low toxicity combined with worthwhile remissions make this an attractive first-line option for elderly patients."	( Phase 2 study of mitozantrone in combination with chlorambucil and prednisolone for relapsed and refractory non-Hodgkins lymphoma. Cotter, FE; Jones, L; Lord, D; Newland, AC, )	0.38
" In conclusion, it seems that prednimustine can be safely used in combination with methotrexate and 5-fluorouracil."	( Prednimustine in combination with methotrexate and 5-fluorouracil in advanced breast cancer: a phase I-II study. Boesen, E; Mouridsen, HT, 1983)	0.27
"Previous studies using murine tumours have shown enhanced action of certain chemotherapeutic compounds when combined with agents that reduce tumour blood flow."	( Enhancement of chlorambucil cytotoxicity by combination with flavone acetic acid in a murine tumour. Chadwick, JA; Chaplin, DJ; Parkins, CS, )	0.48
"Surgery combined with chemotherapy was applied in 34 out of 178 patients (19."	( Chemotherapy combined with surgery in the treatment of gestational trophoblastic disease (GTD). Kietlińska, Z; Sablińska, B; Zieliński, J, 1993)	0.29
" Cladribine was combined with cisplatin, daunorubicin, chlorambucil, paclitaxel or etoposide."	( Cytotoxicity of 2-chlorodeoxadenosine (cladribine, 2-cdA) in combination with other chemotherapy drugs against two lymphoma cell lines. Hoffman, M; Lesser, M; Rai, K; Xu, JC, 1999)	0.55
"We investigated the toxicity and efficacy of the chimaeric anti-CD20 antibody rituximab in combination with standard-dose chlorambucil in newly diagnosed and relapsed/refractory indolent B-cell lymphoma patients."	( Chlorambucil in combination with induction and maintenance rituximab is feasible and active in indolent non-Hodgkin's lymphoma. Bertolini, F; Calleri, A; Cavalli, F; Laszlo, D; Mancuso, P; Martinelli, G; Pastano, R; Santoro, P; Vanazzi, A; Zucca, E, 2003)	1.97
" To evaluate this effect in vivo, we performed a phase I study of chlorambucil combined with imatinib in relapsed CLL patients."	( A phase I study of imatinib mesylate in combination with chlorambucil in previously treated chronic lymphocytic leukemia patients. Aloyz, R; Amrein, L; Assouline, S; Caplan, S; Desjardins, P; Egorin, MJ; Hebb, J; Panasci, L; Rousseau, C, 2011)	0.85
"), a CD20-directed cytolytic antibody, for use in combination with chlorambucil for the treatment of patients with previously untreated chronic lymphocytic leukemia (CLL)."	( U.S. Food and drug administration approval: obinutuzumab in combination with chlorambucil for the treatment of previously untreated chronic lymphocytic leukemia. Bullock, J; DelValle, P; Farrell, AT; Florian, J; Grillo, J; Justice, R; Kaminskas, E; Kane, RC; Ko, CW; Kwitkowski, VE; Lee, HZ; Mehrotra, N; Miller, BW; Nie, L; Pazdur, R; Ricci, S; Saber, H; Shapiro, M; Tolnay, M, 2014)	0.87
" To demonstrate this unique approach, an amphiphilic drug-drug conjugate (ADDC) has been synthesized from the hydrophilic anticancer drug irinotecan (Ir) and the hydrophobic anticancer drug chlorambucil (Cb) via a hydrolyzable ester linkage."	( Combination of small molecule prodrug and nanodrug delivery: amphiphilic drug-drug conjugate for cancer therapy. Cui, D; Huang, P; Huang, W; Su, Y; Wang, D; Yan, D; Zhou, Y; Zhu, X, 2014)	0.59
" The aim of the present study was to evaluate the safety, efficacy and pharmacokinetics of ofatumumab in combination with chlorambucil in Japanese patients with previously untreated CLL who were inappropriate for fludarabine-based therapy."	( Ofatumumab combined with chlorambucil for previously untreated chronic lymphocytic leukemia: a phase I/II, open-label study in Japan. Ando, K; Fujita, T; Hatake, K; Ogura, M; Takada, K; Taniwaki, M; Zhang, F, 2017)	0.97
" Patients undergoing hematopoietic stem cell transplantation (HSCT) are exposed to various types of drugs, and understanding how these drugs interact is of the utmost importance."	( Development of an assay for cellular efflux of pharmaceutically active agents and its relevance to understanding drug interactions. Andersson, BS; Hassan, M; Valdez, BC, 2017)	0.46
" Herein, two different anticancer drugs, camptothecin and chlorambucil, are successfully connected together by a disulfide linkage to get a novel drug-drug conjugated prodrug (G)."	( Construction of drug-drug conjugate supramolecular nanocarriers based on water-soluble pillar[6]arene for combination chemotherapy. Hu, XY; Liu, X; Shao, W; Sun, G; Wang, L; Zhu, JJ, 2018)	0.73
" In this paper, chlorambucil-oxoplatin (Cb-Pt) was prepared to fabricate water-soluble pillar[6]arene (WP[6]) based supramolecular drug-drug self-assemblies (SDSAs)."	( Supramolecular self-assemblies based on water-soluble pillar[6]arene and drug-drug conjugates for the combination of chemotherapy. Bai, Y; Liu, C; Shang, Q; Tian, W; Yang, J, 2022)	1.07
"Venetoclax in combination with obinutuzumab has significantly improved efficacy versus immunochemotherapy (progression-free survival) in patients with chronic lymphocytic leukaemia who have not received prior treatment."	( Cost-utility analysis of venetoclax in combination with obinutuzumab as first-line treatment of chronic lymphocytic leukaemia in Spain. De la Serna-Torroba, J; Escudero-Vilaplana, V; Hernández-Rivas, JÁ; Moreno-Martínez, E; Sánchez-Cuervo, M; Sánchez-Hernández, R, 2022)	0.72
"Venetoclax in combination with obinutuzumab was shown to be a dominant alternative compared to the rest of the treatment alternatives, with a lower cost per patient (€-67,869 compared to chlorambucil in combination with obinutuzumab, €-375,952 compared to ibrutinib, €-61,996 compared to fludarabine in combination with cyclophosphamide and rituximab, and €- 77,398 compared to bendamustine in combination with rituximab)."	( Cost-utility analysis of venetoclax in combination with obinutuzumab as first-line treatment of chronic lymphocytic leukaemia in Spain. De la Serna-Torroba, J; Escudero-Vilaplana, V; Hernández-Rivas, JÁ; Moreno-Martínez, E; Sánchez-Cuervo, M; Sánchez-Hernández, R, 2022)	0.91
"Venetoclax in combination with obinutuzumab is an efficient and dominant alternative for treating previously untreated patients with chronic lymphocytic leukaemia compared to the available alternatives and from the perspective of the Spanish National Health System."	( Cost-utility analysis of venetoclax in combination with obinutuzumab as first-line treatment of chronic lymphocytic leukaemia in Spain. De la Serna-Torroba, J; Escudero-Vilaplana, V; Hernández-Rivas, JÁ; Moreno-Martínez, E; Sánchez-Cuervo, M; Sánchez-Hernández, R, 2022)	0.72

Excerpt	Reference	Relevance
" The mean bioavailability was 14% for chlorambucil, 21% for phenylacetic acid mustard, and 22% for prednisolone, when given as prednimustine, compared to the administration of free compounds in stoichiometrically equivalent doses."	( Comparative pharmacokinetics of chlorambucil and prednimustine after oral administration. Loos, U; Malek, M; Musch, E; Riedel, E, 1991)	0.84
"Previous studies have demonstrated that the bioavailability of melphalan and chlorambucil may be reduced under non-fasting conditions, and that the gastrointestinal and cellular absorption of melphalan is an active process, while that of chlorambucil is passive."	( The effect of dietary amino acids on the gastrointestinal absorption of melphalan and chlorambucil. Adair, CG; McElnay, JC, 1987)	0.73
" The bioavailability of chlorambucil was about five times lower when given as prednimustine as compared to administration of the free drug."	( Pharmacokinetics of chlorambucil in man after administration of the free drug and its prednisolone ester (prednimustine, Leo 1031). Ehrsson, H; Johansson, B; Nilsson, SO; Wallin, I, 1983)	0.9
" the bioavailability of orally administered prednimustine is much lower than that of chlorambucil."	( Studies on the pharmacokinetics of chlorambucil and prednimustine in man. Calvert, AH; Harrap, KR; McElwain, TJ; Newell, DR, 1983)	0.77
" It is suggested that prednisolone plasma levels are as good a parameter of Prednimustine absorption and bioavailability as chlorambucil levels, Prednimustine itself having never been detected in plasma."	( Prednisolone plasma levels after oral administration of Prednimustine. Comparison with levels obtained after administration of an equimolar dose of prednisolone. Hove, WV; Sayed, A; Vermeulen, A, 1981)	0.47
"The mechanisms involved in the bioavailability of chlorambucil or 4-[p-(bis[2-hydroxyethyl]amino)phenyl]-butyric acid are poorly understood."	( Kinetics of chlorambucil in vitro: effects of fluid matrix, human gastric juice, plasma proteins and red cells. Hovinen, J; Löf, K; Reinikainen, P; Seppälä, E; Vilpo, JA; Vilpo, LM, 1997)	0.93
"The quantitative structure-bioavailability relationship of 232 structurally diverse drugs was studied to evaluate the feasibility of constructing a predictive model for the human oral bioavailability of prospective new medicinal agents."	( QSAR model for drug human oral bioavailability. Topliss, JG; Yoshida, F, 2000)	0.31
"The effects of repeated treatment cycles and different doses on intraindividual variation in oral bioavailability of chlorambucil and its first, active, and more toxic metabolite, phenylacetic acid mustard, were studied."	( Pharmacokinetics of chlorambucil in patients with chronic lymphocytic leukaemia: comparison of different days, cycles and doses. Malminiemi, K; Malminiemi, O; Seppälä, E; Silvennoinen, R; Vilpo, J, 2000)	0.84
" Pharmacokinetic studies suggest decreased bioavailability with successive cycles, probably due to accelerated metabolism."	( High dose chlorambucil in the treatment of lymphoid malignancies. Nicolle, A; Proctor, SJ; Summerfield, GP, 2004)	0.73
" Human oral bioavailability is an important pharmacokinetic property, which is directly related to the amount of drug available in the systemic circulation to exert pharmacological and therapeutic effects."	( Hologram QSAR model for the prediction of human oral bioavailability. Andricopulo, AD; Moda, TL; Montanari, CA, 2007)	0.34
"Oral bioavailability (F) is a product of fraction absorbed (Fa), fraction escaping gut-wall elimination (Fg), and fraction escaping hepatic elimination (Fh)."	( Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination. Chang, G; El-Kattan, A; Miller, HR; Obach, RS; Rotter, C; Steyn, SJ; Troutman, MD; Varma, MV, 2010)	0.36
" The preliminary safety evaluations and the seven-fold increase in bioavailability elucidated potentiality for smart intravenous delivery of CHL."	( Long-circulating lipoprotein-mimic nanoparticles for smart intravenous delivery of a practically-insoluble antineoplastic drug: Development, preliminary safety evaluations and preclinical pharmacokinetic studies. Al-Mahallawi, AM; Tadros, MI, 2015)	0.42
"The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs."	( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019)	0.51

Excerpt	Relevance	Reference
" Treatment dosage on a few occasions was decreased and increased again, due to drops in hemoglobin level and white blood cell and platelet counts."	( Long-term survival in a case of stage IV carcinoma of the ovary treated with a single chemotherapeutic agent. Akbiyik, N; Alexander, L; Solisio, E, 1979)	0.26
"A 63-year-old man, with a Waldenström's disease discovered by cryoglobulinemia (ischemic lesions of fingers) was quickly aggravating (hyperviscosity syndrome) under treatment by chlorambucil in a dosage of 8 mg daily."	( [Polychimiotherapy and Waldenström's macroglobulinemia (author's transl)]. Barrier, J; Bouret, O; Grolleau, JY; Ozanne, P; Renault, JJ, )	0.32
" Eleven patients with advanced carcinoma of the lung (5 adenocarcinoma, 3 squamous cell carcinoma, 2 small cell carcinoma and 1 large cell carcinoma) were treated at a dosage of 40 mg."	( Preliminary clinical study of prednimustine in lung cancer. Catane, H; Catane, R; Kaufman, JH; Mittelman, A; Murphy, GP; Takita, H, 1977)	0.26
"A controlled clinical trial was performed using two dosage regimens of chlorambucil to treat children with frequently relapsing nephrotic syndrome."	( Chlorambucil dosage in frequently relapsing nephrotic syndrome: a controlled clinical trial. Baluarte, HJ; Gruskin, AB; Hiner, L, 1978)	1.93
"Thirty-nine patients with gynecological malignancies who had failed on conventional chemotherapeutic agents were treated with Leo 1031 to study the effective dosage and toxicity of the compound in gynecological malignancies."	( Leo 1031 (NSC-134087) in gynecologic malignancies. Barlow, JJ; Lele, SB; Murphy, GP; Piver, MS, 1978)	0.26
" The patients were divided into three groups according to dosage and previous treatment."	( Continuous treatment of non-Hodgkin's malignant lymphoma with prednimustine (Leo 1031). Håkansson, L; Könyves, I; Lindberg, LG; Möller, T, 1978)	0.26
" NZB/W female mice were treated with Cy, Chlor, or nothing on a once-a-month dosage schedule."	( Therapeutic studies in NZB/NZW F1 mice. V. Comparison of cyclophosphamide and chlorambucil. Gerber, NL; Powell, D; Steinberg, AD, )	0.36
" The effect of treatment was to allow a reduction in corticosteroid dosage and a sustained remission of disease activity in patients."	( Rheumatoid arthritis treated with chlorambucil: a five-year follow-up. Thorpe, P, 1976)	0.53
" They type and frequency of malformations differed according to the dosage and day of treatment."	( Teratogenic effects of chlorambucil on in vivo and in vitro organogenesis in mice. Kochhar, DM; Salder, TW, 1975)	0.57
" Dosage adjustments were often necessary during the initial phases of therapy."	( A controlled study in the use of combined drug therapy for metastatic breast cancer. Alberto, P; Brunner, KW; Martz, G; Obrecht, P; Senn, HJ; Sonntag, RW, 1975)	0.25
" Methodology and dosage schemes are discussed."	( Towards curative treatment of advanced Hodgkin's disease. Falkson, G; Falkson, HC, 1975)	0.25
" Each case was associated with prior chlorambucil administration, effective in controlling the clinical manifestations (total dosage 398 and 1,764 mg respectively)."	( Irreversible bone marrow failure with chlorambucil. Epstein, WV; Fries, JF; Rudd, P, 1975)	0.8
" Radical excision of the tumor, if possible, and the remaining thymus, high dosage alternate day prednisone, and radiation therapy, if indicated, seem the treatments of choice."	( Myasthenia gravis and invasive thymoma: a 20-year experience. Brown, WJ; Goldman, AJ; Herrmann, C; Keesey, JC; Mulder, DG, 1975)	0.25
" The spectrum of malformations and the dose-response behavior of both drugs were similar."	( Aspects of the teratology of cyclophosphamide (NSC-26271). Ashby, R; Davis, L; Dewhurst, BB; Espinal, R; Penn, RN; Upshall, DG, 1976)	0.26
" The patients were randomly assigned to receive either alternating one-month courses of methylprednisolone and then chlorambucil for a total of six months (group 1) or methylprednisolone alone for six months at the same cumulative dosage (group 2)."	( Methylprednisolone plus chlorambucil as compared with methylprednisolone alone for the treatment of idiopathic membranous nephropathy. The Italian Idiopathic Membranous Nephropathy Treatment Study Group. Cesana, B; Passerini, P; Ponticelli, C; Zucchelli, P, 1992)	0.8
" Chlorambucil was given to 31 of these patients because complicating diseases or problems made adequate corticosteroid dosage impossible (5 cases) or because of failure of corticosteroid in tolerable doses to control the disease (26 cases)."	( Chlorambucil treatment of sarcoidosis. Israel, HL; McComb, BL, 1991)	2.63
" Reduced ability to produce formazan corresponded to a reduced number of dye-excluding viable cells and a significant correlation was found between dose-response measured in the two assays."	( In vitro chemosensitivity testing in chronic lymphocytic leukaemia patients. Bean, EA; Bentley, DP; Hanson, JA; Moore, JL; Nute, SR, 1991)	0.28
" The corticosteroid dosage administered at the time CyA therapy was initiated was variable and was continued following CyA therapy."	( Long-term cyclosporine A treatment of steroid-resistant and steroid-dependent nephrotic syndrome. Cohen, AH; Fine, RN; Kamil, ES; Melocoton, TL, 1991)	0.28
" Patients who responded less well to treatment tended to be younger, and their disease was more severe in that a higher dosage was required for initial control."	( The use of chlorambucil in the treatment of bullous pemphigoid. Hutchinson, PE; Milligan, A, 1990)	0.67
"Chlorambucil (p-(di-2-chloroethyl)amino-gamma-phenylbutyric acid) is a bifunctional alkylating agent which exhibits acquired drug resistance upon repeated dosing in humans."	( Characterization of glutathione conjugates of chlorambucil by fast atom bombardment and thermospray liquid chromatography/mass spectrometry. Colvin, OM; Dulik, DM; Fenselau, C, 1990)	1.98
" In these 7 children prednisolone dosage could be decreased significantly or discontinued altogether (44."	( Immunoregulation with levamisole in children with frequently relapsing steroid responsive nephrotic syndrome. Alon, U; Drachman, R; Drukker, A; Etzioni, A; Mor, J; Ohali, M; Schlesinger, M; Shapira, H, 1988)	0.27
" All of the compounds were effective against estrogen receptor-positive T-61 with a clear dose-response relationship, while estrogen receptor-negative MX-1 was sensitive to all of the agents except estradiol."	( Mode of action of estra-1,3,5(10)-triene-3,17 beta-diol 3-benzoate 17-[4-(4-bis(2-chloroethyl)amino)phenyl)-1-oxobutoxy)acet ate) on human breast carcinoma xenografts in nude mice. Abe, O; Asano, K; Enomoto, K; Ishibiki, K; Koh, J; Kubota, T; Masui, O; Oka, S; Yamada, Y, 1988)	0.27
" However, tight and constant control of the CsA dosage as performed in this study has, so far, prevented clinical and biochemical nephrotoxic manifestations in patients assigned to this treatment."	( Evaluation of conventional therapy versus cyclosporine A in Behçet's syndrome. BenEzra, D; Chajek, T; Cohen, E; de Courten, C; Friedman, G; Harris, W; Pizanti, S, 1988)	0.27
" The mutagenic and clastogenic actions of both agents were of a dose-response type."	( Mutagenicity and clastogenicity of the antineoplastic agents homo-azasteroidal ester of p-bis(2-chloroethyl)aminophenyl acetic acid and chlorambucil. Arzimanoglou, II; Athanasiou, K, 1986)	0.47
" In the absence of evidence of a dose-response curve for platinum, the lower dosage schedules that can be used with acceptable toxicity on an outpatient basis should be selected."	( Chemotherapy for squamous cell carcinoma of the head and neck: a progress report. Glick, JH; Taylor, SG; Zehngebot, LM, 1980)	0.26
" From 1976 to 1979 patients with Stage IV disease were treated wither with MOPP or with MOPP plus bleomycin at low dosage (B-MOPP); the incidence of complete remission was not significantly different in the two groups of patients (52 vs."	( Combination chemotherapy for stage IV Hodgkin's disease (Report no 14). Goldman, JM, 1981)	0.26
" Cyclic treatment with a combination of chlorambucil, methotrexate and 5-fluorouracil was more myelotoxic and required more extensive dose reductions than treatment with cyclophosphamide, methotrexate and 5-fluorouracil with the dosage used."	( Influence of adjuvant chemotherapy on the blood lymphocyte population in operable breast carcinoma. Comparison between two types of treatments. Baral, E; Blomgren, H; Petrini, B; Strender, LE; Wallgren, A; Wasserman, J, 1982)	0.53
" The latter group, therefore, does not profit from cytotoxic drugs in the dosage used."	( The treatment of minimal change nephrotic syndrome (lipoid nephrosis): cooperative studies of the Arbeitsgemeinschaft für Pädiatrische Nephrologie (APN). Brodehl, J; Ehrich, JH; Krohn, HP, )	0.13
" 3 A preliminary comparison of chlorambucil levels following oral and intravenous administration, and after repeat oral dosage indicated that chlorambucil was well (greater than 70%) and consistently absorbed."	( Studies on the pharmacokinetics of chlorambucil and prednimustine in man. Calvert, AH; Harrap, KR; McElwain, TJ; Newell, DR, 1983)	0.83
" Life-table analysis of two dosage schedules of chlorambucil at four years showed that 91 per cent of patients on low doses and 80 per cent of those on high doses were still in remission."	( Long-term evaluation of chlorambucil plus prednisone in the idiopathic nephrotic syndrome of childhood. Grupe, WE; Ingelfinger, JR; Makker, SP; Williams, SA, 1980)	0.82
" Of the 34 children shows relapses had tended to occur after the prednisone dosage had been reduced or immediately after the drug was discontinued (the steroid-dependent group), 22 also had early relapses after cytotoxic-drug treatment."	( Effect of cytotoxic drugs in frequently relapsing nephrotic syndrome with and without steroid dependence. , 1982)	0.26
" When the glucocorticoid dosage was reduced or the drug discontinued, the nephrotic syndrome recurred."	( [T-cell lymphoma under immunosuppressive treatment in minimal change glomerulopathy with nephrotic syndrome]. Schollmeyer, P; Späth, M, 1995)	0.29
"Prednisone dosage was successfully tapered to 10 to 20 mg/d without worsening symptoms in 10 (38%) of the 26 patients studied."	( Therapeutic considerations in patients with refractory neurosarcoidosis. Agbogu, BN; Sewell, C; Stern, BJ; Yang, G, 1995)	0.29
" The onset of symptoms may occur after only some weeks or after up to several years with no dose-response relationship."	( Interstitial lung disease--an underdiagnosed side effect of chlorambucil? Huhn, D; Kingreen, D; Mohr, M; Rühl, H, 1993)	0.53
" All drugs but mafosfamide, tested in place of cyclophosphamide, were used at concentrations corresponding to the in vivo dosage employed in the CEOP regimen."	( In vitro chemosensitivity of chronic lymphocytic leukemia B-cells to multidrug regimen (CEOP) compounds using the MTT colorimetric assay. Brugiatelli, M; Callea, V; Messina, G; Morabito, F; Nobile, F; Oliva, B; Ramirez, F, )	0.13
" Using this assay in the present study, dose-response relationships of cytotoxicity, PFC response and histology in the spleen were evaluated in rats receiving alkylating agents."	( Dose-response relationships of cytotoxicity, PFC response and histology in the spleen in rats treated with alkylating agents. Doi, T; Nagai, H; Suzuki, T; Tsukuda, R, 1996)	0.29
" The dosage of chlorambucil was decreased with a subsequent decrease in symptomatology."	( Myoclonus due to chlorambucil in two adults with lymphoma. Bayliff, CD; Kovacs, MJ; Wyllie, AR, 1997)	0.99
" One exception might be CBCC patients who were younger (median age 56 years) and who were usually in good general condition so that they might qualify for high dosage chemotherapy and stem cell support."	( Outcome of patients with low-grade B cell non-Hodgkin lymphoma and initial bone marrow involvement: data of a single institution. Heinz, R; Hopfinger, G; Tüchler, H, 1997)	0.3
" However, a dose-response effect was seen only in the DFZ group."	( In vitro improvement of chlorambucil-induced cytotoxicity by deflazacort and 6-methylprednisolone in B-cell chronic lymphocytic leukaemia. Brugiatelli, M; Callea, I; Cartisano, G; Dattola, A; Irrera, G; Morabito, F; Rodinò, A, 1997)	0.6
" No untoward effect from drugs sufficient to alter the dosage used was recorded."	( Clinical features and treatment outcome of idiopathic membranous nephropathy in Chinese patients. Chan, TM; Cheng, IK; Lai, KN; Tang, S, 1999)	0.3
" Relapse-free survival rates increased with the cumulative dosage of CHL and CYC and were higher in children with frequently relapsing than steroid-dependent NS."	( A meta-analysis of cytotoxic treatment for frequently relapsing nephrotic syndrome in children. Ehrich, JH; Latta, K; von Schnakenburg, C, 2001)	0.31
" Gender, age at onset, duration of illness from onset, prednisolone dosage at the most-recent relapse, and regimens of initial steroid therapy at onset were not associated with risk."	( Prediction of subsequent relapse in children with steroid-sensitive nephrotic syndrome. Mizusawa, Y; Simoda, M; Takeda, A; Takimoto, H, 2001)	0.31
" The median duration of treatment with chlorambucil was 12 months (range, 4-50 months), whereas the median daily dosage was 8 mg (range, 4-22 mg)."	( Efficacy and safety of chlorambucil in intractable noninfectious uveitis: the Massachusetts Eye and Ear Infirmary experience. Baltatzis, S; Ekong, A; Foster, CS; Miserocchi, E; Roque, M, 2002)	0.89
" CN was administered intraperitoneally to DBA/2J male mice at a dosage of 0, 500, 1000, or 1500 mg/kg body weight (bw)."	( Chlornaphazine and chlorambucil induce dominant lethal mutations in male mice. Barnett, LB; Lewis, SE, 2003)	0.65
" Additionally, a dose-response for methotrexate at 48 h, and chlorambucil at 24 h were missed using manual scoring."	( Validation of a flow cytometric acridine orange micronuclei methodology in rats. Bleavins, MR; Bulera, S; Criswell, KA; Juneau, P; Krishna, G; Urda, GA; Zielinski, D, 2003)	0.56
"Chlorambucil (4-[p-[bis [2-chloroethyl] amino] phenyl]-butanoic acid; CMB) is a bifunctional alkylating agent that exhibits acquired drug resistance upon repeated dosing in human."	( Relationship between activation of microsomal glutathione S-transferase and metabolism behavior of chlorambucil. Lou, YJ; Zhang, J, 2003)	1.98
" All effects remitted immediately after the final day of the dosing regimen."	( Mood alterations in patients treated with chlorambucil. Dorr, RT; Hehn, ST; Miller, TP, 2003)	0.58
" The optimum dose of chlorambucil has not been defined and there are numerous different dosing schedules available."	( High dose chlorambucil in the treatment of lymphoid malignancies. Nicolle, A; Proctor, SJ; Summerfield, GP, 2004)	1.04
" Information on dosage of prednisolone and immunosuppressive agents was also analyzed."	( Follow-up of linear growth of body height in children with nephrotic syndrome. Hung, YT; Yang, LY, 2006)	0.33
" Unlike conventional and distamycin-based alkylators, little or no cytotoxicities and animal toxicities were observed in mg/kg dosage ranges."	( Small molecules targeting histone H4 as potential therapeutics for chronic myelogenous leukemia. Alvarez, D; Chou, CJ; Dervan, PB; Farkas, ME; Gottesfeld, JM; Tsai, SM, 2008)	0.35
" Finally, drug dosage should be adjusted in cases of chronic renal insufficiency."	( [Treatment of membranous nephropathy with chronic renal insufficiency]. Leoni, A; Passerini, P, )	0.13
"The purpose of this study was to assess the toxicoses and antitumor activity of metronomic chlorambucil at a dosage of 4 mg m(-2) daily in dogs with naturally occurring cancer."	( Prospective trial of metronomic chlorambucil chemotherapy in dogs with naturally occurring cancer. Childress, MO; Greene, SN; Knapp, DW; Lahrman, SR; Leach, TN; Mohamed, AS; Moore, GE; Schrempp, DR, 2012)	0.88
" Etoposide acts weaker (the percentage of cell growth suppression during 48 h does not exceed 50%), but subsequently it has a basis for the creation of new dosage forms with prolonged action of Etoposide and chlorambucil for cancer therapy."	( [Prolonged release of chlorambucil and etoposide from poly-3-oxybutyrate-based microspheres]. Bonartsev, AP; Bonartseva, GA; Filatova, EV; Iakovlev, SG; Makhina, TK; Myshkina, VL, )	0.63
" Dosage tapering lasted 3-9 months; in one center dose tapering lasted for less than 3 months."	( [Focal and segmental glomerulosclerosis in Piedmont and the Aosta Valley in Italy: case study and treatment]. Amore, A; Besso, L; Ferro, M; Giacchino, F; Manganaro, M; Quaglia, M; Rollino, C; Savoldi, S, )	0.13
"To evaluate whether blood-based genotoxicity endpoints can provide temporal and dose-response data within the low-dose carcinogenic range that could contribute to carcinogenic mode of action (MoA) assessments, we evaluated the sensitivity of flow cytometry-based micronucleus and Pig-a gene mutation assays at and below tumorigenic dose rate 50 (TD50) levels."	( Pig-a gene mutation and micronucleated reticulocyte induction in rats exposed to tumorigenic doses of the leukemogenic agents chlorambucil, thiotepa, melphalan, and 1,3-propane sultone. Avlasevich, SL; Bemis, JC; Cottom, J; Dertinger, SD; Macgregor, JT; Mereness, J; Phonethepswath, S; Torous, DK, 2014)	0.61
" Finally, while drug dosage and drug resistance typically limit first-line mono-chemotherapy, HSA-FCBL, with its ability to compromise mitochondrial membrane integrity and damage mtDNA, is expected to overcome those limitations to become an ideal candidate for the treatment of neoplastic disease."	( A Multi-Mitochondrial Anticancer Agent that Selectively Kills Cancer Cells and Overcomes Drug Resistance. Deng, TG; Hu, XX; Jin, C; Li, X; Liu, T; Peng, YB; Sun, Y; Tan, WH; Xie, GJ; Ye, M; Zhang, XB; Zhao, ZL, 2017)	0.46
" Long-term follow-up trials focused on gonadal toxicity and limitation of maximum dosage of cyclophosphamide should been carried out."	( Efficacy and acceptability of immunosuppressive agents for pediatric frequently-relapsing and steroid-dependent nephrotic syndrome: A network meta-analysis of randomized controlled trials. Li, Q; Li, S; Tan, L; Wan, J; Yang, H; Zou, Q, 2019)	0.51
" To more thoroughly investigate the dose-response relationships, benchmark dose (BMD) analyses were performed with PROAST software."	( Pig-a gene mutation assay study design: critical assessment of 3- versus 28-day repeat-dose treatment schedules. Dertinger, SD; Elhajouji, A; Hove, TT; Martus, H; O'Connell, O, 2020)	0.56
" Descriptive statistics were used to evaluate patient demographics, toxicity, duration and dosing of obinutuzumab treatment."	( Real world risk of infusion reactions and effectiveness of front-line obinutuzumab plus chlorambucil compared with other frontline treatments for chronic lymphocytic leukemia. Banerji, V; Bourrier, N; Bucher, O; Dawe, DE; Geirnaert, M; Gibson, SB; Hibbert, I; Johnston, JB; Landego, I; Squires, M; Streu, E; Whiteside, T, 2022)	0.94
" Many patients had difficulty tolerating the full dosage of chlorambucil."	( Real world risk of infusion reactions and effectiveness of front-line obinutuzumab plus chlorambucil compared with other frontline treatments for chronic lymphocytic leukemia. Banerji, V; Bourrier, N; Bucher, O; Dawe, DE; Geirnaert, M; Gibson, SB; Hibbert, I; Johnston, JB; Landego, I; Squires, M; Streu, E; Whiteside, T, 2022)	1.19
" Modifications in chlorambucil dosing and obinutuzumab administration can improve tolerance without significant loss in efficacy."	( Real world risk of infusion reactions and effectiveness of front-line obinutuzumab plus chlorambucil compared with other frontline treatments for chronic lymphocytic leukemia. Banerji, V; Bourrier, N; Bucher, O; Dawe, DE; Geirnaert, M; Gibson, SB; Hibbert, I; Johnston, JB; Landego, I; Squires, M; Streu, E; Whiteside, T, 2022)	1.28
" Ibrutinib dosing was held (≥7 days) for 79 patients and reduced for 31 patients because of AEs; these AEs resolved or improved in 85% (67 of 79) and 90% (28 of 31) of patients, respectively."	( Up to 8-year follow-up from RESONATE-2: first-line ibrutinib treatment for patients with chronic lymphocytic leukemia. Bairey, O; Barr, PM; Burger, JA; Coutre, SE; Dearden, C; Ghia, P; Grosicki, S; Hillmen, P; Hsu, E; Kipps, TJ; Li, JY; McCarthy, H; Moreno, C; Offner, F; Owen, C; Robak, T; Szoke, A; Tedeschi, A; Zhou, C, 2022)	0.72

Role	Description
alkylating agent	Highly reactive chemical that introduces alkyl radicals into biologically active molecules and thereby prevents their proper functioning. It could be used as an antineoplastic agent, but it might be very toxic, with carcinogenic, mutagenic, teratogenic, and immunosuppressant actions. It could also be used as a component of poison gases.
carcinogenic agent	A role played by a chemical compound which is known to induce a process of carcinogenesis by corrupting normal cellular pathways, leading to the acquistion of tumoral capabilities.
antineoplastic agent	A substance that inhibits or prevents the proliferation of neoplasms.
immunosuppressive agent	An agent that suppresses immune function by one of several mechanisms of action. Classical cytotoxic immunosuppressants act by inhibiting DNA synthesis. Others may act through activation of T-cells or by inhibiting the activation of helper cells. In addition, an immunosuppressive agent is a role played by a compound which is exhibited by a capability to diminish the extent and/or voracity of an immune response.
drug allergen	Any drug which causes the onset of an allergic reaction.
[role information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Class	Description
nitrogen mustard	Compounds having two beta-haloalkyl groups bound to a nitrogen atom, as in (X-CH2-CH2)2NR.
organochlorine compound	An organochlorine compound is a compound containing at least one carbon-chlorine bond.
aromatic amine	An amino compound in which the amino group is linked directly to an aromatic system.
tertiary amino compound	A compound formally derived from ammonia by replacing three hydrogen atoms by organyl groups.
monocarboxylic acid	An oxoacid containing a single carboxy group.
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Protein	Taxonomy	Measurement	Average (µ)	Min (ref.)	Avg (ref.)	Max (ref.)	Bioassay(s)
Luciferase	Photinus pyralis (common eastern firefly)	Potency	16.9441	0.0072	15.7588	89.3584	AID588342
interleukin 8	Homo sapiens (human)	Potency	74.9780	0.0473	49.4806	74.9780	AID651758
thioredoxin reductase	Rattus norvegicus (Norway rat)	Potency	23.0217	0.1000	20.8793	79.4328	AID488773; AID588453
RAR-related orphan receptor gamma	Mus musculus (house mouse)	Potency	39.3864	0.0060	38.0041	19,952.5996	AID1159521; AID1159523
NFKB1 protein, partial	Homo sapiens (human)	Potency	8.9125	0.0282	7.0559	15.8489	AID895; AID928
GALC protein	Homo sapiens (human)	Potency	0.7079	28.1838	28.1838	28.1838	AID1159614
GLS protein	Homo sapiens (human)	Potency	28.1838	0.3548	7.9355	39.8107	AID624170
TDP1 protein	Homo sapiens (human)	Potency	7.7066	0.0008	11.3822	44.6684	AID686978; AID686979
GLI family zinc finger 3	Homo sapiens (human)	Potency	39.1968	0.0007	14.5928	83.7951	AID1259369; AID1259392
Microtubule-associated protein tau	Homo sapiens (human)	Potency	19.6333	0.1800	13.5574	39.8107	AID1460
Thrombopoietin	Homo sapiens (human)	Potency	10.0000	0.0251	7.3048	31.6228	AID917; AID918
AR protein	Homo sapiens (human)	Potency	30.8911	0.0002	21.2231	8,912.5098	AID588516; AID743063
thioredoxin glutathione reductase	Schistosoma mansoni	Potency	50.1187	0.1000	22.9075	100.0000	AID485364
caspase 7, apoptosis-related cysteine protease	Homo sapiens (human)	Potency	77.2720	0.0133	26.9810	70.7614	AID1346978
aldehyde dehydrogenase 1 family, member A1	Homo sapiens (human)	Potency	1.8870	0.0112	12.4002	100.0000	AID1030
hypoxia-inducible factor 1, alpha subunit (basic helix-loop-helix transcription factor)	Homo sapiens (human)	Potency	10.2869	0.0013	7.7625	44.6684	AID914; AID915
thyroid stimulating hormone receptor	Homo sapiens (human)	Potency	6.6102	0.0013	18.0743	39.8107	AID926; AID938
nuclear receptor subfamily 1, group I, member 3	Homo sapiens (human)	Potency	30.5867	0.0010	22.6508	76.6163	AID1224838; AID1224893
EWS/FLI fusion protein	Homo sapiens (human)	Potency	23.1748	0.0013	10.1577	42.8575	AID1259252; AID1259253; AID1259255; AID1259256
retinoic acid nuclear receptor alpha variant 1	Homo sapiens (human)	Potency	68.5896	0.0030	41.6115	22,387.1992	AID1159552
estrogen-related nuclear receptor alpha	Homo sapiens (human)	Potency	52.8818	0.0015	30.6073	15,848.9004	AID1224841; AID1224842; AID1224848; AID1224849; AID1259401
pregnane X nuclear receptor	Homo sapiens (human)	Potency	77.2720	0.0054	28.0263	1,258.9301	AID1346982
estrogen nuclear receptor alpha	Homo sapiens (human)	Potency	20.2337	0.0002	29.3054	16,493.5996	AID743069; AID743075; AID743079
bromodomain adjacent to zinc finger domain 2B	Homo sapiens (human)	Potency	56.2341	0.7079	36.9043	89.1251	AID504333
peroxisome proliferator-activated receptor delta	Homo sapiens (human)	Potency	39.8107	0.0010	24.5048	61.6448	AID588534
vitamin D (1,25- dihydroxyvitamin D3) receptor	Homo sapiens (human)	Potency	2.7660	0.0237	23.2282	63.5986	AID743222
caspase-3	Homo sapiens (human)	Potency	77.2720	0.0133	26.9810	70.7614	AID1346978
euchromatic histone-lysine N-methyltransferase 2	Homo sapiens (human)	Potency	22.0267	0.0355	20.9770	89.1251	AID504332
cytochrome P450, family 19, subfamily A, polypeptide 1, isoform CRA_a	Homo sapiens (human)	Potency	16.5352	0.0017	23.8393	78.1014	AID743083
activating transcription factor 6	Homo sapiens (human)	Potency	39.8670	0.1434	27.6121	59.8106	AID1159516
v-jun sarcoma virus 17 oncogene homolog (avian)	Homo sapiens (human)	Potency	43.7154	0.0578	21.1097	61.2679	AID1159526; AID1159528
Histone H2A.x	Cricetulus griseus (Chinese hamster)	Potency	67.6180	0.0391	47.5451	146.8240	AID1224845; AID1224896
Bloom syndrome protein isoform 1	Homo sapiens (human)	Potency	0.0008	0.5406	17.6392	96.1227	AID2364; AID2528
peripheral myelin protein 22 isoform 1	Homo sapiens (human)	Potency	33.8078	23.9341	23.9341	23.9341	AID1967
vitamin D3 receptor isoform VDRA	Homo sapiens (human)	Potency	79.4328	0.3548	28.0659	89.1251	AID504847
chromobox protein homolog 1	Homo sapiens (human)	Potency	28.1838	0.0060	26.1688	89.1251	AID488953
potassium voltage-gated channel subfamily H member 2 isoform d	Homo sapiens (human)	Potency	35.4813	0.0178	9.6374	44.6684	AID588834
thyroid hormone receptor beta isoform 2	Rattus norvegicus (Norway rat)	Potency	33.7847	0.0003	23.4451	159.6830	AID743065; AID743067
nuclear factor erythroid 2-related factor 2 isoform 1	Homo sapiens (human)	Potency	52.3336	0.0006	27.2152	1,122.0200	AID651741; AID720636; AID743202; AID743219
urokinase-type plasminogen activator precursor	Mus musculus (house mouse)	Potency	7.0795	0.1585	5.2879	12.5893	AID540303
plasminogen precursor	Mus musculus (house mouse)	Potency	7.0795	0.1585	5.2879	12.5893	AID540303
urokinase plasminogen activator surface receptor precursor	Mus musculus (house mouse)	Potency	7.0795	0.1585	5.2879	12.5893	AID540303
geminin	Homo sapiens (human)	Potency	20.5113	0.0046	11.3741	33.4983	AID463097; AID624296; AID624297
peripheral myelin protein 22	Rattus norvegicus (Norway rat)	Potency	9.0743	0.0056	12.3677	36.1254	AID624032
survival motor neuron protein isoform d	Homo sapiens (human)	Potency	19.9526	0.1259	12.2344	35.4813	AID1458
muscleblind-like protein 1 isoform 1	Homo sapiens (human)	Potency	100.0000	0.0041	9.9625	28.1838	AID2675
muscarinic acetylcholine receptor M1	Rattus norvegicus (Norway rat)	Potency	35.4813	0.0010	6.0009	35.4813	AID943; AID944
lamin isoform A-delta10	Homo sapiens (human)	Potency	15.5432	0.8913	12.0676	28.1838	AID1459; AID1487
Cellular tumor antigen p53	Homo sapiens (human)	Potency	38.2126	0.0023	19.5956	74.0614	AID651631; AID651743; AID720552
Nuclear receptor ROR-gamma	Homo sapiens (human)	Potency	66.8242	0.0266	22.4482	66.8242	AID651802
Spike glycoprotein	Severe acute respiratory syndrome-related coronavirus	Potency	22.3872	0.0096	10.5250	35.4813	AID1479145
ATPase family AAA domain-containing protein 5	Homo sapiens (human)	Potency	61.8528	0.0119	17.9420	71.5630	AID651632; AID720516
Ataxin-2	Homo sapiens (human)	Potency	61.2549	0.0119	12.2221	68.7989	AID651632
ATP-dependent phosphofructokinase	Trypanosoma brucei brucei TREU927	Potency	8.4921	0.0601	10.7453	37.9330	AID485368
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Protein	Taxonomy	Measurement	Average	Min (ref.)	Avg (ref.)	Max (ref.)	Bioassay(s)
ATP-binding cassette sub-family C member 3	Homo sapiens (human)	IC50 (µMol)	133.0000	0.6315	4.4531	9.3000	AID1473740
Multidrug resistance-associated protein 4	Homo sapiens (human)	IC50 (µMol)	133.0000	0.2000	5.6774	10.0000	AID1473741
Carbonic anhydrase 12	Homo sapiens (human)	Ki	50.0000	0.0002	1.1043	9.9000	AID1425990
Bile salt export pump	Homo sapiens (human)	IC50 (µMol)	134.0000	0.1100	7.1903	10.0000	AID1443980; AID1473738
Carbonic anhydrase 1	Homo sapiens (human)	Ki	50.0000	0.0000	1.3726	10.0000	AID1425987
Carbonic anhydrase 2	Homo sapiens (human)	Ki	50.0000	0.0000	0.7236	9.9200	AID1425988
Cytochrome P450 2D6	Homo sapiens (human)	IC50 (µMol)	65.1000	0.0000	2.0151	10.0000	AID240619
Carbonic anhydrase 9	Homo sapiens (human)	Ki	50.0000	0.0001	0.7874	9.9000	AID1425989
Canalicular multispecific organic anion transporter 1	Homo sapiens (human)	IC50 (µMol)	133.0000	2.4100	6.3433	10.0000	AID1473739
Solute carrier organic anion transporter family member 1B3	Homo sapiens (human)	IC50 (µMol)	80.7000	0.1047	2.7195	7.0795	AID1197747
Solute carrier organic anion transporter family member 1B3	Homo sapiens (human)	Ki	37.4000	0.0800	2.4688	9.8000	AID1197747
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Protein	Taxonomy	Measurement	Average	Min (ref.)	Avg (ref.)	Max (ref.)	Bioassay(s)
FAD-linked sulfhydryl oxidase ALR	Homo sapiens (human)	AC50	0.0050	0.0050	3.2126	22.7870	AID493248
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Process	via Protein(s)	Taxonomy
xenobiotic metabolic process	ATP-binding cassette sub-family C member 3	Homo sapiens (human)
xenobiotic transmembrane transport	ATP-binding cassette sub-family C member 3	Homo sapiens (human)
bile acid and bile salt transport	ATP-binding cassette sub-family C member 3	Homo sapiens (human)
glucuronoside transport	ATP-binding cassette sub-family C member 3	Homo sapiens (human)
xenobiotic transport	ATP-binding cassette sub-family C member 3	Homo sapiens (human)
transmembrane transport	ATP-binding cassette sub-family C member 3	Homo sapiens (human)
leukotriene transport	ATP-binding cassette sub-family C member 3	Homo sapiens (human)
monoatomic anion transmembrane transport	ATP-binding cassette sub-family C member 3	Homo sapiens (human)
transport across blood-brain barrier	ATP-binding cassette sub-family C member 3	Homo sapiens (human)
prostaglandin secretion	Multidrug resistance-associated protein 4	Homo sapiens (human)
cilium assembly	Multidrug resistance-associated protein 4	Homo sapiens (human)
platelet degranulation	Multidrug resistance-associated protein 4	Homo sapiens (human)
xenobiotic metabolic process	Multidrug resistance-associated protein 4	Homo sapiens (human)
xenobiotic transmembrane transport	Multidrug resistance-associated protein 4	Homo sapiens (human)
bile acid and bile salt transport	Multidrug resistance-associated protein 4	Homo sapiens (human)
prostaglandin transport	Multidrug resistance-associated protein 4	Homo sapiens (human)
urate transport	Multidrug resistance-associated protein 4	Homo sapiens (human)
glutathione transmembrane transport	Multidrug resistance-associated protein 4	Homo sapiens (human)
transmembrane transport	Multidrug resistance-associated protein 4	Homo sapiens (human)
cAMP transport	Multidrug resistance-associated protein 4	Homo sapiens (human)
leukotriene transport	Multidrug resistance-associated protein 4	Homo sapiens (human)
monoatomic anion transmembrane transport	Multidrug resistance-associated protein 4	Homo sapiens (human)
export across plasma membrane	Multidrug resistance-associated protein 4	Homo sapiens (human)
transport across blood-brain barrier	Multidrug resistance-associated protein 4	Homo sapiens (human)
guanine nucleotide transmembrane transport	Multidrug resistance-associated protein 4	Homo sapiens (human)
estrous cycle	Carbonic anhydrase 12	Homo sapiens (human)
chloride ion homeostasis	Carbonic anhydrase 12	Homo sapiens (human)
one-carbon metabolic process	Carbonic anhydrase 12	Homo sapiens (human)
fatty acid metabolic process	Bile salt export pump	Homo sapiens (human)
bile acid biosynthetic process	Bile salt export pump	Homo sapiens (human)
xenobiotic metabolic process	Bile salt export pump	Homo sapiens (human)
xenobiotic transmembrane transport	Bile salt export pump	Homo sapiens (human)
response to oxidative stress	Bile salt export pump	Homo sapiens (human)
bile acid metabolic process	Bile salt export pump	Homo sapiens (human)
response to organic cyclic compound	Bile salt export pump	Homo sapiens (human)
bile acid and bile salt transport	Bile salt export pump	Homo sapiens (human)
canalicular bile acid transport	Bile salt export pump	Homo sapiens (human)
protein ubiquitination	Bile salt export pump	Homo sapiens (human)
regulation of fatty acid beta-oxidation	Bile salt export pump	Homo sapiens (human)
carbohydrate transmembrane transport	Bile salt export pump	Homo sapiens (human)
bile acid signaling pathway	Bile salt export pump	Homo sapiens (human)
cholesterol homeostasis	Bile salt export pump	Homo sapiens (human)
response to estrogen	Bile salt export pump	Homo sapiens (human)
response to ethanol	Bile salt export pump	Homo sapiens (human)
xenobiotic export from cell	Bile salt export pump	Homo sapiens (human)
lipid homeostasis	Bile salt export pump	Homo sapiens (human)
phospholipid homeostasis	Bile salt export pump	Homo sapiens (human)
positive regulation of bile acid secretion	Bile salt export pump	Homo sapiens (human)
regulation of bile acid metabolic process	Bile salt export pump	Homo sapiens (human)
transmembrane transport	Bile salt export pump	Homo sapiens (human)
one-carbon metabolic process	Carbonic anhydrase 1	Homo sapiens (human)
morphogenesis of an epithelium	Carbonic anhydrase 2	Homo sapiens (human)
positive regulation of synaptic transmission, GABAergic	Carbonic anhydrase 2	Homo sapiens (human)
positive regulation of cellular pH reduction	Carbonic anhydrase 2	Homo sapiens (human)
angiotensin-activated signaling pathway	Carbonic anhydrase 2	Homo sapiens (human)
regulation of monoatomic anion transport	Carbonic anhydrase 2	Homo sapiens (human)
secretion	Carbonic anhydrase 2	Homo sapiens (human)
regulation of intracellular pH	Carbonic anhydrase 2	Homo sapiens (human)
neuron cellular homeostasis	Carbonic anhydrase 2	Homo sapiens (human)
positive regulation of dipeptide transmembrane transport	Carbonic anhydrase 2	Homo sapiens (human)
regulation of chloride transport	Carbonic anhydrase 2	Homo sapiens (human)
carbon dioxide transport	Carbonic anhydrase 2	Homo sapiens (human)
one-carbon metabolic process	Carbonic anhydrase 2	Homo sapiens (human)
negative regulation of cell population proliferation	Cellular tumor antigen p53	Homo sapiens (human)
regulation of cell cycle	Cellular tumor antigen p53	Homo sapiens (human)
regulation of cell cycle G2/M phase transition	Cellular tumor antigen p53	Homo sapiens (human)
DNA damage response	Cellular tumor antigen p53	Homo sapiens (human)
ER overload response	Cellular tumor antigen p53	Homo sapiens (human)
cellular response to glucose starvation	Cellular tumor antigen p53	Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to DNA damage by p53 class mediator	Cellular tumor antigen p53	Homo sapiens (human)
regulation of apoptotic process	Cellular tumor antigen p53	Homo sapiens (human)
positive regulation of transcription by RNA polymerase II	Cellular tumor antigen p53	Homo sapiens (human)
positive regulation of miRNA transcription	Cellular tumor antigen p53	Homo sapiens (human)
negative regulation of transcription by RNA polymerase II	Cellular tumor antigen p53	Homo sapiens (human)
mitophagy	Cellular tumor antigen p53	Homo sapiens (human)
in utero embryonic development	Cellular tumor antigen p53	Homo sapiens (human)
somitogenesis	Cellular tumor antigen p53	Homo sapiens (human)
release of cytochrome c from mitochondria	Cellular tumor antigen p53	Homo sapiens (human)
hematopoietic progenitor cell differentiation	Cellular tumor antigen p53	Homo sapiens (human)
T cell proliferation involved in immune response	Cellular tumor antigen p53	Homo sapiens (human)
B cell lineage commitment	Cellular tumor antigen p53	Homo sapiens (human)
T cell lineage commitment	Cellular tumor antigen p53	Homo sapiens (human)
response to ischemia	Cellular tumor antigen p53	Homo sapiens (human)
nucleotide-excision repair	Cellular tumor antigen p53	Homo sapiens (human)
double-strand break repair	Cellular tumor antigen p53	Homo sapiens (human)
regulation of DNA-templated transcription	Cellular tumor antigen p53	Homo sapiens (human)
regulation of transcription by RNA polymerase II	Cellular tumor antigen p53	Homo sapiens (human)
protein import into nucleus	Cellular tumor antigen p53	Homo sapiens (human)
autophagy	Cellular tumor antigen p53	Homo sapiens (human)
DNA damage response	Cellular tumor antigen p53	Homo sapiens (human)
DNA damage response, signal transduction by p53 class mediator resulting in cell cycle arrest	Cellular tumor antigen p53	Homo sapiens (human)
DNA damage response, signal transduction by p53 class mediator resulting in transcription of p21 class mediator	Cellular tumor antigen p53	Homo sapiens (human)
transforming growth factor beta receptor signaling pathway	Cellular tumor antigen p53	Homo sapiens (human)
Ras protein signal transduction	Cellular tumor antigen p53	Homo sapiens (human)
gastrulation	Cellular tumor antigen p53	Homo sapiens (human)
neuroblast proliferation	Cellular tumor antigen p53	Homo sapiens (human)
negative regulation of neuroblast proliferation	Cellular tumor antigen p53	Homo sapiens (human)
protein localization	Cellular tumor antigen p53	Homo sapiens (human)
negative regulation of DNA replication	Cellular tumor antigen p53	Homo sapiens (human)
negative regulation of cell population proliferation	Cellular tumor antigen p53	Homo sapiens (human)
determination of adult lifespan	Cellular tumor antigen p53	Homo sapiens (human)
mRNA transcription	Cellular tumor antigen p53	Homo sapiens (human)
rRNA transcription	Cellular tumor antigen p53	Homo sapiens (human)
response to salt stress	Cellular tumor antigen p53	Homo sapiens (human)
response to inorganic substance	Cellular tumor antigen p53	Homo sapiens (human)
response to X-ray	Cellular tumor antigen p53	Homo sapiens (human)
response to gamma radiation	Cellular tumor antigen p53	Homo sapiens (human)
positive regulation of gene expression	Cellular tumor antigen p53	Homo sapiens (human)
cardiac muscle cell apoptotic process	Cellular tumor antigen p53	Homo sapiens (human)
positive regulation of cardiac muscle cell apoptotic process	Cellular tumor antigen p53	Homo sapiens (human)
glial cell proliferation	Cellular tumor antigen p53	Homo sapiens (human)
viral process	Cellular tumor antigen p53	Homo sapiens (human)
glucose catabolic process to lactate via pyruvate	Cellular tumor antigen p53	Homo sapiens (human)
cerebellum development	Cellular tumor antigen p53	Homo sapiens (human)
negative regulation of cell growth	Cellular tumor antigen p53	Homo sapiens (human)
DNA damage response, signal transduction by p53 class mediator	Cellular tumor antigen p53	Homo sapiens (human)
negative regulation of transforming growth factor beta receptor signaling pathway	Cellular tumor antigen p53	Homo sapiens (human)
mitotic G1 DNA damage checkpoint signaling	Cellular tumor antigen p53	Homo sapiens (human)
negative regulation of telomere maintenance via telomerase	Cellular tumor antigen p53	Homo sapiens (human)
T cell differentiation in thymus	Cellular tumor antigen p53	Homo sapiens (human)
tumor necrosis factor-mediated signaling pathway	Cellular tumor antigen p53	Homo sapiens (human)
regulation of tissue remodeling	Cellular tumor antigen p53	Homo sapiens (human)
cellular response to UV	Cellular tumor antigen p53	Homo sapiens (human)
multicellular organism growth	Cellular tumor antigen p53	Homo sapiens (human)
positive regulation of mitochondrial membrane permeability	Cellular tumor antigen p53	Homo sapiens (human)
cellular response to glucose starvation	Cellular tumor antigen p53	Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to DNA damage by p53 class mediator	Cellular tumor antigen p53	Homo sapiens (human)
positive regulation of apoptotic process	Cellular tumor antigen p53	Homo sapiens (human)
negative regulation of apoptotic process	Cellular tumor antigen p53	Homo sapiens (human)
entrainment of circadian clock by photoperiod	Cellular tumor antigen p53	Homo sapiens (human)
mitochondrial DNA repair	Cellular tumor antigen p53	Homo sapiens (human)
regulation of DNA damage response, signal transduction by p53 class mediator	Cellular tumor antigen p53	Homo sapiens (human)
positive regulation of neuron apoptotic process	Cellular tumor antigen p53	Homo sapiens (human)
transcription initiation-coupled chromatin remodeling	Cellular tumor antigen p53	Homo sapiens (human)
negative regulation of proteolysis	Cellular tumor antigen p53	Homo sapiens (human)
negative regulation of DNA-templated transcription	Cellular tumor antigen p53	Homo sapiens (human)
positive regulation of DNA-templated transcription	Cellular tumor antigen p53	Homo sapiens (human)
positive regulation of RNA polymerase II transcription preinitiation complex assembly	Cellular tumor antigen p53	Homo sapiens (human)
positive regulation of transcription by RNA polymerase II	Cellular tumor antigen p53	Homo sapiens (human)
response to antibiotic	Cellular tumor antigen p53	Homo sapiens (human)
fibroblast proliferation	Cellular tumor antigen p53	Homo sapiens (human)
negative regulation of fibroblast proliferation	Cellular tumor antigen p53	Homo sapiens (human)
circadian behavior	Cellular tumor antigen p53	Homo sapiens (human)
bone marrow development	Cellular tumor antigen p53	Homo sapiens (human)
embryonic organ development	Cellular tumor antigen p53	Homo sapiens (human)
positive regulation of peptidyl-tyrosine phosphorylation	Cellular tumor antigen p53	Homo sapiens (human)
protein stabilization	Cellular tumor antigen p53	Homo sapiens (human)
negative regulation of helicase activity	Cellular tumor antigen p53	Homo sapiens (human)
protein tetramerization	Cellular tumor antigen p53	Homo sapiens (human)
chromosome organization	Cellular tumor antigen p53	Homo sapiens (human)
neuron apoptotic process	Cellular tumor antigen p53	Homo sapiens (human)
regulation of cell cycle	Cellular tumor antigen p53	Homo sapiens (human)
hematopoietic stem cell differentiation	Cellular tumor antigen p53	Homo sapiens (human)
negative regulation of glial cell proliferation	Cellular tumor antigen p53	Homo sapiens (human)
type II interferon-mediated signaling pathway	Cellular tumor antigen p53	Homo sapiens (human)
cardiac septum morphogenesis	Cellular tumor antigen p53	Homo sapiens (human)
positive regulation of programmed necrotic cell death	Cellular tumor antigen p53	Homo sapiens (human)
protein-containing complex assembly	Cellular tumor antigen p53	Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to endoplasmic reticulum stress	Cellular tumor antigen p53	Homo sapiens (human)
thymocyte apoptotic process	Cellular tumor antigen p53	Homo sapiens (human)
positive regulation of thymocyte apoptotic process	Cellular tumor antigen p53	Homo sapiens (human)
necroptotic process	Cellular tumor antigen p53	Homo sapiens (human)
cellular response to hypoxia	Cellular tumor antigen p53	Homo sapiens (human)
cellular response to xenobiotic stimulus	Cellular tumor antigen p53	Homo sapiens (human)
cellular response to ionizing radiation	Cellular tumor antigen p53	Homo sapiens (human)
cellular response to gamma radiation	Cellular tumor antigen p53	Homo sapiens (human)
cellular response to UV-C	Cellular tumor antigen p53	Homo sapiens (human)
stem cell proliferation	Cellular tumor antigen p53	Homo sapiens (human)
signal transduction by p53 class mediator	Cellular tumor antigen p53	Homo sapiens (human)
intrinsic apoptotic signaling pathway by p53 class mediator	Cellular tumor antigen p53	Homo sapiens (human)
reactive oxygen species metabolic process	Cellular tumor antigen p53	Homo sapiens (human)
cellular response to actinomycin D	Cellular tumor antigen p53	Homo sapiens (human)
positive regulation of release of cytochrome c from mitochondria	Cellular tumor antigen p53	Homo sapiens (human)
cellular senescence	Cellular tumor antigen p53	Homo sapiens (human)
replicative senescence	Cellular tumor antigen p53	Homo sapiens (human)
oxidative stress-induced premature senescence	Cellular tumor antigen p53	Homo sapiens (human)
intrinsic apoptotic signaling pathway	Cellular tumor antigen p53	Homo sapiens (human)
oligodendrocyte apoptotic process	Cellular tumor antigen p53	Homo sapiens (human)
positive regulation of execution phase of apoptosis	Cellular tumor antigen p53	Homo sapiens (human)
negative regulation of mitophagy	Cellular tumor antigen p53	Homo sapiens (human)
regulation of mitochondrial membrane permeability involved in apoptotic process	Cellular tumor antigen p53	Homo sapiens (human)
regulation of intrinsic apoptotic signaling pathway by p53 class mediator	Cellular tumor antigen p53	Homo sapiens (human)
positive regulation of miRNA transcription	Cellular tumor antigen p53	Homo sapiens (human)
negative regulation of G1 to G0 transition	Cellular tumor antigen p53	Homo sapiens (human)
negative regulation of miRNA processing	Cellular tumor antigen p53	Homo sapiens (human)
negative regulation of glucose catabolic process to lactate via pyruvate	Cellular tumor antigen p53	Homo sapiens (human)
negative regulation of pentose-phosphate shunt	Cellular tumor antigen p53	Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to hypoxia	Cellular tumor antigen p53	Homo sapiens (human)
regulation of fibroblast apoptotic process	Cellular tumor antigen p53	Homo sapiens (human)
negative regulation of reactive oxygen species metabolic process	Cellular tumor antigen p53	Homo sapiens (human)
positive regulation of reactive oxygen species metabolic process	Cellular tumor antigen p53	Homo sapiens (human)
negative regulation of stem cell proliferation	Cellular tumor antigen p53	Homo sapiens (human)
positive regulation of cellular senescence	Cellular tumor antigen p53	Homo sapiens (human)
positive regulation of intrinsic apoptotic signaling pathway	Cellular tumor antigen p53	Homo sapiens (human)
xenobiotic metabolic process	Cytochrome P450 2D6	Homo sapiens (human)
steroid metabolic process	Cytochrome P450 2D6	Homo sapiens (human)
cholesterol metabolic process	Cytochrome P450 2D6	Homo sapiens (human)
estrogen metabolic process	Cytochrome P450 2D6	Homo sapiens (human)
coumarin metabolic process	Cytochrome P450 2D6	Homo sapiens (human)
alkaloid metabolic process	Cytochrome P450 2D6	Homo sapiens (human)
alkaloid catabolic process	Cytochrome P450 2D6	Homo sapiens (human)
monoterpenoid metabolic process	Cytochrome P450 2D6	Homo sapiens (human)
isoquinoline alkaloid metabolic process	Cytochrome P450 2D6	Homo sapiens (human)
xenobiotic catabolic process	Cytochrome P450 2D6	Homo sapiens (human)
retinol metabolic process	Cytochrome P450 2D6	Homo sapiens (human)
long-chain fatty acid biosynthetic process	Cytochrome P450 2D6	Homo sapiens (human)
negative regulation of binding	Cytochrome P450 2D6	Homo sapiens (human)
oxidative demethylation	Cytochrome P450 2D6	Homo sapiens (human)
negative regulation of cellular organofluorine metabolic process	Cytochrome P450 2D6	Homo sapiens (human)
arachidonic acid metabolic process	Cytochrome P450 2D6	Homo sapiens (human)
negative regulation of transcription by RNA polymerase II	Nuclear receptor ROR-gamma	Homo sapiens (human)
xenobiotic metabolic process	Nuclear receptor ROR-gamma	Homo sapiens (human)
regulation of glucose metabolic process	Nuclear receptor ROR-gamma	Homo sapiens (human)
regulation of steroid metabolic process	Nuclear receptor ROR-gamma	Homo sapiens (human)
intracellular receptor signaling pathway	Nuclear receptor ROR-gamma	Homo sapiens (human)
circadian regulation of gene expression	Nuclear receptor ROR-gamma	Homo sapiens (human)
cellular response to sterol	Nuclear receptor ROR-gamma	Homo sapiens (human)
positive regulation of circadian rhythm	Nuclear receptor ROR-gamma	Homo sapiens (human)
regulation of fat cell differentiation	Nuclear receptor ROR-gamma	Homo sapiens (human)
positive regulation of DNA-templated transcription	Nuclear receptor ROR-gamma	Homo sapiens (human)
adipose tissue development	Nuclear receptor ROR-gamma	Homo sapiens (human)
T-helper 17 cell differentiation	Nuclear receptor ROR-gamma	Homo sapiens (human)
regulation of transcription by RNA polymerase II	Nuclear receptor ROR-gamma	Homo sapiens (human)
response to hypoxia	Carbonic anhydrase 9	Homo sapiens (human)
morphogenesis of an epithelium	Carbonic anhydrase 9	Homo sapiens (human)
response to xenobiotic stimulus	Carbonic anhydrase 9	Homo sapiens (human)
response to testosterone	Carbonic anhydrase 9	Homo sapiens (human)
secretion	Carbonic anhydrase 9	Homo sapiens (human)
one-carbon metabolic process	Carbonic anhydrase 9	Homo sapiens (human)
xenobiotic metabolic process	Canalicular multispecific organic anion transporter 1	Homo sapiens (human)
xenobiotic transmembrane transport	Canalicular multispecific organic anion transporter 1	Homo sapiens (human)
negative regulation of gene expression	Canalicular multispecific organic anion transporter 1	Homo sapiens (human)
bile acid and bile salt transport	Canalicular multispecific organic anion transporter 1	Homo sapiens (human)
bilirubin transport	Canalicular multispecific organic anion transporter 1	Homo sapiens (human)
heme catabolic process	Canalicular multispecific organic anion transporter 1	Homo sapiens (human)
xenobiotic export from cell	Canalicular multispecific organic anion transporter 1	Homo sapiens (human)
transmembrane transport	Canalicular multispecific organic anion transporter 1	Homo sapiens (human)
transepithelial transport	Canalicular multispecific organic anion transporter 1	Homo sapiens (human)
leukotriene transport	Canalicular multispecific organic anion transporter 1	Homo sapiens (human)
monoatomic anion transmembrane transport	Canalicular multispecific organic anion transporter 1	Homo sapiens (human)
transport across blood-brain barrier	Canalicular multispecific organic anion transporter 1	Homo sapiens (human)
xenobiotic transport across blood-brain barrier	Canalicular multispecific organic anion transporter 1	Homo sapiens (human)
cell population proliferation	ATPase family AAA domain-containing protein 5	Homo sapiens (human)
positive regulation of B cell proliferation	ATPase family AAA domain-containing protein 5	Homo sapiens (human)
nuclear DNA replication	ATPase family AAA domain-containing protein 5	Homo sapiens (human)
signal transduction in response to DNA damage	ATPase family AAA domain-containing protein 5	Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to DNA damage by p53 class mediator	ATPase family AAA domain-containing protein 5	Homo sapiens (human)
isotype switching	ATPase family AAA domain-containing protein 5	Homo sapiens (human)
positive regulation of DNA replication	ATPase family AAA domain-containing protein 5	Homo sapiens (human)
positive regulation of isotype switching to IgG isotypes	ATPase family AAA domain-containing protein 5	Homo sapiens (human)
DNA clamp unloading	ATPase family AAA domain-containing protein 5	Homo sapiens (human)
regulation of mitotic cell cycle phase transition	ATPase family AAA domain-containing protein 5	Homo sapiens (human)
negative regulation of intrinsic apoptotic signaling pathway in response to DNA damage by p53 class mediator	ATPase family AAA domain-containing protein 5	Homo sapiens (human)
positive regulation of cell cycle G2/M phase transition	ATPase family AAA domain-containing protein 5	Homo sapiens (human)
negative regulation of receptor internalization	Ataxin-2	Homo sapiens (human)
regulation of translation	Ataxin-2	Homo sapiens (human)
RNA metabolic process	Ataxin-2	Homo sapiens (human)
P-body assembly	Ataxin-2	Homo sapiens (human)
stress granule assembly	Ataxin-2	Homo sapiens (human)
RNA transport	Ataxin-2	Homo sapiens (human)
xenobiotic metabolic process	Solute carrier organic anion transporter family member 1B3	Homo sapiens (human)
monoatomic ion transport	Solute carrier organic anion transporter family member 1B3	Homo sapiens (human)
organic anion transport	Solute carrier organic anion transporter family member 1B3	Homo sapiens (human)
bile acid and bile salt transport	Solute carrier organic anion transporter family member 1B3	Homo sapiens (human)
heme catabolic process	Solute carrier organic anion transporter family member 1B3	Homo sapiens (human)
sodium-independent organic anion transport	Solute carrier organic anion transporter family member 1B3	Homo sapiens (human)
transmembrane transport	Solute carrier organic anion transporter family member 1B3	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Process	via Protein(s)	Taxonomy
ATP binding	ATP-binding cassette sub-family C member 3	Homo sapiens (human)
ABC-type xenobiotic transporter activity	ATP-binding cassette sub-family C member 3	Homo sapiens (human)
glucuronoside transmembrane transporter activity	ATP-binding cassette sub-family C member 3	Homo sapiens (human)
ABC-type glutathione S-conjugate transporter activity	ATP-binding cassette sub-family C member 3	Homo sapiens (human)
ABC-type bile acid transporter activity	ATP-binding cassette sub-family C member 3	Homo sapiens (human)
ATP hydrolysis activity	ATP-binding cassette sub-family C member 3	Homo sapiens (human)
ATPase-coupled transmembrane transporter activity	ATP-binding cassette sub-family C member 3	Homo sapiens (human)
xenobiotic transmembrane transporter activity	ATP-binding cassette sub-family C member 3	Homo sapiens (human)
ATPase-coupled inorganic anion transmembrane transporter activity	ATP-binding cassette sub-family C member 3	Homo sapiens (human)
icosanoid transmembrane transporter activity	ATP-binding cassette sub-family C member 3	Homo sapiens (human)
ABC-type transporter activity	ATP-binding cassette sub-family C member 3	Homo sapiens (human)
guanine nucleotide transmembrane transporter activity	Multidrug resistance-associated protein 4	Homo sapiens (human)
protein binding	Multidrug resistance-associated protein 4	Homo sapiens (human)
ATP binding	Multidrug resistance-associated protein 4	Homo sapiens (human)
ABC-type xenobiotic transporter activity	Multidrug resistance-associated protein 4	Homo sapiens (human)
prostaglandin transmembrane transporter activity	Multidrug resistance-associated protein 4	Homo sapiens (human)
urate transmembrane transporter activity	Multidrug resistance-associated protein 4	Homo sapiens (human)
purine nucleotide transmembrane transporter activity	Multidrug resistance-associated protein 4	Homo sapiens (human)
ABC-type glutathione S-conjugate transporter activity	Multidrug resistance-associated protein 4	Homo sapiens (human)
ABC-type bile acid transporter activity	Multidrug resistance-associated protein 4	Homo sapiens (human)
efflux transmembrane transporter activity	Multidrug resistance-associated protein 4	Homo sapiens (human)
15-hydroxyprostaglandin dehydrogenase (NAD+) activity	Multidrug resistance-associated protein 4	Homo sapiens (human)
ATP hydrolysis activity	Multidrug resistance-associated protein 4	Homo sapiens (human)
glutathione transmembrane transporter activity	Multidrug resistance-associated protein 4	Homo sapiens (human)
ATPase-coupled transmembrane transporter activity	Multidrug resistance-associated protein 4	Homo sapiens (human)
xenobiotic transmembrane transporter activity	Multidrug resistance-associated protein 4	Homo sapiens (human)
ATPase-coupled inorganic anion transmembrane transporter activity	Multidrug resistance-associated protein 4	Homo sapiens (human)
ABC-type transporter activity	Multidrug resistance-associated protein 4	Homo sapiens (human)
zinc ion binding	Carbonic anhydrase 12	Homo sapiens (human)
carbonate dehydratase activity	Carbonic anhydrase 12	Homo sapiens (human)
protein binding	Bile salt export pump	Homo sapiens (human)
ATP binding	Bile salt export pump	Homo sapiens (human)
ABC-type xenobiotic transporter activity	Bile salt export pump	Homo sapiens (human)
bile acid transmembrane transporter activity	Bile salt export pump	Homo sapiens (human)
canalicular bile acid transmembrane transporter activity	Bile salt export pump	Homo sapiens (human)
carbohydrate transmembrane transporter activity	Bile salt export pump	Homo sapiens (human)
ABC-type bile acid transporter activity	Bile salt export pump	Homo sapiens (human)
ATP hydrolysis activity	Bile salt export pump	Homo sapiens (human)
arylesterase activity	Carbonic anhydrase 1	Homo sapiens (human)
carbonate dehydratase activity	Carbonic anhydrase 1	Homo sapiens (human)
protein binding	Carbonic anhydrase 1	Homo sapiens (human)
zinc ion binding	Carbonic anhydrase 1	Homo sapiens (human)
hydro-lyase activity	Carbonic anhydrase 1	Homo sapiens (human)
cyanamide hydratase activity	Carbonic anhydrase 1	Homo sapiens (human)
arylesterase activity	Carbonic anhydrase 2	Homo sapiens (human)
carbonate dehydratase activity	Carbonic anhydrase 2	Homo sapiens (human)
protein binding	Carbonic anhydrase 2	Homo sapiens (human)
zinc ion binding	Carbonic anhydrase 2	Homo sapiens (human)
cyanamide hydratase activity	Carbonic anhydrase 2	Homo sapiens (human)
transcription cis-regulatory region binding	Cellular tumor antigen p53	Homo sapiens (human)
RNA polymerase II cis-regulatory region sequence-specific DNA binding	Cellular tumor antigen p53	Homo sapiens (human)
DNA-binding transcription factor activity, RNA polymerase II-specific	Cellular tumor antigen p53	Homo sapiens (human)
cis-regulatory region sequence-specific DNA binding	Cellular tumor antigen p53	Homo sapiens (human)
core promoter sequence-specific DNA binding	Cellular tumor antigen p53	Homo sapiens (human)
TFIID-class transcription factor complex binding	Cellular tumor antigen p53	Homo sapiens (human)
DNA-binding transcription repressor activity, RNA polymerase II-specific	Cellular tumor antigen p53	Homo sapiens (human)
DNA-binding transcription activator activity, RNA polymerase II-specific	Cellular tumor antigen p53	Homo sapiens (human)
protease binding	Cellular tumor antigen p53	Homo sapiens (human)
p53 binding	Cellular tumor antigen p53	Homo sapiens (human)
DNA binding	Cellular tumor antigen p53	Homo sapiens (human)
chromatin binding	Cellular tumor antigen p53	Homo sapiens (human)
DNA-binding transcription factor activity	Cellular tumor antigen p53	Homo sapiens (human)
mRNA 3'-UTR binding	Cellular tumor antigen p53	Homo sapiens (human)
copper ion binding	Cellular tumor antigen p53	Homo sapiens (human)
protein binding	Cellular tumor antigen p53	Homo sapiens (human)
zinc ion binding	Cellular tumor antigen p53	Homo sapiens (human)
enzyme binding	Cellular tumor antigen p53	Homo sapiens (human)
receptor tyrosine kinase binding	Cellular tumor antigen p53	Homo sapiens (human)
ubiquitin protein ligase binding	Cellular tumor antigen p53	Homo sapiens (human)
histone deacetylase regulator activity	Cellular tumor antigen p53	Homo sapiens (human)
ATP-dependent DNA/DNA annealing activity	Cellular tumor antigen p53	Homo sapiens (human)
identical protein binding	Cellular tumor antigen p53	Homo sapiens (human)
histone deacetylase binding	Cellular tumor antigen p53	Homo sapiens (human)
protein heterodimerization activity	Cellular tumor antigen p53	Homo sapiens (human)
protein-folding chaperone binding	Cellular tumor antigen p53	Homo sapiens (human)
protein phosphatase 2A binding	Cellular tumor antigen p53	Homo sapiens (human)
RNA polymerase II-specific DNA-binding transcription factor binding	Cellular tumor antigen p53	Homo sapiens (human)
14-3-3 protein binding	Cellular tumor antigen p53	Homo sapiens (human)
MDM2/MDM4 family protein binding	Cellular tumor antigen p53	Homo sapiens (human)
disordered domain specific binding	Cellular tumor antigen p53	Homo sapiens (human)
general transcription initiation factor binding	Cellular tumor antigen p53	Homo sapiens (human)
molecular function activator activity	Cellular tumor antigen p53	Homo sapiens (human)
promoter-specific chromatin binding	Cellular tumor antigen p53	Homo sapiens (human)
monooxygenase activity	Cytochrome P450 2D6	Homo sapiens (human)
iron ion binding	Cytochrome P450 2D6	Homo sapiens (human)
oxidoreductase activity	Cytochrome P450 2D6	Homo sapiens (human)
oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygen	Cytochrome P450 2D6	Homo sapiens (human)
heme binding	Cytochrome P450 2D6	Homo sapiens (human)
anandamide 8,9 epoxidase activity	Cytochrome P450 2D6	Homo sapiens (human)
anandamide 11,12 epoxidase activity	Cytochrome P450 2D6	Homo sapiens (human)
anandamide 14,15 epoxidase activity	Cytochrome P450 2D6	Homo sapiens (human)
RNA polymerase II cis-regulatory region sequence-specific DNA binding	Nuclear receptor ROR-gamma	Homo sapiens (human)
DNA-binding transcription factor activity, RNA polymerase II-specific	Nuclear receptor ROR-gamma	Homo sapiens (human)
DNA-binding transcription repressor activity, RNA polymerase II-specific	Nuclear receptor ROR-gamma	Homo sapiens (human)
DNA-binding transcription factor activity	Nuclear receptor ROR-gamma	Homo sapiens (human)
protein binding	Nuclear receptor ROR-gamma	Homo sapiens (human)
oxysterol binding	Nuclear receptor ROR-gamma	Homo sapiens (human)
zinc ion binding	Nuclear receptor ROR-gamma	Homo sapiens (human)
ligand-activated transcription factor activity	Nuclear receptor ROR-gamma	Homo sapiens (human)
sequence-specific double-stranded DNA binding	Nuclear receptor ROR-gamma	Homo sapiens (human)
nuclear receptor activity	Nuclear receptor ROR-gamma	Homo sapiens (human)
carbonate dehydratase activity	Carbonic anhydrase 9	Homo sapiens (human)
protein binding	Carbonic anhydrase 9	Homo sapiens (human)
zinc ion binding	Carbonic anhydrase 9	Homo sapiens (human)
molecular function activator activity	Carbonic anhydrase 9	Homo sapiens (human)
protein binding	Canalicular multispecific organic anion transporter 1	Homo sapiens (human)
ATP binding	Canalicular multispecific organic anion transporter 1	Homo sapiens (human)
organic anion transmembrane transporter activity	Canalicular multispecific organic anion transporter 1	Homo sapiens (human)
ABC-type xenobiotic transporter activity	Canalicular multispecific organic anion transporter 1	Homo sapiens (human)
bilirubin transmembrane transporter activity	Canalicular multispecific organic anion transporter 1	Homo sapiens (human)
ABC-type glutathione S-conjugate transporter activity	Canalicular multispecific organic anion transporter 1	Homo sapiens (human)
ATP hydrolysis activity	Canalicular multispecific organic anion transporter 1	Homo sapiens (human)
ATPase-coupled transmembrane transporter activity	Canalicular multispecific organic anion transporter 1	Homo sapiens (human)
xenobiotic transmembrane transporter activity	Canalicular multispecific organic anion transporter 1	Homo sapiens (human)
ATPase-coupled inorganic anion transmembrane transporter activity	Canalicular multispecific organic anion transporter 1	Homo sapiens (human)
ABC-type transporter activity	Canalicular multispecific organic anion transporter 1	Homo sapiens (human)
protein binding	ATPase family AAA domain-containing protein 5	Homo sapiens (human)
ATP binding	ATPase family AAA domain-containing protein 5	Homo sapiens (human)
ATP hydrolysis activity	ATPase family AAA domain-containing protein 5	Homo sapiens (human)
DNA clamp unloader activity	ATPase family AAA domain-containing protein 5	Homo sapiens (human)
DNA binding	ATPase family AAA domain-containing protein 5	Homo sapiens (human)
RNA binding	Ataxin-2	Homo sapiens (human)
epidermal growth factor receptor binding	Ataxin-2	Homo sapiens (human)
protein binding	Ataxin-2	Homo sapiens (human)
mRNA binding	Ataxin-2	Homo sapiens (human)
serine-type endopeptidase inhibitor activity	Solute carrier organic anion transporter family member 1B3	Homo sapiens (human)
organic anion transmembrane transporter activity	Solute carrier organic anion transporter family member 1B3	Homo sapiens (human)
bile acid transmembrane transporter activity	Solute carrier organic anion transporter family member 1B3	Homo sapiens (human)
sodium-independent organic anion transmembrane transporter activity	Solute carrier organic anion transporter family member 1B3	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Process	via Protein(s)	Taxonomy
plasma membrane	ATP-binding cassette sub-family C member 3	Homo sapiens (human)
basal plasma membrane	ATP-binding cassette sub-family C member 3	Homo sapiens (human)
basolateral plasma membrane	ATP-binding cassette sub-family C member 3	Homo sapiens (human)
membrane	ATP-binding cassette sub-family C member 3	Homo sapiens (human)
nucleolus	Multidrug resistance-associated protein 4	Homo sapiens (human)
Golgi apparatus	Multidrug resistance-associated protein 4	Homo sapiens (human)
plasma membrane	Multidrug resistance-associated protein 4	Homo sapiens (human)
membrane	Multidrug resistance-associated protein 4	Homo sapiens (human)
basolateral plasma membrane	Multidrug resistance-associated protein 4	Homo sapiens (human)
apical plasma membrane	Multidrug resistance-associated protein 4	Homo sapiens (human)
platelet dense granule membrane	Multidrug resistance-associated protein 4	Homo sapiens (human)
external side of apical plasma membrane	Multidrug resistance-associated protein 4	Homo sapiens (human)
plasma membrane	Multidrug resistance-associated protein 4	Homo sapiens (human)
plasma membrane	Carbonic anhydrase 12	Homo sapiens (human)
membrane	Carbonic anhydrase 12	Homo sapiens (human)
basolateral plasma membrane	Carbonic anhydrase 12	Homo sapiens (human)
apical plasma membrane	Carbonic anhydrase 12	Homo sapiens (human)
plasma membrane	Carbonic anhydrase 12	Homo sapiens (human)
basolateral plasma membrane	Bile salt export pump	Homo sapiens (human)
Golgi membrane	Bile salt export pump	Homo sapiens (human)
endosome	Bile salt export pump	Homo sapiens (human)
plasma membrane	Bile salt export pump	Homo sapiens (human)
cell surface	Bile salt export pump	Homo sapiens (human)
apical plasma membrane	Bile salt export pump	Homo sapiens (human)
intercellular canaliculus	Bile salt export pump	Homo sapiens (human)
intracellular canaliculus	Bile salt export pump	Homo sapiens (human)
recycling endosome	Bile salt export pump	Homo sapiens (human)
recycling endosome membrane	Bile salt export pump	Homo sapiens (human)
extracellular exosome	Bile salt export pump	Homo sapiens (human)
membrane	Bile salt export pump	Homo sapiens (human)
cytosol	Carbonic anhydrase 1	Homo sapiens (human)
extracellular exosome	Carbonic anhydrase 1	Homo sapiens (human)
cytoplasm	Carbonic anhydrase 2	Homo sapiens (human)
cytosol	Carbonic anhydrase 2	Homo sapiens (human)
plasma membrane	Carbonic anhydrase 2	Homo sapiens (human)
myelin sheath	Carbonic anhydrase 2	Homo sapiens (human)
apical part of cell	Carbonic anhydrase 2	Homo sapiens (human)
extracellular exosome	Carbonic anhydrase 2	Homo sapiens (human)
cytoplasm	Carbonic anhydrase 2	Homo sapiens (human)
plasma membrane	Carbonic anhydrase 2	Homo sapiens (human)
apical part of cell	Carbonic anhydrase 2	Homo sapiens (human)
nuclear body	Cellular tumor antigen p53	Homo sapiens (human)
nucleus	Cellular tumor antigen p53	Homo sapiens (human)
nucleoplasm	Cellular tumor antigen p53	Homo sapiens (human)
replication fork	Cellular tumor antigen p53	Homo sapiens (human)
nucleolus	Cellular tumor antigen p53	Homo sapiens (human)
cytoplasm	Cellular tumor antigen p53	Homo sapiens (human)
mitochondrion	Cellular tumor antigen p53	Homo sapiens (human)
mitochondrial matrix	Cellular tumor antigen p53	Homo sapiens (human)
endoplasmic reticulum	Cellular tumor antigen p53	Homo sapiens (human)
centrosome	Cellular tumor antigen p53	Homo sapiens (human)
cytosol	Cellular tumor antigen p53	Homo sapiens (human)
nuclear matrix	Cellular tumor antigen p53	Homo sapiens (human)
PML body	Cellular tumor antigen p53	Homo sapiens (human)
transcription repressor complex	Cellular tumor antigen p53	Homo sapiens (human)
site of double-strand break	Cellular tumor antigen p53	Homo sapiens (human)
germ cell nucleus	Cellular tumor antigen p53	Homo sapiens (human)
chromatin	Cellular tumor antigen p53	Homo sapiens (human)
transcription regulator complex	Cellular tumor antigen p53	Homo sapiens (human)
protein-containing complex	Cellular tumor antigen p53	Homo sapiens (human)
mitochondrion	Cytochrome P450 2D6	Homo sapiens (human)
endoplasmic reticulum	Cytochrome P450 2D6	Homo sapiens (human)
endoplasmic reticulum membrane	Cytochrome P450 2D6	Homo sapiens (human)
cytoplasm	Cytochrome P450 2D6	Homo sapiens (human)
intracellular membrane-bounded organelle	Cytochrome P450 2D6	Homo sapiens (human)
nucleus	Nuclear receptor ROR-gamma	Homo sapiens (human)
nucleoplasm	Nuclear receptor ROR-gamma	Homo sapiens (human)
nuclear body	Nuclear receptor ROR-gamma	Homo sapiens (human)
chromatin	Nuclear receptor ROR-gamma	Homo sapiens (human)
nucleus	Nuclear receptor ROR-gamma	Homo sapiens (human)
virion membrane	Spike glycoprotein	Severe acute respiratory syndrome-related coronavirus
nucleolus	Carbonic anhydrase 9	Homo sapiens (human)
plasma membrane	Carbonic anhydrase 9	Homo sapiens (human)
membrane	Carbonic anhydrase 9	Homo sapiens (human)
basolateral plasma membrane	Carbonic anhydrase 9	Homo sapiens (human)
microvillus membrane	Carbonic anhydrase 9	Homo sapiens (human)
plasma membrane	Carbonic anhydrase 9	Homo sapiens (human)
plasma membrane	Canalicular multispecific organic anion transporter 1	Homo sapiens (human)
cell surface	Canalicular multispecific organic anion transporter 1	Homo sapiens (human)
apical plasma membrane	Canalicular multispecific organic anion transporter 1	Homo sapiens (human)
intercellular canaliculus	Canalicular multispecific organic anion transporter 1	Homo sapiens (human)
apical plasma membrane	Canalicular multispecific organic anion transporter 1	Homo sapiens (human)
Elg1 RFC-like complex	ATPase family AAA domain-containing protein 5	Homo sapiens (human)
nucleus	ATPase family AAA domain-containing protein 5	Homo sapiens (human)
cytoplasm	Ataxin-2	Homo sapiens (human)
Golgi apparatus	Ataxin-2	Homo sapiens (human)
trans-Golgi network	Ataxin-2	Homo sapiens (human)
cytosol	Ataxin-2	Homo sapiens (human)
cytoplasmic stress granule	Ataxin-2	Homo sapiens (human)
membrane	Ataxin-2	Homo sapiens (human)
perinuclear region of cytoplasm	Ataxin-2	Homo sapiens (human)
ribonucleoprotein complex	Ataxin-2	Homo sapiens (human)
cytoplasmic stress granule	Ataxin-2	Homo sapiens (human)
plasma membrane	Solute carrier organic anion transporter family member 1B3	Homo sapiens (human)
basal plasma membrane	Solute carrier organic anion transporter family member 1B3	Homo sapiens (human)
basolateral plasma membrane	Solute carrier organic anion transporter family member 1B3	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Assay ID	Title	Year	Journal	Article
AID1745845	Primary qHTS for Inhibitors of ATXN expression
AID588497	High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set	2010	Current protocols in cytometry, Oct, Volume: Chapter 13	Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588497	High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set	2006	Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5	Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588497	High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set	2010	Assay and drug development technologies, Feb, Volume: 8, Issue:1	High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID651635	Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
AID588499	High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set	2010	Current protocols in cytometry, Oct, Volume: Chapter 13	Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588499	High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set	2006	Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5	Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588499	High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set	2010	Assay and drug development technologies, Feb, Volume: 8, Issue:1	High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588501	High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set	2010	Current protocols in cytometry, Oct, Volume: Chapter 13	Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588501	High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set	2006	Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5	Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588501	High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set	2010	Assay and drug development technologies, Feb, Volume: 8, Issue:1	High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID1347094	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347119	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for MG 63 (6-TG R) cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347154	Primary screen GU AMC qHTS for Zika virus inhibitors	2020	Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49	Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347107	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347095	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347124	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for RD cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347115	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for NB-EBc1 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1296008	Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening	2020	SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1	Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1346987	P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen	2019	Molecular pharmacology, 11, Volume: 96, Issue:5	A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1347101	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347125	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh18 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347089	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347099	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347126	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh30 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347121	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for control Hh wild type fibroblast cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347113	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for LAN-5 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347128	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for OHS-50 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347111	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-MC cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347129	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-SH cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347118	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for TC32 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347086	qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal	2020	Antiviral research, 01, Volume: 173	A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347122	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for U-2 OS cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347114	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for DAOY cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347097	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347100	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1508630	Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay	2021	Cell reports, 04-27, Volume: 35, Issue:4	A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID1347116	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SJ-GBM2 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347096	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347093	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1346986	P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen	2019	Molecular pharmacology, 11, Volume: 96, Issue:5	A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1347104	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347112	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for BT-12 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347123	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh41 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347108	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347082	qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal	2020	Antiviral research, 01, Volume: 173	A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347102	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347109	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for NB1643 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347083	qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen	2020	Antiviral research, 01, Volume: 173	A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347127	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Saos-2 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347110	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for A673 cells)	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347103	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347091	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347117	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for BT-37 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347092	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347098	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347105	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347106	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347090	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1057216	Induction of nuclear DNA damage in human MIAPaCa2 cells assessed as increase in gammaH2A.X expression after 24 hrs by Western blotting analysis in presence of NAC relative to control	2013	Journal of medicinal chemistry, Nov-27, Volume: 56, Issue:22	A selective mitochondrial-targeted chlorambucil with remarkable cytotoxicity in breast and pancreatic cancers.
AID1437140	Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by MTT assay	2017	Bioorganic & medicinal chemistry letters, 02-15, Volume: 27, Issue:4	Synthesis and biological evaluation of 2-alkoxycarbonylallyl esters as potential anticancer agents.
AID1425995	Cytotoxicity against carbonic anhydrase 9 knockdown MDCK cells assessed as reduction in cell viability after 2 hrs under hypoxic condition by Alamar blue assay	2017	European journal of medicinal chemistry, Feb-15, Volume: 127	New approach of delivering cytotoxic drugs towards CAIX expressing cells: A concept of dual-target drugs.
AID1079948	Times to onset, minimal and maximal, observed in the indexed observations. [column 'DELAI' in source]
AID1185087	Anticancer activity against human Bel7402 cells assessed as growth inhibition by MTT assay	2014	ACS medicinal chemistry letters, Jul-10, Volume: 5, Issue:7	Novel hybrids of natural oridonin-bearing nitrogen mustards as potential anticancer drug candidates.
AID428450	Cytotoxicity against human WiDr cells after 5 days by MTT assay	2009	European journal of medicinal chemistry, Jul, Volume: 44, Issue:7	To determine the cytotoxicity of chlorambucil and one of its nitro-derivatives, conjugated to prasterone and pregnenolone, towards eight human cancer cell-lines.
AID1123203	Toxicity in icv dosed Swiss Webster mouse assessed as change in tail flick latency	1979	Journal of medicinal chemistry, Feb, Volume: 22, Issue:2	Synthesis and pharmacologic characterization of an alkylating analogue (chlornaltrexamine) of naltrexone with ultralong-lasting narcotic antagonist properties.
AID1383598	Antiproliferative activity against human LO2 cells after 72 hrs by MTT assay	2018	European journal of medicinal chemistry, Apr-25, Volume: 150	Novel hybrids of brefeldin A and nitrogen mustards with improved antiproliferative selectivity: Design, synthesis and antitumor biological evaluation.
AID121767	Antitumor activity measured as T/C at 0.066 nmol/kg dose against ip inoculated P388 leukemia in CDF1 mice	1983	Journal of medicinal chemistry, Aug, Volume: 26, Issue:8	1,3-dipalmitoylglycerol ester of chlorambucil as a lymphotropic, orally administrable antineoplastic agent.
AID121763	Antitumor activity measured as T/C at 0.033 nmol/kg dose against ip inoculated P388 leukemia in CDF1 mice	1983	Journal of medicinal chemistry, Aug, Volume: 26, Issue:8	1,3-dipalmitoylglycerol ester of chlorambucil as a lymphotropic, orally administrable antineoplastic agent.
AID1126679	In vitro antiproliferative activity against human K562 cells assessed as decrease in cell viability after 24 hrs by MTT assay	2014	European journal of medicinal chemistry, May-06, Volume: 78	Synthesis and kinase inhibitory activity of new sulfonamide derivatives of pyrazolo[4,3-e][1,2,4]triazines.
AID444050	Fraction unbound in human plasma	2010	Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3	Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID382351	Cytotoxicity against human DLD1 cells by resazurin reduction test	2008	Bioorganic & medicinal chemistry, May-01, Volume: 16, Issue:9	Synthesis and cytotoxic properties of new fluorodeoxyglucose-coupled chlorambucil derivatives.
AID1412106	Induction of apoptosis in human A375 cells assessed as late apoptotic cells at 16 uM after 72 hrs by Alexa Fluor 488 Annexin/propidium iodide staining-based flow cytometric analysis (Rvb = 10.22%)	2018	MedChemComm, Feb-01, Volume: 9, Issue:2	Rational design and characterization of a DNA/HDAC dual-targeting inhibitor containing nitrogen mustard and 2-aminobenzamide moieties.
AID26304	Partition coefficient (logD6.5)	2000	Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13	QSAR model for drug human oral bioavailability.
AID1057243	Cytotoxicity against human MDA-MB-468 cells after 72 hrs by MTT assay	2013	Journal of medicinal chemistry, Nov-27, Volume: 56, Issue:22	A selective mitochondrial-targeted chlorambucil with remarkable cytotoxicity in breast and pancreatic cancers.
AID1185081	Antiproliferative activity against human Bel7402 cells assessed as growth inhibition after 72 hrs by MTT assay	2014	ACS medicinal chemistry letters, Jul-10, Volume: 5, Issue:7	Novel hybrids of natural oridonin-bearing nitrogen mustards as potential anticancer drug candidates.
AID1425994	Cytotoxicity against MDCK cells expressing carbonic anhydrase 9 assessed as reduction in cell viability preincubated for 2 hrs followed by 72 hrs incubation under normoxic condition by Alamar blue assay	2017	European journal of medicinal chemistry, Feb-15, Volume: 127	New approach of delivering cytotoxic drugs towards CAIX expressing cells: A concept of dual-target drugs.
AID1079942	Steatosis, proven histopathologically. Value is number of references indexed. [column 'STEAT' in source]
AID1412087	Induction of DNA damage in human A375 cells assessed as phosphorylation of H2AX at Ser139 residues at 16 uM after 48 hrs relative to control	2018	MedChemComm, Feb-01, Volume: 9, Issue:2	Rational design and characterization of a DNA/HDAC dual-targeting inhibitor containing nitrogen mustard and 2-aminobenzamide moieties.
AID540212	Mean residence time in human after iv administration	2008	Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7	Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID598527	1-Octanol-sodium citrate buffer distribution coefficient, log D of the compound at pH 5.5 by shake-flask method	2011	Bioorganic & medicinal chemistry letters, Jun-15, Volume: 21, Issue:12	Lipophilicity of acidic compounds: impact of ion pair partitioning on drug design.
AID1057217	Induction of nuclear DNA damage in human MIAPaCa2 cells assessed as increase in gammaH2A.X expression after 24 hrs by Western blotting analysis relative to control	2013	Journal of medicinal chemistry, Nov-27, Volume: 56, Issue:22	A selective mitochondrial-targeted chlorambucil with remarkable cytotoxicity in breast and pancreatic cancers.
AID1412089	Antiproliferative activity against human A375 cells after 72 hrs CCK8 assay	2018	MedChemComm, Feb-01, Volume: 9, Issue:2	Rational design and characterization of a DNA/HDAC dual-targeting inhibitor containing nitrogen mustard and 2-aminobenzamide moieties.
AID1412100	Induction of apoptosis in human A375 cells assessed as viable cells at 2 uM after 72 hrs by Alexa Fluor 488 Annexin/propidium iodide staining-based flow cytometric analysis (Rvb = 86.07%)	2018	MedChemComm, Feb-01, Volume: 9, Issue:2	Rational design and characterization of a DNA/HDAC dual-targeting inhibitor containing nitrogen mustard and 2-aminobenzamide moieties.
AID382348	Cytotoxicity against human PC3 cells by resazurin reduction test	2008	Bioorganic & medicinal chemistry, May-01, Volume: 16, Issue:9	Synthesis and cytotoxic properties of new fluorodeoxyglucose-coupled chlorambucil derivatives.
AID1057223	Cell cycle arrest in human MIAPaCa2 cells assessed as increase of haplodiploid cells at 20 uM after 24 to 72 hrs by flow cytometry	2013	Journal of medicinal chemistry, Nov-27, Volume: 56, Issue:22	A selective mitochondrial-targeted chlorambucil with remarkable cytotoxicity in breast and pancreatic cancers.
AID1443980	Inhibition of human BSEP expressed in fall armyworm sf9 cell plasma membrane vesicles assessed as reduction in vesicle-associated [3H]-taurocholate transport preincubated for 10 mins prior to ATP addition measured after 15 mins in presence of [3H]-tauroch	2010	Toxicological sciences : an official journal of the Society of Toxicology, Dec, Volume: 118, Issue:2	Interference with bile salt export pump function is a susceptibility factor for human liver injury in drug development.
AID103944	Tested for in vitro concentration required to inhibit growth by 50% against MCF-7 human breast cancer cell line cell line	2002	Bioorganic & medicinal chemistry letters, Jan-21, Volume: 12, Issue:2	Polyhydroxylated azepanes as new motifs for DNA minor groove binding agents.
AID90117	Alkylating activity of compound remaining after 48 hours of incubation with 10% human blood serum	1998	Journal of medicinal chemistry, Jul-16, Volume: 41, Issue:15	Synthesis and in vitro efficacy of transferrin conjugates of the anticancer drug chlorambucil.
AID1274776	Antiproliferative activity against human MCF7 cells assessed as cell viability pre-incubated for 24 hrs with CO2 followed by compound addition after 72 hrs by MTT assay	2016	Journal of medicinal chemistry, Jan-14, Volume: 59, Issue:1	Synthesis and Biochemical Evaluation of 3-Phenoxy-1,4-diarylazetidin-2-ones as Tubulin-Targeting Antitumor Agents.
AID625287	Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatomegaly	2011	PLoS computational biology, Dec, Volume: 7, Issue:12	Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1126683	Cytostatic activity against human MCF7 cells assessed as decrease in [3H]thymidine incorporation into DNA after 24 hrs by liquid scintillation counting analysis	2014	European journal of medicinal chemistry, May-06, Volume: 78	Synthesis and kinase inhibitory activity of new sulfonamide derivatives of pyrazolo[4,3-e][1,2,4]triazines.
AID229128	Glutathione activity was measured after incubation with a conc. of 500 uM; ND= not determined	2001	Journal of medicinal chemistry, Mar-01, Volume: 44, Issue:5	Antimitotic antitumor agents: synthesis, structure-activity relationships, and biological characterization of N-aryl-N'-(2-chloroethyl)ureas as new selective alkylating agents.
AID116394	Antitumor a dose 0.16 nmol/kg against po inoculated P388 leukemia in CDF1 mice; Toxic	1983	Journal of medicinal chemistry, Aug, Volume: 26, Issue:8	1,3-dipalmitoylglycerol ester of chlorambucil as a lymphotropic, orally administrable antineoplastic agent.
AID47480	Growth inhibition against CH-1 wild-type ovarian cell lines	2004	Journal of medicinal chemistry, Mar-25, Volume: 47, Issue:7	Synthesis and biological evaluation of novel chloroethylaminoanthraquinones with potent cytotoxic activity against cisplatin-resistant tumor cells.
AID1272173	Half life in mouse liver homogenates by LC-MS analysis	2016	Bioorganic & medicinal chemistry, Jan-15, Volume: 24, Issue:2	Synthesis, biological studies and molecular dynamics of new anticancer RGD-based peptide conjugates for targeted drug delivery.
AID1378205	Cell cycle arrest in human WM266.4 cells assessed as accumulation at S phase at 10 uM cotreated with amonafide after 24 hrs by propidium iodide staining based flow cytometry (Rvb = 27%)	2017	European journal of medicinal chemistry, Sep-29, Volume: 138	Discovery of potent molecular chimera (CM358) to treat human metastatic melanoma.
AID75441	Glutathione reductase activity was measured after incubation with a conc. of 500 uM; ND= not determined	2001	Journal of medicinal chemistry, Mar-01, Volume: 44, Issue:5	Antimitotic antitumor agents: synthesis, structure-activity relationships, and biological characterization of N-aryl-N'-(2-chloroethyl)ureas as new selective alkylating agents.
AID104088	In vitro inhibitory activity against mammary carcinoma (MCF-7) cell line.	1998	Journal of medicinal chemistry, Jul-16, Volume: 41, Issue:15	Synthesis and in vitro efficacy of transferrin conjugates of the anticancer drug chlorambucil.
AID116386	Antitumor a dose 0.050 nmol/kg against ip inoculated P388 leukemia in CDF1 mice	1983	Journal of medicinal chemistry, Aug, Volume: 26, Issue:8	1,3-dipalmitoylglycerol ester of chlorambucil as a lymphotropic, orally administrable antineoplastic agent.
AID224901	In vivo antitumor activity against murine S-180 sarcoma at a dose of 1.3 mg/kg administered intraperitoneally 7qd in mice expressed effect on tumor weight	2001	Bioorganic & medicinal chemistry letters, May-07, Volume: 11, Issue:9	2-[N1-2-pyrimidyl-aminobenzenesulfonamido] ethyl 4-bis(2-chloroethyl) aminophenyl butyrate: a potent antitumor agent.
AID1473741	Inhibition of human MRP4 overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 20 mins by membrane vesicle transport assay	2013	Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1	A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID1437142	Antiproliferative activity against mouse 4T1 cells after 72 hrs by MTT assay	2017	Bioorganic & medicinal chemistry letters, 02-15, Volume: 27, Issue:4	Synthesis and biological evaluation of 2-alkoxycarbonylallyl esters as potential anticancer agents.
AID428552	Cytotoxicity against human A375 cells after 5 days by MTT assay	2009	European journal of medicinal chemistry, Jul, Volume: 44, Issue:7	To determine the cytotoxicity of chlorambucil and one of its nitro-derivatives, conjugated to prasterone and pregnenolone, towards eight human cancer cell-lines.
AID428443	Chemical stability in phosphate buffer saline assessed as half life by HPLC analysis	2009	European journal of medicinal chemistry, Jul, Volume: 44, Issue:7	To determine the cytotoxicity of chlorambucil and one of its nitro-derivatives, conjugated to prasterone and pregnenolone, towards eight human cancer cell-lines.
AID1465330	Antiproliferative activity against human HepG2 cells treated for 24 hrs measured after 72 hrs by MTT assay	2017	Bioorganic & medicinal chemistry letters, 11-15, Volume: 27, Issue:22	Design and synthesis of novel nitrogen mustard-evodiamine hybrids with selective antiproliferative activity.
AID1555213	Antiproliferative activity against human A549 cells incubated for 72 hrs by SRB assay
AID1473738	Inhibition of human BSEP overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-taurocholate in presence of ATP measured after 15 to 20 mins by membrane vesicle transport assay	2013	Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1	A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID1365048	Cell cycle arrest in human A375 cells assessed as accumulation at S phase at 8 uM after 72 hrs by propidium iodide staining based flow cytometry (Rvb = 3.8%)	2017	Bioorganic & medicinal chemistry letters, 09-15, Volume: 27, Issue:18	Rational design, synthesis and preliminary antitumor activity evaluation of a chlorambucil derivative with potent DNA/HDAC dual-targeting inhibitory activity.
AID539168	Cytotoxicity against estrogen receptor-negative human MDA-MB-468 cells by MTT assay	2010	Bioorganic & medicinal chemistry letters, Dec-15, Volume: 20, Issue:24	Synthesis of D- and L-tyrosine-chlorambucil analogs active against breast cancer cell lines.
AID101660	Dose required to inhibit cell growth was determined against MDA-MB-231 cell line of human non-hormone dependent breast carcinoma	2001	Journal of medicinal chemistry, Mar-01, Volume: 44, Issue:5	Antimitotic antitumor agents: synthesis, structure-activity relationships, and biological characterization of N-aryl-N'-(2-chloroethyl)ureas as new selective alkylating agents.
AID1383594	Antiproliferative activity against human HL60 cells after 72 hrs by MTT assay	2018	European journal of medicinal chemistry, Apr-25, Volume: 150	Novel hybrids of brefeldin A and nitrogen mustards with improved antiproliferative selectivity: Design, synthesis and antitumor biological evaluation.
AID230686	Ratio of activities reducing surviving fraction to 10% (T10) under aerobic vs hypoxic conditions	1995	Journal of medicinal chemistry, Mar-31, Volume: 38, Issue:7	Hypoxia-selective antitumor agents. 11. Chlorambucil N-oxide: a reappraisal of its synthesis, stability, and selective toxicity for hypoxic cells.
AID9478	Activity to reduce the surviving fraction to 10% (CT10) was used as an inverse measure of cytotoxic potency in aerobic conditions	1995	Journal of medicinal chemistry, Mar-31, Volume: 38, Issue:7	Hypoxia-selective antitumor agents. 11. Chlorambucil N-oxide: a reappraisal of its synthesis, stability, and selective toxicity for hypoxic cells.
AID1665881	Stability in simulated gastric fluid assessed as parent compound remaining at 1 uM measured after 4 hrs at pH 1.2 by LC-MS/MS analysis	2020	Journal of medicinal chemistry, 09-10, Volume: 63, Issue:17	Non-rigid Diarylmethyl Analogs of Baloxavir as Cap-Dependent Endonuclease Inhibitors of Influenza Viruses.
AID1365037	Induction of apoptosis in human A375 cells assessed as necrotic cells at 2 uM after 72 hrs by Annexin/propidium iodide staining based flow cytometry (Rvb = 1.36%)	2017	Bioorganic & medicinal chemistry letters, 09-15, Volume: 27, Issue:18	Rational design, synthesis and preliminary antitumor activity evaluation of a chlorambucil derivative with potent DNA/HDAC dual-targeting inhibitory activity.
AID382347	Cytotoxicity against human primary fibroblasts by resazurin reduction test	2008	Bioorganic & medicinal chemistry, May-01, Volume: 16, Issue:9	Synthesis and cytotoxic properties of new fluorodeoxyglucose-coupled chlorambucil derivatives.
AID1665950	Protein binding in human plasma at 1 uM measured after 4 hrs by LC-MS/MS analysis	2020	Journal of medicinal chemistry, 09-10, Volume: 63, Issue:17	Non-rigid Diarylmethyl Analogs of Baloxavir as Cap-Dependent Endonuclease Inhibitors of Influenza Viruses.
AID39711	Compound was evaluated for the antineoplastic activity on B16 Melanoma cells at the optimal dose of 24 mg/kg through intraperitoneal route on days 1,5,9	1985	Journal of medicinal chemistry, Nov, Volume: 28, Issue:11	Synthesis and properties of bis(2,2-dimethylaziridinyl)phosphinic amides: a series of new antineoplastic agents.
AID1365045	Induction of apoptosis in human A375 cells assessed as necrotic cells at 16 uM after 72 hrs by Annexin/propidium iodide staining based flow cytometry (Rvb = 1.36%)	2017	Bioorganic & medicinal chemistry letters, 09-15, Volume: 27, Issue:18	Rational design, synthesis and preliminary antitumor activity evaluation of a chlorambucil derivative with potent DNA/HDAC dual-targeting inhibitory activity.
AID315486	Cytotoxicity against PAT active CHO cells after 48 hrs	2008	Journal of medicinal chemistry, Mar-13, Volume: 51, Issue:5	A comparison of chloroambucil- and xylene-containing polyamines leads to improved ligands for accessing the polyamine transport system.
AID510599	Cytotoxicity against human H460 cells after 24 hrs by MTT assay	2010	European journal of medicinal chemistry, Sep, Volume: 45, Issue:9	Synthesis and biological evaluation of cyclic nitrogen mustards based on carnitine framework.
AID1378118	Growth inhibition of human MDA-MB-231 cells preincubated for 6 hrs cotreated with amonafide followed compound washout measured after 24 hrs by XTT assay	2017	European journal of medicinal chemistry, Sep-29, Volume: 138	Discovery of potent molecular chimera (CM358) to treat human metastatic melanoma.
AID1474167	Liver toxicity in human assessed as induction of drug-induced liver injury by measuring verified drug-induced liver injury concern status	2016	Drug discovery today, Apr, Volume: 21, Issue:4	DILIrank: the largest reference drug list ranked by the risk for developing drug-induced liver injury in humans.
AID1057244	Cytotoxicity against wild type human MDA-MB-435 cells after 72 hrs by MTT assay	2013	Journal of medicinal chemistry, Nov-27, Volume: 56, Issue:22	A selective mitochondrial-targeted chlorambucil with remarkable cytotoxicity in breast and pancreatic cancers.
AID382022	Antitumor activity in BDF1 mouse bearing P388 cells assessed as mean survival days at 7.5 mg/kg/day, ip	2008	Bioorganic & medicinal chemistry, May-01, Volume: 16, Issue:9	Rational design, synthesis, and in vivo evaluation of the antileukemic activity of six new alkylating steroidal esters.
AID1412095	Anticlonogenic activity against human A375 cells at 2 to 16 umol/L after 7 days by crystal violet staining based assay	2018	MedChemComm, Feb-01, Volume: 9, Issue:2	Rational design and characterization of a DNA/HDAC dual-targeting inhibitor containing nitrogen mustard and 2-aminobenzamide moieties.
AID315482	Cytotoxicity against mouse L1210 cells in presence of ODC inhibitor difluoromethylornithine	2008	Journal of medicinal chemistry, Mar-13, Volume: 51, Issue:5	A comparison of chloroambucil- and xylene-containing polyamines leads to improved ligands for accessing the polyamine transport system.
AID94466	Dose required to inhibit cell growth was determined against K562 cell line of chronic myelogenous leukemia	2001	Journal of medicinal chemistry, Mar-01, Volume: 44, Issue:5	Antimitotic antitumor agents: synthesis, structure-activity relationships, and biological characterization of N-aryl-N'-(2-chloroethyl)ureas as new selective alkylating agents.
AID1140115	Cytostatic activity against human MCF7 cells assessed as inhibition of DNA synthesis after 24 hrs by [3H]thymidine incorporation assay	2014	Bioorganic & medicinal chemistry, May-01, Volume: 22, Issue:9	Pyrazolo[4,3-e][1,2,4]triazine sulfonamides as carbonic anhydrase inhibitors with antitumor activity.
AID1378113	Growth inhibition of human PC3 cells preincubated for 6 hrs followed compound washout measured after 24 hrs by XTT assay	2017	European journal of medicinal chemistry, Sep-29, Volume: 138	Discovery of potent molecular chimera (CM358) to treat human metastatic melanoma.
AID1140117	Inhibition of collagen synthesis in human MCF7 cells assessed as 5-[3H]-proline incorporation into proteins susceptible to action of bacterial collagenase after 24 hrs	2014	Bioorganic & medicinal chemistry, May-01, Volume: 22, Issue:9	Pyrazolo[4,3-e][1,2,4]triazine sulfonamides as carbonic anhydrase inhibitors with antitumor activity.
AID1425987	Binding affinity to recombinant human carbonic anhydrase 1 after 15 mins by stopped-flow CO2 hydration assay	2017	European journal of medicinal chemistry, Feb-15, Volume: 127	New approach of delivering cytotoxic drugs towards CAIX expressing cells: A concept of dual-target drugs.
AID39869	In vitro cytotoxicity activity against B16 cells, by colony forming assay	2002	Journal of medicinal chemistry, May-09, Volume: 45, Issue:10	Synthesis and in vitro evaluation of quaternary ammonium derivatives of chlorambucil and melphalan, anticancer drugs designed for the chemotherapy of chondrosarcoma.
AID1584442	Antiproliferative activity against human NCI60 cells after 48 hrs by SRB assay	2018	Journal of medicinal chemistry, 10-25, Volume: 61, Issue:20	Discovery of Novel Topoisomerase II Inhibitors by Medicinal Chemistry Approaches.
AID215307	Growth inhibition activity was measured in repair deficient UV4 cells under aerobic conditions (4 hours drug exposure)	1995	Journal of medicinal chemistry, Mar-31, Volume: 38, Issue:7	Hypoxia-selective antitumor agents. 11. Chlorambucil N-oxide: a reappraisal of its synthesis, stability, and selective toxicity for hypoxic cells.
AID121773	Antitumor activity measured as T/C at 0.16 nmol/kg dose against po inoculated P388 leukemia in CDF1 mice; Toxic	1983	Journal of medicinal chemistry, Aug, Volume: 26, Issue:8	1,3-dipalmitoylglycerol ester of chlorambucil as a lymphotropic, orally administrable antineoplastic agent.
AID1057245	Cytotoxicity against wild type human MDA-MB-231 cells after 72 hrs by MTT assay	2013	Journal of medicinal chemistry, Nov-27, Volume: 56, Issue:22	A selective mitochondrial-targeted chlorambucil with remarkable cytotoxicity in breast and pancreatic cancers.
AID1412090	Antiproliferative activity against human SMMC7721 cells after 72 hrs CCK8 assay	2018	MedChemComm, Feb-01, Volume: 9, Issue:2	Rational design and characterization of a DNA/HDAC dual-targeting inhibitor containing nitrogen mustard and 2-aminobenzamide moieties.
AID689901	Induction of RARalpha recruitment to [gamma-32P]-5'-end labeled pUC18 DNA fragment at 1 mM after 30 mins by EMSA	2011	Bioorganic & medicinal chemistry letters, Jul-15, Volume: 21, Issue:14	A transcription factor hijacking to regulate RARα by using a chimeric molecule of retinoic acid and a DNA alkylator.
AID382352	Cytotoxicity against human M4Beu cells by resazurin reduction test	2008	Bioorganic & medicinal chemistry, May-01, Volume: 16, Issue:9	Synthesis and cytotoxic properties of new fluorodeoxyglucose-coupled chlorambucil derivatives.
AID1690736	Inhibition of EGFR phosphorylation in human PC-9 cells at 1 to 10 uM preincubated for 2 hrs followed by EGF stimulation and measured after 30 mins by Western blot analysis	2020	European journal of medicinal chemistry, Apr-15, Volume: 192	Comparative analysis of the dual EGFR-DNA targeting and growth inhibitory properties of 6-mono-alkylamino- and 6,6-dialkylaminoquinazoline-based type II combi-molecules.
AID1246952	Cytotoxicity against human MDA-MB-231 cells assessed as cell viability after 5 days by cell viability analyzer	2015	European journal of medicinal chemistry, Sep-18, Volume: 102	Design and synthesis of novel hydroxyanthraquinone nitrogen mustard derivatives as potential anticancer agents via a bioisostere approach.
AID1633074	Cytotoxicity against mouse NIH/3T3 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay	2017	Bioorganic & medicinal chemistry, 10-15, Volume: 25, Issue:20	A novel delocalized lipophilic cation-chlorambucil conjugate inhibits P-glycoprotein in HepG2/ADM cells.
AID1465333	Antiproliferative activity against human PBMC treated for 24 hrs measured after 72 hrs by MTT assay	2017	Bioorganic & medicinal chemistry letters, 11-15, Volume: 27, Issue:22	Design and synthesis of novel nitrogen mustard-evodiamine hybrids with selective antiproliferative activity.
AID711668	Inhibition of Pgp-mediated drug efflux in human A2780 cells overexpressing Pgp assessed as increase in intracellular adriamycin level at 5 uM after 40 mins by flow cytometry analysis	2011	ACS medicinal chemistry letters, Jun-09, Volume: 2, Issue:6	Peptide-chlorambucil conjugates combat pgp-dependent drug efflux.
AID625289	Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver disease	2011	PLoS computational biology, Dec, Volume: 7, Issue:12	Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID224890	Antitumor activity against murine S-180 sarcoma at dose of LD50 X 1/20 equal toxicity	2001	Bioorganic & medicinal chemistry letters, May-07, Volume: 11, Issue:9	2-[N1-2-pyrimidyl-aminobenzenesulfonamido] ethyl 4-bis(2-chloroethyl) aminophenyl butyrate: a potent antitumor agent.
AID1365042	Induction of apoptosis in human A375 cells assessed as live cells at 16 uM after 72 hrs by Annexin/propidium iodide staining based flow cytometry (Rvb = 86.07%)	2017	Bioorganic & medicinal chemistry letters, 09-15, Volume: 27, Issue:18	Rational design, synthesis and preliminary antitumor activity evaluation of a chlorambucil derivative with potent DNA/HDAC dual-targeting inhibitory activity.
AID625292	Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) combined score	2011	PLoS computational biology, Dec, Volume: 7, Issue:12	Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1378224	Toxicity in athymic Foxn1 nu mouse xenografted with human WM266.4 cells assessed as body weight loss at 10 mg/kg, ip cotreated with amonafide administered once daily for 7 days followed by resting period of 2 days repeated for 4 weeks starting from 5 days	2017	European journal of medicinal chemistry, Sep-29, Volume: 138	Discovery of potent molecular chimera (CM358) to treat human metastatic melanoma.
AID536572	Growth inhibition of human SF268 cells after 7 days by celltiter-glo assay	2010	Journal of medicinal chemistry, Nov-25, Volume: 53, Issue:22	Assessment of chemoselective neoglycosylation methods using chlorambucil as a model.
AID1378216	Antitumor activity against human WM266.4 cells xenografted in athymic Foxn1 nu mouse assessed as tumor growth inhibition at 10 mg/kg, ip cotreated with amonafide administered once daily for 3 days followed by resting period of 4 days repeated for 4 weeks	2017	European journal of medicinal chemistry, Sep-29, Volume: 138	Discovery of potent molecular chimera (CM358) to treat human metastatic melanoma.
AID1057246	Cytotoxicity against human MCF7 cells after 72 hrs by MTT assay	2013	Journal of medicinal chemistry, Nov-27, Volume: 56, Issue:22	A selective mitochondrial-targeted chlorambucil with remarkable cytotoxicity in breast and pancreatic cancers.
AID1378124	Growth inhibition of human A172 cells preincubated for 6 hrs cotreated with amonafide followed compound washout measured after 24 hrs by XTT assay	2017	European journal of medicinal chemistry, Sep-29, Volume: 138	Discovery of potent molecular chimera (CM358) to treat human metastatic melanoma.
AID1079940	Granulomatous liver disease, proven histopathologically. Value is number of references indexed. [column 'GRAN' in source]
AID1663615	Anticancer activity against human MCF7 cells assessed as cell growth inhibition measured after 48 hrs by MTT assay	2020	Bioorganic & medicinal chemistry letters, 07-15, Volume: 30, Issue:14	Synthesis and anticancer activity of open-resorcinarene conjugates.
AID1378204	Cell cycle arrest in human WM266.4 cells assessed as accumulation at G1 phase at 10 uM cotreated with amonafide after 24 hrs by propidium iodide staining based flow cytometry (Rvb = 59%)	2017	European journal of medicinal chemistry, Sep-29, Volume: 138	Discovery of potent molecular chimera (CM358) to treat human metastatic melanoma.
AID39712	Compound was evaluated for the antineoplastic activity on B16 Melanoma cells at the optimal dose of 36 mg/kg through intraperitoneal route on days 1,5, 9	1985	Journal of medicinal chemistry, Nov, Volume: 28, Issue:11	Synthesis and properties of bis(2,2-dimethylaziridinyl)phosphinic amides: a series of new antineoplastic agents.
AID1393845	Antiproliferative activity against human Bel7402/5-FU cells after 72 hrs by MTT assay	2018	European journal of medicinal chemistry, Feb-25, Volume: 146	Novel enmein-type diterpenoid hybrids coupled with nitrogen mustards: Synthesis of promising candidates for anticancer therapeutics.
AID467611	Dissociation constant, pKa of the compound	2009	European journal of medicinal chemistry, Nov, Volume: 44, Issue:11	Prediction of volume of distribution values in human using immobilized artificial membrane partitioning coefficients, the fraction of compound ionized and plasma protein binding data.
AID465021	Anticancer activity against human MDA-MB-436 cells assessed as cell survival after 72 hrs by MTT assay	2010	Bioorganic & medicinal chemistry letters, Mar-01, Volume: 20, Issue:5	Design, synthesis and biological evaluation of estradiol-chlorambucil hybrids as anticancer agents.
AID1079943	Malignant tumor, proven histopathologically. Value is number of references indexed. [column 'T.MAL' in source]
AID1079944	Benign tumor, proven histopathologically. Value is number of references indexed. [column 'T.BEN' in source]
AID444051	Total clearance in human	2010	Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3	Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID111726	Antitumor activity measured as Body weight change (BWC) between day 1 and 5 at 0.066 nmol/kg dose against sc inoculated P388 leukemia in CDF1 mice	1983	Journal of medicinal chemistry, Aug, Volume: 26, Issue:8	1,3-dipalmitoylglycerol ester of chlorambucil as a lymphotropic, orally administrable antineoplastic agent.
AID224880	In vivo antitumor activity against murine S-180 sarcoma at a dose of 1.3 mg/kg administered intraperitoneally 7qd in mice expressed as percent inhibition	2001	Bioorganic & medicinal chemistry letters, May-07, Volume: 11, Issue:9	2-[N1-2-pyrimidyl-aminobenzenesulfonamido] ethyl 4-bis(2-chloroethyl) aminophenyl butyrate: a potent antitumor agent.
AID465020	Anticancer activity against human MCF7 cells assessed as cell survival after 72 hrs by MTT assay	2010	Bioorganic & medicinal chemistry letters, Mar-01, Volume: 20, Issue:5	Design, synthesis and biological evaluation of estradiol-chlorambucil hybrids as anticancer agents.
AID111717	Antitumor activity measured as Body weight change (BWC) between day 1 and 5 at 0.033 nmol/kg dose against sc inoculated P388 leukemia in CDF1 mice	1983	Journal of medicinal chemistry, Aug, Volume: 26, Issue:8	1,3-dipalmitoylglycerol ester of chlorambucil as a lymphotropic, orally administrable antineoplastic agent.
AID1140114	Cytotoxicity against human MDA-MB-231 cells assessed as growth inhibition after 24 hrs by MTT assay	2014	Bioorganic & medicinal chemistry, May-01, Volume: 22, Issue:9	Pyrazolo[4,3-e][1,2,4]triazine sulfonamides as carbonic anhydrase inhibitors with antitumor activity.
AID1393843	Antiproliferative activity against human PC3 cells after 72 hrs by MTT assay	2018	European journal of medicinal chemistry, Feb-25, Volume: 146	Novel enmein-type diterpenoid hybrids coupled with nitrogen mustards: Synthesis of promising candidates for anticancer therapeutics.
AID382021	Acute toxicity in ip dosed BALB/c mouse after 30 days	2008	Bioorganic & medicinal chemistry, May-01, Volume: 16, Issue:9	Rational design, synthesis, and in vivo evaluation of the antileukemic activity of six new alkylating steroidal esters.
AID1250812	Induction of alkylation of 5'-FAM-labelled scrambled duplex oligonucleotide DNA (unknown origin) at guanine residues G1 to G4 at 50 uM after 24 hrs by sequencing gel analysis	2015	Bioorganic & medicinal chemistry letters, Oct-15, Volume: 25, Issue:20	Synthesis and evaluation of a bis-3-chloropiperidine derivative incorporating an anthraquinone pharmacophore.
AID1412108	Induction of apoptosis in human A375 cells assessed as viable cells at 16 uM after 72 hrs by Alexa Fluor 488 Annexin/propidium iodide staining-based flow cytometric analysis (Rvb = 86.07%)	2018	MedChemComm, Feb-01, Volume: 9, Issue:2	Rational design and characterization of a DNA/HDAC dual-targeting inhibitor containing nitrogen mustard and 2-aminobenzamide moieties.
AID1690737	Inhibition of EGFR phosphorylation in human A549 cells at 1 to 10 uM preincubated for 2 hrs followed by EGF stimulation and measured after 30 mins by Western blot analysis	2020	European journal of medicinal chemistry, Apr-15, Volume: 192	Comparative analysis of the dual EGFR-DNA targeting and growth inhibitory properties of 6-mono-alkylamino- and 6,6-dialkylaminoquinazoline-based type II combi-molecules.
AID229940	Hypersensitivity factor(HF) was determined from the ratio of IC50(AA8) / IC50(UV4)	1990	Journal of medicinal chemistry, Apr, Volume: 33, Issue:4	DNA-directed alkylating agents. 1. Structure-activity relationships for acridine-linked aniline mustards: consequences of varying the reactivity of the mustard.
AID224899	In vivo antitumor activity against murine S-180 sarcoma at a dose of 6.8 mg/kg administered intraperitoneally 7qd in Male TA1 mice; 9 survived out of 10 mice	2001	Bioorganic & medicinal chemistry letters, May-07, Volume: 11, Issue:9	2-[N1-2-pyrimidyl-aminobenzenesulfonamido] ethyl 4-bis(2-chloroethyl) aminophenyl butyrate: a potent antitumor agent.
AID382038	Antitumor activity in BDF1 mouse L1210 cells assessed as mean survival days at 7.5 mg/kg/day, ip	2008	Bioorganic & medicinal chemistry, May-01, Volume: 16, Issue:9	Rational design, synthesis, and in vivo evaluation of the antileukemic activity of six new alkylating steroidal esters.
AID1079933	Acute liver toxicity defined via clinical observations and clear clinical-chemistry results: serum ALT or AST activity > 6 N or serum alkaline phosphatases activity > 1.7 N. This category includes cytolytic, choleostatic and mixed liver toxicity. Value is
AID1140116	Cytostatic activity against human MDA-MB-231 cells assessed as inhibition of DNA synthesis after 24 hrs by [3H]thymidine incorporation assay	2014	Bioorganic & medicinal chemistry, May-01, Volume: 22, Issue:9	Pyrazolo[4,3-e][1,2,4]triazine sulfonamides as carbonic anhydrase inhibitors with antitumor activity.
AID350562	Cytotoxicity against human MT3 cells assessed as cell viability after 48 hrs by MTT assay	2009	Journal of medicinal chemistry, May-28, Volume: 52, Issue:10	Synthesis and biophysical characterization of chlorambucil anticancer ether lipid prodrugs.
AID540213	Half life in human after iv administration	2008	Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7	Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID1633592	Induction of Escherichia coli pBR322 DNA cleavage in BPE buffer at 5 to 50 uM incubated for 18 hrs by electrophoresis method	2019	ACS medicinal chemistry letters, Apr-11, Volume: 10, Issue:4	Behind the Mirror: Chirality Tunes the Reactivity and Cytotoxicity of Chloropiperidines as Potential Anticancer Agents.
AID1365031	Antiproliferative activity against human A375 cells after 72 hrs by CCK8 assay	2017	Bioorganic & medicinal chemistry letters, 09-15, Volume: 27, Issue:18	Rational design, synthesis and preliminary antitumor activity evaluation of a chlorambucil derivative with potent DNA/HDAC dual-targeting inhibitory activity.
AID1412086	Induction of DNA damage in human A375 cells assessed as phosphorylation of H2AX at Ser139 residues at 8 uM after 48 hrs relative to control	2018	MedChemComm, Feb-01, Volume: 9, Issue:2	Rational design and characterization of a DNA/HDAC dual-targeting inhibitor containing nitrogen mustard and 2-aminobenzamide moieties.
AID9655	Cytotoxicity against AA8 cell line	1990	Journal of medicinal chemistry, Nov, Volume: 33, Issue:11	DNA-directed alkylating agents. 3. Structure-activity relationships for acridine-linked aniline mustards: consequences of varying the length of the linker chain.
AID1365044	Induction of apoptosis in human A375 cells assessed as late apoptotic cells at 16 uM after 72 hrs by Annexin/propidium iodide staining based flow cytometry (Rvb = 6.95%)	2017	Bioorganic & medicinal chemistry letters, 09-15, Volume: 27, Issue:18	Rational design, synthesis and preliminary antitumor activity evaluation of a chlorambucil derivative with potent DNA/HDAC dual-targeting inhibitory activity.
AID1633092	Induction of apoptosis in human HepG2/ADM cells assessed as early apoptotic cells at 20 uM incubated for 72 hrs in presence of ADM by Annexin V-FITC/SYTOX Red staining based flow cytometric analysis (Rvb = 8.58%)	2017	Bioorganic & medicinal chemistry, 10-15, Volume: 25, Issue:20	A novel delocalized lipophilic cation-chlorambucil conjugate inhibits P-glycoprotein in HepG2/ADM cells.
AID1123204	Inhibition of morphine-induced analgesia in Swiss Webster mouse assessed as change in morphine ED50 at 2.4 nmol, icv after 2 hrs by tail flick test	1979	Journal of medicinal chemistry, Feb, Volume: 22, Issue:2	Synthesis and pharmacologic characterization of an alkylating analogue (chlornaltrexamine) of naltrexone with ultralong-lasting narcotic antagonist properties.
AID449933	Cytotoxicity against human NCI60 cells after 48 hrs by sulforhodamine B assay	2009	Bioorganic & medicinal chemistry, Sep-01, Volume: 17, Issue:17	Synthesis and evaluation of anticancer activity of 2-arylamino-6-trifluoromethyl-3-(hydrazonocarbonyl)pyridines.
AID1383596	Antiproliferative activity against human Bel7402 cells after 72 hrs by MTT assay	2018	European journal of medicinal chemistry, Apr-25, Volume: 150	Novel hybrids of brefeldin A and nitrogen mustards with improved antiproliferative selectivity: Design, synthesis and antitumor biological evaluation.
AID1633094	Induction of apoptosis in human HepG2/ADM cells assessed as necrotic cells at 20 uM incubated for 72 hrs in presence of ADM by Annexin V-FITC/SYTOX Red staining based flow cytometric analysis (Rvb =0.1%)	2017	Bioorganic & medicinal chemistry, 10-15, Volume: 25, Issue:20	A novel delocalized lipophilic cation-chlorambucil conjugate inhibits P-glycoprotein in HepG2/ADM cells.
AID1425989	Binding affinity to recombinant human carbonic anhydrase 9 after 15 mins by stopped-flow CO2 hydration assay	2017	European journal of medicinal chemistry, Feb-15, Volume: 127	New approach of delivering cytotoxic drugs towards CAIX expressing cells: A concept of dual-target drugs.
AID224736	Antitumor activity against murine S-180 sarcoma at dose of 0.008(mmol/kg)	2001	Bioorganic & medicinal chemistry letters, May-07, Volume: 11, Issue:9	2-[N1-2-pyrimidyl-aminobenzenesulfonamido] ethyl 4-bis(2-chloroethyl) aminophenyl butyrate: a potent antitumor agent.
AID1126682	In vitro antiproliferative activity against human CCRF-CEM cells assessed as decrease in cell viability after 24 hrs by MTT assay	2014	European journal of medicinal chemistry, May-06, Volume: 78	Synthesis and kinase inhibitory activity of new sulfonamide derivatives of pyrazolo[4,3-e][1,2,4]triazines.
AID28901	Partition coefficient (logD) (octanol/phosphate buffer)	2002	Journal of medicinal chemistry, May-09, Volume: 45, Issue:10	Synthesis and in vitro evaluation of quaternary ammonium derivatives of chlorambucil and melphalan, anticancer drugs designed for the chemotherapy of chondrosarcoma.
AID1079935	Cytolytic liver toxicity, either proven histopathologically or where the ratio of maximal ALT or AST activity above normal to that of Alkaline Phosphatase is > 5 (see ACUTE). Value is number of references indexed. [column 'CYTOL' in source]
AID510598	Cytotoxicity against human A375 cells after 24 hrs by MTT assay	2010	European journal of medicinal chemistry, Sep, Volume: 45, Issue:9	Synthesis and biological evaluation of cyclic nitrogen mustards based on carnitine framework.
AID1623667	Half life in simulated gastric fluid	2019	European journal of medicinal chemistry, Feb-15, Volume: 164	Identification of substituted 5-membered heterocyclic compounds as potential anti-leukemic agents.
AID1126680	In vitro antiproliferative activity against human BV173 cells assessed as decrease in cell viability after 24 hrs by MTT assay	2014	European journal of medicinal chemistry, May-06, Volume: 78	Synthesis and kinase inhibitory activity of new sulfonamide derivatives of pyrazolo[4,3-e][1,2,4]triazines.
AID536735	Growth inhibition of human SKOV3 cells after 7 days by celltiter-glo assay	2010	Journal of medicinal chemistry, Nov-25, Volume: 53, Issue:22	Assessment of chemoselective neoglycosylation methods using chlorambucil as a model.
AID1365047	Cell cycle arrest in human A375 cells assessed as accumulation at G0/G1 phase at 8 uM after 72 hrs by propidium iodide staining based flow cytometry (Rvb = 83.6%)	2017	Bioorganic & medicinal chemistry letters, 09-15, Volume: 27, Issue:18	Rational design, synthesis and preliminary antitumor activity evaluation of a chlorambucil derivative with potent DNA/HDAC dual-targeting inhibitory activity.
AID444055	Fraction absorbed in human	2010	Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3	Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID444054	Oral bioavailability in human	2010	Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3	Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID1633596	Cytotoxicity against human 2008 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay	2019	ACS medicinal chemistry letters, Apr-11, Volume: 10, Issue:4	Behind the Mirror: Chirality Tunes the Reactivity and Cytotoxicity of Chloropiperidines as Potential Anticancer Agents.
AID444058	Volume of distribution at steady state in human	2010	Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3	Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID101739	In vitro cytotoxic activity against M4 Beu cells, by colony forming assay	2002	Journal of medicinal chemistry, May-09, Volume: 45, Issue:10	Synthesis and in vitro evaluation of quaternary ammonium derivatives of chlorambucil and melphalan, anticancer drugs designed for the chemotherapy of chondrosarcoma.
AID1079949	Proposed mechanism(s) of liver damage. [column 'MEC' in source]
AID1378127	Growth inhibition of human NCI-H1299 cells preincubated for 6 hrs cotreated with amonafide followed compound washout measured after 24 hrs by XTT assay	2017	European journal of medicinal chemistry, Sep-29, Volume: 138	Discovery of potent molecular chimera (CM358) to treat human metastatic melanoma.
AID536575	Growth inhibition of human HT-29 cells after 7 days by celltiter-glo assay	2010	Journal of medicinal chemistry, Nov-25, Volume: 53, Issue:22	Assessment of chemoselective neoglycosylation methods using chlorambucil as a model.
AID90116	Alkylating activity of compound remaining after 24 hours of incubation with 10% human blood serum	1998	Journal of medicinal chemistry, Jul-16, Volume: 41, Issue:15	Synthesis and in vitro efficacy of transferrin conjugates of the anticancer drug chlorambucil.
AID153340	Cytotoxicity against P388 leukemia cell line	1990	Journal of medicinal chemistry, Nov, Volume: 33, Issue:11	DNA-directed alkylating agents. 3. Structure-activity relationships for acridine-linked aniline mustards: consequences of varying the length of the linker chain.
AID444057	Fraction escaping hepatic elimination in human	2010	Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3	Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID1555215	Antiproliferative activity against mouse B16F10 cells incubated for 72 hrs by MTT assay
AID121765	Antitumor activity measured as T/C at 0.050 nmol/kg dose against ip inoculated P388 leukemia in CDF1 mice	1983	Journal of medicinal chemistry, Aug, Volume: 26, Issue:8	1,3-dipalmitoylglycerol ester of chlorambucil as a lymphotropic, orally administrable antineoplastic agent.
AID408557	Antiproliferative activity against human 5637 cells after 96 hrs by crystal violet assay	2008	Bioorganic & medicinal chemistry, May-15, Volume: 16, Issue:10	Synthesis of indirubin-N'-glycosides and their anti-proliferative activity against human cancer cell lines.
AID1365035	Induction of apoptosis in human A375 cells assessed as early apoptotic cells at 2 uM after 72 hrs by Annexin/propidium iodide staining based flow cytometry (Rvb = 1.62%)	2017	Bioorganic & medicinal chemistry letters, 09-15, Volume: 27, Issue:18	Rational design, synthesis and preliminary antitumor activity evaluation of a chlorambucil derivative with potent DNA/HDAC dual-targeting inhibitory activity.
AID1365212	Cytotoxicity against human MCF7 assessed as inhibition of cell growth incubated for 48 hrs by resazurin reduction test	2017	Bioorganic & medicinal chemistry, 10-15, Volume: 25, Issue:20	Linker structure-activity relationships in fluorodeoxyglucose chlorambucil conjugates for tumor-targeted chemotherapy.
AID9646	Growth inhibition activity was measured in repair proficient AA8 cells under aerobic conditions (4 hours drug exposure)	1995	Journal of medicinal chemistry, Mar-31, Volume: 38, Issue:7	Hypoxia-selective antitumor agents. 11. Chlorambucil N-oxide: a reappraisal of its synthesis, stability, and selective toxicity for hypoxic cells.
AID536581	Growth inhibition of human NCI-H460 cells after 7 days by celltiter-glo assay	2010	Journal of medicinal chemistry, Nov-25, Volume: 53, Issue:22	Assessment of chemoselective neoglycosylation methods using chlorambucil as a model.
AID103747	In vitro cytotoxic activity against MCF7, by colony forming assay	2002	Journal of medicinal chemistry, May-09, Volume: 45, Issue:10	Synthesis and in vitro evaluation of quaternary ammonium derivatives of chlorambucil and melphalan, anticancer drugs designed for the chemotherapy of chondrosarcoma.
AID1663616	Anticancer activity against human SKLU1 cells assessed as cell growth inhibition measured after 48 hrs by MTT assay	2020	Bioorganic & medicinal chemistry letters, 07-15, Volume: 30, Issue:14	Synthesis and anticancer activity of open-resorcinarene conjugates.
AID444056	Fraction escaping gut-wall elimination in human	2010	Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3	Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID382360	Effect on oxidative stress in mouse L929 cells assessed as glutathione depletion at 6.25 uM after 4 hrs	2008	Bioorganic & medicinal chemistry, May-01, Volume: 16, Issue:9	Synthesis and cytotoxic properties of new fluorodeoxyglucose-coupled chlorambucil derivatives.
AID52790	Inhibition of chymotrypsin at 250 uM	2003	Journal of medicinal chemistry, Oct-09, Volume: 46, Issue:21	Identification and prediction of promiscuous aggregating inhibitors among known drugs.
AID428555	Alkylating activity in 0.2 M acetate buffer of pH 5.6 at 0.1 to 1 mM after 4 hrs by spectrophotometry relative to chlorambucil	2009	European journal of medicinal chemistry, Jul, Volume: 44, Issue:7	To determine the cytotoxicity of chlorambucil and one of its nitro-derivatives, conjugated to prasterone and pregnenolone, towards eight human cancer cell-lines.
AID1405136	Alkylating activity at DNA (unknown origin) after 90 mins by colorimetric NBP assay	2018	European journal of medicinal chemistry, Jul-15, Volume: 155	Preparation, characterisation and biological evaluation of new N-phenyl amidobenzenesulfonates and N-phenyl ureidobenzenesulfonates inducing DNA double-strand breaks. Part 3. Modulation of ring A.
AID588212	Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in rodents	2010	Chemical research in toxicology, Jan, Volume: 23, Issue:1	Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.
AID22551	Half-life after NBP alkylation	1990	Journal of medicinal chemistry, Jun, Volume: 33, Issue:6	Phenyl selenones: alkyl transfer by selenium-carbon bond cleavage.
AID1365028	Antiproliferative activity against human HepG2 cells after 72 hrs by CCK8 assay	2017	Bioorganic & medicinal chemistry letters, 09-15, Volume: 27, Issue:18	Rational design, synthesis and preliminary antitumor activity evaluation of a chlorambucil derivative with potent DNA/HDAC dual-targeting inhibitory activity.
AID428453	Cytotoxicity against human MDA-MB-468 cells transfected with NAD(P)H: quinone oxidoreductase NQO1 after 5 days by MTT assay	2009	European journal of medicinal chemistry, Jul, Volume: 44, Issue:7	To determine the cytotoxicity of chlorambucil and one of its nitro-derivatives, conjugated to prasterone and pregnenolone, towards eight human cancer cell-lines.
AID47482	Growth inhibition against CH-1 cisplatin resistant wild-type ovarian cell lines	2004	Journal of medicinal chemistry, Mar-25, Volume: 47, Issue:7	Synthesis and biological evaluation of novel chloroethylaminoanthraquinones with potent cytotoxic activity against cisplatin-resistant tumor cells.
AID444053	Renal clearance in human	2010	Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3	Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID1365039	Induction of apoptosis in human A375 cells assessed as early apoptotic cells at 8 uM after 72 hrs by Annexin/propidium iodide staining based flow cytometry (Rvb = 1.62%)	2017	Bioorganic & medicinal chemistry letters, 09-15, Volume: 27, Issue:18	Rational design, synthesis and preliminary antitumor activity evaluation of a chlorambucil derivative with potent DNA/HDAC dual-targeting inhibitory activity.
AID625284	Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatic failure	2011	PLoS computational biology, Dec, Volume: 7, Issue:12	Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID101870	In vitro cytotoxicity activity against M4 Dau, by colony forming assay	2002	Journal of medicinal chemistry, May-09, Volume: 45, Issue:10	Synthesis and in vitro evaluation of quaternary ammonium derivatives of chlorambucil and melphalan, anticancer drugs designed for the chemotherapy of chondrosarcoma.
AID101656	DNA damages caused in MDA-MB-231 cells after 2 hr exposure to a concentration of 400 uM	2001	Journal of medicinal chemistry, Mar-01, Volume: 44, Issue:5	Antimitotic antitumor agents: synthesis, structure-activity relationships, and biological characterization of N-aryl-N'-(2-chloroethyl)ureas as new selective alkylating agents.
AID1079936	Choleostatic liver toxicity, either proven histopathologically or where the ratio of maximal ALT or AST activity above normal to that of Alkaline Phosphatase is < 2 (see ACUTE). Value is number of references indexed. [column 'CHOLE' in source]
AID1365030	Antiproliferative activity against human HCT116 cells after 72 hrs by CCK8 assay	2017	Bioorganic & medicinal chemistry letters, 09-15, Volume: 27, Issue:18	Rational design, synthesis and preliminary antitumor activity evaluation of a chlorambucil derivative with potent DNA/HDAC dual-targeting inhibitory activity.
AID1057231	Cytotoxicity against mitochondrial DNA-deficient human MDA-MB-435 rho theta-W02 cells after 72 hrs by MTT assay	2013	Journal of medicinal chemistry, Nov-27, Volume: 56, Issue:22	A selective mitochondrial-targeted chlorambucil with remarkable cytotoxicity in breast and pancreatic cancers.
AID315480	Inhibition of [3H]spermidine uptake at PAT in mouse L1210 cells	2008	Journal of medicinal chemistry, Mar-13, Volume: 51, Issue:5	A comparison of chloroambucil- and xylene-containing polyamines leads to improved ligands for accessing the polyamine transport system.
AID1412099	Induction of apoptosis in human A375 cells assessed as necrotic cells at 2 uM after 72 hrs by Alexa Fluor 488 Annexin/propidium iodide staining-based flow cytometric analysis (Rvb = 1.64%)	2018	MedChemComm, Feb-01, Volume: 9, Issue:2	Rational design and characterization of a DNA/HDAC dual-targeting inhibitor containing nitrogen mustard and 2-aminobenzamide moieties.
AID315487	Ratio of IC50 for PAT deficient CHO-MG cells to IC50 for PAT active CHO cells	2008	Journal of medicinal chemistry, Mar-13, Volume: 51, Issue:5	A comparison of chloroambucil- and xylene-containing polyamines leads to improved ligands for accessing the polyamine transport system.
AID1079946	Presence of at least one case with successful reintroduction. [column 'REINT' in source]
AID116388	Antitumor a dose 0.066 nmol/kg against ip inoculated P388 leukemia in CDF1 mice	1983	Journal of medicinal chemistry, Aug, Volume: 26, Issue:8	1,3-dipalmitoylglycerol ester of chlorambucil as a lymphotropic, orally administrable antineoplastic agent.
AID1132021	Toxicity in rat allografted with rat Walker 256 cells	1978	Journal of medicinal chemistry, Jan, Volume: 21, Issue:1	Structure-activity relationships in antitumor aniline mustards.
AID539167	Cytotoxicity against estrogen receptor-negative human MDA-MB-436 cells by MTT assay	2010	Bioorganic & medicinal chemistry letters, Dec-15, Volume: 20, Issue:24	Synthesis of D- and L-tyrosine-chlorambucil analogs active against breast cancer cell lines.
AID116382	Antitumor a dose 0.033 nmol/Kg against ip inoculated P388 leukemia in CDF1 mice	1983	Journal of medicinal chemistry, Aug, Volume: 26, Issue:8	1,3-dipalmitoylglycerol ester of chlorambucil as a lymphotropic, orally administrable antineoplastic agent.
AID1633090	Induction of apoptosis in human HepG2/ADM cells assessed as necrotic cells at 20 uM incubated for 72 hrs by Annexin V-FITC/SYTOX Red staining based flow cytometric analysis (Rvb =0%)	2017	Bioorganic & medicinal chemistry, 10-15, Volume: 25, Issue:20	A novel delocalized lipophilic cation-chlorambucil conjugate inhibits P-glycoprotein in HepG2/ADM cells.
AID1690738	Inhibition of EGFR phosphorylation in human NCI-H1975 cells at 1 to 10 uM preincubated for 2 hrs followed by EGF stimulation and measured after 30 mins by Western blot analysis	2020	European journal of medicinal chemistry, Apr-15, Volume: 192	Comparative analysis of the dual EGFR-DNA targeting and growth inhibitory properties of 6-mono-alkylamino- and 6,6-dialkylaminoquinazoline-based type II combi-molecules.
AID1250809	Induction of Escherichia coli supercoiled pBR322 DNA cleavage at 50 uM after 24 hrs at 25 degC by agarose gel electrophoresis	2015	Bioorganic & medicinal chemistry letters, Oct-15, Volume: 25, Issue:20	Synthesis and evaluation of a bis-3-chloropiperidine derivative incorporating an anthraquinone pharmacophore.
AID1633091	Induction of apoptosis in human HepG2/ADM cells assessed as viable cells at 20 uM incubated for 72 hrs in presence of ADM by Annexin V-FITC/SYTOX Red staining based flow cytometric analysis (Rvb = 88.7%)	2017	Bioorganic & medicinal chemistry, 10-15, Volume: 25, Issue:20	A novel delocalized lipophilic cation-chlorambucil conjugate inhibits P-glycoprotein in HepG2/ADM cells.
AID1057241	Cytotoxicity against human Hs578T cells after 72 hrs by MTT assay	2013	Journal of medicinal chemistry, Nov-27, Volume: 56, Issue:22	A selective mitochondrial-targeted chlorambucil with remarkable cytotoxicity in breast and pancreatic cancers.
AID1633071	Cytotoxicity against human HepG2 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay	2017	Bioorganic & medicinal chemistry, 10-15, Volume: 25, Issue:20	A novel delocalized lipophilic cation-chlorambucil conjugate inhibits P-glycoprotein in HepG2/ADM cells.
AID1378119	Growth inhibition of human WM266.4 cells preincubated for 6 hrs followed compound washout measured after 24 hrs by XTT assay	2017	European journal of medicinal chemistry, Sep-29, Volume: 138	Discovery of potent molecular chimera (CM358) to treat human metastatic melanoma.
AID200268	Growth inhibition against SKOV3 wild-type ovarian cell lines	2004	Journal of medicinal chemistry, Mar-25, Volume: 47, Issue:7	Synthesis and biological evaluation of novel chloroethylaminoanthraquinones with potent cytotoxic activity against cisplatin-resistant tumor cells.
AID1123201	Toxicity in icv dosed Swiss Webster mouse assessed as suppression of startle reflex to loud and abrupt auditory stimulus	1979	Journal of medicinal chemistry, Feb, Volume: 22, Issue:2	Synthesis and pharmacologic characterization of an alkylating analogue (chlornaltrexamine) of naltrexone with ultralong-lasting narcotic antagonist properties.
AID1357937	Cytotoxicity against human COLO205 cells assessed as reduction in cell viability after 3 days by MTT assay	2018	European journal of medicinal chemistry, May-10, Volume: 151	Therapeutic journery of nitrogen mustard as alkylating anticancer agents: Historic to future perspectives.
AID1412103	Induction of apoptosis in human A375 cells assessed as necrotic cells at 8 uM after 72 hrs by Alexa Fluor 488 Annexin/propidium iodide staining-based flow cytometric analysis (Rvb = 1.64%)	2018	MedChemComm, Feb-01, Volume: 9, Issue:2	Rational design and characterization of a DNA/HDAC dual-targeting inhibitor containing nitrogen mustard and 2-aminobenzamide moieties.
AID1365215	Cytotoxicity against human PA1 assessed as inhibition of cell growth incubated for 48 hrs by resazurin reduction test	2017	Bioorganic & medicinal chemistry, 10-15, Volume: 25, Issue:20	Linker structure-activity relationships in fluorodeoxyglucose chlorambucil conjugates for tumor-targeted chemotherapy.
AID524794	Antiplasmodial activity against Plasmodium falciparum GB4 after 72 hrs by SYBR green assay	2009	Nature chemical biology, Oct, Volume: 5, Issue:10	Genetic mapping of targets mediating differential chemical phenotypes in Plasmodium falciparum.
AID625281	Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cholelithiasis	2011	PLoS computational biology, Dec, Volume: 7, Issue:12	Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1584825	Growth inhibition of human MDA-MB-468 cells after 48 hrs by fluorescence polarisation assay	2018	Journal of medicinal chemistry, 10-25, Volume: 61, Issue:20	Discovery and Optimization of Novel Hydrogen Peroxide Activated Aromatic Nitrogen Mustard Derivatives as Highly Potent Anticancer Agents.
AID1123195	Analgesic activity in Swiss Webster mouse at 4 nmol, icv after 10 to 120 mins by tail flick test	1979	Journal of medicinal chemistry, Feb, Volume: 22, Issue:2	Synthesis and pharmacologic characterization of an alkylating analogue (chlornaltrexamine) of naltrexone with ultralong-lasting narcotic antagonist properties.
AID1231556	Cytotoxic activity against human MDA-MB-231 cells assessed as reduction in cell viability incubated for 24 hrs by MTT assay	2015	Bioorganic & medicinal chemistry, Jul-01, Volume: 23, Issue:13	New pyrazolo[4,3-e][1,2,4]triazine sulfonamides as carbonic anhydrase inhibitors.
AID1412088	Antiproliferative activity against human A549 cells after 72 hrs CCK8 assay	2018	MedChemComm, Feb-01, Volume: 9, Issue:2	Rational design and characterization of a DNA/HDAC dual-targeting inhibitor containing nitrogen mustard and 2-aminobenzamide moieties.
AID1465332	Antiproliferative activity against human HL60 cells treated for 24 hrs measured after 72 hrs by MTT assay	2017	Bioorganic & medicinal chemistry letters, 11-15, Volume: 27, Issue:22	Design and synthesis of novel nitrogen mustard-evodiamine hybrids with selective antiproliferative activity.
AID1057226	Cell cycle arrest in human MIAPaCa2 cells assessed as accumulation at G2/M phase at 20 uM after 24 to 48 hrs by flow cytometry	2013	Journal of medicinal chemistry, Nov-27, Volume: 56, Issue:22	A selective mitochondrial-targeted chlorambucil with remarkable cytotoxicity in breast and pancreatic cancers.
AID1365043	Induction of apoptosis in human A375 cells assessed as early apoptotic cells at 16 uM after 72 hrs by Annexin/propidium iodide staining based flow cytometry (Rvb = 1.62%)	2017	Bioorganic & medicinal chemistry letters, 09-15, Volume: 27, Issue:18	Rational design, synthesis and preliminary antitumor activity evaluation of a chlorambucil derivative with potent DNA/HDAC dual-targeting inhibitory activity.
AID1425993	Cytotoxicity against carbonic anhydrase 9 knockdown MDCK cells assessed as reduction in cell viability preincubated for 2 hrs followed by 72 hrs incubation under normoxic condition by Alamar blue assay	2017	European journal of medicinal chemistry, Feb-15, Volume: 127	New approach of delivering cytotoxic drugs towards CAIX expressing cells: A concept of dual-target drugs.
AID89242	Resistance factor (IC50 in the resistant cell line/IC50 in the parent cell line)	2004	Journal of medicinal chemistry, Mar-25, Volume: 47, Issue:7	Synthesis and biological evaluation of novel chloroethylaminoanthraquinones with potent cytotoxic activity against cisplatin-resistant tumor cells.
AID45400	Effect on cross resistance of CHO cells resistant to colchicine (CHRC5)	1990	Journal of medicinal chemistry, Jul, Volume: 33, Issue:7	Structure-activity relationships of antineoplastic agents in multidrug resistance.
AID1412107	Induction of apoptosis in human A375 cells assessed as necrotic cells at 16 uM after 72 hrs by Alexa Fluor 488 Annexin/propidium iodide staining-based flow cytometric analysis (Rvb = 1.64%)	2018	MedChemComm, Feb-01, Volume: 9, Issue:2	Rational design and characterization of a DNA/HDAC dual-targeting inhibitor containing nitrogen mustard and 2-aminobenzamide moieties.
AID1633591	Induction of Escherichia coli pBR322 DNA cleavage in BPE buffer at 5 to 50 uM incubated for 2 hrs by electrophoresis method	2019	ACS medicinal chemistry letters, Apr-11, Volume: 10, Issue:4	Behind the Mirror: Chirality Tunes the Reactivity and Cytotoxicity of Chloropiperidines as Potential Anticancer Agents.
AID121769	Antitumor activity measured as T/C at 0.066 nmol/kg dose against po inoculated P388 leukemia in CDF1 mice	1983	Journal of medicinal chemistry, Aug, Volume: 26, Issue:8	1,3-dipalmitoylglycerol ester of chlorambucil as a lymphotropic, orally administrable antineoplastic agent.
AID1383597	Antiproliferative activity against human Bel7402/5-FU cells after 72 hrs by MTT assay	2018	European journal of medicinal chemistry, Apr-25, Volume: 150	Novel hybrids of brefeldin A and nitrogen mustards with improved antiproliferative selectivity: Design, synthesis and antitumor biological evaluation.
AID425652	Total body clearance in human	2009	Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15	Physicochemical determinants of human renal clearance.
AID1185088	Cytotoxicity against human L02 cells by MTT assay	2014	ACS medicinal chemistry letters, Jul-10, Volume: 5, Issue:7	Novel hybrids of natural oridonin-bearing nitrogen mustards as potential anticancer drug candidates.
AID1412102	Induction of apoptosis in human A375 cells assessed as late apoptotic cells at 8 uM after 72 hrs by Alexa Fluor 488 Annexin/propidium iodide staining-based flow cytometric analysis (Rvb = 10.22%)	2018	MedChemComm, Feb-01, Volume: 9, Issue:2	Rational design and characterization of a DNA/HDAC dual-targeting inhibitor containing nitrogen mustard and 2-aminobenzamide moieties.
AID1079947	Comments (NB not yet translated). [column 'COMMENTAIRES' in source]
AID1246953	Cytotoxicity against human HeLa cells assessed as cell viability after 5 days by cell viability analyzer	2015	European journal of medicinal chemistry, Sep-18, Volume: 102	Design and synthesis of novel hydroxyanthraquinone nitrogen mustard derivatives as potential anticancer agents via a bioisostere approach.
AID1633099	Inhibition of Pgp in human HepG2/ADM cells assessed as potentiation of ADM-induced cytotoxicity by measuring reduction in ADM IC50 at 100 uM incubated for 72 hrs by MTT assay relative to control	2017	Bioorganic & medicinal chemistry, 10-15, Volume: 25, Issue:20	A novel delocalized lipophilic cation-chlorambucil conjugate inhibits P-glycoprotein in HepG2/ADM cells.
AID232850	Alkylating activity by using 4-(4-nitrobenzyl)-pyridine (NBP) colorimetric assay	2001	Journal of medicinal chemistry, Mar-01, Volume: 44, Issue:5	Antimitotic antitumor agents: synthesis, structure-activity relationships, and biological characterization of N-aryl-N'-(2-chloroethyl)ureas as new selective alkylating agents.
AID84306	Tested for in vitro concentration required to inhibit growth by 50% against HT-29 human colon cancer cell line	2002	Bioorganic & medicinal chemistry letters, Jan-21, Volume: 12, Issue:2	Polyhydroxylated azepanes as new motifs for DNA minor groove binding agents.
AID1378226	Toxicity in athymic Foxn1 nu mouse xenografted with human WM266.4 cells assessed as body weight loss at 10 mg/kg, ip cotreated with amonafide administered once daily for 3 days followed by resting period of 4 days repeated for 4 weeks starting from 5 days	2017	European journal of medicinal chemistry, Sep-29, Volume: 138	Discovery of potent molecular chimera (CM358) to treat human metastatic melanoma.
AID224739	In vivo antitumor activity against murine S-180 sarcoma at a dose of 1.3 mg/kg administered intraperitoneally 7qd in mice; Body wt initial/Final = 19.9/23.4	2001	Bioorganic & medicinal chemistry letters, May-07, Volume: 11, Issue:9	2-[N1-2-pyrimidyl-aminobenzenesulfonamido] ethyl 4-bis(2-chloroethyl) aminophenyl butyrate: a potent antitumor agent.
AID1465329	Antiproliferative activity against human PC3 cells treated for 24 hrs measured after 72 hrs by MTT assay	2017	Bioorganic & medicinal chemistry letters, 11-15, Volume: 27, Issue:22	Design and synthesis of novel nitrogen mustard-evodiamine hybrids with selective antiproliferative activity.
AID1132032	Stability of the compound in acetone assessed as hydrolysis at 66 degC after 30 mins	1978	Journal of medicinal chemistry, Jan, Volume: 21, Issue:1	Structure-activity relationships in antitumor aniline mustards.
AID1425996	Cytotoxicity against MDCK cells expressing carbonic anhydrase 9 assessed as reduction in cell viability after 2 hrs under hypoxic condition by Alamar blue assay	2017	European journal of medicinal chemistry, Feb-15, Volume: 127	New approach of delivering cytotoxic drugs towards CAIX expressing cells: A concept of dual-target drugs.
AID106806	Inhibition of malate dehydrogenase (MDH) at 400 uM	2003	Journal of medicinal chemistry, Oct-09, Volume: 46, Issue:21	Identification and prediction of promiscuous aggregating inhibitors among known drugs.
AID152767	Tested for the in vitro cytotoxicity against P388 murine leukemia	1990	Journal of medicinal chemistry, Apr, Volume: 33, Issue:4	DNA-directed alkylating agents. 1. Structure-activity relationships for acridine-linked aniline mustards: consequences of varying the reactivity of the mustard.
AID382060	Antitumor activity in BDF1 mouse L1210 cells assessed as number of cured mouse at 7.5 mg/kg/day, ip after 90 days	2008	Bioorganic & medicinal chemistry, May-01, Volume: 16, Issue:9	Rational design, synthesis, and in vivo evaluation of the antileukemic activity of six new alkylating steroidal esters.
AID111720	Antitumor activity measured as Body weight change (BWC) between day 1 and 5 at 0.050 nmol/kg dose against ip inoculated P388 leukemia in CDF1 mice	1983	Journal of medicinal chemistry, Aug, Volume: 26, Issue:8	1,3-dipalmitoylglycerol ester of chlorambucil as a lymphotropic, orally administrable antineoplastic agent.
AID1378199	Cell cycle arrest in human WM266.4 cells assessed as accumulation at S phase at 10 uM cotreated with amonafide after 2 hrs by propidium iodide staining based flow cytometry (Rvb = 27%)	2017	European journal of medicinal chemistry, Sep-29, Volume: 138	Discovery of potent molecular chimera (CM358) to treat human metastatic melanoma.
AID1079945	Animal toxicity known. [column 'TOXIC' in source]
AID1424625	Antiproliferative activity in human MCF7 cells assessed as inhibition of cell proliferation	2017	European journal of medicinal chemistry, Dec-15, Volume: 142	1,3,5-Triazines: A promising scaffold for anticancer drugs development.
AID1057214	Antitumor activity against human MIAPaCa2 cells xenografted in athymic nude mouse assessed as inhibition of tumor growth at 10 mg/kg, ip administered 5 times a week for 36 days	2013	Journal of medicinal chemistry, Nov-27, Volume: 56, Issue:22	A selective mitochondrial-targeted chlorambucil with remarkable cytotoxicity in breast and pancreatic cancers.
AID746835	Cytotoxicity against human MA9.3 cells after 48 hrs by MTT assay	2013	Bioorganic & medicinal chemistry letters, May-15, Volume: 23, Issue:10	Novel ROS-activated agents utilize a tethered amine to selectively target acute myeloid leukemia.
AID1365038	Induction of apoptosis in human A375 cells assessed as live cells at 8 uM after 72 hrs by Annexin/propidium iodide staining based flow cytometry (Rvb = 86.07%)	2017	Bioorganic & medicinal chemistry letters, 09-15, Volume: 27, Issue:18	Rational design, synthesis and preliminary antitumor activity evaluation of a chlorambucil derivative with potent DNA/HDAC dual-targeting inhibitory activity.
AID753787	Cytotoxicity against androgen receptor deficient human PC3 cells after 72 hrs by MTT assay	2013	European journal of medicinal chemistry, Jun, Volume: 64	Synthesis and preliminary in vitro biological evaluation of 7α-testosterone-chlorambucil hybrid designed for the treatment of prostate cancer.
AID1185082	Antiproliferative activity against human MGC803 cells assessed as growth inhibition after 72 hrs by MTT assay	2014	ACS medicinal chemistry letters, Jul-10, Volume: 5, Issue:7	Novel hybrids of natural oridonin-bearing nitrogen mustards as potential anticancer drug candidates.
AID1272175	Chemical stability of the compound at pH 5.2 assessed as half life by LC-MS analysis	2016	Bioorganic & medicinal chemistry, Jan-15, Volume: 24, Issue:2	Synthesis, biological studies and molecular dynamics of new anticancer RGD-based peptide conjugates for targeted drug delivery.
AID315485	Cytotoxicity against PAT deficient CHO-MG cells after 48 hrs	2008	Journal of medicinal chemistry, Mar-13, Volume: 51, Issue:5	A comparison of chloroambucil- and xylene-containing polyamines leads to improved ligands for accessing the polyamine transport system.
AID465022	Anticancer activity against human MDA-MB-468 cells assessed as cell survival after 72 hrs by MTT assay	2010	Bioorganic & medicinal chemistry letters, Mar-01, Volume: 20, Issue:5	Design, synthesis and biological evaluation of estradiol-chlorambucil hybrids as anticancer agents.
AID1633597	Cytotoxicity against human BxPC3 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay	2019	ACS medicinal chemistry letters, Apr-11, Volume: 10, Issue:4	Behind the Mirror: Chirality Tunes the Reactivity and Cytotoxicity of Chloropiperidines as Potential Anticancer Agents.
AID224747	In vivo antitumor activity against murine S-180 sarcoma at a dose of 6.8 mg/kg administered intraperitoneally 7qd in mice; Body wt initial/Final = 19.8/18.4	2001	Bioorganic & medicinal chemistry letters, May-07, Volume: 11, Issue:9	2-[N1-2-pyrimidyl-aminobenzenesulfonamido] ethyl 4-bis(2-chloroethyl) aminophenyl butyrate: a potent antitumor agent.
AID1357939	Cytotoxicity against human IMR32 cells assessed as reduction in cell viability after 3 days by MTT assay	2018	European journal of medicinal chemistry, May-10, Volume: 151	Therapeutic journery of nitrogen mustard as alkylating anticancer agents: Historic to future perspectives.
AID1633089	Induction of apoptosis in human HepG2/ADM cells assessed as late apoptotic cells at 20 uM incubated for 72 hrs by Annexin V-FITC/SYTOX Red staining based flow cytometric analysis (Rvb =0.04%)	2017	Bioorganic & medicinal chemistry, 10-15, Volume: 25, Issue:20	A novel delocalized lipophilic cation-chlorambucil conjugate inhibits P-glycoprotein in HepG2/ADM cells.
AID229741	Hypersensitivity factor (HF) of IC50 (AA8) / IC50 (EM-9) of compound for repair deffective mutants	1989	Journal of medicinal chemistry, Jan, Volume: 32, Issue:1	Hypoxia-selective antitumor agents. 2. Electronic effects of 4-substituents on the mechanisms of cytotoxicity and metabolic stability of nitracrine derivatives.
AID247839	Cytotoxicity against human leukemia cell line K562	2004	Journal of medicinal chemistry, Sep-09, Volume: 47, Issue:19	Design and synthesis of a nitrogen mustard derivative stabilized by apo-neocarzinostatin.
AID1378206	Cell cycle arrest in human WM266.4 cells assessed as accumulation at G2 phase at 10 uM cotreated with amonafide after 24 hrs by propidium iodide staining based flow cytometry (Rvb = 11%)	2017	European journal of medicinal chemistry, Sep-29, Volume: 138	Discovery of potent molecular chimera (CM358) to treat human metastatic melanoma.
AID1378198	Cell cycle arrest in human WM266.4 cells assessed as accumulation at G1 phase at 10 uM cotreated with amonafide after 2 hrs by propidium iodide staining based flow cytometry (Rvb = 59%)	2017	European journal of medicinal chemistry, Sep-29, Volume: 138	Discovery of potent molecular chimera (CM358) to treat human metastatic melanoma.
AID1378116	Growth inhibition of human MDA-MB-231 cells preincubated for 6 hrs followed compound washout measured after 24 hrs by XTT assay	2017	European journal of medicinal chemistry, Sep-29, Volume: 138	Discovery of potent molecular chimera (CM358) to treat human metastatic melanoma.
AID444052	Hepatic clearance in human	2010	Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3	Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID1412101	Induction of apoptosis in human A375 cells assessed as early apoptotic cells at 8 uM after 72 hrs by Alexa Fluor 488 Annexin/propidium iodide staining-based flow cytometric analysis (Rvb = 2.07%)	2018	MedChemComm, Feb-01, Volume: 9, Issue:2	Rational design and characterization of a DNA/HDAC dual-targeting inhibitor containing nitrogen mustard and 2-aminobenzamide moieties.
AID1412097	Induction of apoptosis in human A375 cells assessed as early apoptotic cells at 2 uM after 72 hrs by Alexa Fluor 488 Annexin/propidium iodide staining-based flow cytometric analysis (Rvb = 2.07%)	2018	MedChemComm, Feb-01, Volume: 9, Issue:2	Rational design and characterization of a DNA/HDAC dual-targeting inhibitor containing nitrogen mustard and 2-aminobenzamide moieties.
AID588211	Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in humans	2010	Chemical research in toxicology, Jan, Volume: 23, Issue:1	Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.
AID1057236	Cytotoxicity against human BxPC3 cells after 72 hrs by MTT assay	2013	Journal of medicinal chemistry, Nov-27, Volume: 56, Issue:22	A selective mitochondrial-targeted chlorambucil with remarkable cytotoxicity in breast and pancreatic cancers.
AID1197742	Stimulation of human OATP1B1-mediated [3H]estrone 3-sulfate at 100 uM after 5 mins relative to control	2015	European journal of medicinal chemistry, Mar-06, Volume: 92	Interaction of human organic anion transporter polypeptides 1B1 and 1B3 with antineoplastic compounds.
AID1378202	Cell cycle arrest in human WM266.4 cells assessed as accumulation at S phase at 10 uM cotreated with amonafide after 8 hrs by propidium iodide staining based flow cytometry (Rvb = 27%)	2017	European journal of medicinal chemistry, Sep-29, Volume: 138	Discovery of potent molecular chimera (CM358) to treat human metastatic melanoma.
AID382358	Effect on oxidative stress in mouse L929 cells assessed as ROS production at 6.25 uM after 4 hrs by 2',7'-dichlorofluorescein-diacetate assay	2008	Bioorganic & medicinal chemistry, May-01, Volume: 16, Issue:9	Synthesis and cytotoxic properties of new fluorodeoxyglucose-coupled chlorambucil derivatives.
AID467612	Fraction unbound in human plasma	2009	European journal of medicinal chemistry, Nov, Volume: 44, Issue:11	Prediction of volume of distribution values in human using immobilized artificial membrane partitioning coefficients, the fraction of compound ionized and plasma protein binding data.
AID1465331	Antiproliferative activity against human THP1 cells treated for 24 hrs measured after 72 hrs by MTT assay	2017	Bioorganic & medicinal chemistry letters, 11-15, Volume: 27, Issue:22	Design and synthesis of novel nitrogen mustard-evodiamine hybrids with selective antiproliferative activity.
AID1663611	Anticancer activity against human U251 cells assessed as cell growth inhibition measured after 48 hrs by MTT assay	2020	Bioorganic & medicinal chemistry letters, 07-15, Volume: 30, Issue:14	Synthesis and anticancer activity of open-resorcinarene conjugates.
AID1126684	Cytostatic activity against human MDA-MB-231 cells assessed as decrease in [3H]thymidine incorporation into DNA after 24 hrs by liquid scintillation counting analysis	2014	European journal of medicinal chemistry, May-06, Volume: 78	Synthesis and kinase inhibitory activity of new sulfonamide derivatives of pyrazolo[4,3-e][1,2,4]triazines.
AID1393846	Antiproliferative activity against human LO2 cells after 72 hrs by MTT assay	2018	European journal of medicinal chemistry, Feb-25, Volume: 146	Novel enmein-type diterpenoid hybrids coupled with nitrogen mustards: Synthesis of promising candidates for anticancer therapeutics.
AID1365049	Cell cycle arrest in human A375 cells assessed as accumulation at G2/M phase at 8 uM after 72 hrs by propidium iodide staining based flow cytometry (Rvb = 12.6%)	2017	Bioorganic & medicinal chemistry letters, 09-15, Volume: 27, Issue:18	Rational design, synthesis and preliminary antitumor activity evaluation of a chlorambucil derivative with potent DNA/HDAC dual-targeting inhibitory activity.
AID598526	1-Octanol-water distribution coefficient, log D of the compound at pH 7.4 by shake-flask method	2011	Bioorganic & medicinal chemistry letters, Jun-15, Volume: 21, Issue:12	Lipophilicity of acidic compounds: impact of ion pair partitioning on drug design.
AID1489294	Cytotoxicity against human DU145 cells assessed as decrease in cell viability after 48 hrs by MTS assay	2017	Journal of medicinal chemistry, 12-14, Volume: 60, Issue:23	Amphiphilic Modulation of Glycosylated Antitumor Ether Lipids Results in a Potent Triamino Scaffold against Epithelial Cancer Cell Lines and BT474 Cancer Stem Cells.
AID1633072	Cytotoxicity against human HepG2/ADM cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay	2017	Bioorganic & medicinal chemistry, 10-15, Volume: 25, Issue:20	A novel delocalized lipophilic cation-chlorambucil conjugate inhibits P-glycoprotein in HepG2/ADM cells.
AID101741	Comparative cellular uptake study performed on M4 Beu (melanoma cell line)	2002	Journal of medicinal chemistry, May-09, Volume: 45, Issue:10	Synthesis and in vitro evaluation of quaternary ammonium derivatives of chlorambucil and melphalan, anticancer drugs designed for the chemotherapy of chondrosarcoma.
AID1185089	Selectivity index, ratio of IC50 for human L02 cells to ratio of IC50 for human Bel-7402 cells	2014	ACS medicinal chemistry letters, Jul-10, Volume: 5, Issue:7	Novel hybrids of natural oridonin-bearing nitrogen mustards as potential anticancer drug candidates.
AID151245	Inhibition of cell growth in culture against wild type P388 murine leukemia	1991	Journal of medicinal chemistry, May, Volume: 34, Issue:5	DNA-directed alkylating agents. 4. 4-anilinoquinoline-based minor groove directed aniline mustards.
AID111716	Antitumor activity measured as Body weight change (BWC) between day 1 and 5 at 0.033 nmol/kg dose against ip inoculated P388 leukemia in CDF1 mice	1983	Journal of medicinal chemistry, Aug, Volume: 26, Issue:8	1,3-dipalmitoylglycerol ester of chlorambucil as a lymphotropic, orally administrable antineoplastic agent.
AID1425988	Binding affinity to recombinant human carbonic anhydrase 2 after 15 mins by stopped-flow CO2 hydration assay	2017	European journal of medicinal chemistry, Feb-15, Volume: 127	New approach of delivering cytotoxic drugs towards CAIX expressing cells: A concept of dual-target drugs.
AID210600	Therapeutic Index was determined	2001	Bioorganic & medicinal chemistry letters, May-07, Volume: 11, Issue:9	2-[N1-2-pyrimidyl-aminobenzenesulfonamido] ethyl 4-bis(2-chloroethyl) aminophenyl butyrate: a potent antitumor agent.
AID625283	Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for elevated liver function tests	2011	PLoS computational biology, Dec, Volume: 7, Issue:12	Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1378217	Antitumor activity against human WM266.4 cells xenografted in athymic Foxn1 nu mouse assessed as tumor growth inhibition at 10 mg/kg, ip cotreated with amonafide administered once daily for 7 days followed by resting period of 2 days repeated for 4 weeks	2017	European journal of medicinal chemistry, Sep-29, Volume: 138	Discovery of potent molecular chimera (CM358) to treat human metastatic melanoma.
AID39710	Compound was evaluated for the antineoplastic activity on B16 Melanoma cells at the optimal dose of 18 mg/kg through intraperitoneal route on days 1,5, 9	1985	Journal of medicinal chemistry, Nov, Volume: 28, Issue:11	Synthesis and properties of bis(2,2-dimethylaziridinyl)phosphinic amides: a series of new antineoplastic agents.
AID746836	Cytotoxicity against human CD34-positive blood stem/progenitor cells after 48 hrs by MTT assay	2013	Bioorganic & medicinal chemistry letters, May-15, Volume: 23, Issue:10	Novel ROS-activated agents utilize a tethered amine to selectively target acute myeloid leukemia.
AID1126677	In vitro antiproliferative activity against human MCF7 cells assessed as decrease cell viability after 24 hrs by MTT assay	2014	European journal of medicinal chemistry, May-06, Volume: 78	Synthesis and kinase inhibitory activity of new sulfonamide derivatives of pyrazolo[4,3-e][1,2,4]triazines.
AID625280	Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cholecystitis	2011	PLoS computational biology, Dec, Volume: 7, Issue:12	Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID224892	In vivo antitumor activity against murine S-180 sarcoma at a dose of 1.3 mg/kg administered intraperitoneally 7qd in Male TA1 mice; 10 survived out of 10 mice	2001	Bioorganic & medicinal chemistry letters, May-07, Volume: 11, Issue:9	2-[N1-2-pyrimidyl-aminobenzenesulfonamido] ethyl 4-bis(2-chloroethyl) aminophenyl butyrate: a potent antitumor agent.
AID1057242	Cytotoxicity against human CAMA1 cells after 72 hrs by MTT assay	2013	Journal of medicinal chemistry, Nov-27, Volume: 56, Issue:22	A selective mitochondrial-targeted chlorambucil with remarkable cytotoxicity in breast and pancreatic cancers.
AID1489292	Cytotoxicity against human BT474 cells assessed as decrease in cell viability after 48 hrs by MTS assay	2017	Journal of medicinal chemistry, 12-14, Volume: 60, Issue:23	Amphiphilic Modulation of Glycosylated Antitumor Ether Lipids Results in a Potent Triamino Scaffold against Epithelial Cancer Cell Lines and BT474 Cancer Stem Cells.
AID142438	Percentage increase in lifespan of drug-related tumor bearing animals when heated at the optimal dose and tested in murine leukemia P388 cell lines.	1991	Journal of medicinal chemistry, Jan, Volume: 34, Issue:1	Synthesis and evaluation of DNA-targeted spatially separated bis(aniline mustards) as potential alkylating agents with enhanced DNA cross-linking capability.
AID1140113	Cytotoxicity against human MCF7 cells assessed as growth inhibition after 24 hrs by MTT assay	2014	Bioorganic & medicinal chemistry, May-01, Volume: 22, Issue:9	Pyrazolo[4,3-e][1,2,4]triazine sulfonamides as carbonic anhydrase inhibitors with antitumor activity.
AID1378203	Cell cycle arrest in human WM266.4 cells assessed as accumulation at G2 phase at 10 uM cotreated with amonafide after 8 hrs by propidium iodide staining based flow cytometry (Rvb = 11%)	2017	European journal of medicinal chemistry, Sep-29, Volume: 138	Discovery of potent molecular chimera (CM358) to treat human metastatic melanoma.
AID536578	Growth inhibition of human p53 deficient H1299 cells after 7 days by celltiter-glo assay	2010	Journal of medicinal chemistry, Nov-25, Volume: 53, Issue:22	Assessment of chemoselective neoglycosylation methods using chlorambucil as a model.
AID428451	Cytotoxicity against human DaOY cells after 5 days by MTT assay	2009	European journal of medicinal chemistry, Jul, Volume: 44, Issue:7	To determine the cytotoxicity of chlorambucil and one of its nitro-derivatives, conjugated to prasterone and pregnenolone, towards eight human cancer cell-lines.
AID116389	Antitumor a dose 0.066 nmol/kg against ip inoculated P388 leukemia in CDF1 mice; Toxic	1983	Journal of medicinal chemistry, Aug, Volume: 26, Issue:8	1,3-dipalmitoylglycerol ester of chlorambucil as a lymphotropic, orally administrable antineoplastic agent.
AID1126678	In vitro antiproliferative activity against human MDA-MB-231 cells assessed as decrease in cell vaibility after 24 hrs by MTT assay	2014	European journal of medicinal chemistry, May-06, Volume: 78	Synthesis and kinase inhibitory activity of new sulfonamide derivatives of pyrazolo[4,3-e][1,2,4]triazines.
AID382353	Cytotoxicity against human PA1 cells by resazurin reduction test	2008	Bioorganic & medicinal chemistry, May-01, Volume: 16, Issue:9	Synthesis and cytotoxic properties of new fluorodeoxyglucose-coupled chlorambucil derivatives.
AID536565	Growth inhibition of human DU145 cells after 7 days by celltiter-glo assay	2010	Journal of medicinal chemistry, Nov-25, Volume: 53, Issue:22	Assessment of chemoselective neoglycosylation methods using chlorambucil as a model.
AID105659	In vitro inhibitory activity against acute lymphoblastic leukemia (MOLT4) cell line.	1998	Journal of medicinal chemistry, Jul-16, Volume: 41, Issue:15	Synthesis and in vitro efficacy of transferrin conjugates of the anticancer drug chlorambucil.
AID625291	Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver function tests abnormal	2011	PLoS computational biology, Dec, Volume: 7, Issue:12	Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1489290	Cytotoxicity against human JIMT1 cells assessed as decrease in cell viability after 48 hrs by MTS assay	2017	Journal of medicinal chemistry, 12-14, Volume: 60, Issue:23	Amphiphilic Modulation of Glycosylated Antitumor Ether Lipids Results in a Potent Triamino Scaffold against Epithelial Cancer Cell Lines and BT474 Cancer Stem Cells.
AID240619	Inhibitory concentration against cytochrome P450 2D6	2004	Journal of medicinal chemistry, Oct-21, Volume: 47, Issue:22	Validation of model of cytochrome P450 2D6: an in silico tool for predicting metabolism and inhibition.
AID1079934	Highest frequency of acute liver toxicity observed during clinical trials, expressed as a percentage. [column '% AIGUE' in source]
AID24033	Time required to reduce the alkylating activity of 10% human blood serum from its initial value by 50%.	1998	Journal of medicinal chemistry, Jul-16, Volume: 41, Issue:15	Synthesis and in vitro efficacy of transferrin conjugates of the anticancer drug chlorambucil.
AID224885	In vivo antitumor activity against murine S-180 sarcoma at a dose of 5 mg/kg administered intraperitoneally 7qd in mice expressed as percent inhibition	2001	Bioorganic & medicinal chemistry letters, May-07, Volume: 11, Issue:9	2-[N1-2-pyrimidyl-aminobenzenesulfonamido] ethyl 4-bis(2-chloroethyl) aminophenyl butyrate: a potent antitumor agent.
AID85435	Dose required to inhibit cell growth was determined against HT-29 cell line of human adenocarcinoma	2001	Journal of medicinal chemistry, Mar-01, Volume: 44, Issue:5	Antimitotic antitumor agents: synthesis, structure-activity relationships, and biological characterization of N-aryl-N'-(2-chloroethyl)ureas as new selective alkylating agents.
AID1473740	Inhibition of human MRP3 overexpressed in Sf9 insect cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 10 mins by membrane vesicle transport assay	2013	Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1	A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID1365034	Induction of apoptosis in human A375 cells assessed as live cells at 2 uM after 72 hrs by Annexin/propidium iodide staining based flow cytometry (Rvb = 86.07%)	2017	Bioorganic & medicinal chemistry letters, 09-15, Volume: 27, Issue:18	Rational design, synthesis and preliminary antitumor activity evaluation of a chlorambucil derivative with potent DNA/HDAC dual-targeting inhibitory activity.
AID224742	In vivo antitumor activity against murine S-180 sarcoma at a dose of 2.5 mg/kg administered intraperitoneally 7qd in mice; Body wt initial/Final = 20.0/21.3	2001	Bioorganic & medicinal chemistry letters, May-07, Volume: 11, Issue:9	2-[N1-2-pyrimidyl-aminobenzenesulfonamido] ethyl 4-bis(2-chloroethyl) aminophenyl butyrate: a potent antitumor agent.
AID1412105	Induction of apoptosis in human A375 cells assessed as early apoptotic cells at 16 uM after 72 hrs by Alexa Fluor 488 Annexin/propidium iodide staining-based flow cytometric analysis (Rvb = 2.07%)	2018	MedChemComm, Feb-01, Volume: 9, Issue:2	Rational design and characterization of a DNA/HDAC dual-targeting inhibitor containing nitrogen mustard and 2-aminobenzamide moieties.
AID1365211	Cytotoxicity against human PC3 assessed as inhibition of cell growth incubated for 48 hrs by resazurin reduction test	2017	Bioorganic & medicinal chemistry, 10-15, Volume: 25, Issue:20	Linker structure-activity relationships in fluorodeoxyglucose chlorambucil conjugates for tumor-targeted chemotherapy.
AID1378121	Growth inhibition of human WM266.4 cells preincubated for 6 hrs cotreated with amonafide followed compound washout measured after 24 hrs by XTT assay	2017	European journal of medicinal chemistry, Sep-29, Volume: 138	Discovery of potent molecular chimera (CM358) to treat human metastatic melanoma.
AID1272174	Chemical stability of the compound at pH 7.4 assessed as half life by LC-MS analysis	2016	Bioorganic & medicinal chemistry, Jan-15, Volume: 24, Issue:2	Synthesis, biological studies and molecular dynamics of new anticancer RGD-based peptide conjugates for targeted drug delivery.
AID1123199	Toxicity in Swiss Webster mouse assessed as lethargic behavior at 4 nmol, icv	1979	Journal of medicinal chemistry, Feb, Volume: 22, Issue:2	Synthesis and pharmacologic characterization of an alkylating analogue (chlornaltrexamine) of naltrexone with ultralong-lasting narcotic antagonist properties.
AID1412093	Antiproliferative activity against human H460 cells after 72 hrs CCK8 assay	2018	MedChemComm, Feb-01, Volume: 9, Issue:2	Rational design and characterization of a DNA/HDAC dual-targeting inhibitor containing nitrogen mustard and 2-aminobenzamide moieties.
AID382350	Cytotoxicity against human A549 cells by resazurin reduction test	2008	Bioorganic & medicinal chemistry, May-01, Volume: 16, Issue:9	Synthesis and cytotoxic properties of new fluorodeoxyglucose-coupled chlorambucil derivatives.
AID1584783	Induction of DNA-interstanded-cross-link formation in [32P]-labeled 49-mer duplex DNA (unknown origin) at 1 mM in absence of H2O2 after 16 hrs by PAGE relative to control	2018	Journal of medicinal chemistry, 10-25, Volume: 61, Issue:20	Discovery and Optimization of Novel Hydrogen Peroxide Activated Aromatic Nitrogen Mustard Derivatives as Highly Potent Anticancer Agents.
AID588213	Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in non-rodents	2010	Chemical research in toxicology, Jan, Volume: 23, Issue:1	Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.
AID9661	Compound was evaluated for in vitro cytotoxicities against Chinese hamster ovary derived AA8 cell lines.	1991	Journal of medicinal chemistry, Jan, Volume: 34, Issue:1	Synthesis and evaluation of DNA-targeted spatially separated bis(aniline mustards) as potential alkylating agents with enhanced DNA cross-linking capability.
AID224897	In vivo antitumor activity against murine S-180 sarcoma at a dose of 5 mg/kg administered intraperitoneally 7qd in Male TA1 mice; 9 survived out of 10 mice	2001	Bioorganic & medicinal chemistry letters, May-07, Volume: 11, Issue:9	2-[N1-2-pyrimidyl-aminobenzenesulfonamido] ethyl 4-bis(2-chloroethyl) aminophenyl butyrate: a potent antitumor agent.
AID408558	Antiproliferative activity against human A427 cells after 96 hrs by crystal violet assay	2008	Bioorganic & medicinal chemistry, May-15, Volume: 16, Issue:10	Synthesis of indirubin-N'-glycosides and their anti-proliferative activity against human cancer cell lines.
AID81692	Tested for in vitro concentration required to inhibit growth by 50% against HCT116 human colon cancer cell line	2002	Bioorganic & medicinal chemistry letters, Jan-21, Volume: 12, Issue:2	Polyhydroxylated azepanes as new motifs for DNA minor groove binding agents.
AID9992	Compound was evaluated for growth inhibition against A2780 wild-type ovarian cell lines; No data	2004	Journal of medicinal chemistry, Mar-25, Volume: 47, Issue:7	Synthesis and biological evaluation of novel chloroethylaminoanthraquinones with potent cytotoxic activity against cisplatin-resistant tumor cells.
AID1197747	Inhibition of human OATP1B3-mediated [3H]CCK-8 after 5 mins by Dixon plot method	2015	European journal of medicinal chemistry, Mar-06, Volume: 92	Interaction of human organic anion transporter polypeptides 1B1 and 1B3 with antineoplastic compounds.
AID536576	Growth inhibition of human HCT15 cells after 7 days by celltiter-glo assay	2010	Journal of medicinal chemistry, Nov-25, Volume: 53, Issue:22	Assessment of chemoselective neoglycosylation methods using chlorambucil as a model.
AID1665952	Protein binding in mouse plasma at 1 uM measured after 4 hrs by LC-MS/MS analysis	2020	Journal of medicinal chemistry, 09-10, Volume: 63, Issue:17	Non-rigid Diarylmethyl Analogs of Baloxavir as Cap-Dependent Endonuclease Inhibitors of Influenza Viruses.
AID1231558	Inhibition of DNA synthesis in human MDA-MB-231 cells assessed as reduction in [3H]-thymidine incorporation incubated for 24 hrs by liquid scintillation counting method	2015	Bioorganic & medicinal chemistry, Jul-01, Volume: 23, Issue:13	New pyrazolo[4,3-e][1,2,4]triazine sulfonamides as carbonic anhydrase inhibitors.
AID1393844	Antiproliferative activity against human Bel7402 cells after 72 hrs by MTT assay	2018	European journal of medicinal chemistry, Feb-25, Volume: 146	Novel enmein-type diterpenoid hybrids coupled with nitrogen mustards: Synthesis of promising candidates for anticancer therapeutics.
AID1123202	Toxicity in icv dosed Swiss Webster mouse assessed as decrease in locomotor activity	1979	Journal of medicinal chemistry, Feb, Volume: 22, Issue:2	Synthesis and pharmacologic characterization of an alkylating analogue (chlornaltrexamine) of naltrexone with ultralong-lasting narcotic antagonist properties.
AID1365033	Anticlonogenic activity against human A375 cells at 2 to 16 uM after 7 days by crystal violet staining based assay	2017	Bioorganic & medicinal chemistry letters, 09-15, Volume: 27, Issue:18	Rational design, synthesis and preliminary antitumor activity evaluation of a chlorambucil derivative with potent DNA/HDAC dual-targeting inhibitory activity.
AID1663612	Anticancer activity against human PC3 cells assessed as cell growth inhibition measured after 48 hrs by MTT assay	2020	Bioorganic & medicinal chemistry letters, 07-15, Volume: 30, Issue:14	Synthesis and anticancer activity of open-resorcinarene conjugates.
AID449958	Solubility in DMSO assessed per gram of body weight at 100 mg	2009	Bioorganic & medicinal chemistry, Sep-01, Volume: 17, Issue:17	Synthesis and evaluation of anticancer activity of 2-arylamino-6-trifluoromethyl-3-(hydrazonocarbonyl)pyridines.
AID536732	Growth inhibition of human A549 cells expressing p53 after 7 days by celltiter-glo assay	2010	Journal of medicinal chemistry, Nov-25, Volume: 53, Issue:22	Assessment of chemoselective neoglycosylation methods using chlorambucil as a model.
AID116390	Antitumor a dose 0.066 nmol/kg against po inoculated P388 leukemia in CDF1 mice	1983	Journal of medicinal chemistry, Aug, Volume: 26, Issue:8	1,3-dipalmitoylglycerol ester of chlorambucil as a lymphotropic, orally administrable antineoplastic agent.
AID1663617	Cytotoxicity against African green monkey COS7 cells assessed as cell growth inhibition measured after 48 hrs by MTT assay	2020	Bioorganic & medicinal chemistry letters, 07-15, Volume: 30, Issue:14	Synthesis and anticancer activity of open-resorcinarene conjugates.
AID1378201	Cell cycle arrest in human WM266.4 cells assessed as accumulation at G1 phase at 10 uM cotreated with amonafide after 8 hrs by propidium iodide staining based flow cytometry (Rvb = 59%)	2017	European journal of medicinal chemistry, Sep-29, Volume: 138	Discovery of potent molecular chimera (CM358) to treat human metastatic melanoma.
AID40757	The compound was tested for inhibition of B16-BL6 melanoma cells growing in culture with 0.25 mM DFMO.	1992	Journal of medicinal chemistry, Nov-13, Volume: 35, Issue:23	Synthesis and evaluation of novel spermidine derivatives as targeted cancer chemotherapeutic agents.
AID384312	Neurotoxicity in ip dosed mouse by rotarod test	2008	European journal of medicinal chemistry, Apr, Volume: 43, Issue:4	Design, synthesis and antiproliferative activity of some 3-benzylidene-2,3-dihydro-1-benzopyran-4-ones which display selective toxicity for malignant cells.
AID1393842	Antiproliferative activity against human HL60 cells after 72 hrs by MTT assay	2018	European journal of medicinal chemistry, Feb-25, Volume: 146	Novel enmein-type diterpenoid hybrids coupled with nitrogen mustards: Synthesis of promising candidates for anticancer therapeutics.
AID1057239	Cytotoxicity against human BT549 cells after 72 hrs by MTT assay	2013	Journal of medicinal chemistry, Nov-27, Volume: 56, Issue:22	A selective mitochondrial-targeted chlorambucil with remarkable cytotoxicity in breast and pancreatic cancers.
AID40758	The compound was tested for inhibition of B16-BL6 melanoma cells growing in culture.	1992	Journal of medicinal chemistry, Nov-13, Volume: 35, Issue:23	Synthesis and evaluation of novel spermidine derivatives as targeted cancer chemotherapeutic agents.
AID1663613	Anticancer activity against human K562 cells assessed as cell growth inhibition measured after 48 hrs by MTT assay	2020	Bioorganic & medicinal chemistry letters, 07-15, Volume: 30, Issue:14	Synthesis and anticancer activity of open-resorcinarene conjugates.
AID1633093	Induction of apoptosis in human HepG2/ADM cells assessed as apoptotic cells at 20 uM incubated for 72 hrs in presence of ADM by Annexin V-FITC/SYTOX Red staining based flow cytometric analysis (Rvb = 2.60%)	2017	Bioorganic & medicinal chemistry, 10-15, Volume: 25, Issue:20	A novel delocalized lipophilic cation-chlorambucil conjugate inhibits P-glycoprotein in HepG2/ADM cells.
AID153345	In vivo percentage increase in lifespan of drug treated tumor-bearing mice at a dose of 225 mg/kg	1990	Journal of medicinal chemistry, Apr, Volume: 33, Issue:4	DNA-directed alkylating agents. 1. Structure-activity relationships for acridine-linked aniline mustards: consequences of varying the reactivity of the mustard.
AID977599	Inhibition of sodium fluorescein uptake in OATP1B1-transfected CHO cells at an equimolar substrate-inhibitor concentration of 10 uM	2013	Molecular pharmacology, Jun, Volume: 83, Issue:6	Structure-based identification of OATP1B1/3 inhibitors.
AID1148043	Acute toxicity in CF1 mouse	1977	Journal of medicinal chemistry, Dec, Volume: 20, Issue:12	Antineoplastic agents. 1. N-Protected vinyl, 1,2-dihaloethyl, and cyanomethyl esters of phenylalanine.
AID1148055	Acute toxicity in CF1 mouse	1977	Journal of medicinal chemistry, Dec, Volume: 20, Issue:12	Antineoplastic agents. 2. Structure-activity studies on N-protected vinyl, 1,2-dibromoethyl, and cyanomethyl esters of several amino acids.
AID1412109	Cell cycle arrest in human A375 cells assessed as accumulation at G2/M phase at 8 uM after 72 hrs by propidium iodide/RNase staining based flow cytometric analysis relative to control	2018	MedChemComm, Feb-01, Volume: 9, Issue:2	Rational design and characterization of a DNA/HDAC dual-targeting inhibitor containing nitrogen mustard and 2-aminobenzamide moieties.
AID311524	Oral bioavailability in human	2007	Bioorganic & medicinal chemistry, Dec-15, Volume: 15, Issue:24	Hologram QSAR model for the prediction of human oral bioavailability.
AID625285	Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatic necrosis	2011	PLoS computational biology, Dec, Volume: 7, Issue:12	Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1246954	Cytotoxicity against human MCF7 cells assessed as cell viability after 5 days by cell viability analyzer	2015	European journal of medicinal chemistry, Sep-18, Volume: 102	Design and synthesis of novel hydroxyanthraquinone nitrogen mustard derivatives as potential anticancer agents via a bioisostere approach.
AID1357938	Cytotoxicity against human U87 cells assessed as reduction in cell viability after 3 days by MTT assay	2018	European journal of medicinal chemistry, May-10, Volume: 151	Therapeutic journery of nitrogen mustard as alkylating anticancer agents: Historic to future perspectives.
AID625282	Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cirrhosis	2011	PLoS computational biology, Dec, Volume: 7, Issue:12	Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1690729	Growth inhibition of human NCI-H1975 cells incubated for 5 days by SRB assay	2020	European journal of medicinal chemistry, Apr-15, Volume: 192	Comparative analysis of the dual EGFR-DNA targeting and growth inhibitory properties of 6-mono-alkylamino- and 6,6-dialkylaminoquinazoline-based type II combi-molecules.
AID1473739	Inhibition of human MRP2 overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 20 mins by membrane vesicle transport assay	2013	Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1	A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID315483	Cytotoxicity against mouse L1210 cells after 24 hrs in presence of spermidine	2008	Journal of medicinal chemistry, Mar-13, Volume: 51, Issue:5	A comparison of chloroambucil- and xylene-containing polyamines leads to improved ligands for accessing the polyamine transport system.
AID315481	Cytotoxicity against mouse L1210 cells after 48 hrs	2008	Journal of medicinal chemistry, Mar-13, Volume: 51, Issue:5	A comparison of chloroambucil- and xylene-containing polyamines leads to improved ligands for accessing the polyamine transport system.
AID408560	Antiproliferative activity against human MCF7 cells after 96 hrs by crystal violet assay	2008	Bioorganic & medicinal chemistry, May-15, Volume: 16, Issue:10	Synthesis of indirubin-N'-glycosides and their anti-proliferative activity against human cancer cell lines.
AID1185080	Antiproliferative activity against human MCF7 cells assessed as growth inhibition after 72 hrs by MTT assay	2014	ACS medicinal chemistry letters, Jul-10, Volume: 5, Issue:7	Novel hybrids of natural oridonin-bearing nitrogen mustards as potential anticancer drug candidates.
AID428554	Partition coefficient, log P after 1 hr by UV spectroscopy	2009	European journal of medicinal chemistry, Jul, Volume: 44, Issue:7	To determine the cytotoxicity of chlorambucil and one of its nitro-derivatives, conjugated to prasterone and pregnenolone, towards eight human cancer cell-lines.
AID47684	Dose required to inhibit cell growth was determined against CHO cell line	2001	Journal of medicinal chemistry, Mar-01, Volume: 44, Issue:5	Antimitotic antitumor agents: synthesis, structure-activity relationships, and biological characterization of N-aryl-N'-(2-chloroethyl)ureas as new selective alkylating agents.
AID1421495	Antiproliferative activity against human Bel7402 cells after 72 hrs by MTT assay	2018	European journal of medicinal chemistry, Oct-05, Volume: 158	Synthesis of scutellarein derivatives with antiproliferative activity and selectivity through the intrinsic pathway.
AID1132020	Antitumor activity against rat Walker 256 cells allografted in rat	1978	Journal of medicinal chemistry, Jan, Volume: 21, Issue:1	Structure-activity relationships in antitumor aniline mustards.
AID211849	Acute toxicity in mice	2003	Bioorganic & medicinal chemistry letters, Aug-04, Volume: 13, Issue:15	Synthesis of poly(ethylene glycol) with sulfadiazine and chlorambucil end groups and investigation of its antitumor activity.
AID753788	Cytotoxicity against human LNCAP cells expressing androgen receptor after 72 hrs by MTT assay	2013	European journal of medicinal chemistry, Jun, Volume: 64	Synthesis and preliminary in vitro biological evaluation of 7α-testosterone-chlorambucil hybrid designed for the treatment of prostate cancer.
AID477295	Octanol-water partition coefficient, log P of the compound	2010	European journal of medicinal chemistry, Apr, Volume: 45, Issue:4	QSPR modeling of octanol/water partition coefficient of antineoplastic agents by balance of correlations.
AID224891	Antitumor activity against murine S-180 sarcoma at dose of LD50 X 1/40 equal toxicity	2001	Bioorganic & medicinal chemistry letters, May-07, Volume: 11, Issue:9	2-[N1-2-pyrimidyl-aminobenzenesulfonamido] ethyl 4-bis(2-chloroethyl) aminophenyl butyrate: a potent antitumor agent.
AID103785	Tested for in vitro concentration required to inhibit growth by 50% against MCF-7/ADR human breast cancer cell line cell line	2002	Bioorganic & medicinal chemistry letters, Jan-21, Volume: 12, Issue:2	Polyhydroxylated azepanes as new motifs for DNA minor groove binding agents.
AID1665951	Protein binding in rat plasma at 1 uM measured after 4 hrs by LC-MS/MS analysis	2020	Journal of medicinal chemistry, 09-10, Volume: 63, Issue:17	Non-rigid Diarylmethyl Analogs of Baloxavir as Cap-Dependent Endonuclease Inhibitors of Influenza Viruses.
AID1489293	Cytotoxicity against human MIAPaCa2 cells assessed as decrease in cell viability after 48 hrs by MTS assay	2017	Journal of medicinal chemistry, 12-14, Volume: 60, Issue:23	Amphiphilic Modulation of Glycosylated Antitumor Ether Lipids Results in a Potent Triamino Scaffold against Epithelial Cancer Cell Lines and BT474 Cancer Stem Cells.
AID94800	Cytotoxicity against K562 leukemia cells in vitro, expressed as the minimal concentration necessary to inhibit incorporation of [3H]thymidine by 50%	2003	Bioorganic & medicinal chemistry letters, Feb-10, Volume: 13, Issue:3	Synthesis and preliminary cytotoxicity of nitrogen mustard derivatives of distamycin A.
AID428452	Cytotoxicity against human MDA-MB-468 cells expressing estrogen receptor after 5 days by MTT assay	2009	European journal of medicinal chemistry, Jul, Volume: 44, Issue:7	To determine the cytotoxicity of chlorambucil and one of its nitro-derivatives, conjugated to prasterone and pregnenolone, towards eight human cancer cell-lines.
AID1057232	Cytotoxicity against mitochondrial DNA-deficient human MDA-MB-435 rho theta-W01 cells after 72 hrs by MTT assay	2013	Journal of medicinal chemistry, Nov-27, Volume: 56, Issue:22	A selective mitochondrial-targeted chlorambucil with remarkable cytotoxicity in breast and pancreatic cancers.
AID224906	In vivo antitumor activity against murine S-180 sarcoma at a dose of 5 mg/kg administered intraperitoneally 7qd in mice expressed effect on tumor weight	2001	Bioorganic & medicinal chemistry letters, May-07, Volume: 11, Issue:9	2-[N1-2-pyrimidyl-aminobenzenesulfonamido] ethyl 4-bis(2-chloroethyl) aminophenyl butyrate: a potent antitumor agent.
AID625290	Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver fatty	2011	PLoS computational biology, Dec, Volume: 7, Issue:12	Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1365041	Induction of apoptosis in human A375 cells assessed as necrotic cells at 8 uM after 72 hrs by Annexin/propidium iodide staining based flow cytometry (Rvb = 1.36%)	2017	Bioorganic & medicinal chemistry letters, 09-15, Volume: 27, Issue:18	Rational design, synthesis and preliminary antitumor activity evaluation of a chlorambucil derivative with potent DNA/HDAC dual-targeting inhibitory activity.
AID227560	Alkylating activity of compound was determined by the NBP assay at 570 nm.	2002	Journal of medicinal chemistry, May-09, Volume: 45, Issue:10	Synthesis and in vitro evaluation of quaternary ammonium derivatives of chlorambucil and melphalan, anticancer drugs designed for the chemotherapy of chondrosarcoma.
AID1079941	Liver damage due to vascular disease: peliosis hepatitis, hepatic veno-occlusive disease, Budd-Chiari syndrome. Value is number of references indexed. [column 'VASC' in source]
AID1412098	Induction of apoptosis in human A375 cells assessed as late apoptotic cells at 2 uM after 72 hrs by Alexa Fluor 488 Annexin/propidium iodide staining-based flow cytometric analysis (Rvb = 10.22%)	2018	MedChemComm, Feb-01, Volume: 9, Issue:2	Rational design and characterization of a DNA/HDAC dual-targeting inhibitor containing nitrogen mustard and 2-aminobenzamide moieties.
AID467613	Volume of distribution at steady state in human	2009	European journal of medicinal chemistry, Nov, Volume: 44, Issue:11	Prediction of volume of distribution values in human using immobilized artificial membrane partitioning coefficients, the fraction of compound ionized and plasma protein binding data.
AID1421496	Cytotoxicity against human LO2 cells assessed as decrease in cell viability after 72 hrs by MTT assay	2018	European journal of medicinal chemistry, Oct-05, Volume: 158	Synthesis of scutellarein derivatives with antiproliferative activity and selectivity through the intrinsic pathway.
AID224882	In vivo antitumor activity against murine S-180 sarcoma at a dose of 2.5 mg/kg administered intraperitoneally 7qd in mice expressed as percent inhibition	2001	Bioorganic & medicinal chemistry letters, May-07, Volume: 11, Issue:9	2-[N1-2-pyrimidyl-aminobenzenesulfonamido] ethyl 4-bis(2-chloroethyl) aminophenyl butyrate: a potent antitumor agent.
AID1079939	Cirrhosis, proven histopathologically. Value is number of references indexed. [column 'CIRRH' in source]
AID1057220	Induction of nuclear DNA damage in human MIAPaCa2 cells assessed as increase in gammaH2A.X expression at 75 uM by Western blotting analysis	2013	Journal of medicinal chemistry, Nov-27, Volume: 56, Issue:22	A selective mitochondrial-targeted chlorambucil with remarkable cytotoxicity in breast and pancreatic cancers.
AID116383	Antitumor a dose 0.033 nmol/kg against ip inoculated P388 leukemia in CDF1 mice	1983	Journal of medicinal chemistry, Aug, Volume: 26, Issue:8	1,3-dipalmitoylglycerol ester of chlorambucil as a lymphotropic, orally administrable antineoplastic agent.
AID1365214	Cytotoxicity against human M4Beu assessed as inhibition of cell growth incubated for 48 hrs by resazurin reduction test	2017	Bioorganic & medicinal chemistry, 10-15, Volume: 25, Issue:20	Linker structure-activity relationships in fluorodeoxyglucose chlorambucil conjugates for tumor-targeted chemotherapy.
AID1057219	Induction of nuclear DNA damage in human MDA-MB-468 cells assessed as increase in gammaH2A.X expression at 20 uM by Western blotting analysis	2013	Journal of medicinal chemistry, Nov-27, Volume: 56, Issue:22	A selective mitochondrial-targeted chlorambucil with remarkable cytotoxicity in breast and pancreatic cancers.
AID121772	Antitumor activity measured as T/C at 0.11 nmol/kg dose against po inoculated P388 leukemia in CDF1 mice; Toxic	1983	Journal of medicinal chemistry, Aug, Volume: 26, Issue:8	1,3-dipalmitoylglycerol ester of chlorambucil as a lymphotropic, orally administrable antineoplastic agent.
AID382354	Growth inhibition in mouse L929 cells after 48 hrs	2008	Bioorganic & medicinal chemistry, May-01, Volume: 16, Issue:9	Synthesis and cytotoxic properties of new fluorodeoxyglucose-coupled chlorambucil derivatives.
AID536743	Growth inhibition of human MCF7 cells after 7 days by celltiter-glo assay	2010	Journal of medicinal chemistry, Nov-25, Volume: 53, Issue:22	Assessment of chemoselective neoglycosylation methods using chlorambucil as a model.
AID1633095	Inhibition of Pgp in human HepG2/ADM cells assessed as potentiation of ADM-induced cytotoxicity by measuring reduction in ADM IC50 at 50 uM incubated for 72 hrs by MTT assay relative to control	2017	Bioorganic & medicinal chemistry, 10-15, Volume: 25, Issue:20	A novel delocalized lipophilic cation-chlorambucil conjugate inhibits P-glycoprotein in HepG2/ADM cells.
AID1057215	Cytotoxicity against human MDA-MB-468 cells after 72 hrs by MTT assay in presence of NAC	2013	Journal of medicinal chemistry, Nov-27, Volume: 56, Issue:22	A selective mitochondrial-targeted chlorambucil with remarkable cytotoxicity in breast and pancreatic cancers.
AID111725	Antitumor activity measured as Body weight change (BWC) between day 1 and 5 at 0.066 nmol/kg dose against po inoculated P388 leukemia in CDF1 mice	1983	Journal of medicinal chemistry, Aug, Volume: 26, Issue:8	1,3-dipalmitoylglycerol ester of chlorambucil as a lymphotropic, orally administrable antineoplastic agent.
AID521220	Inhibition of neurosphere proliferation of mouse neural precursor cells by MTT assay	2007	Nature chemical biology, May, Volume: 3, Issue:5	Chemical genetics reveals a complex functional ground state of neural stem cells.
AID1555212	Antiproliferative activity against human MV4-11 cells incubated for 72 hrs by MTT assay
AID1425990	Binding affinity to recombinant human carbonic anhydrase 12 after 15 mins by stopped-flow CO2 hydration assay	2017	European journal of medicinal chemistry, Feb-15, Volume: 127	New approach of delivering cytotoxic drugs towards CAIX expressing cells: A concept of dual-target drugs.
AID153644	Increase in life span of the drug treated animals against P388 leukemia when treated at a optimal dose of 225 mg/kg	1990	Journal of medicinal chemistry, Nov, Volume: 33, Issue:11	DNA-directed alkylating agents. 3. Structure-activity relationships for acridine-linked aniline mustards: consequences of varying the length of the linker chain.
AID224745	In vivo antitumor activity against murine S-180 sarcoma at a dose of 5 mg/kg administered intraperitoneally 7qd in mice; Body wt initial/Final = 19.7/19.1	2001	Bioorganic & medicinal chemistry letters, May-07, Volume: 11, Issue:9	2-[N1-2-pyrimidyl-aminobenzenesulfonamido] ethyl 4-bis(2-chloroethyl) aminophenyl butyrate: a potent antitumor agent.
AID1555216	Antiproliferative activity against mouse BALB/3T3 cells incubated for 72 hrs by SRB assay
AID465023	Anticancer activity against human MDA-MB-231 cells assessed as cell survival after 72 hrs by MTT assay	2010	Bioorganic & medicinal chemistry letters, Mar-01, Volume: 20, Issue:5	Design, synthesis and biological evaluation of estradiol-chlorambucil hybrids as anticancer agents.
AID226473	Relative cytotoxic potency given as Hypersensitivity ratio of (IC50 for AA8 cell line) to (IC50 for P388 leukemia cell line)	1990	Journal of medicinal chemistry, Nov, Volume: 33, Issue:11	DNA-directed alkylating agents. 3. Structure-activity relationships for acridine-linked aniline mustards: consequences of varying the length of the linker chain.
AID540210	Clearance in human after iv administration	2008	Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7	Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID1633088	Induction of apoptosis in human HepG2/ADM cells assessed as viable cell at 20 uM incubated for 72 hrs by Annexin V-FITC/SYTOX Red staining based flow cytometric analysis (Rvb = 94.4%)	2017	Bioorganic & medicinal chemistry, 10-15, Volume: 25, Issue:20	A novel delocalized lipophilic cation-chlorambucil conjugate inhibits P-glycoprotein in HepG2/ADM cells.
AID428456	Cytotoxicity against human OVCA3 cells after 5 days by MTT assay	2009	European journal of medicinal chemistry, Jul, Volume: 44, Issue:7	To determine the cytotoxicity of chlorambucil and one of its nitro-derivatives, conjugated to prasterone and pregnenolone, towards eight human cancer cell-lines.
AID1197745	Inhibition of human OATP1B3-mediated [3H]CCK-8 at 100 uM after 5 mins relative to control	2015	European journal of medicinal chemistry, Mar-06, Volume: 92	Interaction of human organic anion transporter polypeptides 1B1 and 1B3 with antineoplastic compounds.
AID1057238	Cytotoxicity against human BT474 cells after 72 hrs by MTT assay	2013	Journal of medicinal chemistry, Nov-27, Volume: 56, Issue:22	A selective mitochondrial-targeted chlorambucil with remarkable cytotoxicity in breast and pancreatic cancers.
AID524796	Antiplasmodial activity against Plasmodium falciparum W2 after 72 hrs by SYBR green assay	2009	Nature chemical biology, Oct, Volume: 5, Issue:10	Genetic mapping of targets mediating differential chemical phenotypes in Plasmodium falciparum.
AID1274777	Cytotoxicity against human MCF7 cells assessed as induction of cell death at 10 uM after 72 hrs by LDH assay	2016	Journal of medicinal chemistry, Jan-14, Volume: 59, Issue:1	Synthesis and Biochemical Evaluation of 3-Phenoxy-1,4-diarylazetidin-2-ones as Tubulin-Targeting Antitumor Agents.
AID1357936	Cytotoxicity against human A549 cells assessed as reduction in cell viability after 3 days by MTT assay	2018	European journal of medicinal chemistry, May-10, Volume: 151	Therapeutic journery of nitrogen mustard as alkylating anticancer agents: Historic to future perspectives.
AID1079931	Moderate liver toxicity, defined via clinical-chemistry results: ALT or AST serum activity 6 times the normal upper limit (N) or alkaline phosphatase serum activity of 1.7 N. Value is number of references indexed. [column 'BIOL' in source]
AID79239	Comparative cellular uptake study performed on H-EMC-SS (chondrosarcoma cell line)	2002	Journal of medicinal chemistry, May-09, Volume: 45, Issue:10	Synthesis and in vitro evaluation of quaternary ammonium derivatives of chlorambucil and melphalan, anticancer drugs designed for the chemotherapy of chondrosarcoma.
AID1365029	Antiproliferative activity against human A549 cells after 72 hrs by CCK8 assay	2017	Bioorganic & medicinal chemistry letters, 09-15, Volume: 27, Issue:18	Rational design, synthesis and preliminary antitumor activity evaluation of a chlorambucil derivative with potent DNA/HDAC dual-targeting inhibitory activity.
AID746834	Therapeutic index, ratio of IC50 for human CD34-positive blood stem/progenitor cells to IC50 for human MA9.3 cells	2013	Bioorganic & medicinal chemistry letters, May-15, Volume: 23, Issue:10	Novel ROS-activated agents utilize a tethered amine to selectively target acute myeloid leukemia.
AID1690731	Growth inhibition of human A549 cells incubated for 5 days by SRB assay	2020	European journal of medicinal chemistry, Apr-15, Volume: 192	Comparative analysis of the dual EGFR-DNA targeting and growth inhibitory properties of 6-mono-alkylamino- and 6,6-dialkylaminoquinazoline-based type II combi-molecules.
AID1421494	Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay	2018	European journal of medicinal chemistry, Oct-05, Volume: 158	Synthesis of scutellarein derivatives with antiproliferative activity and selectivity through the intrinsic pathway.
AID428454	Cytotoxicity against human MCF7 cells expressing estrogen and progesterone receptor after 5 days by MTT assay	2009	European journal of medicinal chemistry, Jul, Volume: 44, Issue:7	To determine the cytotoxicity of chlorambucil and one of its nitro-derivatives, conjugated to prasterone and pregnenolone, towards eight human cancer cell-lines.
AID1130928	Antitumor activity against mouse B16 cells allografted in BDF mouse assessed as increase in life span at 8 mg/kg, ip administered for 9 days relative to untreated control	1979	Journal of medicinal chemistry, Oct, Volume: 22, Issue:10	Structure-activity relationship of aniline mustards acting against B-16 melanoma in mice.
AID1365213	Cytotoxicity against human A549 assessed as inhibition of cell growth incubated for 48 hrs by resazurin reduction test	2017	Bioorganic & medicinal chemistry, 10-15, Volume: 25, Issue:20	Linker structure-activity relationships in fluorodeoxyglucose chlorambucil conjugates for tumor-targeted chemotherapy.
AID224738	Antitumor activity against murine S-180 sarcoma at dose of 0.022(mmol/kg)	2001	Bioorganic & medicinal chemistry letters, May-07, Volume: 11, Issue:9	2-[N1-2-pyrimidyl-aminobenzenesulfonamido] ethyl 4-bis(2-chloroethyl) aminophenyl butyrate: a potent antitumor agent.
AID43581	Inhibition of beta-lactamase at 100 uM	2003	Journal of medicinal chemistry, Oct-09, Volume: 46, Issue:21	Identification and prediction of promiscuous aggregating inhibitors among known drugs.
AID19006	Calculated membrane partition coefficient (Kmemb)	2004	Journal of medicinal chemistry, Mar-25, Volume: 47, Issue:7	Surface activity profiling of drugs applied to the prediction of blood-brain barrier permeability.
AID382349	Cytotoxicity against human MCF7 cells by resazurin reduction test	2008	Bioorganic & medicinal chemistry, May-01, Volume: 16, Issue:9	Synthesis and cytotoxic properties of new fluorodeoxyglucose-coupled chlorambucil derivatives.
AID116393	Antitumor a dose 0.11 nmol/kg against po inoculated P388 leukemia in CDF1 mice; Toxic	1983	Journal of medicinal chemistry, Aug, Volume: 26, Issue:8	1,3-dipalmitoylglycerol ester of chlorambucil as a lymphotropic, orally administrable antineoplastic agent.
AID625286	Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatitis	2011	PLoS computational biology, Dec, Volume: 7, Issue:12	Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1412092	Antiproliferative activity against human H1299 cells after 72 hrs CCK8 assay	2018	MedChemComm, Feb-01, Volume: 9, Issue:2	Rational design and characterization of a DNA/HDAC dual-targeting inhibitor containing nitrogen mustard and 2-aminobenzamide moieties.
AID1690748	Induction of DNA damage in human A549 cells at 0.1 to 10 uM after 2 hrs by comet assay	2020	European journal of medicinal chemistry, Apr-15, Volume: 192	Comparative analysis of the dual EGFR-DNA targeting and growth inhibitory properties of 6-mono-alkylamino- and 6,6-dialkylaminoquinazoline-based type II combi-molecules.
AID154140	Dose required to inhibit cell growth was determined against P388D1 cell line of murine lymphocytotic leukemia	2001	Journal of medicinal chemistry, Mar-01, Volume: 44, Issue:5	Antimitotic antitumor agents: synthesis, structure-activity relationships, and biological characterization of N-aryl-N'-(2-chloroethyl)ureas as new selective alkylating agents.
AID79238	In vitro cytotoxicity in chondrosarcoma cell line (H-EMC-SS) by Hoechst 33342 DNA Fluorometric assay	2002	Journal of medicinal chemistry, May-09, Volume: 45, Issue:10	Synthesis and in vitro evaluation of quaternary ammonium derivatives of chlorambucil and melphalan, anticancer drugs designed for the chemotherapy of chondrosarcoma.
AID152672	Optimal dose of drug administered as a single dose in 0.1 or 0.2 mL of 30% v/v ethanol/water on day one after ip inoculation of 10e6 P388 leukemia cells	1990	Journal of medicinal chemistry, Apr, Volume: 33, Issue:4	DNA-directed alkylating agents. 1. Structure-activity relationships for acridine-linked aniline mustards: consequences of varying the reactivity of the mustard.
AID151252	Evaluation in vivo against P338 cell line for percentage increase in lifespan of drug-treated tumor-bearing animals when treated at 225 mg/kg dose.(ILS)	1991	Journal of medicinal chemistry, May, Volume: 34, Issue:5	DNA-directed alkylating agents. 4. 4-anilinoquinoline-based minor groove directed aniline mustards.
AID1555214	Antiproliferative activity against human MCF7 cells incubated for 72 hrs by SRB assay
AID1437141	Antiproliferative activity against human MIAPaCa2 cells after 72 hrs by MTT assay	2017	Bioorganic & medicinal chemistry letters, 02-15, Volume: 27, Issue:4	Synthesis and biological evaluation of 2-alkoxycarbonylallyl esters as potential anticancer agents.
AID1231557	Inhibition of DNA synthesis in human MCF7 cells assessed as reduction in [3H]-thymidine incorporation incubated for 24 hrs by liquid scintillation counting method	2015	Bioorganic & medicinal chemistry, Jul-01, Volume: 23, Issue:13	New pyrazolo[4,3-e][1,2,4]triazine sulfonamides as carbonic anhydrase inhibitors.
AID1365027	Induction of DNA damage in human A375 cells assessed as increase in gammaH2AX level at 16 uM after 48 hrs by high throughput assay relative to control	2017	Bioorganic & medicinal chemistry letters, 09-15, Volume: 27, Issue:18	Rational design, synthesis and preliminary antitumor activity evaluation of a chlorambucil derivative with potent DNA/HDAC dual-targeting inhibitory activity.
AID224735	Antitumor activity against murine S-180 sarcoma at dose of 0.004(mmol/kg)	2001	Bioorganic & medicinal chemistry letters, May-07, Volume: 11, Issue:9	2-[N1-2-pyrimidyl-aminobenzenesulfonamido] ethyl 4-bis(2-chloroethyl) aminophenyl butyrate: a potent antitumor agent.
AID45745	Inhibitory activity of compound for AA8 cells to reduce cell density by 50% (exposed to compound for 4 hours)	1989	Journal of medicinal chemistry, Jan, Volume: 32, Issue:1	Hypoxia-selective antitumor agents. 2. Electronic effects of 4-substituents on the mechanisms of cytotoxicity and metabolic stability of nitracrine derivatives.
AID1365210	Cytotoxicity against human fibroblasts assessed as inhibition of cell growth incubated for 48 hrs by resazurin reduction test	2017	Bioorganic & medicinal chemistry, 10-15, Volume: 25, Issue:20	Linker structure-activity relationships in fluorodeoxyglucose chlorambucil conjugates for tumor-targeted chemotherapy.
AID1665882	Stability in simulated intestinal fluid assessed as parent compound remaining at 1 uM measured after 4 hrs at pH 1.2 by LC-MS/MS analysis	2020	Journal of medicinal chemistry, 09-10, Volume: 63, Issue:17	Non-rigid Diarylmethyl Analogs of Baloxavir as Cap-Dependent Endonuclease Inhibitors of Influenza Viruses.
AID153651	Optimal dose (i.p.) given after inoculation with wild type 10 E 6 P388/W leukemia cell lines, measured on day 1	1990	Journal of medicinal chemistry, Nov, Volume: 33, Issue:11	DNA-directed alkylating agents. 3. Structure-activity relationships for acridine-linked aniline mustards: consequences of varying the length of the linker chain.
AID1365040	Induction of apoptosis in human A375 cells assessed as late apoptotic cells at 8 uM after 72 hrs by Annexin/propidium iodide staining based flow cytometry (Rvb = 6.95%)	2017	Bioorganic & medicinal chemistry letters, 09-15, Volume: 27, Issue:18	Rational design, synthesis and preliminary antitumor activity evaluation of a chlorambucil derivative with potent DNA/HDAC dual-targeting inhibitory activity.
AID1690730	Growth inhibition of human PC-9 cells incubated for 5 days by SRB assay	2020	European journal of medicinal chemistry, Apr-15, Volume: 192	Comparative analysis of the dual EGFR-DNA targeting and growth inhibitory properties of 6-mono-alkylamino- and 6,6-dialkylaminoquinazoline-based type II combi-molecules.
AID142437	Optimal dose administered as a single dose by intraperitoneal inoculation of 10 X E6 murine leukemia P388 cell lines.	1991	Journal of medicinal chemistry, Jan, Volume: 34, Issue:1	Synthesis and evaluation of DNA-targeted spatially separated bis(aniline mustards) as potential alkylating agents with enhanced DNA cross-linking capability.
AID229745	Hypersensitivity factor value is IC50 of (AA8) to that of UV4 where UV4 is a mutant AA8 line lacking the ability to perform incision repair	1991	Journal of medicinal chemistry, May, Volume: 34, Issue:5	DNA-directed alkylating agents. 4. 4-anilinoquinoline-based minor groove directed aniline mustards.
AID1378122	Growth inhibition of human A172 cells preincubated for 6 hrs followed compound washout measured after 24 hrs by XTT assay	2017	European journal of medicinal chemistry, Sep-29, Volume: 138	Discovery of potent molecular chimera (CM358) to treat human metastatic melanoma.

Timeframe	Studies, This Drug (%)	All Drugs %
pre-1990	2087 (57.52)	18.7374
1990's	580 (15.99)	18.2507
2000's	439 (12.10)	29.6817
2010's	406 (11.19)	24.3611
2020's	116 (3.20)	2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Publication Type	This drug (%)	All Drugs (%)
Trials	388 (9.92%)	5.53%
Reviews	350 (8.95%)	6.00%
Case Studies	637 (16.29%)	4.05%
Observational	5 (0.13%)	0.25%
Other	2,531 (64.71%)	84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (52)

Trial Overview

Trial	Phase	Enrollment	Study Type	Start Date	Status
Study of Bendamustine Hydrochloride Injection in Previously Untreated Chronic Lymphocytic Leukemia Patients [NCT01109264]	Phase 2	147 participants (Actual)	Interventional	2010-03-31	Completed
A Prospective, Open-Label, Multicenter Randomized Phase III Trial to Compare The Efficacy and Safety of A Combined Regimen of Obinutuzumab and Venetoclax Versus Obinutuzumab and Chlorambucil in Previously Untreated Patients With CLL and Coexisting Medical [NCT02242942]	Phase 3	445 participants (Actual)	Interventional	2014-12-31	Active, not recruiting
A Multicenter, Double-Blind, Randomized, and Placebo-controlled Phase Ib Study Evaluating the Safety of Adding Tocilizumab to Standard Premedications Prior to Administration of Obinutuzumab in Combination With Chlorambucil in Patients With Previously Untr [NCT02336048]	Phase 1	38 participants (Actual)	Interventional	2015-06-26	Terminated(stopped due to This study was terminated early because premedication with tocilizumab was unlikely to reduce the risk of IRR.)
A Multi-center Phase I/Ib Study Evaluating the Efficacy and Safety of TGR-1202, a Novel PI3K Delta Inhibitor, in Combination With Obinutuzumab and Chlorambucil in Patients With Chronic Lymphocytic Leukemia (CLL) [NCT02100852]	Phase 1	19 participants (Actual)	Interventional	2014-03-12	Completed
A Phase II Study of Chlorambucil in Combination With Subcutaneous Rituximab Followed by Maintenance Therapy With Subcutaneous Rituximab in Patients With Extranodal Marginal Zone B-cell Lymphoma of Mucosa Associated Lymphoid Tissue (MALT Lymphoma) [NCT01808599]	Phase 2	112 participants (Actual)	Interventional	2013-12-31	Active, not recruiting
A Randomized, Controlled, Open, Multicenter Phase 3 Study to Evaluate ICP-022 Versus Chlorambucil Combined With Rituximab for Primary Treatment of Chronic Lymphocytic Leukemia(CLL)/ Small Lymphocytic Lymphoma(SLL) [NCT04578613]	Phase 3	218 participants (Anticipated)	Interventional	2021-01-08	Recruiting
A Phase 3, Multicenter, Randomized, Openlabel, Parallel-Group Study of the Efficacy and Safety of Lenalidomide (Revlimid®) Versus Chlorambucil as First-Line Therapy for Previously Untreated Elderly Patients With B-Cell Chronic Lymphocytic Leukemia (The Or [NCT00910910]	Phase 3	450 participants (Actual)	Interventional	2009-10-13	Completed
Multicenter Uveitis Steroid Treatment (MUST) Trial [NCT00132691]	Phase 4	255 participants (Actual)	Interventional	2005-09-30	Completed
A Multicenter, Single Arm, Non-Interventional, Observational Study of Obinutuzumab to Evaluate Efficacy, Safety and Cost of Disease Management in Patients With Chronic Lymphocytic Leukemia and Comorbidities in Greece [NCT02915224]		50 participants (Actual)	Observational	2016-11-23	Completed
A Study of Chlorambucil Plus MabThera as Induction Therapy Followed in Responders by Maintenance Therapy Versus Observation on Response Rate in Patients >=60 Years With Previously Untreated Chronic Lymphocytic Leukemia [NCT00738374]	Phase 2	97 participants (Actual)	Interventional	2008-11-03	Completed
A Randomised Trial of Chlorambucil Versus Fludarabine as Initial Therapy of Waldenström's Macroglobulinaemia and Splenic Lymphoma With Villous Lymphocytes [NCT00608374]	Phase 3	400 participants (Anticipated)	Interventional	2006-06-30	Completed
A Phase 3, Randomized Study to Assess the Efficacy and Safety of Ublituximab in Combination With TGR-1202 Compared to Obinutuzumab in Combination With Chlorambucil in Patients With Chronic Lymphocytic Leukemia (CLL) [NCT02612311]	Phase 3	603 participants (Actual)	Interventional	2015-11-19	Completed
A Phase III, Open Label, Randomized, Multicenter Trial of Ofatumumab Added to Chlorambucil Versus Chlorambucil Monotherapy in Previously Untreated Patients With Chronic Lymphocytic Leukemia [NCT00748189]	Phase 3	447 participants (Actual)	Interventional	2008-12-22	Terminated(stopped due to Majority of patients (62%) had been treated with next line therapies, including new highly effective therapies confounding the interpretation of the OS results.)
A Randomized, Multi-Center, Phase II Study to Investigate the Safety and Efficacy of SDX-101 (R-etodolac) in Combination With Chlorambucil, and That of Chlorambucil Alone, in Patients With Chronic Lymphocytic Leukemia (CLL) [NCT00151736]	Phase 2	88 participants (Actual)	Interventional	2004-09-30	Terminated
Randomized Trial Comparing the Efficacy of Chlorambucil to Fludarabine in Patients With Advanced Waldenström Macroglobulinemia,Lymphoplasmacytic Lymphoma or Splenic Marginal Zone Lymphoma [NCT00566332]	Phase 3	414 participants (Actual)	Interventional	2001-06-30	Completed
Randomized Trial of MCD Versus FMD in Untreated Advanced Follicular Lymphoma [NCT00006250]	Phase 3	500 participants (Anticipated)	Interventional	2000-05-31	Active, not recruiting
A Phase I Study to Investigate the Safety and Clinical Activity of Idelalisib in Combination With Chemotherapeutic Agents, Immunomodulatory Agents and Anti-CD20 mAb in Subjects With Relapsed or Refractory Indolent B-cell Non-Hodgkin Lymphoma, Mantle Cell [NCT01088048]	Phase 1	241 participants (Actual)	Interventional	2010-03-25	Completed
An Open-label Extension Study in Patients 65 Years or Older With Chronic Lymphocytic Leukemia (CLL) or Small Lymphocytic Lymphoma (SLL) Who Participated in Study PCYC-1115-CA (Ibrutinib Versus Chlorambucil) [NCT01724346]	Phase 3	232 participants (Actual)	Interventional	2012-08-28	Completed
An Open-Label Study to Characterize the Safety and Response Rate of MabThera (Rituximab) Plus Chlorambucil in Previously Untreated Patients With CD20-Positive B-Cell Chronic Lymphocytic Leukemia [NCT00532129]	Phase 2	100 participants (Actual)	Interventional	2007-11-30	Completed
An Open-label, Multi-center, Three Arm Randomized Study to Investigate the Safety and Efficacy on Progression-free Survival of RO5072759 + Chlorambucil (GClb) Compared to Rituximab + Chlorambucil (RClb) or Chlorambucil (Clb) Alone in Previously Untreated [NCT01010061]	Phase 3	787 participants (Actual)	Interventional	2009-12-21	Completed
A Pilot Study of Chlorambucil in Pre-treated Metastatic Pancreatic Adenocarcinoma Patients Bearing a Germ Line BRCA or Other DNA Defects Repair (DDR) Mutations. [NCT04692740]	Phase 2	20 participants (Actual)	Interventional	2020-12-18	Active, not recruiting
Prospective Randomized Study to Compare Efficacy and Safety of RFC-Lite (Rituximab, Fludarabine, Cyclophosphamide) Regimen With LR (Rituximab, Chlorambucil) as a First-Line Therapy in Patients With B-Cell Chronic Lymphocytic Leukemia and Unfavorable Somat [NCT01283386]	Phase 4	26 participants (Actual)	Interventional	2011-04-27	Terminated
Chronic Lymphocytic Leukemia Trial 4: A Randomized Comparison of Chlorambucil, Fludarabine and Fludarabine Plus Cyclophosphamide [NCT00004218]	Phase 3	0 participants	Interventional	1999-10-31	Completed
Fludarabine Versus Chlorambucil in First Line Therapy of Elderly Patients (More Than 65 Years) With Advanced Chronic Lymphocytic Leukemia [NCT00262795]	Phase 3	206 participants (Actual)	Interventional	2003-09-30	Completed
Hodgkin's Disease Study [NCT00416377]		353 participants (Anticipated)	Interventional		Active, not recruiting
A Phase I-II Trial of Gleevec (Imatinib Mesylate) in Combination With Chlorambucil in Previously Treated Chronic Lymphocytic Leukemia (CLL) Patients [NCT00558961]	Phase 1/Phase 2	13 participants (Actual)	Interventional	2005-10-31	Terminated(stopped due to Unsatisfactory enrollment)
A Prospective Randomized Open-label Study to Compare Mycophenolate Mofetil and Corticosteroid With Conventional Immunosuppressive Treatment on Proteinuria in Idiopathic Membranous Nephropathy (MN) and Focal Segmental Glomerulosclerosis (FSGS) [NCT00404833]	Phase 3	16 participants (Anticipated)	Interventional	2003-01-31	Completed
Low Dose Chlorambucil Maintenance Vs. No Treatment Following High-Dose Chlorambucil Induction In Patients With Advanced B-Chronic Lymphocytic Leukemia. A Randomized Phase III Study Of The EORTC LG (CLL-3) [NCT00017108]	Phase 3	0 participants	Interventional	2001-03-31	Active, not recruiting
Protocol For The Treatment Of Children And Adolescents With Hodgkin's Disease [NCT00025064]	Phase 2	260 participants (Anticipated)	Interventional	2000-01-31	Active, not recruiting
Chlorambucil Versus 2x2 Gy Involved Field Radiotherapy in Stage III/IV Previously Untreated Follicular Lymphoma Patients. A Prospective, Randomized Phase III Clinical Trial [NCT00028691]	Phase 3	0 participants	Interventional	2002-12-31	Active, not recruiting
Randomized, Multicenter, Open-label, Phase 3 Study of the Bruton's Tyrosine Kinase Inhibitor Ibrutinib Versus Chlorambucil in Patients 65 Years or Older With Treatment-naive Chronic Lymphocytic Leukemia or Small Lymphocytic Lymphoma [NCT01722487]	Phase 3	269 participants (Actual)	Interventional	2013-03-31	Completed
A Randomised Investigation of Alternative Ofatumumab-containing Regimens in Less Fit Patients With CLL [NCT01678430]	Phase 3	670 participants (Anticipated)	Interventional	2011-12-31	Recruiting
Hodgkins Disease Study [NCT00417014]		358 participants (Anticipated)	Interventional		Active, not recruiting
Treatment in First Line of Mantle Cell Lymphoma for Patients Under 66 Years by the VAD-CHLORAMBUCIL -Rituximab Regimen Followed by Intensification and Autologous PBSC Transplantation After Marrow Purging With Rituximab [NCT00285389]	Phase 2	39 participants (Actual)	Interventional	2002-02-28	Completed
Study of Bendamustine Hydrochloride Injection in Previously Untreated Chronic Lymphocytic Leukemia Patients [NCT01657955]	Phase 3	96 participants (Anticipated)	Interventional	2011-01-31	Recruiting
Phase I-II Multicenter Study to Assess the Efficacy and Safety of the Chlorambucil + Lenalidomide Combination and Lenalidomide Maintenance Therapy in Untreated Elderly Pts With CLL. EudraCT Number 2009-013415-35 [NCT01403246]	Phase 1/Phase 2	9 participants (Actual)	Interventional	2011-11-30	Terminated(stopped due to Slow patient enrollment and new molecules for chronic lymphoid leukemia, have importantly reduced the interest of conducting the phase II of this study.)
Multicenter Randomized Trial of Chlorambucil Versus Chlorambucil Plus Rituximab Versus Rituximab in Extranodal Marginal Zone B-cell Lymphoma of Mucosa Associated Lymphoid Tissue (MALT Lymphoma) [NCT00210353]	Phase 3	454 participants (Actual)	Interventional	2003-01-31	Completed
A Randomized Study to Assess the Effect on Response Rate of MabThera (Rituximab) Added to a Standard Chemotherapy, Bendamustine or Chlorambucil, in Patients With Chronic Lymphocytic Leukemia [NCT01056510]	Phase 4	357 participants (Actual)	Interventional	2010-03-31	Completed
A UKLG Randomised Trial of Initial Chemotherapy for Advanced Stage Hodgkins Disease [NCT00003421]	Phase 3	800 participants (Anticipated)	Interventional	1998-06-30	Completed
A Randomized, Multi-center, Open-label, Phase 3 Study of the Bruton's Tyrosine Kinase Inhibitor Ibrutinib in Combination With Obinutuzumab Versus Chlorambucil in Combination With Obinutuzumab in Subjects With Treatment-naïve Chronic Lymphocytic Leukemia o [NCT02264574]	Phase 3	229 participants (Actual)	Interventional	2014-10-06	Completed
Randomised Controlled Trial of CID (Chlorambucil, Idarubicin, Dexamethasone) Versus CD (Chlorambucil, Dexamethasone) for Induction of Remission in Low Grade Non-Hodgkin's Lymphoma (Kiel Classification) Followed by Randomised Controlled Assessment of Stand [NCT00003639]	Phase 3	200 participants (Anticipated)	Interventional	1993-11-30	Active, not recruiting
An Open-label, Multi-center, Three Arm Randomized Study to Investigate the Safety and Efficacy on Progression-free Survival of RO5072759 + Chlorambucil (GClb) Compared to Rituximab + Chlorambucil (RClb) or Chlorambucil (Clb) Alone in Previously Untreated [NCT01998880]	Phase 3	787 participants (Actual)	Interventional	2009-12-22	Completed
A Randomized, Multicenter, Open-Label, Phase 3 Study to Evaluate the Efficacy and Safety of Acalabrutinib Versus Chlorambucil Plus Rituximab in Subjects With Previously Untreated Chronic Lymphocytic Leukemia [NCT04075292]	Phase 3	155 participants (Actual)	Interventional	2020-01-20	Active, not recruiting
A Multicenter, Open-Label, Single-Arm, Phase IIIb, International Study Evaluating the Safety of Obinutuzumab Alone or in Combination With Chemotherapy in Patients With Previously Untreated or Relapsed/Refractory Chronic Lymphocytic Leukemia [NCT01905943]	Phase 3	979 participants (Actual)	Interventional	2013-11-04	Completed
An Expanded Access, Open-Label Study of Obinutuzumab (GA101) Plus Chlorambucil in Patients With Previously Untreated Chronic Lymphocytic Leukemia [NCT01868893]	Phase 2	20 participants (Actual)	Interventional	2013-08-31	Completed
A Phase 3, Randomized, Open-Label Study Evaluating the Efficacy and Safety of Idelalisib in Combination With Obinutuzumab Compared to Chlorambucil in Combination With Obinutuzumab for Previously Untreated Chronic Lymphocytic Leukemia [NCT01980875]	Phase 3	57 participants (Actual)	Interventional	2015-04-21	Terminated
A Randomized, Multicenter, Open-Label, 3 Arm Phase 3 Study of Obinutuzumab in Combination With Chlorambucil, Acalabrutinib (ACP-196) in Combination With Obinutuzumab, and Acalabrutinib Monotherapy in Subjects With Previously Untreated CLL [NCT02475681]	Phase 3	535 participants (Actual)	Interventional	2015-06-26	Active, not recruiting
A Randomized, Open-label, Phase 3 Study of the Combination of Ibrutinib Plus Venetoclax Versus Chlorambucil Plus Obinutuzumab for the First-line Treatment of Subjects With Chronic Lymphocytic Leukemia (CLL)/Small Lymphocytic Lymphoma (SLL). [NCT03462719]	Phase 3	211 participants (Actual)	Interventional	2018-04-17	Active, not recruiting
Protocol for a Randomised Trial of Observation Versus Chlorambucil After Anti-Helicobacter Therapy in Low Grade Gastric Lymphoma [NCT00003617]	Phase 3	200 participants (Anticipated)	Interventional	1995-03-31	Active, not recruiting
A Phase I/II, Open-label Study of Ofatumumab Added to Chlorambucil in Previously Untreated Japanese Patients With Chronic Lymphocytic Leukemia [NCT01563055]	Phase 2	10 participants (Actual)	Interventional	2012-04-30	Completed
A Phase II, Open Label, Single Arm, Multicenter Study of Chlorambucil in Japanese Previously Untreated Patients With Chronic Lymphocytic Leukemia [NCT01808326]	Phase 2	5 participants (Actual)	Interventional	2013-04-30	Completed
An Open-label, Multi-center, Three Arm Randomized Study to Investigate the Safety and Efficacy on Progression-free Survival of RO5072759 + Chlorambucil (GClb) Compared to Rituximab + Chlorambucil (RClb) or Chlorambucil (Clb) Alone in Previously Untreated [NCT02053610]	Phase 3	787 participants (Actual)	Interventional	2009-12-31	Completed
[information is prepared from clinicaltrials.gov, extracted Sep-2024]

Trial Outcomes

Trial	Outcome
NCT00132691 (17) [back to overview]	Mortality
NCT00132691 (17) [back to overview]	Intraocular Pressure - Incident IOP Elevation >= 10 mmHg Above Baseline
NCT00132691 (17) [back to overview]	Intraocular Pressure - Incident IOP Greater Than or Equal to 24 mm Hg
NCT00132691 (17) [back to overview]	Change in Best-corrected Visual Acuity (Change in the Numbers of Letters Read From a Standard ETDRS Eye Chart) From Baseline to 24 Months in Eyes With Uveitis
NCT00132691 (17) [back to overview]	Change in Self-reported Vision-related Function as Measured by the National Eye Institute 25-Item Visual Function Questionnaire (NEI-VFQ 25) Vision Targeted Composite Score From Baseline to 24 Months
NCT00132691 (17) [back to overview]	Change in SF-36 Mental Component Score From Baseline to 24 Months
NCT00132691 (17) [back to overview]	Change in SF-36 Physical Component Score From Baseline to 24 Months
NCT00132691 (17) [back to overview]	Diabetes Mellitus
NCT00132691 (17) [back to overview]	Glaucoma - Incident
NCT00132691 (17) [back to overview]	Intraocular Pressure - Incident IOP Greater Than or Equal to 30 mm Hg
NCT00132691 (17) [back to overview]	Intraocular Pressure - IOP-lowering Surgery
NCT00132691 (17) [back to overview]	Intraocular Pressure (IOP) - Incident Use of IOP-lowering Medical Therapy (Percentage of Eyes With Uveitis That Were Not Being Treated With IOP-lowering Medical Therapy at Baseline and Underwent IOP Lowering Therapy During the 24 Month Follow-up.
NCT00132691 (17) [back to overview]	Macular Edema
NCT00132691 (17) [back to overview]	Cataract - Incident Cataract
NCT00132691 (17) [back to overview]	Hyperlipidemia - Incident
NCT00132691 (17) [back to overview]	Uveitis Activity
NCT00132691 (17) [back to overview]	Hypertension Diagnosis Requiring Treatment
NCT00210353 (5) [back to overview]	Event-free-survival (EFS)
NCT00210353 (5) [back to overview]	Complete and Partial Remission Rate - Percentage of Patients With Complete and Partial Response at the End of Treatment
NCT00210353 (5) [back to overview]	Response Duration (Time to Relapse or Progression) - Percentage of Patients in Continuous Remission at Five Years From Trial Registration
NCT00210353 (5) [back to overview]	Progression-free-survival (PFS)
NCT00210353 (5) [back to overview]	Overall Survival
NCT00532129 (15) [back to overview]	Percentage of Participants With BOR of Partial Response (PR)
NCT00532129 (15) [back to overview]	Percentage of Participants With BOR of Progressive Disease (PD)
NCT00532129 (15) [back to overview]	Percentage of Participants With BOR of Stable Disease (SD)
NCT00532129 (15) [back to overview]	Percentage of Participants With Objective Response (CR or PR)
NCT00532129 (15) [back to overview]	Percentage of Participants With Treatment-Emergent Adverse Events (AEs)
NCT00532129 (15) [back to overview]	Progression Free Survival (PFS) Time
NCT00532129 (15) [back to overview]	Mean Change From Baseline (CFB) in European Organisation for Research and Treatment of Cancer Quality of Life Questionnaire Core 30 (EORTC QLQ-C30) Scores
NCT00532129 (15) [back to overview]	Percentage of Participants With Best Overall Response (BOR) of Clinical CR or Confirmed CR
NCT00532129 (15) [back to overview]	Percentage of Participants With BOR of Nodular Partial Response (nPR)
NCT00532129 (15) [back to overview]	Percentage of Participants Who Died
NCT00532129 (15) [back to overview]	Percentage of Participants Who Achieved Minimal Residual Disease (MRD) Negativity
NCT00532129 (15) [back to overview]	Duration of Response (DoR)
NCT00532129 (15) [back to overview]	Disease Free Survival (DFS) Time
NCT00532129 (15) [back to overview]	Overall Survival (OS) Time
NCT00532129 (15) [back to overview]	Percentage of Participant With Disease Progression or Death
NCT00738374 (20) [back to overview]	Number of Participants With Immunophenotypic CR - BM, Immunophenotypic CR - Peripheral Blood (PB), Molecular CR - BM, or Molecular CR - PB at the End of Induction Treatment
NCT00738374 (20) [back to overview]	Percentage of Participants With CR, CRi, PR, SD, PD, or Relapse at the End of Study
NCT00738374 (20) [back to overview]	Percentage of Participants With CR, CRi, PR, Stable Disease (SD), Progressive Disease (PD), Relapse, or Nodular PR at the End of Induction Treatment
NCT00738374 (20) [back to overview]	Percentage of Participants With CR, PR, SD, PD, Relapse, or Nodular PR at the End of Study
NCT00738374 (20) [back to overview]	Percentage of Participants With Immunophenotypic CR - BM or Immunophenotypic CR - PB at the End of Study
NCT00738374 (20) [back to overview]	Percentage of Participants With Molecular CR - BM or Molecular CR - PB at the End of Study
NCT00738374 (20) [back to overview]	Disease-Free Survival
NCT00738374 (20) [back to overview]	Duration of Response
NCT00738374 (20) [back to overview]	EFS
NCT00738374 (20) [back to overview]	Number of Participants Who Died
NCT00738374 (20) [back to overview]	Number of Participants With Disease Progression or Death
NCT00738374 (20) [back to overview]	Number of Participants With Disease Progression, Relapse, Death, Withdrawal Because of an Adverse Event (AE), or New CLL Treatment
NCT00738374 (20) [back to overview]	Number of Participants With New CLL Treatment or Death
NCT00738374 (20) [back to overview]	Number of Participants With PD or Death After a Confirmed CR, CRi, or PR
NCT00738374 (20) [back to overview]	Number of Participants With PD or Death After a Confirmed CR/CRi
NCT00738374 (20) [back to overview]	OS
NCT00738374 (20) [back to overview]	Percentage of Participants With Documented CR, CRi, or PR at the End of Induction Treatment
NCT00738374 (20) [back to overview]	Percentage of Participants With Documented CR, CRi, or PR at the End of Study
NCT00738374 (20) [back to overview]	PFS
NCT00738374 (20) [back to overview]	Time to Next Treatment (TTNT)
NCT00748189 (25) [back to overview]	Duration of Response (DOR), as Assessed by the IRC
NCT00748189 (25) [back to overview]	Number of Participants With Any Adverse Event (AE) or Serious Adverse Event (SAE)
NCT00748189 (25) [back to overview]	Number of Participants With AEs and SAEs of Maximum Severity of Grade 3 or Higher
NCT00748189 (25) [back to overview]	Number of Participants With Improvement in Constitutional Symptoms (CS)
NCT00748189 (25) [back to overview]	Number of Participants With Improvement in ECOG Performance Status of 0 or 1
NCT00748189 (25) [back to overview]	Number of Participants With the Best Overall Response (OR), as Assessed by the IRC
NCT00748189 (25) [back to overview]	Progression-Free Survival (PFS), as Assessed by the Independent Review Committee (IRC)
NCT00748189 (25) [back to overview]	Number of Participants With a Human Anti-human Antibody (HAHA) Positive Result
NCT00748189 (25) [back to overview]	Number of Participants With at Least One Grade 3/Grade 4 Myelosuppression (Anemia, Neutropenia, and Thrombocytopenia)
NCT00748189 (25) [back to overview]	Number of Participants With Autoimmune Hemolytic Anaemia (AIHA) Disease
NCT00748189 (25) [back to overview]	Overall Survival
NCT00748189 (25) [back to overview]	Plasma Half Life (t1/2) of Ofatumumab
NCT00748189 (25) [back to overview]	Volume of Distribution at Steady State (Vss) of Ofatumumab
NCT00748189 (25) [back to overview]	Time to Next Therapy
NCT00748189 (25) [back to overview]	Time to Progression, as Assessed by the IRC
NCT00748189 (25) [back to overview]	Time to Response, as Assessed by the IRC
NCT00748189 (25) [back to overview]	Total Plasma Clearance (CL) of Ofatumumab
NCT00748189 (25) [back to overview]	AUC(0-tau) of Ofatumumab
NCT00748189 (25) [back to overview]	Change From Baseline in Health Related Quality of Life (HRQOL)
NCT00748189 (25) [back to overview]	Cmax and Ctrough of Ofatumumab
NCT00748189 (25) [back to overview]	Dose-normalized AUC(0-6) and AUC(0-inf) of Chlorambucil and Dose-normalized AUC(0-6) of Phenylacetic Acid Mustard (PAAM)
NCT00748189 (25) [back to overview]	Dose-normalized Cmax of Chlorambucil and Phenylacetic Acid Mustard (PAAM)
NCT00748189 (25) [back to overview]	Mean Change From Baseline in the Immunoglobulin (Ig) Antibodies IgA, IgG, and IgM
NCT00748189 (25) [back to overview]	Number of Participants Who Received no Transfusion or at Least One Transfusion During the Study
NCT00748189 (25) [back to overview]	Number of Participants Who Were Negative for Minimal Residual Disease (MRD)
NCT00910910 (14) [back to overview]	Kaplan Meier Estimate for Overall Survival at the Final Analysis
NCT00910910 (14) [back to overview]	Kaplan-Meier Estimate for Duration of Response
NCT00910910 (14) [back to overview]	Kaplan-Meier Estimate for Duration of Response With a Later Cut-off Date of 31 March 2014
NCT00910910 (14) [back to overview]	Time to Response
NCT00910910 (14) [back to overview]	Kaplan Meier Estimate of Overall Survival
NCT00910910 (14) [back to overview]	Number of Participants With Adverse Events With a Later Cut-off Date of 31 March 2014
NCT00910910 (14) [back to overview]	Number of Participants With Adverse Events (AEs)
NCT00910910 (14) [back to overview]	Number of Participants and Types of Subsequent Anti-cancer Therapies Received Post Treatment
NCT00910910 (14) [back to overview]	Time to Response for a Later Cut-off Date of 31 March 2014
NCT00910910 (14) [back to overview]	Percentage of Participants With the Best Overall Response Based on the International Workshop on Chronic Lymphocytic Leukemia (IWCLL) Guidelines
NCT00910910 (14) [back to overview]	Percentage of Participants With a Best Overall Response Based on IWCLL Guidelines With a Later Cut-off Date of 31 March 2014
NCT00910910 (14) [back to overview]	Number of Participants Deaths During the Treatment and Survival Follow-Up Phase
NCT00910910 (14) [back to overview]	Kaplan-Meier Estimate of Progression Free Survival (PFS) With a Later Cut-off Date of 14 March 2014
NCT00910910 (14) [back to overview]	Kaplan-Meier Estimate of Progression Free Survival (PFS)
NCT01010061 (14) [back to overview]	Event Free Survival
NCT01010061 (14) [back to overview]	Overall Survival
NCT01010061 (14) [back to overview]	Duration of Response
NCT01010061 (14) [back to overview]	Percentage of Participants With Molecular Remission at the End of Treatment
NCT01010061 (14) [back to overview]	Percentage of Participants With Progression Free Survival Events Based on Independent Review Committee (IRC) Data
NCT01010061 (14) [back to overview]	Progression Free Survival Based on Independent Review Committee (IRC) Data
NCT01010061 (14) [back to overview]	Progression-free Survival (PFS)
NCT01010061 (14) [back to overview]	Time to Re-Treatment/New-antileukemic Therapy
NCT01010061 (14) [back to overview]	European Organization for Research and Treatment of Cancer (EORTC) QLQ-C30 Questionnaire Score
NCT01010061 (14) [back to overview]	European Organization for Research and Treatment of Cancer (EORTC) QLQ-CLL16 Questionnaire Score
NCT01010061 (14) [back to overview]	Percentage of Participants With Best Overall Response
NCT01010061 (14) [back to overview]	Percentage of Participants With Progression Free Survival Events
NCT01010061 (14) [back to overview]	Pharmacokinetics of Obinutuzumab (RO5072759) in Combination With Chlorambucil (Clb)
NCT01010061 (14) [back to overview]	Percentage of Participants With End of Treatment Response (EOTR)
NCT01056510 (20) [back to overview]	Percentage of Participants Achieving Confirmed Complete Response (CR) According to International Workshop on Chronic Lymphocytic Leukemia (IWCLL) 2008 Guidelines in the First-Line Subpopulation After 6 Cycles of Therapy
NCT01056510 (20) [back to overview]	Percentage of Participants Achieving Confirmed CR According to IWCLL 2008 Guidelines in the Pooled Population After 6 Cycles of Therapy
NCT01056510 (20) [back to overview]	Percentage of Participants Achieving Confirmed CR According to IWCLL 2008 Guidelines in the Second-Line Subpopulation After 6 Cycles of Therapy
NCT01056510 (20) [back to overview]	Percentage of Participants Achieving Molecular Response in the First-Line Subpopulation
NCT01056510 (20) [back to overview]	Percentage of Participants by Disease Response Category in the First-Line Subpopulation
NCT01056510 (20) [back to overview]	Disease-Free Survival (DFS) in the First-Line Subpopulation
NCT01056510 (20) [back to overview]	Duration of Response in the First-Line Subpopulation
NCT01056510 (20) [back to overview]	Event-Free Survival (EFS) in the First-Line Subpopulation
NCT01056510 (20) [back to overview]	Overall Survival (OS) in the First-Line Subpopulation
NCT01056510 (20) [back to overview]	Percentage of Participants Experiencing Death in the First-Line Subpopulation
NCT01056510 (20) [back to overview]	Percentage of Participants Experiencing PD or Death in the First-Line Subpopulation
NCT01056510 (20) [back to overview]	Percentage of Participants Experiencing PD, Documented Intake of New Leukemia Therapy, or Death in the First-Line Subpopulation
NCT01056510 (20) [back to overview]	Percentage of Participants With Documented Intake of New Leukemia Therapy in the First-Line Subpopulation
NCT01056510 (20) [back to overview]	Percentage of Participants With Tumor Response of CR or CRi Experiencing PD or Death in the First-Line Subpopulation
NCT01056510 (20) [back to overview]	Percentage of Participants With Tumor Response of CR, CRi, PR, or nPR Experiencing PD or Death in the First-Line Subpopulation
NCT01056510 (20) [back to overview]	Progression-Free Survival (PFS) in the First-Line Subpopulation
NCT01056510 (20) [back to overview]	Proportion of Malignant B-cells in Normal B-cells Among Participants With a Positive Outcome for MRD in the First-Line Subpopulation
NCT01056510 (20) [back to overview]	Time to Next Leukemia Treatment (TNLT) in the First-Line Subpopulation
NCT01056510 (20) [back to overview]	Number of Participants With Positive and Negative Outcome for MRD in the First-Line Subpopulation
NCT01056510 (20) [back to overview]	Percentage of Participants Achieving a Best Overall Response of CR, CR With Incomplete Marrow Recovery (CRi), Partial Response (PR), or Nodular PR (nPR) in the First-Line Subpopulation
NCT01088048 (15) [back to overview]	Plasma Concentration of Lenalidomide
NCT01088048 (15) [back to overview]	Sub-study: Plasma Concentration of IDELA (Cohorts 1-4)
NCT01088048 (15) [back to overview]	Duration of Exposure to IDELA
NCT01088048 (15) [back to overview]	Duration of Response
NCT01088048 (15) [back to overview]	Overall Response Rate
NCT01088048 (15) [back to overview]	Overall Survival
NCT01088048 (15) [back to overview]	Progression-free Survival
NCT01088048 (15) [back to overview]	Time to Response
NCT01088048 (15) [back to overview]	Toxicity of Administration of IDELA
NCT01088048 (15) [back to overview]	Plasma Concentration of Bendamustine
NCT01088048 (15) [back to overview]	Plasma Concentration of Everolimus
NCT01088048 (15) [back to overview]	Plasma Concentration of IDELA (Cohort 1, Cohorts 2 and 3, Cohort 5)
NCT01088048 (15) [back to overview]	Plasma Concentration of IDELA (Cohort 4)
NCT01088048 (15) [back to overview]	Plasma Concentration of IDELA (Cohort 6)
NCT01088048 (15) [back to overview]	Plasma Concentration of IDELA (Cohort 7)
NCT01283386 (10) [back to overview]	Duration of Response
NCT01283386 (10) [back to overview]	Event-free Survival
NCT01283386 (10) [back to overview]	Overall Survival
NCT01283386 (10) [back to overview]	Percentage of Participants With Complete Remission
NCT01283386 (10) [back to overview]	Percentage of Participants With Disease Progression
NCT01283386 (10) [back to overview]	Percentage of Participants With Partial Remission
NCT01283386 (10) [back to overview]	Percentage of Participants With Phenotypic Remission
NCT01283386 (10) [back to overview]	Percentage of Participants With Stable Disease
NCT01283386 (10) [back to overview]	Progression-free Survival
NCT01283386 (10) [back to overview]	Percentage of Participants With Adverse Events (AEs) and Serious AEs
NCT01403246 (1) [back to overview]	Number of Dose Limiting Toxic Events (DLT) of Lenalidomide Given in Combination With Chlorambucil.
NCT01563055 (55) [back to overview]	Progression-free Survival (PFS), as Assessed by the IRC and the Investigator
NCT01563055 (55) [back to overview]	Plasma Half-life (t1/2) of Phenyl Acetic Acid Mustard
NCT01563055 (55) [back to overview]	Plasma Half-life (t1/2) of Ofatumumab
NCT01563055 (55) [back to overview]	Plasma Half-life (t1/2) of Chlorambucil
NCT01563055 (55) [back to overview]	Number of Participants With the Indicated Results for Human Anti-human Antibody (HAHA) at the Indicated Time Points
NCT01563055 (55) [back to overview]	Number of Participants With the Indicated Grade 3 or Grade 4 Adverse Events
NCT01563055 (55) [back to overview]	Number of Participants With Overall Response, as Assessed by the Independent Review Committee (IRC) With CT, IRC and Investigator
NCT01563055 (55) [back to overview]	Number of Participants With no B-symptoms (Constitutional Symptoms) and With at Least One B-symptom (Constitutional Symptoms) at the Indicated Time Points
NCT01563055 (55) [back to overview]	Number of Participants With Improvement in Eastern Cooperative Oncology Group (ECOG) Performance Status (PS)
NCT01563055 (55) [back to overview]	Number of Participants With CR, as Assessed by the IRC, IRC With CT, and the Investigator
NCT01563055 (55) [back to overview]	Number of Participants With Any Adverse Event (AE) or Serious Adverse Event (SAE)
NCT01563055 (55) [back to overview]	Duration of Response, as Assessed by the IRC
NCT01563055 (55) [back to overview]	Beta-2 Microglobulin at Cycle 1-Day 1
NCT01563055 (55) [back to overview]	Area Under the Plasma Concentration-time Curve From Time Zero to Infinity (AUC[0-infinity]) for Ofatumumab
NCT01563055 (55) [back to overview]	%AUC_extrap of Ofatumumab
NCT01563055 (55) [back to overview]	Time to Maximum Concentration (Tmax) of Chlorambucil
NCT01563055 (55) [back to overview]	Time to Maximum Concentration (Tmax) of Ofatumumab
NCT01563055 (55) [back to overview]	Time to Maximum Concentration (Tmax) of Phenyl Acetic Acid Mustard
NCT01563055 (55) [back to overview]	Cmax of Serum Phenyl Acetic Acid Mustard
NCT01563055 (55) [back to overview]	Number of Participants With AEs of Maximum Severity
NCT01563055 (55) [back to overview]	Number of Participants Who Were Positive or Negative for Minimal Residual Disease (MRD), as Assessed by IRC With CT
NCT01563055 (55) [back to overview]	Minimum Plasma Concentration (Cmin) of Ofatumumab
NCT01563055 (55) [back to overview]	Mean Residence Time Inf (MRTinf) of Phenyl Acetic Acid Mustard
NCT01563055 (55) [back to overview]	Mean Residence Time Inf (MRTinf) of Chlorambucil
NCT01563055 (55) [back to overview]	Mean Change From Baseline in the Immunoglobulins (Ig) Antibodies IgA, IgG, and IgM at the Indicated Time Points
NCT01563055 (55) [back to overview]	Maximum (Peak) Plasma Concentration (Cmax) of Ofatumumab
NCT01563055 (55) [back to overview]	Dose Normalized Cmax (Cmax/D) for Chlorambucil
NCT01563055 (55) [back to overview]	Complement (CH50) at Cycle 1-Day 1 and Cycle 4-Day 85
NCT01563055 (55) [back to overview]	Cmin of Phenyl Acetic Acid Mustard
NCT01563055 (55) [back to overview]	Cmin of Chlorambucil
NCT01563055 (55) [back to overview]	Cmax/D for Phenyl Acetic Acid Mustard
NCT01563055 (55) [back to overview]	%AUC_extrap of Phenyl Acetic Acid Mustard
NCT01563055 (55) [back to overview]	Cmax of Serum Chlorambucil
NCT01563055 (55) [back to overview]	Change From Baseline in CD5+CD19+ and CD5-CD19+ Cell Counts at the Indicated Time Points
NCT01563055 (55) [back to overview]	AUC(0-tau) of Phenyl Acetic Acid Mustard
NCT01563055 (55) [back to overview]	AUC(0-tau) of Chlorambucil
NCT01563055 (55) [back to overview]	AUC(0-infinity) for Phenyl Acetic Acid Mustard
NCT01563055 (55) [back to overview]	AUC(0-infinity) for Chlorambucil
NCT01563055 (55) [back to overview]	AUC (0-t) of Phenyl Acetic Acid Mustard
NCT01563055 (55) [back to overview]	AUC (0-t) of Ofatumumab
NCT01563055 (55) [back to overview]	AUC (0-t) of Chlorambucil
NCT01563055 (55) [back to overview]	AUC (0-6)/D, AUC(0-24)/D, AUC (0-inf)/D, and AUC (0-tau)/D of Chlorambucil
NCT01563055 (55) [back to overview]	AUC (0-6)/D, AUC(0-24)/D, AUC (0-inf)/D and AUC (0-tau)/D of Phenyl Acetic Acid Mustard
NCT01563055 (55) [back to overview]	Apparent Volume of Distribution During Terminal Phase (Vz/F) of Chlorambucil
NCT01563055 (55) [back to overview]	Apparent Total Clearance of the Drug From Plasma (CL/F) for Chlorambucil
NCT01563055 (55) [back to overview]	%AUC_extrap of Chlorambucil
NCT01563055 (55) [back to overview]	Volume of Distribution at Steady State (Vss) of Ofatumumab
NCT01563055 (55) [back to overview]	Volume of Distribution (Vz) of Ofatumumab
NCT01563055 (55) [back to overview]	Area Under the Drug Plasma Concentration-time Curve From Dosing to Time Tau (AUC[0-tau]) of Ofatumumab
NCT01563055 (55) [back to overview]	Total Plasma Clearance (CL) of Ofatumumab
NCT01563055 (55) [back to overview]	Time to Response, as Assessed by the IRC
NCT01563055 (55) [back to overview]	Time to Next Chronic Lymphocytic Leukemia (CLL) Therapy
NCT01563055 (55) [back to overview]	Overall Survival
NCT01563055 (55) [back to overview]	Number of Participants Who Developed Toxicity Requiring Discontinuation From Study Treatment During Cycle 1
NCT01563055 (55) [back to overview]	Mean Residence Time to Infinity (MRTinf) of Ofatumumab
NCT01722487 (7) [back to overview]	Proportion of Sustained Platelet Improvement in Subjects With Baseline Thrombocytopenia
NCT01722487 (7) [back to overview]	ORR (Overall Response Rate)
NCT01722487 (7) [back to overview]	Overall Survival (OS)
NCT01722487 (7) [back to overview]	PFS (Progression Free Survival)
NCT01722487 (7) [back to overview]	Proportion of Sustained Hemoglobin Improvement
NCT01722487 (7) [back to overview]	Proportion of Sustained Hemoglobin Improvement in Subjects With Baseline Anemia
NCT01722487 (7) [back to overview]	Proportion of Sustained Platelet Improvement
NCT01808326 (24) [back to overview]	Expression of Complement CH50
NCT01808326 (24) [back to overview]	Progression Free Survival (PFS), as Assessed by the Investigator and the IRC
NCT01808326 (24) [back to overview]	Change From Baseline in the Immunoglobulin(Ig) Antibodies IgA, IgG, and IgM
NCT01808326 (24) [back to overview]	Time of Maximum Serum Concentration (Tmax) for Chlorambucil
NCT01808326 (24) [back to overview]	Duration of Response, as Assessed by the IRC
NCT01808326 (24) [back to overview]	Expression of Beta 2 Microglobulin
NCT01808326 (24) [back to overview]	Number of Participants With Positive Minimal Residual Disease (MRD)
NCT01808326 (24) [back to overview]	Overall Survival (OS)
NCT01808326 (24) [back to overview]	Time to Next Chronic Lymphocytic Leukemia (CLL) Therapy
NCT01808326 (24) [back to overview]	Time to Response, as Assessed by the IRC
NCT01808326 (24) [back to overview]	Area Under the Serum Concentration-time (AUC) for Chlorambucil
NCT01808326 (24) [back to overview]	Area Under the Serum Concentration-time (AUC) for Phenyl Acetic Acid Mustard
NCT01808326 (24) [back to overview]	Time of Maximum Serum Concentration (Tmax) for Phenyl Acetic Acid Mustard
NCT01808326 (24) [back to overview]	Elimination Half-life (t1/2) for Chlorambucil
NCT01808326 (24) [back to overview]	Elimination Half-life (t1/2) for Phenyl Acetic Acid Mustard
NCT01808326 (24) [back to overview]	Maximum Serum Concentration (Cmax), and Minimum Serum Concentration (Cmin) for Chlorambucil
NCT01808326 (24) [back to overview]	Maximum Serum Concentration (Cmax), and Minimum Serum Concentration (Cmin) for Phenyl Acetic Acid Mustard
NCT01808326 (24) [back to overview]	Number of Participants With a Best Response of Either Complete Remission (CR), Nodular Partial Remission (nPR), Complete Remission-incomplete (CRi) or Partial Remission (PR), as Assessed by the Investigator, IRC and IRC With CT
NCT01808326 (24) [back to overview]	Number of Participants With Adverse Events by the Indicated Maximum Toxicity Grade
NCT01808326 (24) [back to overview]	Number of Participants With Any Adverse Events (AE) or Serious Adverse Events (SAE)
NCT01808326 (24) [back to overview]	Number of Participants With at Least One Grade 3/Grade 4 Adverse Event of Infection or Myelosuppression (Anemia, Neutropenia, and Thrombocytopenia)
NCT01808326 (24) [back to overview]	Number of Participants With Improvement in Eastern Cooperative Oncology Group (ECOG) Performance Status (PS)
NCT01808326 (24) [back to overview]	Number of Participants With no B-symptoms and With at Least One B-symptom Over Time
NCT01808326 (24) [back to overview]	Number of Participants With the Best Overall Response (OR), as Assessed by the Investigator, IRC and IRC With CT
NCT01868893 (3) [back to overview]	Number of Participants With Adverse Events (AEs), AEs of Grade 3 and Above Severity, AEs of Special Interest (AESI), AEs Leading to Obinutuzumab Discontinuation or Dose Delays, Serious Adverse Events (SAEs), and Death
NCT01868893 (3) [back to overview]	Number of Participants With Objective Response
NCT01868893 (3) [back to overview]	Number of Participants Who Received Obinutuzumab and Chlorambucil in the Study
NCT01905943 (12) [back to overview]	Median Time to Overall Survival (OS)
NCT01905943 (12) [back to overview]	Median Time to Progression-Free Survival (PFS)
NCT01905943 (12) [back to overview]	Median Time to Response (TTR)
NCT01905943 (12) [back to overview]	Percentage of Participants With Best Overall Response (BOR)
NCT01905943 (12) [back to overview]	Percentage of Participants With Overall Response (OR) at Final Response Assessment (FRA)
NCT01905943 (12) [back to overview]	Number of Participants With Adverse Events (AEs)
NCT01905943 (12) [back to overview]	Number of Participants With Adverse Events of Particular Interest (AEPIs)
NCT01905943 (12) [back to overview]	Number of Participants With Adverse Events of Special Interest (AESIs)
NCT01905943 (12) [back to overview]	Percentage of Participants With Minimal Residual Disease (MRD)-Negativity as Assessed by Flow Cytometry
NCT01905943 (12) [back to overview]	Median Time to Event-Free Survival (EFS)
NCT01905943 (12) [back to overview]	Median Time to Duration of Response (DoR)
NCT01905943 (12) [back to overview]	Median Time to New Anti-Leukemia Therapy (TTNT)
NCT01998880 (13) [back to overview]	Progression Free Survival Based on Independent Review Committee (IRC) Data
NCT01998880 (13) [back to overview]	Percentage of Participants With Progression Free Survival Events Based on Independent Review Committee (IRC) Data
NCT01998880 (13) [back to overview]	Percentage of Participants With Progression Free Survival Events
NCT01998880 (13) [back to overview]	Percentage of Participants With Molecular Remission at the End of Treatment
NCT01998880 (13) [back to overview]	Overall Survival
NCT01998880 (13) [back to overview]	Event Free Survival
NCT01998880 (13) [back to overview]	Duration of Response
NCT01998880 (13) [back to overview]	Progression-free Survival (PFS)
NCT01998880 (13) [back to overview]	Time to Re-Treatment/New-antileukemic Therapy
NCT01998880 (13) [back to overview]	European Organization for Research and Treatment of Cancer (EORTC) QLQ-C30 Questionnaire Score
NCT01998880 (13) [back to overview]	European Organization for Research and Treatment of Cancer (EORTC) QLQ-CLL16 Questionnaire Score
NCT01998880 (13) [back to overview]	Percentage of Participants With End of Treatment Response (EOTR)
NCT01998880 (13) [back to overview]	Percentage of Participants With Best Overall Response
NCT02053610 (13) [back to overview]	Progression-free Survival (PFS)
NCT02053610 (13) [back to overview]	Time to Re-Treatment/New Anti-leukemic Therapy
NCT02053610 (13) [back to overview]	Percentage of Participants With Molecular Remission at the End of Treatment
NCT02053610 (13) [back to overview]	European Organization for Research and Treatment of Cancer (EORTC) QLQ-C30 Questionnaire
NCT02053610 (13) [back to overview]	European Organization for Research and Treatment of Cancer (EORTC) QLQ-CLL16 Questionnaire
NCT02053610 (13) [back to overview]	Percentage of Participants With Best Overall Response
NCT02053610 (13) [back to overview]	Percentage of Participants With End of Treatment Response (EOTR)
NCT02053610 (13) [back to overview]	Duration of Response
NCT02053610 (13) [back to overview]	Event Free Survival
NCT02053610 (13) [back to overview]	Overall Survival
NCT02053610 (13) [back to overview]	Percentage of Participants With Progression Free Survival Events
NCT02053610 (13) [back to overview]	Percentage of Participants With Progression Free Survival Events Based on Independent Review Committee (IRC) Data
NCT02053610 (13) [back to overview]	Progression Free Survival Based on Independent Review Committee (IRC) Data
NCT02242942 (12) [back to overview]	Percentage of Participants With an Overall Response (OR) at Completion of Treatment, as Determined by the Investigator According to IWCLL Criteria
NCT02242942 (12) [back to overview]	Percentage of Participants With a Complete Response Rate (CRR) at the Completion of Treatment Assessment as Determined by the Investigator According to IWCLL Criteria
NCT02242942 (12) [back to overview]	Serum Concentrations of Obinutuzumab
NCT02242942 (12) [back to overview]	Plasma Concentrations of Venetoclax
NCT02242942 (12) [back to overview]	Percentage of Participants By Best Response Achieved (CR, CRi, PR, Stable Disease (SD), or PD)
NCT02242942 (12) [back to overview]	Progression Free Survival (PFS) Based on Investigator Assessment According to IWCLL Criteria
NCT02242942 (12) [back to overview]	Percentage of Participants With MRD Negativity in Bone Marrow as Measured by ASO-PCR at Completion of Combination Treatment Assessment
NCT02242942 (12) [back to overview]	Percentage of Participants With MRD Negativity in Bone Marrow as Measured by ASO-PCR at Completion of Treatment
NCT02242942 (12) [back to overview]	Percentage of Participants With MRD Negativity in Peripheral Blood as Measured by ASO-PCR at Completion of Combination Treatment Assessment
NCT02242942 (12) [back to overview]	Percentage of Participants With OR at Completion of Combination Treatment Response Assessment
NCT02242942 (12) [back to overview]	Progression Free Survival (PFS) Based on Institutional Review Committee (IRC)-Assessments According to International Workshop on Chronic Lymphocytic Leukemia (IWCLL) Criteria
NCT02242942 (12) [back to overview]	Percentage of Participants With Minimal Residual Disease (MRD) Negativity in Peripheral Blood as Measured by Allele-Specific Oligonucleotide Polymerase Chain Reaction (ASO-PCR) at Completion of Treatment
NCT02264574 (16) [back to overview]	Primary Analysis: Rate of Grade ≥ 3 or Serious Infusion-Related Reaction (IRR) Adverse Events
NCT02264574 (16) [back to overview]	Primary Analysis: Rate of Sustained Platelet Improvement
NCT02264574 (16) [back to overview]	Primary Analysis: Rate of Minimal Residual Disease (MRD)-Negative Response
NCT02264574 (16) [back to overview]	Primary Analysis: Rate of Clinically Meaningful Improvement in European Organization for Research and Treatment of Cancer Quality of Life Questionnaire EuroQol Five-Dimension (EQ-5D-5L)
NCT02264574 (16) [back to overview]	Primary Analysis: Progression Free Survival (PFS) Based on Independent Review Committee (IRC) Assessment - Kaplan Meier Landmark Estimates at Month 30
NCT02264574 (16) [back to overview]	Primary Analysis: PFS in High-Risk Sub-Population (del17p/TP53 Mutation/Del 11q) Based on IRC Assessment - Kaplan Meier Landmark Estimates at Month 30
NCT02264574 (16) [back to overview]	Primary Analysis: Overall Survival (OS) - Kaplan Meier Landmark Estimates at Month 30
NCT02264574 (16) [back to overview]	Primary Analysis: Overall Response Rate (ORR) Based on IRC Assessment
NCT02264574 (16) [back to overview]	Final Analysis: Rate of Sustained Platelet Improvement
NCT02264574 (16) [back to overview]	Final Analysis: Rate of Sustained Hemoglobin Improvement
NCT02264574 (16) [back to overview]	Final Analysis: Rate of Minimal Residual Disease (MRD)-Negative Response
NCT02264574 (16) [back to overview]	Final Analysis: PFS in High-Risk Population (del17p/TP53 Mutation/Del 11q/Unmutated Immunoglobulin Heavy Chain Variable Region [IGHV]) Based on Investigator Assessment - Kaplan Meier Landmark Estimates at Month 48
NCT02264574 (16) [back to overview]	Final Analysis: PFS Based on Investigator Assessment - Kaplan Meier Landmark Estimates at Month 48
NCT02264574 (16) [back to overview]	Final Analysis: Overall Survival (OS) - Kaplan Meier Landmark Estimates at Month 48
NCT02264574 (16) [back to overview]	Final Analysis: ORR Based on Investigator Assessment
NCT02264574 (16) [back to overview]	Primary Analysis: Rate of Sustained Hemoglobin Improvement
NCT02475681 (5) [back to overview]	Time to Next Treatment (TTNT) in Arm A Versus Arm B and Arm A Versus Arm C
NCT02475681 (5) [back to overview]	Progression-free Survival by IRC Assessment Arm A Versus Arm C
NCT02475681 (5) [back to overview]	Progression-free Survival by IRC (Independent Review Committee) Assessment in Arm A Compared to Arm B
NCT02475681 (5) [back to overview]	Overall Survival (OS) in Arm A Versus Arm B and Arm A Versus Arm C
NCT02475681 (5) [back to overview]	IRC-assessed Objective Response Rate (ORR) in Arm A Versus Arm B and Arm A Versus Arm C
NCT03462719 (15) [back to overview]	Progression Free Survival (PFS)
NCT03462719 (15) [back to overview]	Percentage of Participants With Sustained Platelet Improvement
NCT03462719 (15) [back to overview]	Plasma Concentration of Ibrutinib and Venetoclax
NCT03462719 (15) [back to overview]	Time to Worsening and Time to Improvement as Measured by Functional Assessment of Chronic Illness Therapy (FACIT)-Fatigue Total Score
NCT03462719 (15) [back to overview]	Time to Worsening as Measured by Using EuroQol 5 Dimension 5 Level Questionnaire (EQ-5D-5L)
NCT03462719 (15) [back to overview]	Percentage of Participants With Sustained Hemoglobin Improvement
NCT03462719 (15) [back to overview]	Time to Worsening Measured by European Organization for Research and Treatment of Cancer-Quality of Life Questionnaire (EORTC QLQ)-C30)
NCT03462719 (15) [back to overview]	Overall Survival (OS)
NCT03462719 (15) [back to overview]	Overall Response Rate (ORR)
NCT03462719 (15) [back to overview]	Number of Participants With Adverse Events (AEs) as a Measure of Safety and Tolerability
NCT03462719 (15) [back to overview]	Number of Participants With Abnormal Clinical Laboratory Findings
NCT03462719 (15) [back to overview]	Minimal Residual Disease (MRD) Negative Rate
NCT03462719 (15) [back to overview]	Duration of Response (DOR)
NCT03462719 (15) [back to overview]	Complete Response Rate (CRR)
NCT03462719 (15) [back to overview]	Time-to-Next Treatment

Mortality

(NCT00132691)
Timeframe: 24 months

Intervention	percentage of participants (Number)
Flucinolone Acetonide Implant	1.6
Systemic Therapy	0

Intervention	percentage of patients (Number)
ARM A - Chlorambucil	51
ARM B - Rituximab + Chlorambucil	68
ARM C (Since April 2006) - Rituximab	51

Intervention	percentage of patients (Number)
ARM A - Chlorambucil	85.5
ARM B - Rituximab + Chlorambucil	94.7
ARM C (Since April 2006) - Rituximab	78.3

Intervention	percentage of patients (Number)
ARM A - Chlorambucil	59
ARM B - Rituximab + Chlorambucil	72
ARM C (Since April 2006) - Ritiximab	57

Intervention	units on scale (Mean)
	GHS/QoL score-baseline (n=91)	CFB in GHS/QoL Score-Cycle 5 (n=59)	CFB in GHS/QoL Score-Cycle 11 (n=40)	CFB in GHS/QoL Score-24m FU (n=17)	Physical functioning score-baseline (n=91)	CFB in physical functioning score-Cycle 5 (n=59)	CFB in physical functioning score-Cycle 11 (n=40)	CFB in physical functioning score-24m FU (n=17)	Role functioning score-baseline (n=91)	CFB in role functioning score-Cycle 5 (n=59)	CFB in role functioning score-Cycle 11 (n=40)	CFB in role functioning score-24m FU (n=17)	Emotional functioning score-baseline (n=91)	CFB in emotional functioning score-Cycle 5 (n=59)	CFB in emotional functioning score-Cycle 11 (n=40)	CFB in emotional functioning score-24m FU (n=17)	Cognitive functioning score-baseline (n=91)	CFB in cognitive functioning score-Cycle 5 (n=59)	CFB in cognitive functioning-Cycle 11 (n=40)	CFB in cognitive functioning-24m FU (n=17)	Social functioning score-baseline (n=91)	CFB in social functioning score-Cycle 5 (n=59)	CFB in social functioning score-Cycle 11 (n=40)	CFB in social functioning score-at 24m FU (n=17)	Fatigue score-baseline (n=91)	CFB in fatigue score-Cycle 5 (n=59)	CFB in fatigue score-Cycle 11 (n=40)	CFB in fatigue score-24m FU (n=17)	Nausea/vomiting score-baseline (n=91)	CFB in nausea/vomiting score-Cycle 5 (n=59)	CFB in nausea/vomiting score-Cycle 11 (n=40)	CFB in nausea/vomiting score-24m FU (n=17)	Pain score-baseline (n=91)	CFB in pain score-Cycle 5 (n=59)	CFB in pain score-Cycle 11 (n=40)	CFB in pain score-24m FU (n=17)
Rituximab + Chlorambucil	65.7	6.4	6.2	2.0	77.0	1.0	3.4	-2.0	73.4	0.0	3.8	3.9	82.5	1.0	-0.1	0.5	84.1	-1.9	-0.4	5.2	82.2	2.5	0.0	5.2	33.4	-1.4	-6.1	-5.6	6.2	1.7	0.4	-2.9	17.8	-3.4	-1.3	0.0

Intervention	percentage of participants (Number)
	Clinical CR	Confirmed CR	Clinical CR or Confirmed CR
Rituximab + Chlorambucil	37.0	10.0	47.0

Intervention	participants (Number)
	Immunophenotypic CR - BM	Immunophenotypic CR - PB	Molecular CR - BM	Molecular CR - PB
CLB + R: Induction Treatment	2	3	0	0

Intervention	percentage of participants (Number)
	CR	CRi	PR
CLB + R: Maintenance Treatment	29.4	0.0	26.4
CLB + R: Observation	18.7	0.0	12.5

Intervention	percentage of participants (Number)
	CR	CRi	PR	SD	PD	Relapse	Nodular PR	Unknown
CLB + R: Induction Treatment	16.5	2.4	60.0	4.7	3.5	0.0	3.5	9.4

Intervention	days (Mean)
CLB + R: Maintenance Treatment	699.91
CLB + R: Observation	732.28

Intervention	days (Mean)
CLB + R: Maintenance Treatment	840.87
CLB + R: Observation	747.82

Intervention	Participants (Number)
	Any AE	Any SAE
Chlorambucil	205	84
Ofatumumab + Chlorambucil	208	97

Intervention	Participants (Number)
	Any AE, Grade 3	Any AE, Grade 4	Any AE, Grade 5	Any SAE, Grade 3	Any SAE, Grade 4	Any SAE, Grade 5
Chlorambucil	54	31	25	36	13	25
Ofatumumab + Chlorambucil	67	36	36	34	19	36

Intervention	Participants (Number)
	CS present, Baseline, n=226, 221	CS present, Cycle 3 Day 1, n=198, 199	CS present, 1 Month Follow-up, n=198, 200
Chlorambucil	120	44	23
Ofatumumab + Chlorambucil	118	33	22

Intervention	Participants (Number)
	ECOG (0, 1) at Baseline	ECOG (0, 1) at Cycle 3 Day 1	ECOG (0, 1) 1 Month Follow-up
Chlorambucil	209	184	183
Ofatumumab + Chlorambucil	200	189	191

Intervention	Liters (Geometric Mean)
	Vss, Cycle 1 Day 1, n=0, 193	Vss, Cycle 1 Day 8, n=0, 208	Vss, Cycle 4 Day 1, n=0, 183
Ofatumumab + Chlorambucil	7.78	7.77	8.06

Intervention	µg x hours/mL (Geometric Mean)
	Cycle 1 Day 1, n=0, 193	Cycle 1 Day 8, n=0, 208	Cycle 4 Day 1, n=0, 183
Ofatumumab + Chlorambucil	2621	25369	65100

Intervention	Scores on a scale (Mean)
	P1, Cycle 4 Day 1, QLQC30 GHS/QoL score, n=139,159	P1, Cycle 7 Day 1, QLQC30 GHS/QoL score, n=52, 55	P1,Cycle 4 Day 1,QLQCLL16 fatigue score, n=145,163	P1, Cycle 7 Day 1,QLQCLL16 fatigue score, n=55,57	P2,1 month FU, QLQC30 GHS/QoL score, n=118, 150	P2, 6 month FU, QLQC30 GHS/QoL score, n=83, 129	P2, 12 month FU, QLQC30 GHS/QoL score, n=48, 96	P2, 1 month FU, QLQCLL16 fatigue score, n=121, 152	P2, 6 month FU, QLQCLL16 fatigue score, n=85, 131	P2, 12 month FU, QLQCLL16 fatigue score, n=51, 95
Chlorambucil	1.92	8.01	-4.71	-1.21	4.79	3.01	3.82	-1.24	-7.06	-2.94
Ofatumumab + Chlorambucil	6.08	6.97	-4.60	-9.36	0.56	3.75	1.22	-0.33	-2.93	0.88

Intervention	Micrograms/Milliliter (µg/mL) (Geometric Mean)
	Cmax, Cycle 1 Day 1, n=0, 176	Cmax, Cycle 1 Day 8, n=0, 193	Cmax, Cycle 4 Day 1, n=0, 169	Ctrough, Cycle 1 Day 8, n=0, 99	Ctrough, Cycle 2 Day 1, n=0, 138	Ctrough, Cycle 3 Day 1, n=0, 142	Ctrough, Cycle 4 Day 1, n=0, 147	Ctrough, Cycle 5 Day 1, n=0, 149	Ctrough, Cycle 6 Day 1, n=0, 155	Ctrough, Cycle 9 Day 1, n=0, 56
Ofatumumab + Chlorambucil	51.8	241	285	2.5	5.2	6.2	15.5	33.5	45.9	55.6

Intervention	Hours*nanogram/milliliter/milligram (Geometric Mean)
	Chlorambucil AUC(0-6)/Dose	Chlorambucil AUC(0-inf)/Dose	PAAM AUC(0-6)/Dose
Study LEUA1001: Chlorambucil	65.43	67.10	80.32
Study OMB110911: Ofatumumab + Chlorambucil	67.84	74.42	71.52

Intervention	nanograms per milliliter per milligram (Geometric Mean)
	Chlorambucil Cmax/Dose	PAAM Cmax/Dose
Study LEUA1001: Chlorambucil	38.4	24.3
Study OMB110911: Ofatumumab + Chlorambucil	27.1	19.3

chlorambucil

Description

Cross-References

Synonyms (256)

Research Excerpts

Overview

Effects

Actions

Treatment

Toxicity

Pharmacokinetics

Compound-Compound Interactions

Bioavailability

Dosage Studied

Roles (5)

Drug Classes (5)

Protein Targets (65)

Potency Measurements

Inhibition Measurements

Other Measurements

Biological Processes (226)

Molecular Functions (79)

Ceullar Components (46)

Bioassays (609)

Research

Studies (3,628)

Market Indicators

Research Demand Index: 64.72

Study Types

Clinical Trials (52)

Trial Overview

Trial Outcomes

Mortality

Intraocular Pressure - Incident IOP Elevation >= 10 mmHg Above Baseline

Intraocular Pressure - Incident IOP Greater Than or Equal to 24 mm Hg

Change in Best-corrected Visual Acuity (Change in the Numbers of Letters Read From a Standard ETDRS Eye Chart) From Baseline to 24 Months in Eyes With Uveitis

Change in Self-reported Vision-related Function as Measured by the National Eye Institute 25-Item Visual Function Questionnaire (NEI-VFQ 25) Vision Targeted Composite Score From Baseline to 24 Months

Change in SF-36 Mental Component Score From Baseline to 24 Months

Change in SF-36 Physical Component Score From Baseline to 24 Months

Diabetes Mellitus

Glaucoma - Incident

Intraocular Pressure - Incident IOP Greater Than or Equal to 30 mm Hg

Intraocular Pressure - IOP-lowering Surgery

Intraocular Pressure (IOP) - Incident Use of IOP-lowering Medical Therapy (Percentage of Eyes With Uveitis That Were Not Being Treated With IOP-lowering Medical Therapy at Baseline and Underwent IOP Lowering Therapy During the 24 Month Follow-up.

Macular Edema

Cataract - Incident Cataract

Hyperlipidemia - Incident

Uveitis Activity

Hypertension Diagnosis Requiring Treatment

Event-free-survival (EFS)

Complete and Partial Remission Rate - Percentage of Patients With Complete and Partial Response at the End of Treatment

Response Duration (Time to Relapse or Progression) - Percentage of Patients in Continuous Remission at Five Years From Trial Registration

Progression-free-survival (PFS)

Overall Survival

Percentage of Participants With BOR of Partial Response (PR)

Percentage of Participants With BOR of Progressive Disease (PD)

Percentage of Participants With BOR of Stable Disease (SD)

Percentage of Participants With Objective Response (CR or PR)

Percentage of Participants With Treatment-Emergent Adverse Events (AEs)

Progression Free Survival (PFS) Time

Mean Change From Baseline (CFB) in European Organisation for Research and Treatment of Cancer Quality of Life Questionnaire Core 30 (EORTC QLQ-C30) Scores

Percentage of Participants With Best Overall Response (BOR) of Clinical CR or Confirmed CR

Percentage of Participants With BOR of Nodular Partial Response (nPR)

Percentage of Participants Who Died

Percentage of Participants Who Achieved Minimal Residual Disease (MRD) Negativity

Duration of Response (DoR)

Disease Free Survival (DFS) Time

Overall Survival (OS) Time

Percentage of Participant With Disease Progression or Death

Number of Participants With Immunophenotypic CR - BM, Immunophenotypic CR - Peripheral Blood (PB), Molecular CR - BM, or Molecular CR - PB at the End of Induction Treatment

Percentage of Participants With CR, CRi, PR, SD, PD, or Relapse at the End of Study

Percentage of Participants With CR, CRi, PR, Stable Disease (SD), Progressive Disease (PD), Relapse, or Nodular PR at the End of Induction Treatment

Percentage of Participants With CR, PR, SD, PD, Relapse, or Nodular PR at the End of Study

Percentage of Participants With Immunophenotypic CR - BM or Immunophenotypic CR - PB at the End of Study

Percentage of Participants With Molecular CR - BM or Molecular CR - PB at the End of Study

Disease-Free Survival

Duration of Response

EFS

Number of Participants Who Died

Number of Participants With Disease Progression or Death

Intervention	Gram per liter (Mean)
	IgA, n=175, 186	IgG, n=175, 186	IgM n=175, 186
Chlorambucil	0.047	-0.458	-0.398
Ofatumumab + Chlorambucil	0.048	-0.268	-0.031

Intervention	Participants (Number)
	No transfusions	At least one transfusion
Chlorambucil	159	68
Ofatumumab + Chlorambucil	168	49

Intervention	Participants (Number)
	MRD negative, irrespective of response	MRD negative, with an IRC-assessed CR
Chlorambucil	8	0
Ofatumumab + Chlorambucil	26	10

Intervention	participants (Number)
	≥ 1 TEAE	≥ 1 TEAE related to study drug	≥ 1 NCI CTC Grade 3-4 TEAE	Grade 3-4 adverse event related to any study drug	≥ 1 NCI CTC Grade 5 TEAE	≥ Grade 5 adverse event related to any study drug	≥ 1 Serious TEAE	≥ 1 Serious TEAE related to any study drug	≥1 TEAE leading to stopping either study drug	≥1 Related TEAE leading to stopping either drug
Chlorambucil	202	155	131	90	11	1	90	53	42	23
Lenalidomide	216	194	188	157	21	6	148	107	70	46

Intervention	participants (Number)
	Participants receiving additional CLL therapy	Participants receiving alkylating agents	Participants receiving antineoplastic aents	Participants receiving antimetabolites	Participants receiving corticosteroids	Participants receiving plant alkaloids	Participants receiving cytotoxic antibiotics	Participants receiving immunosuppressants	Participants receiving therapeutic products	Participants receiving other unspecified products	Antihistamine For Systemic Use	Drugs for Peptic ulcer and Gastric Reflex	Immunoglobulins	Other Analgesics and Antipyretics	Specific Antirheumatic Agents	Antiemetics and Antinauseants	Corticosteriods for Systemic Use	Immunostimulants
Chlorambucil	120	106	86	24	16	11	3	2	3	2	1	0	2	1	0	1	1	1
Lenalidomide	125	107	93	34	27	22	10	3	4	0	1	1	1	1	1	0	0	0

Intervention	Months (Median)
Obinutuzumab + Chlorambucil (GClb)	28.7
Chlorambucil (Clb)	10.8

Intervention	Percentage of participants (Number)
Obinutuzumab + Chlorambucil (GClb)	37.4
Chlorambucil (Clb)	76.3

Intervention	Months (Median)
Obinutuzumab + Chlorambucil (GClb)	27.2
Chlorambucil (Clb)	11.2

Intervention	Months (Median)
Obinutuzumab + Chlorambucil (GClb)	31.1
Chlorambucil (Clb)	11.1

Intervention	Months (Median)
Obinutuzumab + Chlorambucil (GClb)	55.7
Chlorambucil (Clb)	15.1