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ChEMBL ligand: CHEMBL107 (Gloperba, Colchicine, NSC-757, Colcrys, Mitigare) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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ABCB1/P-glycoprotein 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4302] [GtoPdb: 768] [UniProtKB: P08183] | ||||||||
ChEMBL | Inhibition of P-glycoprotein using calcein-AM assay transfected in porcine PBCEC | F | 4.3 | pIC50 | >50000 | nM | IC50 | J. Med. Chem. (2003) 46: 1716-1725 [PMID:12699389] |
ChEMBL | Inhibition of P-glycoprotein, human L-MDR1 expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assay | F | 4.3 | pIC50 | >50000 | nM | IC50 | J. Med. Chem. (2003) 46: 1716-1725 [PMID:12699389] |
ChEMBL | TP_TRANSPORTER: inhibition of Calcein-AM efflux in MDR1-expressing LLC-PK1 cells | F | 4.3 | pIC50 | >50000 | nM | IC50 | J. Med. Chem. (2003) 46: 1716-1725 [PMID:12699389] |
P-glycoprotein 1 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3467] [UniProtKB: P06795] | ||||||||
ChEMBL | Inhibition of P-glycoprotein, mouse L-mdr1b expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assay | F | 4.3 | pIC50 | >50000 | nM | IC50 | J. Med. Chem. (2003) 46: 1716-1725 [PMID:12699389] |
ChEMBL | TP_TRANSPORTER: inhibition of Calcein-AM efflux in Mdr1b-expressing LLC-PK1 cells | F | 4.3 | pIC50 | >50000 | nM | IC50 | J. Med. Chem. (2003) 46: 1716-1725 [PMID:12699389] |
ABCB1/P-glycoprotein 3 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2573] [GtoPdb: 768] [UniProtKB: P21447] | ||||||||
ChEMBL | Inhibition of P-glycoprotein, mouse L-mdr1a expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assay | F | 4.3 | pIC50 | >50000 | nM | IC50 | J. Med. Chem. (2003) 46: 1716-1725 [PMID:12699389] |
ChEMBL | TP_TRANSPORTER: inhibition of Calcein-AM efflux in Mdr1a-expressing LLC-PK1 cells | F | 4.3 | pIC50 | >50000 | nM | IC50 | J. Med. Chem. (2003) 46: 1716-1725 [PMID:12699389] |
Plasmodium falciparum (target type: ORGANISM) [ChEMBL: CHEMBL364] | ||||||||
ChEMBL | Antiplasmodial activity against Plasmodium falciparum D10 after 72 hrs by SYBR green assay | F | 4.9 | pIC50 | 12589.25 | nM | IC50 | Nat. Chem. Biol. (2009) 5: 765-771 [PMID:19734910] |
ChEMBL | Antiplasmodial activity against Plasmodium falciparum GB4 after 72 hrs by SYBR green assay | F | 4.9 | pIC50 | 12589.25 | nM | IC50 | Nat. Chem. Biol. (2009) 5: 765-771 [PMID:19734910] |
ChEMBL | Antiplasmodial activity against Plasmodium falciparum HB3 after 72 hrs by SYBR green assay | F | 4.9 | pIC50 | 12589.25 | nM | IC50 | Nat. Chem. Biol. (2009) 5: 765-771 [PMID:19734910] |
ChEMBL | Antiplasmodial activity against Plasmodium falciparum 3D7 after 72 hrs by SYBR green assay | F | 5 | pIC50 | 10000 | nM | IC50 | Nat. Chem. Biol. (2009) 5: 765-771 [PMID:19734910] |
ChEMBL | Antiplasmodial activity against Plasmodium falciparum 7G8 after 72 hrs by SYBR green assay | F | 5 | pIC50 | 10000 | nM | IC50 | Nat. Chem. Biol. (2009) 5: 765-771 [PMID:19734910] |
ChEMBL | Antiplasmodial activity against Plasmodium falciparum W2 after 72 hrs by SYBR green assay | F | 5 | pIC50 | 10000 | nM | IC50 | Nat. Chem. Biol. (2009) 5: 765-771 [PMID:19734910] |
Pim-1 proto-oncogene, serine/threonine kinase/Serine/threonine-protein kinase PIM1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2147] [GtoPdb: 2158] [UniProtKB: P11309] | ||||||||
ChEMBL | Inhibition of human PIM1 measured after 5 mins by ELISA relative to control | B | 5.37 | pIC50 | 4300 | nM | IC50 | Eur J Med Chem (2017) 134: 357-365 [PMID:28431341] |
Organic cation transporter 3/Solute carrier family 22 member 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2073673] [GtoPdb: 1021] [UniProtKB: O75751] | ||||||||
ChEMBL | TP_TRANSPORTER: inhibition of MPP+ uptake in OCT3-expressing HEK293 cells | F | 6.92 | pKi | 120 | nM | Ki | Nat. Neurosci. (1998) 1: 349-351 [PMID:10196521] |
tubulin beta class I/tubulin alpha 4a/tubulin beta 4B class IVb/tubulin beta 3 class III/tubulin beta 8 class VIII/tubulin alpha 1a/Tubulin in Human (target type: PROTEIN COMPLEX GROUP) [ChEMBL: CHEMBL2095182] [GtoPdb: 2640, 2639, 2641, 2752, 2753, 2638] [UniProtKB: P04350, P07437, P0DPH7, P68363, P68366, P68371, Q13509, Q13885, Q3ZCM7, Q6PEY2, Q71U36, Q9BQE3, Q9BUF5, Q9BVA1, Q9H4B7] | ||||||||
ChEMBL | Binding affinity to tubulin (unknown origin) assessed as dissociation constant by SPR analysis | B | 4.95 | pKd | 11300 | nM | Kd | Eur J Med Chem (2019) 170: 73-86 [PMID:30878833] |
ChEMBL | Binding affinity to tubulin (unknown origin) by ITC method | B | 7.24 | pKd | 58 | nM | Kd | Eur J Med Chem (2017) 141: 460-472 [PMID:29055869] |
ChEMBL | Displacement of [3H]-colchicine from biotin-labeled tubulin (unknown origin) after 2 hrs by scintillation proximity assay | B | 5.62 | pKi | 2400 | nM | Ki | J. Med. Chem. (2013) 56: 8008-8018 [PMID:24106982] |
ChEMBL | Inhibition of brain tubulin (unknown origin) polymerization measured up to 15 to 30 mins | B | 5.11 | pIC50 | 7800 | nM | IC50 | J. Med. Chem. (2015) 58: 6678-6696 [PMID:26226379] |
ChEMBL | Inhibition of tubulin (unknown origin) polymerization by spectrophotometry | B | 5.27 | pIC50 | 5400 | nM | IC50 | Bioorg. Med. Chem. (2014) 22: 4917-4923 [PMID:25059503] |
ChEMBL | In vitro inhibition of tubulin polymerization. | F | 5.38 | pIC50 | 4200 | nM | IC50 | J. Med. Chem. (1993) 36: 1474-1479 [PMID:8496915] |
ChEMBL | Inhibition of tubulin polymerization | F | 5.48 | pIC50 | 3300 | nM | IC50 | J. Med. Chem. (2006) 49: 6656-6659 [PMID:17154496] |
ChEMBL | Inhibition of tubulin polymerization | F | 5.49 | pIC50 | 3200 | nM | IC50 | J. Med. Chem. (2006) 49: 6412-6415 [PMID:17034147] |
ChEMBL | Inhibition of tubulin (unknown origin) polymerization incubated 15 mins prior to GTP addition by spectrophotometry | B | 5.49 | pIC50 | 3200 | nM | IC50 | J. Med. Chem. (2014) 57: 6531-6552 [PMID:25025991] |
ChEMBL | Inhibition of tubulin (unknown origin) assembly preincubated for 15 mins followed by GTP addition measured for 20 mins by spectrophotometric analysis | B | 5.49 | pIC50 | 3200 | nM | IC50 | J. Med. Chem. (2015) 58: 5789-5807 [PMID:26132075] |
ChEMBL | Inhibition of tubulin polymerization (unknown origin) incubated for 15 mins followed by GTP addition and measured for 20 mins by spectrophotometry | B | 5.49 | pIC50 | 3200 | nM | IC50 | Eur J Med Chem (2020) 185: 111828-111828 [PMID:31727471] |
ChEMBL | Inhibition of tubulin polymerization (unknown origin) preincubated for 15 mins followed by GTP addition measured for 20 mins by spectrophotometric method | B | 5.49 | pIC50 | 3200 | nM | IC50 | Eur J Med Chem (2018) 152: 283-297 [PMID:29730191] |
ChEMBL | Inhibition of tubulin polymerization | B | 5.49 | pIC50 | 3200 | nM | IC50 | J. Med. Chem. (2004) 47: 6120-6123 [PMID:15566282] |
ChEMBL | Inhibition of tubulin polymerization | B | 5.49 | pIC50 | 3200 | nM | IC50 | J. Med. Chem. (2007) 50: 2865-2874 [PMID:17497841] |
ChEMBL | Inhibition of tubulin (unknown origin) polymerization preincubated for 15 mins by spectrophotometry | B | 5.49 | pIC50 | 3200 | nM | IC50 | J. Med. Chem. (2013) 56: 123-149 [PMID:23214452] |
ChEMBL | Inhibition of tubulin polymerization in presence of microtubule associated proteins after 30 mins | B | 5.54 | pIC50 | 2900 | nM | IC50 | J. Med. Chem. (2007) 50: 4548-4552 [PMID:17685504] |
ChEMBL | Inhibition of tubulin polymerization | B | 5.57 | pIC50 | 2700 | nM | IC50 | J. Med. Chem. (2006) 49: 2357-2360 [PMID:16570932] |
ChEMBL | Inhibition of tubulin polymerization (unknown origin) by DAPI staining-based fluorescence microscopy | B | 5.59 | pIC50 | 2600 | nM | IC50 | J. Med. Chem. (2014) 57: 6364-6382 [PMID:25061803] |
ChEMBL | Displacement of [3H]-colchicine from tubulin (unknown origin) preincubated with protein for 1 hr followed by [3H]-colchicine addition measured after 3 hrs by scintillation counting analysis | B | 5.66 | pIC50 | 2210 | nM | IC50 | J. Med. Chem. (2015) 58: 6549-6558 [PMID:26241032] |
ChEMBL | Inhibition of tubulin polymerization | F | 5.72 | pIC50 | 1900 | nM | IC50 | J. Med. Chem. (1993) 36: 1146-1156 [PMID:8387598] |
ChEMBL | Inhibition of microtubule polymerization | F | 5.77 | pIC50 | 1700 | nM | IC50 | Bioorg. Med. Chem. Lett. (2006) 16: 2761-2764 [PMID:16504507] |
ChEMBL | Inhibition of Tubulin polymerization after 20 minutes of administration at 30 degree Centigrade | F | 5.82 | pIC50 | 1500 | nM | IC50 | J. Med. Chem. (1997) 40: 961-966 [PMID:9083485] |
ChEMBL | In vitro inhibition of mammalian tubulin polymerization by 50% | B | 5.82 | pIC50 | 1500 | nM | IC50 | J. Med. Chem. (1998) 41: 1956-1961 [PMID:9599244] |
ChEMBL | Inhibition of tubulin polymerization in human K562 cells | B | 5.85 | pIC50 | 1400 | nM | IC50 | Eur. J. Med. Chem. (2010) 45: 3354-3364 [PMID:20546980] |
ChEMBL | In vitro inhibitory activity against tubulin polymerization (10 uM) | B | 5.85 | pIC50 | 1400 | nM | IC50 | J. Med. Chem. (1998) 41: 2333-2338 [PMID:9632366] |
ChEMBL | Inhibition of tubulin polymerization (unknown origin) preincubated for 10 mins followed by GTP addition measured after 20 mins by Coomassie blue staining based SDS-PAGE analysis | B | 5.88 | pIC50 | 1320 | nM | IC50 | Eur J Med Chem (2017) 141: 460-472 [PMID:29055869] |
ChEMBL | Displacement of [3H]colchicine from biotinylated tubulin by scintillation proximity assay | B | 5.98 | pIC50 | 1050 | nM | IC50 | J. Med. Chem. (2007) 50: 6059-6066 [PMID:17973361] |
ChEMBL | Inhibition of [3H]colchicine binding to beta tubulin | B | 6.3 | pIC50 | 500 | nM | IC50 | J. Med. Chem. (2006) 49: 5769-5776 [PMID:16970401] |
ChEMBL | Inhibition of tubulin (unknown origin) polymerization preincubated for 45 mins followed by GTP addition measured after 2 hrs by fluorescence assay | B | 6.44 | pIC50 | 360 | nM | IC50 | Eur. J. Med. Chem. (2015) 93: 93-100 [PMID:25659770] |
GtoPdb | - | - | 7.96 | pIC50 | 11 | nM | IC50 | Bioorg Med Chem Lett (2006) 16: 2761-4 [PMID:16504507] |
Tubulin in Bovine (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2111464] [UniProtKB: Q6B856, Q862F3] | ||||||||
ChEMBL | Inhibition of bovine brain tubulin polymerization extent after 20 mins by turbidimetrically | B | 5.58 | pIC50 | 2620 | nM | IC50 | Eur. J. Med. Chem. (2015) 99: 125-137 [PMID:26070164] |
ChEMBL | Inhibition of bovine brain tubulin polymerization after 30 mins | B | 5.72 | pIC50 | 1900 | nM | IC50 | Bioorg. Med. Chem. (2015) 23: 4230-4236 [PMID:26160020] |
Tubulin alpha chain in Pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3658] [UniProtKB: P02550] | ||||||||
ChEMBL | Compound was evaluated for its ability to inhibit the binding of [3H]-colchicine to tubulin in competitive binding assay | B | 5.6 | pKi | 2500 | nM | Ki | Bioorg. Med. Chem. Lett. (1991) 1: 471-476 |
ChEMBL | Inhibition of tubulin polymerization interacting at the colchicine binding site. | B | 5.38 | pIC50 | 4168.69 | nM | IC50 | J. Med. Chem. (2000) 43: 167-176 [PMID:10649972] |
ChEMBL | Tested for 50 % inhibition of tubulin polymerization by turbidimetric assay | B | 5.72 | pIC50 | 1900 | nM | IC50 | Bioorg. Med. Chem. Lett. (1993) 3: 581-584 |
ChEMBL | The compound was evaluated in vitro for the mammalian brain tubulin polymerization using standard assay. | F | 5.82 | pIC50 | 1500 | nM | IC50 | Bioorg. Med. Chem. Lett. (1992) 2: 1257-1262 |
ChEMBL | Inhibition of tubulin polymerization (ITP) | B | 6.1 | pIC50 | 800 | nM | IC50 | J. Med. Chem. (2001) 44: 3932-3936 [PMID:11689079] |
tubulin beta class I/Tubulin beta-5 chain in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5444] [GtoPdb: 2640] [UniProtKB: P07437] | ||||||||
ChEMBL | Inhibition of tubulin beta polymerization in human Caco2 cells after 48 hrs by ELISA | B | 5.11 | pIC50 | 7710 | nM | IC50 | MedChemComm (2018) 9: 1511-1528 |
ChEMBL | Inhibition of tubulin beta polymerization in human MCF7 cells after 18 to 24 hrs by ELISA based spectrophotometric analysis | B | 5.16 | pIC50 | 6930 | nM | IC50 | Bioorg Med Chem (2018) 26: 3474-3490 [PMID:29793751] |
ChEMBL | Inhibition of tubulin beta polymerization in human MCF7 cells after 48 hrs by ELISA | B | 5.34 | pIC50 | 4590 | nM | IC50 | MedChemComm (2018) 9: 1511-1528 |
GtoPdb | - | - | 7.96 | pIC50 | 11 | nM | IC50 | Bioorg Med Chem Lett (2006) 16: 2761-4 [PMID:16504507] |
Tubulin beta chain in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3394] [UniProtKB: Q6B856] | ||||||||
ChEMBL | Binding constant at colchicine site of bovine brain tubulin | B | 6.11 | pKi | 780 | nM | Ki | Bioorg. Med. Chem. Lett. (2002) 12: 465-469 [PMID:11814821] |
ChEMBL | Compound was evaluated for in vitro inhibitory activity against polymerization of tubulin into microtubules isolated from bovine brain at 1 mg/mL tubulin concentration | B | 5.46 | pIC50 | 3500 | nM | IC50 | Bioorg. Med. Chem. Lett. (1993) 3: 565-570 |
ChEMBL | Inhibitory effect on the polymerization of purified bovine brain tubulin. | F | 5.62 | pIC50 | 2400 | nM | IC50 | J. Med. Chem. (1990) 33: 567-571 [PMID:2299625] |
ChEMBL | Inhibition of tubulin polymerization | F | 6.1 | pIC50 | 800 | nM | IC50 | J. Med. Chem. (1994) 37: 1126-1135 [PMID:8164254] |
ChEMBL | Inhibition of bovine tubulin polymerization | F | 6.1 | pIC50 | 800 | nM | IC50 | J. Med. Chem. (1997) 40: 2266-2275 [PMID:9216846] |
Tubulin polymerization-promoting protein in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2366491] [UniProtKB: Q27957] | ||||||||
ChEMBL | Inhibition of Bos taurus (bovine) brain tubulin polymerization | B | 6.12 | pEC50 | 750 | nM | EC50 | Bioorg. Med. Chem. Lett. (2001) 11: 1393-1396 [PMID:11378362] |
glycine receptor α1 subunit in Human [GtoPdb: 423] [UniProtKB: P23415] | ||||||||
GtoPdb | - | - | 3.5 | pIC50 | 324000 | nM | IC50 | |
glycine receptor α2 subunit in Human [GtoPdb: 424] [UniProtKB: P23416] | ||||||||
GtoPdb | - | - | 4.2 | pIC50 | 64000 | nM | IC50 | |
bromodomain containing 4 in Human [GtoPdb: 1945] [UniProtKB: O60885] | ||||||||
GtoPdb | - | - | 4.7 | pKd | 20000 | nM | Kd | Angew Chem Int Ed Engl (2013) 52: 14055-9 [PMID:24272870] |
ChEMBL data shown on this page come from version 28:
Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]