colchicine [Ligand Id: 2367] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL107 (Colchcine, (-)-colchicine, Colchicine, Colchicinum, Colchineos, Colchisol, Colcrys, Gloperba, Lodoco, Mitigare, NSC-757) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| 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 | Inhibition of tubulin polymerization (unknown origin) by fluorescence based analysis | B | 5.37 | pIC50 | 4280 | nM | IC50 | Eur J Med Chem (2022) 238: 114450-114450 [PMID:35576703] |
| 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 (unknown origin) polymerization preincubated for 15 mins followed by GTP addition by turbidity based spectrophotometer analysis | B | 5.49 | pIC50 | 3200 | nM | IC50 | ACS Med Chem Lett (2017) 8: 521-526 [PMID:28523104] |
| 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 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 (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) 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 (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 (unknown origin) by competitive binding assay | B | 5.53 | pIC50 | 2930 | nM | IC50 | Eur J Med Chem (2022) 227: 113897-113897 [PMID:34649064] |
| 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 (unknown origin) measured every 30 secs for 90 mins | B | 5.54 | pIC50 | 2900 | nM | IC50 | Bioorg Med Chem Lett (2021) 40: 127968-127968 [PMID:33753264] |
| 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) assessed as fluorescence intensity emission at 410 nm for 60 mins | B | 5.58 | pIC50 | 2650 | nM | IC50 | J Med Chem (2022) 65: 4687-4708 [PMID:35282680] |
| 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 (unknown origin) by turbidimetric analysis | B | 5.7 | pIC50 | 2000 | nM | IC50 | J Med Chem (2021) 64: 15702-15715 [PMID:34670362] |
| ChEMBL | Inhibition of tubulin polymerization | F | 5.72 | pIC50 | 1900 | nM | IC50 | J Med Chem (1993) 36: 1146-1156 [PMID:8387598] |
| ChEMBL | Inhibition of tubulin polymerization (unknown origin) incubated for 15 mins in presence of GTP by fluorescence-based tubulin polymerization assay kit | B | 5.75 | pIC50 | 1770 | nM | IC50 | Eur J Med Chem (2021) 209: 112904-112904 [PMID:33077264] |
| ChEMBL | Inhibition of microtubule polymerization | F | 5.77 | pIC50 | 1700 | nM | IC50 | Bioorg Med Chem Lett (2006) 16: 2761-2764 [PMID:16504507] |
| 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 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 | Inhibition of tubulin polymerization (unknown origin) | B | 5.82 | pIC50 | 1500 | nM | IC50 | J Med Chem (2020) 63: 10618-10651 [PMID:32432867] |
| ChEMBL | Inhibition of tubulin polymerization (unknown origin) incubated for 20 mins | B | 5.82 | pIC50 | 1500 | nM | IC50 | J Med Chem (2020) 63: 10618-10651 [PMID:32432867] |
| ChEMBL | Inhibition of [3H]colchicine binding to tubulin (unknown origin) by competitive binding assay | B | 5.83 | pIC50 | 1470 | nM | IC50 | J Med Chem (2022) 65: 4687-4708 [PMID:35282680] |
| ChEMBL | Displacement of [3H]colchicine from tubulin (unknown origin) incubated for 60 mins by competitive binding assay | B | 5.84 | pIC50 | 1460 | nM | IC50 | Eur J Med Chem (2020) 203: 112506-112506 [PMID:32688198] |
| 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 in human MCF7 cells by ELISA | B | 5.85 | pIC50 | 1400 | nM | IC50 | RSC Med Chem (2022) 13: 929-943 [PMID:36092142] |
| 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 | Inhibition of tubulin polymerization (unknown origin) relative to control | B | 5.89 | pIC50 | 1280 | nM | IC50 | Bioorg Med Chem (2020) 28: 115674-115674 [PMID:33065442] |
| 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] |
| ChEMBL | Inhibition of tubulin polymerization (unknown origin) incubated for 1 hr by fluorescence based assay | B | 6.72 | pIC50 | 190 | nM | IC50 | RSC Med Chem (2020) 11: 327-348 [PMID:33479639] |
| GtoPdb | - | - | 7.96 | pIC50 | 11 | nM | IC50 | Bioorg Med Chem Lett (2006) 16: 2761-4 [PMID:16504507] |
| ChEMBL | Inhibition of tubulin polymerization in human HeLa cells assessed as dynamic tyrosinated microtubules content by incubated for 2 hrs by immunofluorescence staining based assay | B | 6.7 | pEC50 | 200 | nM | EC50 | Eur J Med Chem (2021) 215: 113275-113275 [PMID:33618157] |
| 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 [PMID:30288225] |
| 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 [PMID:30288225] |
| 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 | |
| TAS2R4 in Human [GtoPdb: 661] [UniProtKB: Q9NYW5] | ||||||||
| GtoPdb | - | - | 2.99 | pEC50 | 1025000 | nM | EC50 | Chem Senses (2010) 35: 157-70 [PMID:20022913] |
| TAS2R46 in Human [GtoPdb: 679] [UniProtKB: P59540] | ||||||||
| GtoPdb | - | - | 2.8 | pEC50 | 1580000 | nM | EC50 | Chem Senses (2010) 35: 157-70 [PMID:20022913] |
| 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 34:
Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]
